Comprehensive Study Notes: Lipids, Cellular Structure & Signaling, Genetics, and Metabolism

Lipid Synthesis & Storage

  • Four major plasma lipoproteins (named by density; smallest to highest density) and the four major lipid classes they carry

    • Chylomicrons (not a true lipoprotein class for density labeling but included): carry dietary TAGs

    • Very Low Density Lipoproteins (VLDL): carry endogenous TAGs from liver to tissues

    • Intermediate Density Lipoproteins (IDL/VLDL remnants): remnants after TAG hydrolysis

    • Low Density Lipoproteins (LDL): deliver cholesterol to cells

    • High Density Lipoproteins (HDL): pick up cholesterol from tissues and deliver to liver (reverse transport)

  • Major apolipoproteins by lipoprotein class

    • Chylomicrons: apoB-48, apoC-II, apoE

    • VLDL: apoB-100, apoC-II, apoE

    • IDL: apoB-100, apoE

    • LDL: apoB-100

    • HDL: apoA-1, apoC-II, apoE; apoA-1 activates LCAT to produce cholesterol esters

  • Core structure and function of lipoproteins

    • Lipoproteins = fat bubbles with a phospholipid exterior and hollow interior that transports TAGs

    • Cholesterol in the phospholipid membrane helps fluidity while limiting permeability

    • TAGs stored in hollow interior for transport

    • Difference between chylomicrons and lipoproteins: TAG origin and apolipoproteins governing circulation

  • Roles of apolipoproteins and enzymes in lipoprotein metabolism

    • apoC-II activates Lipoprotein Lipase (LPL) on capillary endothelium; LPL hydrolyzes TAGs in chylomicrons and VLDLs

    • apoE is used for hepatic uptake of remnants (IDL, chylomicron remnants)

    • apoB-48: synthesized in intestine for chylomicrons; apoB-100: synthesized in liver for VLDL/LDL

    • ApoA-1 in HDL activates LCAT (lecithin–cholesterol acyltransferase) to convert cholesterol to cholesterol esters for HDL

  • Lipoprotein transport and the liver

    • Chylomicron route: dietary fats → lymphatics (lacteals) → bloodstream → tissues (adipose, muscle); remnants taken up by liver via apoB-48 interactions (apoE, apoC-II)

    • Chylomicron remnants and LDL receptor–mediated uptake contribute to hepatic cholesterol management

    • Liver roles: packages fatty acids into VLDL for export; performs endocytosis of chylomicrons via apoB-48; central regulator of lipid transport and metabolism

  • Lipid storage and utilization in tissues

    • Adipose tissue stores triacylglycerol (TAG); muscle tissue uses fatty acids for energy

    • Insulin regulates lipid storage by activating LPL in adipose tissue (and muscle) to hydrolyze TAGs in circulating lipoproteins for storage or energy

  • Lipoprotein lipase (LPL) activity and TAG hydrolysis

    • LPL sits on luminal surface of capillaries in adipose and muscle

    • Activated by apoC-II; hydrolyzes TAGs in circulating lipoproteins to free fatty acids (FFAs) for uptake and storage in adipose tissue or oxidation in muscle

  • Lipogenesis and TAG storage in the fed state

    • Insulin promotes fatty acid storage and lipogenesis; citrate exported to cytosol activates acetyl-CoA carboxylase to form malonyl-CoA

    • Acetyl-CoA carboxylase requires ATP, biotin, and CO2 to form malonyl-CoA

    • Fatty acid synthase elongates growing fatty acid by 2-carbon units; NADPH (from PPP) provides reducing equivalents

  • De novo fatty acid synthesis from acetyl-CoA

    1. Transfer Acetyl-CoA from mitochondria to cytosol via citrate shuttle

    • Acetyl-CoA cannot cross mitochondrial membranes directly; citrate synthase forms citrate; citrate lyase cleaves citrate to OAA and acetyl-CoA

    • extAcetylCoAfromcitrateextMalonylCoAextviaacetylCoAcarboxylaseext{Acetyl-CoA from citrate} \rightarrow ext{Malonyl-CoA} ext{ via acetyl-CoA carboxylase}

    1. Acetyl-CoA → Malonyl-CoA (AC carboxylase) requires ATP, biotin, CO2

    2. From malonyl-CoA, two-carbon units are added by fatty acid synthase; NADPH supplies reducing equivalents

    3. Palmitate (C16:0) produced as the end product of de novo synthesis

    • Overall stoichiometry (palmitate synthesis):
      8extAcetylCoA+7ATP+14NADPH+6H+palmitate+14NADP++6H2O+7ADP+7Pi8\, ext{Acetyl-CoA} + 7\,\text{ATP} + 14\,\text{NADPH} + 6\,\text{H}^+ \rightarrow \text{palmitate} + 14\,\text{NADP}^+ + 6\,\text{H}_2\text{O} + 7\,\text{ADP} + 7\,\text{Pi}

  • Fatty liver diseases and apoB-100 dependence

    • Alcoholic fatty liver disease: ethanol inhibits VLDL transport from liver; fatty liver results from trapped VLDL and accumulated fatty acids

    • Nonalcoholic fatty liver disease (NAFLD): related to disruptions in apoB-100 and VLDL export; insulin resistance contributes to impaired lipoprotein processing

  • Triacylglycerol synthesis in liver and adipose tissue

    • TAGs are synthesized in liver by combining 3 fatty acids with glycerol-3-phosphate head

    • Glycerol-3-phosphate sources:

    • Phosphorylation of free glycerol via glycerol kinase

    • Reduction of DHAP via glycerol-3-phosphate dehydrogenase (adipose and liver)

    • Adipose tissue lacks glycerol kinase and relies on glucose uptake to generate DHAP for TAG synthesis

  • Cholesterol biosynthesis and regulation

    • Pathway overview 1) Acetyl-CoA + Acetoacetyl-CoA → HMG-CoA 2) HMG-CoA reduced by HMG-CoA reductase to mevalonate (rate-limiting step)

      • Denoted as the rate-limiting enzyme; inhibited by cholesterol, glucagon, and statins
        3) Mevalonate → cholesterol through several steps

    • Key regulatory enzyme

    • HMG-CoA reductase (rate-limiting in cholesterol de novo synthesis)

    • Regulation and clinical relevance

    • Negative feedback by cholesterol; pharmacologic statins inhibit HMG-CoA reductase to lower cholesterol synthesis

Cytoskeleton & Extracellular Matrix (ECM)

  • Three major types of cytoskeletal filaments

    • Actin Filaments (microfilaments)

    • Polarity with barbed (+) and pointed (-) ends; subunits: G-actin (globular) and F-actin (filamentous)

    • Polymerization helpers:

      • Formin: nucleates and elongates, adds ATP-bound G-actin to barbed end

      • Profilin: promotes ATP binding on G-actin

      • Arp2/3: nucleates new branches and growth

      • Capping proteins: cap both ends to prevent depolymerization

      • Coflin: cleaves filament to create new ends for growth

    • Roles: contractile rings in cytokinesis; vesicular transport highways; microvilli structure (fimbrin, villin as bundling proteins)

    • Structures: pseudopodia, lamellipodia, filopodia

    • Microtubules

    • Composed of α- and β-tubulin dimers; form hollow tubes with minus end anchored at centrosome (γ-tubulin ring) and plus end outward

    • Microtubule-associated proteins (MAPs): polymerases and depolymerases

    • Motor proteins: kinesin (anterograde, toward plus end), dynein (retrograde, toward minus end)

    • Cilia & flagella: 9+2 microtubule structure; dynein drives bending motions

    • Intermediate Filaments

    • Dimer-based, tetramer assembly; form apolar filaments (twizzler-like)

    • Provide mechanical resilience and connect to desmosomes/hemidesmosomes

  • ECM components and their roles

    • Fibrous proteins: collagen (most abundant; triple helix with glycine every third residue; hydroxyproline contributes to scurvy), forms bone, tendon, basal lamina; basal lamina filters molecules

    • Glycosaminoglycans (GAGs) & Proteoglycans: repeating disaccharide units; proteoglycans bind core proteins; hyaluronan is a unique, non-sulfated GAG; proteoglycans form aggregates (aggrecan) and form a gel-like ECM

    • Adhesion proteins: fibronectin (binds proteoglycans to collagen; recognized by integrins), laminin (forms networks in basal laminae)

  • Diseases linked to ECM/cytoskeleton disruptions

    • Scurvy: vitamin C deficiency; impaired prolyl hydroxylase → weakened collagen; symptoms include gingival bleeding, skin lesions

    • Osteogenesis Imperfecta: COL1A1/COL1A2 mutations (type I collagen) → brittle bones

    • Ehlers-Danlos Syndrome: COL3A1 mutation (type III collagen) → hyperflexible skin, joints, tissue fragility

    • Marfan Syndrome: FBN1 mutation (fibrillin-1) → abnormal TGF-β signaling; arachnodactyly, lens dislocation, risk of aortic aneurysm/dissection

    • Loeys-Dietz Syndrome: mutations in TGFBR1/2 or SMAD3 → severe cardiovascular manifestations without lens subluxation

    • Deafness: GJB2 (connexin-26) mutations affecting gap junctions in the ear

  • Cell–ECM junctions and adhesion structures

    • Focal adhesions: actin–integrin connections via talin, vinculin, and α-actinin

    • Hemidesmosomes: intermediate filament–integrin connections to the basal lamina

    • Desmosomes: cadherin-based cell–cell junctions linked to intermediate filaments

    • Tight junctions (occludin, claudins): seal epithelial layers

    • Gap junctions: connexins forming channels for intercellular communication

Cell Membranes & Cellular Homeostasis

  • Membrane composition and properties

    • Phospholipids: amphipathic; hydrophilic head (choline, phosphate, glycerol) and hydrophobic tails (often cis double bonds for fluidity)

    • Phosphoglycerides, sphingolipids, and glycolipids (glycolipids face extracellular surface) comprise the membrane

    • Lipid rafts: microdomains rich in cholesterol, sphingolipids, and certain proteins; promote coordinated signaling

    • Gangliosides: glycolipids with sialic acids; Tay-Sachs disease due to HEXA frameshift mutation leading to accumulation of gangliosides in lysosomes

    • Cholesterol: modulates membrane rigidity and permeability

  • Membrane-associated proteins

    • Flippase: flips phospholipids across leaflets (rare, but contributes to asymmetry)

    • Lectins: proteins that bind carbohydrate sequences on cells (e.g., leukocytes, platelets, epithelial cells)

  • Membrane transport mechanisms

    • Carriers: undergo conformational changes; may be active or passive

    • Channels: can be constitutively open or ligand-gated; selective for ions/molecules

    • Endocytosis / Exocytosis

    • Phagocytosis, Caveolae-mediated endocytosis, Receptor-mediated endocytosis, Transcytosis

  • Aquaporins and ion channels: selective for substrates based on size and pore properties

  • Key transporter systems and clinical examples

    • CFTR: chloride channel; mutations cause cystic fibrosis (autosomal recessive) with hypertonic sweat and respiratory infections; CFTR modulates ENaC activity in epithelia

    • Cholera toxin: activates adenylyl cyclase via Gs, raises cAMP, opens CFTR → Cl− and water secretion into intestinal lumen (secretory diarrhea)

    • Na+/K+ ATPase: basolateral pump maintaining gradients (example in gastric parietal cells for acid secretion)

    • Omeprazole: inhibits H+/K+-ATPase (gastric acid secretion)

  • Receptors and signaling architectures

    • Receptors: extracellular ligand binding triggers intracellular signaling

    • Intracellular signaling often begins with receptor activation and propagates via second messengers or kinase cascades

Receptors & Cell Signaling

  • General signaling framework
    1) Signaling cell emits ligand; receiver cell must have compatible receptor
    2) Receptor activation triggers intracellular signaling cascades
    3) Signaling cascades alter effector proteins and cell behavior

  • Categories of extracellular signaling and receptor types

    • Intracellular signals: hydrophobic molecules (steroids, NO) can diffuse through membranes and bind intracellular receptors (nuclear receptors) to modulate transcription

    • Extracellular signals: hydrophilic or large molecules (peptides, growth factors, prostaglandins, neurotransmitters) often bind surface receptors

    • Peptide hormones vs neuropeptides vs growth factors

    • Neurotransmitters act at ligand-gated ion channels or GPCRs

    • Eicosanoids (e.g., prostaglandins) bind cell-surface receptors

  • Key receptor families and pathways

    • Ion-channel coupled receptors (ionotropic): ligand-gated ion channels regulate ionic flow and neuronal signaling

    • G protein-coupled receptors (GPCRs): 7-transmembrane domain receptors; signal via G proteins (Gs, Gi, Gq)

    • Gs: activates adenylyl cyclase → ↑cAMP

    • Gi: inhibits adenylyl cyclase ↓cAMP

    • Gq: activates phospholipase C → IP3 and DAG; IP3 raises intracellular Ca2+, DAG activates protein kinase C (PKC)

    • Receptor tyrosine kinases (RTKs): ligand-induced dimerization and trans-phosphorylation; downstream pathways include Ras–Raf–MEK–ERK

    • Tyrosine kinase–associated receptors: JAK/STAT signaling

    • Receptor guanylyl cyclases: produce cGMP as second messenger

    • Serine/threonine kinase receptors: TGF-β signaling via SMAD transcription factors

    • Notch signaling: proteolytic cleavage releases intracellular domain that acts as transcription factor in nucleus

    • Wnt/Frizzled signaling: β-catenin stabilization and transcriptional activation

    • Hedgehog/Patched-Smoothened: Hedgehog ligand relieves Patched inhibition; Smoothened promotes transcription

    • SHH, FGFs, BMPs, Nodal and related players in development

  • Notable downstream pathways and second messengers

    • cAMP: formed by adenylyl cyclase; degraded by phosphodiesterases; activates PKA

    • cGMP: formed by guanylyl cyclase; degrades by phosphodiesterases; activates PKG, ion channels

    • IP3/DAG: PLC cleaves PIP2 to generate IP3 (Ca2+ mobilization) and DAG (PKC activation)

    • MAPK cascade: Ras → Raf → MEK → ERK; drives cell growth and differentiation

    • JAK/STAT: cytokine receptors activate JAK; STATs translocate to nucleus to drive transcription

    • TGF-β/SMAD: serine/threonine kinase receptors phosphorylate SMADs; SMADs regulate transcription

    • NF-κB: resting IκB inhibits NF-κB; stimuli activate IκB kinase → degradation of IκB → NF-κB translocates to nucleus

  • Integrins and signaling

    • Integrins link ECM to cytoskeleton in focal adhesions and can initiate signaling via focal adhesion kinase (FAK) autophosphorylation

  • Death receptors and apoptosis

    • Fas receptor family (death receptors) cluster cytosolic death domains to trigger intrinsic apoptosis or inflammatory signaling

Lipid Mobilization, Catabolism & Ketone Bodies

  • Fatty acid mobilization and transport

    • Lipolysis in adipose tissue liberates FFAs and glycerol from TAGs via hormone sensitive lipase (HSL) activation by glucagon/epinephrine

    • FFAs bind albumin in blood for transport to tissues

  • Mitochondrial entry of fatty acids for beta-oxidation

    • Activation: fatty acids are converted to fatty acyl-CoA by acyl-CoA synthetase (acyl-CoA formation requires ATP)

    • Outer mitochondrial membrane: carnitine palmitoyltransferase I (CPT I) transfers the fatty acyl group to carnitine

    • Inner mitochondrial membrane: CPT II transfers the fatty acyl group back to CoA inside matrix

    • Beta-oxidation in mitochondria yields acetyl-CoA, FADH2, and NADH; acetyl-CoA enters TCA or ketogenesis depending on metabolic state

  • Beta-oxidation yield (palmitate, C16:0)

    • Beta-oxidation cycles yield 7 FADH2, 7 NADH, and 8 acetyl-CoA per palmitate

    • Per palmitate, total ATP yield is given as: extATPexttotal=7(1.5)+7(2.5)+8(10)2ext(activationcost)=106extATP(net,commonlycited)ext{ATP}_{ ext{total}} = 7(1.5) + 7(2.5) + 8(10) - 2 ext{ (activation cost)} = 106 ext{ ATP (net, commonly cited)}

    • In this material, the total yield is stated as 129 ATP per palmitate

  • Carnitine role and disorders

    • Carnitine shuttles long-chain fatty acids into mitochondria

    • Deficiencies: CPT II deficiency (myopathic symptoms, brown urine), carnitine deficiency (muscle pain, high triglycerides)

    • Peroxisomal defects (Zellweger syndrome) affect VLCFA metabolism; phytanic acid accumulation with Phyh deficiency

  • Peroxisomal transport and VLCFA metabolism

    • VLCFAs require peroxisomes for β-oxidation; defects disrupt metabolism

  • Ketone bodies and ketogenesis

    • Ketone bodies: acetone, 3-hydroxybutyrate, acetoacetate

    • Ketogenesis in liver mitochondria: HMG-CoA synthase and HMG-CoA lyase generate ketone bodies

    • Rate-limiting step: HMG-CoA synthase (in ketogenesis)

    • Ketone bodies serve as fuels for extrahepatic tissues during fasting or carbohydrate deprivation; brain and muscle can utilize ketones; liver and RBCs cannot use ketone bodies (liver lacks thiophorase; RBCs lack mitochondria)

    • Ketosis and ketoacidosis can occur in alcohol abuse, Type I diabetes, prolonged fasting, and some children; acetone imparts fruity breath

Fatty Liver Disease, Metabolism & Regulation

  • Alcoholic fatty liver disease

    • Ethanol inhibits VLDL export from liver; cholesterol synthesis and palmitate production continue, but VLDL cannot leave the liver

  • Nonalcoholic fatty liver disease (NAFLD)

    • Often linked to apoB-100 transport defects and hepatic lipid accumulation; insulin resistance contributes to NAFLD progression

  • Regulation of hepatic VLDL secretion by diet & hormones

    • Fed state: insulin promotes lipogenesis; insulin also activates LPL to process circulating lipoproteins

    • LPL action on VLDL and chylomicrons hydrolyzes TAGs to FFAs for storage or energy

Cholesterol Biosynthesis & Regulation (Expanded)

  • Pathway overview

    • Acetyl-CoA + Acetoacetyl-CoA → HMG-CoA

    • HMG-CoA reductase reduces HMG-CoA to mevalonate (rate-limiting step)

    • Mevalonate → cholesterol through downstream steps

  • Regulation of HMG-CoA reductase

    • Inhibited by cholesterol via negative feedback, by glucagon, and by statins

    • Activation stimulates cholesterol synthesis; regulation matches cellular cholesterol needs

Hormones, Signaling & Genomic Regulation

  • Hormone types and hydrophilicity/hydrophobicity

    • Hydrophilic hormones (e.g., peptide hormones, catecholamines): stored in vesicles; short-to-intermediate half-lives; act on surface receptors

    • Hydrophobic hormones (steroids, thyroid hormones): diffuse through membranes; long half-lives; often bind to intracellular receptors (nuclear receptor family), regulating gene transcription

  • Four signal transduction pathways for hydrophilic hormones

    • Integrin-mediated signaling (growth signals)

    • Ligand-gated ion channels (neurohormones)

    • Receptor tyrosine kinases / receptor enzymes (example: leptin via JAK/STAT)

    • GPCRs (adenylyl cyclase–cAMP, PKC–Ca2+ pathways)

  • Nuclear receptors for hydrophobic signals

    • Ligand binding leads to receptor activation, dimerization, nuclear translocation, and transcriptional regulation

  • Hormone signaling regulation concepts

    • Up-regulation vs down-regulation: receptor density changes with hormone levels to maintain homeostasis

    • Negative and positive feedback in hormonal systems

    • Hormone half-life and pharmacodynamics

  • Hormone signaling in pharmacology

    • Agonists vs antagonists; receptor modulation; therapeutic targeting

  • Types of hormone interactions and signaling networks

    • NOTCH, WNT/β-catenin, Hedgehog (Patched/Smoothened), SHH, Nodal

    • TGF-β/SMAD signaling; JAK/STAT; RTKs; GPCRs; NF-κB pathways

  • Second messengers and their synthesis/degradation

    • cAMP: ATP → cAMP via adenylyl cyclase; degraded by phosphodiesterases; acts on PKA

    • cGMP: GTP → cGMP via guanylyl cyclase; degraded to GMP by phosphodiesterases; activates PKG and other targets

    • IP3 and DAG: PLC cleaves PIP2 to IP3 (Ca2+ mobilization) and DAG (PKC activation)

Amino Acid Metabolism & Nitrogen Handling

  • Aminotransferases, glutamate dehydrogenase and glutaminase in nitrogen metabolism

    • Transaminases (aminotransferases) require vitamin B6; transfer amino groups to form α-keto acids and glutamate

    • Glutamate dehydrogenase converts glutamate to α-ketoglutarate, producing NH4+ (reductive amination or deamination via NAD+/NADH)

    • Glutaminase converts glutamine → glutamate + NH4+; NH4+ is excreted as urea

  • Urea biosynthesis (urea cycle): subcellular location and regulation

    • 5 key enzymes: CPS I (mitochondrial), OTC (mitochondrial), argininosuccinate synthetase (cytosol), argininosuccinate lyase (cytosol), arginase (cytosol)

    • Regulation: CPS I activated by N-acetylglutamate (allosteric activator)

    • Liver function tests (LFTs): AST and ALT reflect hepatic health; hyperammonemia results from defects in any cycle step

Epigenetics, Genomics & Inheritance

  • Epigenetics: definitions and scope

    • Genome: complete set of genetic material in an organism

    • Genetics: study of individual genes and their inheritance

    • Epigenome: the full set of epigenetic marks across the genome

    • Epigenetics: heritable changes in gene expression not caused by DNA sequence changes (e.g., DNA methylation, histone modification, chromatin remodeling, imprinting)

  • Types of epigenetic modifications

    • DNA methylation (CpG islands): generally silences gene expression

    • Histone methylation (HMT) and demethylation (HDM)

    • Histone acetylation (HAT) opens chromatin and promotes transcription; HDACs remove acetyl groups to repress transcription

  • Imprinting and developmental reprogramming

    • Imprinting: selective silencing of one parental allele in certain genes; can affect expression and disease risk if the active allele is mutated

    • Epigenetic reprogramming during fertilization and implantation erases most marks except imprinted genes

    • Transgenerational epigenetics: parental experiences can influence offspring via epigenetic mechanisms (e.g., famine exposure, agouti gene methylation, glucocorticoid gene methylation)

  • Epigenetic diseases and notable studies

    • Famine studies (Dutch Hunger Winter) showing transgenerational epigenetic effects

    • Agouti mouse model: methylation status affects phenotype; diet can influence offspring health

    • Aging and cancer: global hypomethylation and locus-specific hypermethylation with age

Genetic Inheritance, Pedigrees & Population Genetics

  • Mendelian inheritance overview

    • Autosomal vs gonosomal (X-linked) inheritance

    • Dominant vs recessive; penetrance and expressivity; incomplete penetrance and pleiotropy

    • Heterozygous vs homozygous manifestations; incomplete dominance and codominance possible

  • Pedigree analysis fundamentals

    • Pedigree symbols indicate gender, affected status; consanguinity indicated by double lines

    • Patterns suggesting autosomal recessive vs dominant; X-linked recessive mostly affects males

    • Mitochondrial inheritance indicated when affected individuals are all maternal descendants

    • Use Punnett squares to estimate offspring risk (e.g., Aa x Aa → 25% AA, 50% Aa, 25% aa)

    • X-linked recessive: carrier mother x unaffected male yields 25% affected sons, 25% affected daughters if mother is carrier, etc.

  • Genetic nomenclature and karyotypes

    • Chromosome arms: P (short) and Q (long); e.g., 17q indicates long arm of chromosome 17

    • Common karyotype descriptors: 46, XX; 46, XY; autosomal vs sex chromosome abnormalities

  • Aneuploidy and mosaicism

    • Trisomy (2n+1) and monosomy (2n-1); viable trisomies: chromosomes 13, 18, 21; monosomy generally lethal unless gonosomes

    • Mosaicism: different cell lines with varying chromosomal complements; chromosomal mosaicism vs non-chromosomal mosaicism (gene mutations)

  • Chromosomal structural abnormalities

    • Deletion, ring chromosome, microdeletion; inversion, isochromosome; translocations (balanced vs unbalanced; Robertsonian translocations common between acrocentrics 13,14,15,21,22)

    • Uniparental disomy (two homologous chromosomes from one parent) can disrupt imprinting

  • FH (Familial Hypercholesterolemia) genetics

    • Gene mutations: APOB-100 mutation (impaired VLDL transport) and LDLR mutation (impaired uptake)

    • LDL receptor pathway and feedback regulation by cholesterol

    • LDL receptor mutations cause autosomal dominant FH; heterozygotes show elevated LDL and premature atherosclerosis; homozygotes more severely affected

    • LDLR domains and endocytosis: ligand-binding domain, membrane-spanning domain, FxNPxY motif for endocytosis, O-linked sugars

    • Five classes of FH mutations (I–V) affecting synthesis, folding, ligand-binding, endocytosis, or receptor trafficking

    • Prevalence: many different mutations across the LDLR gene (allelic heterogeneity)

Clinical Connections: Lipid & Membrane Disorders

  • Cystic fibrosis (CFTR) and chloride transport

    • CFTR mutations (e.g., delta-F508) impair chloride and bicarbonate transport; hypertonic sweat and thick mucus; respiratory infections common

    • CFTR interacts with ENaC in epithelia; defective CFTR disturbs ion and water balance in airways and pancreatic ducts

  • Ion channels and channelopathies

    • Brugada syndrome: SCN5A Na+ channel mutation; cardiac arrhythmias and sudden death during sleep; characteristic ECG patterns

  • Drug interactions with transport and signaling

    • Omeprazole inhibits H+/K+-ATPase in stomach; cholera toxin increases cAMP via Gs, activating CFTR and causing secretory diarrhea

  • Stomach acid secretion and intestinal absorption

    • Gastric parietal cells utilize H+/K+-ATPase for acid secretion; bicarbonate exchange and CO2/H2O conversion; SGLT1 (Na+-glucose cotransporter) for carbohydrate uptake; GLUT2 for basolateral exit

  • Regulation of blood glucose and lipid handling by hormones

    • Insulin stimulates fatty acid storage and LPL activity in adipose tissue; glucagon promotes lipolysis

  • Pharmacology and precision medicine concepts

    • Pharmacogenomics tailors drug treatment based on individual genomes

    • CRISPR-Cas9 as a genome-editing tool with Cas9 enzyme and guide RNA; PAM requirements; controversies and emerging therapeutic potential

Lipoprotein Remnants, Transport, and Metabolism (Consolidated)

  • Dietary fats are emulsified and digested into fatty acids and monoglycerides; absorbed by enterocytes

  • Chylomicrons assemble in enterocytes (apoB-48-containing); secreted into lymphatics and then blood

  • In tissues, LPL hydrolyzes TAGs to FFAs for storage or oxidation; chylomicron remnants cleared by liver via apoE interactions

  • The liver exports VLDL (apoB-100) carrying TAGs; in capillaries, LPL removes TAGs; remnants become IDL and then LDL (cholesterol-rich)

  • HDL scavenges cholesterol from tissues and returns it to liver; HDL metabolism involves apoA-1 activating LCAT to form cholesterol esters

  • De novo synthesis of fatty acids proceeds in the cytosol of hepatocytes via citrate shuttle, acetyl-CoA carboxylase forming malonyl-CoA, and fatty acid synthase extending palmitate; the process is regulated by insulin and citrate

Key Formulas and Quick References

  • De novo fatty acid synthesis (palmitate)
    8 AcetylCoA+7 ATP+14 NADPH+6H+palmitate+14 NADP++6H2O+7 ADP+7 Pi8\ Acetyl\text{CoA} + 7\ ATP + 14\ NADPH + 6H^+ \rightarrow \text{palmitate} + 14\ NADP^+ + 6H_2O + 7\ ADP + 7\ Pi

  • Acetyl-CoA carboxylase reaction (to malonyl-CoA)
    Acetyl-CoA+CO2+ATPMalonyl-CoA\text{Acetyl-CoA} + CO_2 + ATP \rightarrow \text{Malonyl-CoA}

  • Cholesterol biosynthesis (simplified)

    • Acetyl-CoA + Acetoacetyl-CoA → HMG-CoA

    • HMG-CoA reductase reduces HMG-CoA to mevalonate (rate-limiting step)
      HMG-CoA+2 NADPHMevalonate+2 NADP++CoA\text{HMG-CoA} + 2\ NADPH \rightarrow \text{Mevalonate} + 2\ NADP^+ + CoA

  • Ketogenesis (ketone bodies)

    • Acetoacetyl-CoA + acetyl-CoA → HMG-CoA (via HMG-CoA synthase) → acetoacetate via HMG-CoA lyase

    • Acetoacetate ⇌ 3-hydroxybutyrate (via β-hydroxybutyrate dehydrogenase)

    • Acetone formed by spontaneous decarboxylation of acetoacetate

  • Beta-oxidation yields for palmitate (per the material)

    • 129 ATP per palmitate (as stated in notes) in the summarized pathway

Cross-References to Real-World Relevance

  • Lipid transport balance and disease risk (FH, FH mutations, LDL receptor defects) contribute to premature atherosclerosis and cardiovascular risk; understanding LDLR domain functions helps explain pathogenesis and genotype–phenotype correlations

  • Epigenetics and transgenerational effects provide insight into how lifestyle and environmental factors can influence disease susceptibility in offspring; agouti model demonstrates a direct link between maternal diet and offspring phenotype

  • CFTR malfunction and ENaC interaction explain cystic fibrosis pathology and salty sweat; cholera toxin exploits CFTR to cause severe diarrhea, highlighting the importance of ion transport in health and disease

  • Developmental signaling pathways (Notch, Wnt, SHH, TGF-β/SMAD) tie molecular events to congenital malformations and syndromic disorders (e.g., FGFR-related conditions, HOX gene defects)

  • Ketogenesis and fatty acid metabolism illustrate metabolic flexibility during fasting or carbohydrate restriction; imbalances can lead to ketosis or ketoacidosis in certain clinical contexts

Glossary of Selected Terms

  • ApoB-48, ApoB-100: apolipoproteins critical for chylomicron and VLDL/LDL assembly and receptor interactions

  • LCAT: enzyme that esterifies cholesterol on HDL, promoting maturation

  • LPL: lipoprotein lipase; hydrolyzes TAGs in circulating lipoproteins in peripheral tissues

  • HMG-CoA reductase: rate-limiting enzyme in cholesterol biosynthesis; target of statins

  • CPT I/II: carnitine shuttle enzymes that import fatty acids into mitochondria for β-oxidation

  • Imprinting: epigenetic marking leading to parent-of-origin–specific gene expression

  • HOX genes: transcription factors that determine body plan along the anterior–posterior axis

  • Notch, Wnt, SHH, TGF-β/SMAD: key signaling pathways governing development

  • FH mutations: autosomal dominant disorder with elevated LDL and risk of early cardiovascular disease

  • PKU, MSUD, Albinism, Alkaptonuria, Homocystinuria: classic inborn errors of metabolism with specific enzyme defects and dietary interventions

Notes on Specific Data Points from the Transcript

  • Lipoprotein composition table (summary)

    • Chylomicrons: apoB-48, apoC-II, apoE

    • VLDL: apoB-100, apoC-II, apoE

    • IDL: apoB-100, apoE

    • LDL: apoB-100

    • HDL: apoA-1, apoC-II, apoE

  • LPL activation and TG hydrolysis location: luminal surface of capillary endothelium in adipose tissue and muscle

  • De novo FA synthesis steps include citrate shuttle, acetyl-CoA carboxylase, NADPH supply from PPP

  • Alcoholic vs nonalcoholic fatty liver disease causes revolve around VLDL export and apoB-100 handling

  • Ketone body production is favored in starvation; liver cannot use ketones due to lack of thiophorase; RBCs lack mitochondria


Lipid Synthesis & Storage

  • Four major plasma lipoproteins (named by density; smallest to highest density) and the four major lipid classes they carry- Chylomicrons (not a true lipoprotein class for density labeling but included): carry dietary TAGs

    • Very Low Density Lipoproteins (VLDL): carry endogenous TAGs from liver to tissues

    • Intermediate Density Lipoproteins (IDL/VLDL remnants): remnants after TAG hydrolysis

    • Low Density Lipoproteins (LDL): deliver cholesterol to cells

    • High Density Lipoproteins (HDL): pick up cholesterol from tissues and deliver to liver (reverse transport)

  • Major apolipoproteins by lipoprotein class- Chylomicrons: apoB-48, apoC-II, apoE

    • VLDL: apoB-100, apoC-II, apoE

    • IDL: apoB-100, apoE

    • LDL: apoB-100

    • HDL: apoA-1, apoC-II, apoE; apoA-1 activates LCAT to produce cholesterol esters

  • Core structure and function of lipoproteins- Lipoproteins = fat bubbles with a phospholipid exterior and hollow interior that transports TAGs

    • Cholesterol in the phospholipid membrane helps fluidity while limiting permeability

    • TAGs stored in hollow interior for transport

    • Difference between chylomicrons and lipoproteins: TAG origin and apolipoproteins governing circulation

  • Roles of apolipoproteins and enzymes in lipoprotein metabolism- apoC-II activates Lipoprotein Lipase (LPL) on capillary endothelium; LPL hydrolyzes TAGs in chylomicrons and VLDLs

    • apoE is used for hepatic uptake of remnants (IDL, chylomicron remnants)

    • apoB-48: synthesized in intestine for chylomicrons; apoB-100: synthesized in liver for VLDL/LDL

    • ApoA-1 in HDL activates LCAT (lecithin

--cholesterol acyltransferase) to convert cholesterol to cholesterol esters for HDL

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  • Lipoprotein transport and the liver- Chylomicron route: dietary fats

lymphatics (lacteals)

bloodstream

tissues (adipose, muscle); remnants taken up by liver via apoB-48 interactions (apoE, apoC-II)
- Chylomicron remnants and LDL receptor

--mediated uptake contribute to hepatic cholesterol management
- Liver roles: packages fatty acids into VLDL for export; performs endocytosis of chylomicrons via apoB-48; central regulator of lipid transport and metabolism

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  • Lipid storage and utilization in tissues- Adipose tissue stores triacylglycerol (TAG); muscle tissue uses fatty acids for energy

    • Insulin regulates lipid storage by activating LPL in adipose tissue (and muscle) to hydrolyze TAGs in circulating lipoproteins for storage or energy

  • Lipoprotein lipase (LPL) activity and TAG hydrolysis- LPL sits on luminal surface of capillaries in adipose and muscle

    • Activated by apoC-II; hydrolyzes TAGs in circulating lipoproteins to free fatty acids (FFAs) for uptake and storage in adipose tissue or oxidation in muscle

  • Lipogenesis and TAG storage in the fed state- Insulin promotes fatty acid storage and lipogenesis; citrate exported to cytosol activates acetyl-CoA carboxylase to form malonyl-CoA

    • Acetyl-CoA carboxylase requires ATP, biotin, and CO2 to form malonyl-CoA

    • Fatty acid synthase elongates growing fatty acid by 2-carbon units; NADPH (from PPP) provides reducing equivalents

  • De novo fatty acid synthesis from acetyl-CoA1. Transfer Acetyl-CoA from mitochondria to cytosol via citrate shuttle

    • Acetyl-CoA cannot cross mitochondrial membranes directly; citrate synthase forms citrate; citrate lyase cleaves citrate to OAA and acetyl-CoA

    • ext{Acetyl-CoA from citrate}
      ightarrow ext{Malonyl-CoA} ext{ via acetyl-CoA carboxylase}

    1. Acetyl-CoA

    Malonyl-CoA (AC carboxylase) requires ATP, biotin, CO2

    1. From malonyl-CoA, two-carbon units are added by fatty acid synthase; NADPH supplies reducing equivalents

    2. Palmitate (C16:0) produced as the end product of de novo synthesis

    • Overall stoichiometry (palmitate synthesis):

      8Acetyl-CoA+7ATP+14NADPH+6H+palmitate+14NADP++6H2O+7ADP+7Pi8\, \text{Acetyl-CoA} + 7\,\text{ATP} + 14\,\text{NADPH} + 6\,\text{H}^+ \rightarrow \text{palmitate} + 14\,\text{NADP}^+ + 6\,\text{H}_2\text{O} + 7\,\text{ADP} + 7\,\text{Pi}

  • Fatty liver diseases and apoB-100 dependence- Alcoholic fatty liver disease: ethanol inhibits VLDL transport from liver; fatty liver results from trapped VLDL and accumulated fatty acids

    • Nonalcoholic fatty liver disease (NAFLD): related to disruptions in apoB-100 and VLDL export; insulin resistance contributes to impaired lipoprotein processing

  • Triacylglycerol synthesis in liver and adipose tissue- TAGs are synthesized in liver by combining 3 fatty acids with glycerol-3-phosphate head

    • Glycerol-3-phosphate sources:

    • Phosphorylation of free glycerol via glycerol kinase

    • Reduction of DHAP via glycerol-3-phosphate dehydrogenase (adipose and liver)

    • Adipose tissue lacks glycerol kinase and relies on glucose uptake to generate DHAP for TAG synthesis

  • Cholesterol biosynthesis and regulation- Pathway overview 1) Acetyl-CoA + Acetoacetyl-CoA

    HMG-CoA 2) HMG-CoA reduced by HMG-CoA reductase to mevalonate (rate-limiting step)- Denoted as the rate-limiting enzyme; inhibited by cholesterol, glucagon, and statins

     3) Mevalonate 
    

    cholesterol through several steps

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    • Key regulatory enzyme

    • HMG-CoA reductase (rate-limiting in cholesterol de novo synthesis)

    • Regulation and clinical relevance

    • Negative feedback by cholesterol; pharmacologic statins inhibit HMG-CoA reductase to lower cholesterol synthesis

Cytoskeleton & Extracellular Matrix (ECM)

  • Three major types of cytoskeletal filaments- Actin Filaments (microfilaments)

    • Polarity with barbed (+) and pointed (-) ends; subunits: G-actin (globular) and F-actin (filamentous)

    • Polymerization helpers:- Formin: nucleates and elongates, adds ATP-bound G-actin to barbed end

      • Profilin: promotes ATP binding on G-actin

      • Arp2/3: nucleates new branches and growth

      • Capping proteins: cap both ends to prevent depolymerization

      • Coflin: cleaves filament to create new ends for growth

    • Roles: contractile rings in cytokinesis; vesicular transport highways; microvilli structure (fimbrin, villin as bundling proteins)

    • Structures: pseudopodia, lamellipodia, filopodia

    • Microtubules

    • Composed of \alpha- and \beta-tubulin dimers; form hollow tubes with minus end anchored at centrosome (\gamma-tubulin ring) and plus end outward

    • Microtubule-associated proteins (MAPs): polymerases and depolymerases

    • Motor proteins: kinesin (anterograde, toward plus end), dynein (retrograde, toward minus end)

    • Cilia & flagella: 9+2 microtubule structure; dynein drives bending motions

    • Intermediate Filaments

    • Dimer-based, tetramer assembly; form apolar filaments (twizzler-like)

    • Provide mechanical resilience and connect to desmosomes/hemidesmosomes

  • ECM components and their roles- Fibrous proteins: collagen (most abundant; triple helix with glycine every third residue; hydroxyproline contributes to scurvy), forms bone, tendon, basal lamina; basal lamina filters molecules

    • Glycosaminoglycans (GAGs) & Proteoglycans: repeating disaccharide units; proteoglycans bind core proteins; hyaluronan is a unique, non-sulfated GAG; proteoglycans form aggregates (aggrecan) and form a gel-like ECM

    • Adhesion proteins: fibronectin (binds proteoglycans to collagen; recognized by integrins), laminin (forms networks in basal laminae)

  • Diseases linked to ECM/cytoskeleton disruptions- Scurvy: vitamin C deficiency; impaired prolyl hydroxylase

    weakened collagen; symptoms include gingival bleeding, skin lesions

    • Osteogenesis Imperfecta: COL1A1/COL1A2 mutations (type I collagen)

    brittle bones

    • Ehlers-Danlos Syndrome: COL3A1 mutation (type III collagen)

    hyperflexible skin, joints, tissue fragility

    • Marfan Syndrome: FBN1 mutation (fibrillin-1)

    abnormal TGF-\beta signaling; arachnodactyly, lens dislocation, risk of aortic aneurysm/dissection

    • Loeys-Dietz Syndrome: mutations in TGFBR1/2 or SMAD3

    severe cardiovascular manifestations without lens subluxation

    • Deafness: GJB2 (connexin-26) mutations affecting gap junctions in the ear

  • Cell

-ECM junctions and adhesion structures- Focal adhesions: actin

-

integrin connections via talin, vinculin, and \alpha-actinin
- Hemidesmosomes: intermediate filament

integrin connections to the basal lamina
- Desmosomes: cadherin-based cell

-cell junctions linked to intermediate filaments
- Tight junctions (occludin, claudins): seal epithelial layers
- Gap junctions: connexins forming channels for intercellular communication

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Cell Membranes & Cellular Homeostasis

  • Membrane composition and properties- Phospholipids: amphipathic; hydrophilic head (choline, phosphate, glycerol) and hydrophobic tails (often cis double bonds for fluidity)

    • Phosphoglycerides, sphingolipids, and glycolipids (glycolipids face extracellular surface) comprise the membrane

    • Lipid rafts: microdomains rich in cholesterol, sphingolipids, and certain proteins; promote coordinated signaling

    • Gangliosides: glycolipids with sialic acids; Tay-Sachs disease due to HEXA frameshift mutation leading to accumulation of gangliosides in lysosomes

    • Cholesterol: modulates membrane rigidity and permeability

  • Membrane-associated proteins- Flippase: flips phospholipids across leaflets (rare, but contributes to asymmetry)

    • Lectins: proteins that bind carbohydrate sequences on cells (e.g., leukocytes, platelets, epithelial cells)

  • Membrane transport mechanisms- Carriers: undergo conformational changes; may be active or passive

    • Channels: can be constitutively open or ligand-gated; selective for ions/molecules

    • Endocytosis / Exocytosis

    • Phagocytosis, Caveolae-mediated endocytosis, Receptor-mediated endocytosis, Transcytosis

  • Aquaporins and ion channels: selective for substrates based on size and pore properties

  • Key transporter systems and clinical examples- CFTR: chloride channel; mutations cause cystic fibrosis (autosomal recessive) with hypertonic sweat and respiratory infections; CFTR modulates ENaC activity in epithelia

    • Cholera toxin: activates adenylyl cyclase via Gs, raises cAMP, opens CFTR

Cl- and water secretion into intestinal lumen (secretory diarrhea)
- Na+/K+ ATPase: basolateral pump maintaining gradients (example in gastric parietal cells for acid secretion)
- Omeprazole: inhibits H+/K+

ATPase (gastric acid secretion)

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  • Receptors and signaling architectures- Receptors: extracellular ligand binding triggers intracellular signaling

    • Intracellular signaling often begins with receptor activation and propagates via second messengers or kinase cascades

Receptors & Cell Signaling

  • General signaling framework

    1) Signaling cell emits ligand; receiver cell must have compatible receptor

    2) Receptor activation triggers intracellular signaling cascades

    3) Signaling cascades alter effector proteins and cell behavior

  • Categories of extracellular signaling and receptor types- Intracellular signals: hydrophobic molecules (steroids, NO) can diffuse through membranes and bind intracellular receptors (nuclear receptors) to modulate transcription

    • Extracellular signals: hydrophilic or large molecules (peptides, growth factors, prostaglandins, neurotransmitters) often bind surface receptors

    • Peptide hormones vs neuropeptides vs growth factors

    • Neurotransmitters act at ligand-gated ion channels or GPCRs

    • Eicosanoids (e.g., prostaglandins) bind cell-surface receptors

  • Key receptor families and pathways- Ion-channel coupled receptors (ionotropic): ligand-gated ion channels regulate ionic flow and neuronal signaling

    • G protein-coupled receptors (GPCRs): 7-transmembrane domain receptors; signal via G proteins (Gs, Gi, Gq)

    • Gs: activates adenylyl cyclase

    ↑cAMP

    • Gi: inhibits adenylyl cyclase

    ↓cAMP

    • Gq: activates phospholipase C

IP3 and DAG; IP3 raises intracellular Ca2+, DAG activates protein kinase C (PKC)
- Receptor tyrosine kinases (RTKs): ligand-induced dimerization and trans-phosphorylation; downstream pathways include Ras

Raf

MEK

ERK; drives cell growth and differentiation
- Tyrosine kinase

-

associated receptors: JAK/STAT signaling
- Receptor guanylyl cyclases: produce cGMP as second messenger
- Serine/threonine kinase receptors: TGF-\beta signaling via SMAD transcription factors
- Notch signaling: proteolytic cleavage releases intracellular domain that acts as transcription factor in nucleus
- Wnt/Frizzled signaling: \beta-catenin stabilization and transcriptional activation
- Hedgehog/Patched-Smoothened: Hedgehog ligand relieves Patched inhibition; Smoothened promotes transcription
- SHH, FGFs, BMPs, Nodal and related players in development

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  • Notable downstream pathways and second messengers- cAMP: formed by adenylyl cyclase; degraded by phosphodiesterases; activates PKA

    • cGMP: formed by guanylyl cyclase; degrades by phosphodiesterases; activates PKG, ion channels

    • IP3/DAG: PLC cleaves PIP2 to generate IP3 (Ca2+ mobilization) and DAG (PKC activation)

    • MAPK cascade: Ras

    Raf

    MEK

    ERK; drives cell growth and differentiation

    • JAK/STAT: cytokine receptors activate JAK; STATs translocate to nucleus to drive transcription

    • TGF-\beta/SMAD: serine/threonine kinase receptors phosphorylate SMADs; SMADs regulate transcription

    • NF-\kappaB: resting I\kappaB inhibits NF-\kappaB; stimuli activate I\kappaB kinase

    degrad

    ation of I\kappaB

NF-\kappaB translocates to nucleus

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  • Integrins and signaling- Integrins link ECM to cytoskeleton in focal adhesions and can initiate signaling via focal adhesion kinase (FAK) autophosphorylation

  • Death receptors and apoptosis- Fas receptor family (death receptors) cluster cytosolic death domains to trigger intrinsic apoptosis or inflammatory signaling

Lipid Mobilization, Catabolism & Ketone Bodies

  • Fatty acid mobilization and transport- Lipolysis in adipose tissue liberates FFAs and glycerol from TAGs via hormone sensitive lipase (HSL) activation by glucagon/epinephrine

    • FFAs bind albumin in blood for transport to tissues

  • Mitochondrial entry of fatty acids for beta-oxidation- Activation: fatty acids are converted to fatty acyl-CoA by acyl-CoA synthetase (acyl-CoA formation requires ATP)

    • Outer mitochondrial membrane: carnitine palmitoyltransferase I (CPT I) transfers the fatty acyl group to carnitine

    • Inner mitochondrial membrane: CPT II transfers the fatty acyl group back to CoA inside matrix

    • Beta-oxidation in mitochondria yields acetyl-CoA, FADH2, and NADH; acetyl-CoA enters TCA or ketogenesis depending on metabolic state

  • Beta-oxidation yield (palmitate, C16:0)- Beta-oxidation cycles yield 7 FADH2, 7 NADH, and 8 acetyl-CoA per palmitate

    • Per palmitate, total ATP yield is given as: extATPtotal=7(1.5)+7(2.5)+8(10)2ext(activationcost)=106extATP(net,commonlycited)ext{ATP}_{\text{total}} = 7(1.5) + 7(2.5) + 8(10) - 2 ext{ (activation cost)} = 106 ext{ ATP (net, commonly cited)}

    • In this material, the total yield is stated as 129 ATP per palmitate

  • Carnitine role and disorders- Carnitine shuttles long-chain fatty acids into mitochondria

    • Deficiencies: CPT II deficiency (myopathic symptoms, brown urine), carnitine deficiency (muscle pain, high triglycerides)

    • Peroxisomal defects (Zellweger syndrome) affect VLCFA metabolism; phytanic acid accumulation with Phyh deficiency

  • Peroxisomal transport and VLCFA metabolism- VLCFAs require peroxisomes for \beta-oxidation; defects disrupt metabolism

  • Ketone bodies and ketogenesis- Ketone bodies: acetone, 3-hydroxybutyrate, acetoacetate

    • Ketogenesis in liver mitochondria: HMG-CoA synthase and HMG-CoA lyase generate ketone bodies

    • Rate-limiting step: HMG-CoA synthase (in ketogenesis)

    • Ketone bodies serve as fuels for extrahepatic tissues during fasting or carbohydrate deprivation; brain and muscle can utilize ketones; liver and RBCs cannot use ketone bodies (liver lacks thiophorase; RBCs lack mitochondria)

    • Ketosis and ketoacidosis can occur in alcohol abuse, Type I diabetes, prolonged fasting, and some children; acetone imparts fruity breath

Fatty Liver Disease, Metabolism & Regulation

  • Alcoholic fatty liver disease- Ethanol inhibits VLDL export from liver; cholesterol synthesis and palmitate production continue, but VLDL cannot leave the liver

  • Nonalcoholic fatty liver disease (NAFLD)- Often linked to apoB-100 transport defects and hepatic lipid accumulation; insulin resistance contributes to NAFLD progression

  • Regulation of hepatic VLDL secretion by diet & hormones- Fed state: insulin promotes lipogenesis; insulin also activates LPL to process circulating lipoproteins

    • LPL action on VLDL and chylomicrons hydrolyzes TAGs to FFAs for storage or energy

Cholesterol Biosynthesis & Regulation (Expanded)

  • Pathway overview- Acetyl-CoA + Acetoacetyl-CoA

    HMG-CoA

    • HMG-CoA reductase reduces HMG-CoA to mevalonate (rate-limiting step)

    • Mevalonate

-

cholesterol through downstream steps

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  • Regulation of HMG-CoA reductase- Inhibited by cholesterol via negative feedback, by glucagon, and by statins

    • Activation stimulates cholesterol synthesis; regulation matches cellular cholesterol needs

Hormones, Signaling & Genomic Regulation

  • Hormone types and hydrophilicity/hydrophobicity- Hydrophilic hormones (e.g., peptide hormones, catecholamines): stored in vesicles; short-to-intermediate half-lives; act on surface receptors

    • Hydrophobic hormones (steroids, thyroid hormones): diffuse through membranes; long half-lives; often bind to intracellular receptors (nuclear receptor family), regulating gene transcription

  • Four signal transduction pathways for hydrophilic hormones- Integrin-mediated signaling (growth signals)

    • Ligand-gated ion channels (neurohormones)

    • Receptor tyrosine kinases / receptor enzymes (example: leptin via JAK/STAT)

    • GPCRs (adenylyl cyclase

--cAMP, PKC