GENES

Tyrosine kinases of the Janus family

What enzyme family is related to cytokine receptors?

Nuclear receptors

What type of receptors, when activated, bind directly to DNA and act as transcription factors?

Enoyl reductase (mycobacterial)

What enzyme, produced by M. tuberculosis, is inhibited by the drug Isoniazid?

Cyclooxygenase (COX)

What enzyme, also known as prostaglandin endoperoxide synthase, converts arachidonic acid into prostaglandins and is inhibited by acetylsalicylic acid?

Prostaglandin endoperoxide synthase

What is another name for Cyclooxygenase, an enzyme that converts arachidonic acid into prostaglandins?

Bacterial serine protease

What enzyme is directly inhibited by beta-lactams like penicillin?

Carbonic anhydrase

What enzyme in the eye maintains fluid balance and is inhibited by Acetazolamide?

Human antithrombin

What human protein is activated by heparins to prevent blood clotting?

DNA/RNA

What nucleic acids are established drug targets?

Tyrosine kinases

What are dimeric enzyme receptors that have intrinsic enzyme activity?

Insulin Receptor (IR)

What specific receptor type triggers a sequence of enzymes to ensure the target cell takes up glucose?

IL-2 receptor

What cytokine receptor is associated with tyrosine kinases of the Janus family and utilizes the JAK/STAT pathway?

JAK/STAT pathway

What signaling pathway acts as an expressway from the extracellular environment to the nucleus, resulting in quicker and more direct effects?

Nuclear receptors

What type of receptor needs to undergo dimerization and be activated by molecules like hormones to directly recognize DNA sequences?

Nuclear receptors

What type of receptor has generalized and broad outcomes, and has been linked to the development of certain cancers?

G-protein coupled receptors (GPCRs)

What type of receptors respond to neurotransmitters like serotonin and insulin, and can amplify a single molecule's signal up to 100 million times?

Wnt and Hedgehog pathways

What are other signaling pathways, distinct from GPCRs, that involve 7-pass transmembrane proteins and different secondary messengers?

NTR1

What neurotensin receptor, when acting as a heterodimer with D2R, can inhibit D2R?

D2R

What dopamine receptor can be inhibited by NTR1 in a heterodimeric interaction?

MAPK-SRE pathway

What specific signaling pathway can have its cell signaling pathway preserved despite interactions between different receptors like NTR1 and D2R?

Toll-like receptors (TLRs)

What receptors are involved in positive signal crosstalk within the immune system, contributing to synchronized inflammatory responses?

Wnt and Notch system

What specific cell growth and differentiation pathways contribute to positive signal crosstalk, such as in supporting the creation of new tissues?

Free form of drugs

What form of drugs in the blood is the active form and binds to receptors to exert an effect?

Protein-bound drugs

What form of drugs in the blood are initially inactivated unless released from plasma proteins like albumin?

Albumin

What specific plasma protein is the primary one for non-specific drug binding, acting as a reservoir for drugs and whose alterations can affect free drug concentrations?

Globulin

What plasma protein, along with albumin, can bind to drugs and affects their distribution and metabolism?

Microsomal P-450 enzymes

What enzymes are unable to metabolize drugs when they are bound nonspecifically to plasma proteins?

Glomerulus

What part of the kidney cannot filter drugs that are bound nonspecifically to plasma proteins?

CYP enzyme (Cytochrome P450)

What enzyme is centrally involved in drug biotransformation, converting lipophilic substances to water-soluble compounds for excretion?

UGT-UDP-GA (UDP-Glucuronosyltransferase)

What enzyme facilitates the conjugation of metabolites like 4-Hydroxy-phenytoin by adding glucuronide, making them highly water-soluble?

Gastric acid

What initial substance in the GI tract can metabolize or modify oral drugs, significantly reducing the absorption of drugs like Penicillin?

Esterases and lipases (digestive enzymes)

What enzymes in the gastrointestinal wall contribute to the metabolism of orally administered drugs such as Insulin and Epinephrine?

B-glucuronidase

What enzyme, found in the GI wall, specifically hydrolyzes glucuronide to aid in drug absorption?

Bacterial flora

What component of the gastrointestinal wall can perform metabolic reductions of aromatic nitro and azo compounds?

Oxidative enzymes

What type of enzymes, crucial for Phase 1 reactions, are predominantly located in the smooth endoplasmic reticulum (SER) of the liver?

Cytochrome P450 (P450)

What is the central enzyme of the Phase 1 oxidative cycle, responsible for attaching an -OH group to drugs, making them more polar?

NADPH

What molecule provides electrons to P450 Reductase, which are then used by P450 to oxidize drug substrates?

P450 Reductase

What enzyme acts as an intermediary, accepting electrons from NADPH and transferring them to Cytochrome P450 during the oxidative cycle?

CYP3A4/5

What specific CYP enzyme family mediates 50% of all Phase 1 metabolic reactions in the liver?

UDP-Glucuronosyltransferase (UGT)

What is the most prevalent transferase enzyme in Phase 2 reactions, primarily responsible for glucuronidation?

CYP3A4/5 and UGT

What two major enzyme systems are responsible for metabolizing three-quarters of all currently used drugs?

CYP1A1

What specific CYP enzyme is involved in the metabolism of Caffeine, Testosterone, and R-Warfarin?

CYP1A2

What specific CYP enzyme is involved in the metabolism of Acetaminophen, Caffeine, Phenacetin, and R-Warfarin?

CYP2A6

What specific CYP enzyme is involved in the metabolism of 17β-Estradiol and Testosterone?

CYP2B6

What specific CYP enzyme is involved in the metabolism of Cyclophosphamide, Erythromycin, and Testosterone?

CYP2C-family (CYP2C8, 2C9, 2C19)

What specific CYP enzyme family is involved in the metabolism of Acetaminophen, Tolbutamide, Hexobarbital, S-Warfarin, Phenytoin, Testosterone, and Zidovudine?

CYP2E1

What specific CYP enzyme is involved in the metabolism of Acetaminophen, Caffeine, Chlorzoxazone, and Halothane?

CYP2D6

What specific CYP enzyme is involved in the metabolism of Acetaminophen, Codeine, and Debrisoquine?

CYP3A4

What specific CYP enzyme has the broadest substrate specificity, metabolizing a large number of prescription drugs, including Carbamazepine, Cortisol, and Phenytoin?

Flavin monooxygenase

What enzyme carries out CYP450-independent oxidation reactions?

Transferases

What general class of enzymes is required for Phase 2 reactions to couple drugs with endogenous substances?

Glutathione S-transferase (GST)

What specific transferase catalyzes the conjugation of electrophilic compounds (e.g., epoxides, nitro groups) with glutathione for detoxification?

N-Acetyltransferase (NAT)

What specific transferase catalyzes the addition of an acetyl group to amine-containing drugs like isoniazid and sulfonamides?

Sulfotransferase (SULT)

What specific transferase catalyzes the addition of a sulfate group to phenols, alcohols, and aromatic amines?

Thiopurine methyltransferase (TPMT)

What specific transferase is mentioned as contributing to Phase 2 metabolism?

Acyl-CoA glycine transferase

What specific transferase, found in the mitochondria, is involved in conjugating acyl-CoA derivatives of carboxylic acids with glycine?

Methyltransferase

What general class of transferase enzymes is involved in methylation, a minor pathway that inactivates drugs and is crucial for biosynthesis of some compounds?

Phenol-O-methyltransferase

What specific methyltransferase is involved in Phase 2 methylation?

Nonspecific N-methyltransferase

What specific methyltransferase is involved in Phase 2 methylation?

S-methyltransferase

What specific methyltransferase is involved in Phase 2 methylation?

Catechol-O-methyltransferase (COMT)

What specific methyltransferase is widely distributed and responsible for inactivating biogenic amines like dopamine and norepinephrine?

N-acetyltransferase 2 (NAT2)

What specific enzyme is responsible for the acetylation of isoniazid, and whose genetic polymorphism ("rapid acetylators" vs. "slow acetylators") affects isoniazid dosage?

Carboxyl esterases

What enzymes metabolize the inactive pro-drug Enalapril into its active form, Enalaprilat?

Alcohol dehydrogenase

What liver enzyme is the primary enzyme converting ethanol to acetaldehyde?

Aldehyde dehydrogenase

What enzyme converts acetaldehyde to acetate, and a deficiency in which leads to the "Asian flush" phenomenon and increased toxicity from alcohol?

Catalase

What enzyme contributes to the conversion of ethanol to acetaldehyde?

P4502E1

What enzyme system contributes to the conversion of ethanol to acetaldehyde, besides alcohol dehydrogenase and catalase?

Pyridoxine Phosphokinase

What enzyme is inhibited by isoniazid hydrazones, preventing the conversion of vitamin B6 into its active form (pyridoxal 5’ phosphate)?

Isoniazid hydrazones

What specific metabolites of isoniazid cause toxicity by inhibiting Pyridoxine Phosphokinase?

Glutamic acid decarboxylase

What enzyme, whose function is to convert glutamic acid to GABA, is inhibited by isoniazid, leading to neurological side effects?

Hepatic microsomal enzymes

What enzymes can be induced, leading to an increased rate of drug metabolism, decreased drug plasma concentration, and reduced bioavailability?

P450s

What specific enzymes can be inactivated or have their degradation enhanced by inflammatory mediators, cytokines, and nitric oxide, thereby impairing drug metabolism?

CYP1A

What specific CYP enzyme can be induced by consuming charcoal-grilled meat and cruciferous vegetables?

CYP3A

What specific CYP enzyme is notably inhibited by grapefruit consumption?

Glutathione (GSH)

What endogenous substance conjugates with the toxic NAPQI form of acetaminophen, converting it into non-toxic forms like cysteine and mercapturic acid?

Plasma proteins

What substances, when bound by highly protein-binding drugs like sulfonamides in neonates, can displace bilirubin, leading to hyperbilirubinemia and brain damage (kernicterus)?

Lidocaine

What common anesthetic drug targets voltage-gated ion channels by affecting membrane potential?

Tetrodotoxin

What toxin drug, obtained from fugu, targets voltage-gated channels and can paralyze the lungs and diaphragm, causing numbness?

Acetylcholine

What specific molecule or drug stimulates ligand-gated ion channels, important for homeostasis?

Serotonin

What specific molecule or drug stimulates ligand-gated ion channels?

GABA

What specific molecule or drug stimulates ligand-gated ion channels?

Glutamate

What specific molecule or drug stimulates ligand-gated ion channels?

Streptomycin

What antibiotic drug targets tension-gated ion channels?

Gadolinium

What imaging contrast agent drug targets tension-gated ion channels?

Tarantula venom

What substance is an example of a molecule targeting tension-gated ion channels?

Enzymes

What drug targets catalyze reactions through initiation (reactants binding to active site), transition state facilitation (lowering activation energy), and termination (product release), while remaining unchanged?

Receptors

What drug targets respond to environmental stimuli, are distance-dependent, and are distributed both inside and outside cells, near or far from effector molecules?

Ion transporters

What are a type of cell surface receptor that mediates drug-effector interaction?

Ion channels

What are a type of cell surface receptor that mediates drug-effector interaction?

GPCR (G-protein Coupled Receptors)

What are a type of cell surface receptor that mediates drug-effector interaction?

Enzyme-linked receptors

What are a type of cell surface receptor that mediates drug-effector interaction?

Nicotinic cholinoceptor

What ligand-gated ion channel is rapidly acting and is a heteropentamer of four subunit types in the neuromuscular junction?

Nicotinic cholinoceptor

What ligand-gated ion channel in the brain can be a heteropentamer or homopentamer composed of two subunit types?

Muscarinic cholinoceptors

What G protein-coupled receptors have acetylcholine as a common ligand and are membrane-bound, found at the cytosol surface?

G protein-coupled receptors (GPCRs)

What receptors are characterized by a 7-pass protein configuration, where a single polypeptide chain passes the lipid bilayer seven times?

G protein-coupled receptors (GPCRs)

What receptors utilize various second messengers such as Ca2+, cAMP, and inositol-3-phosphate, which contribute to their diverse effects?

Gi (GPCR subtype)

What specific GPCR subtype is responsible for the cycling of cAMP and can inhibit adenylyl cyclase?

Gq (GPCR subtype)

What specific GPCR subtype involves the production of phospholipase C and uses diacylglycerol (DAG), inositol-3-phosphate (IP3), and Calcium (Ca2+) as second messengers?

Receptor Tyrosine Kinase (RTK)

What type of dimeric enzyme receptor has intrinsic enzyme activity and utilizes scaffolding proteins to keep signaling modules in close proximity, enhancing specificity?

Insulin receptor (IR)

What specific RTK exhibits high specificity due to signaling and scaffolding proteins, triggering a sequence of enzymes that ensures targeted glucose uptake?