Med Chem :))

(at least the pharmacology exam is moved but i feel like a dog set to be put down given chocolate)

Ion Channel receptor

G Protein-Coupled Receptor

Catalytic receptor

Enzyme-coupled receptor

Intracellular cytoplasmic/nuclear receptor

Enzyme targets

Nuclear receptors

Catalytic receptor

Enzyme-coupled receptor

Ion channel

GPCRs

GPCR

5-HT2B Receptor

GPCR

5-HT2C

GPCR

Muscarinic receptor

GPCR

Opioid Receptor

GPCR

Nicotinic Receptor

Ion channel

GABA-A receptor

Ion channel

GABA-A Receptor

Ion channel

GABA-A

Ion channel - top view

Muscimol

GABA Agonist

Bicuculline

GABA Antagonist (ion channel)

Alprazolam (benzodiazepine)

1,2,4-triazole

GABA agonist (ion channel)

Name of bond in red?

Peptide bond

Norepinephrine (R)

GPCR agonist (all catecholamines are)

(R)-(--)-Epinephrine: more interactions w/binding pocket

Morphine

opioid agonist (GPCR)

Gepirone

5-HT1a agonist (GPCR)

Steroid

6-6-6-5 ring structure

9-cis-retinoic acid

Nuclear receptor binder (PPAR-RXR dimer)

Derived from vitamin A

nuclear receptor

Retinoid x receptor

nuclear receptor

Retinoid x receptor

captopril

SH binds Zinc (II) on ACE

(enzyme-coupled receptor - intracellular cytoplasmic target)

Enalaprilat

COOH binds Zinc (II) on ACE

(enzyme-coupled receptor )

Enalapril

EtOOC = ester prodrug for oral use

(enzyme-coupled receptor )

PDE-5

(enzyme-coupled receptor - intracellular cytoplasmic target)

sildenafil (PDE-5 inhibitor)

Protein inhibitor (enzyme-coupled receptor - intracellular cytoplasmic target)

sildenafil PDE5 complex

pyrazole N binds to H2O that is H bonded to another water coordinating to Zn ion and to tyrosine

beta lactamase

(enzyme-coupled receptor - intracellular cytoplasmic target)

Clavulanic acid

Beta lactamase inhibitor (suicide inhibitor)

Covalent modification of serine of beta lactamase

(enzyme-coupled receptor - intracellular cytoplasmic target)

DNA topoisomerase I

Cuts DNA during replication and critical for DNA repair

(enzyme-coupled receptor - intracellular cytoplasmic target)

Topotecan

Topoisomerase I inhibitor —> arrests cell cycle at S-phase

Drug will stack right in with DNA base pairs

Topotecan binding topoisomerase I

HMG-CoA Reductase

(enzyme-coupled receptor - intracellular cytoplasmic target)

Lipitor

HmG-CoA reductase inhibitor

(enzyme-coupled receptor - intracellular cytoplasmic target)

Fluoride binds w/arginine

CIpP Protease

Function: regulates degradation of misfolded proteins in human cells

Bortezomib

Proteasome inhibitor (reversible)

Boron (electrophile) has 6 pi electrons and an empty P orbital that can be attached by alcohol-bearing residues — COVALENT BOND W/SERINE OH

Has a pyrazine

HIV-1 Reverse Transcriptase

Used by HIV to do RNA —> DNA

azidothymidine (AZT)

Reverse transcriptase inhibitor

Arrow points to thing that helps inhibit DNA formation - b/c that can’t make the phosphate backbone

EGFR (epidermal growth factor receptor) Tyrosine Kinase

Target for cancer therapy

gefitinib

EGFR inhibitor

Tyrosine kinase target (catalytic receptor)

Afatinib

EGFR inhibitor

Tyrosine kinase target (catalytic receptor)

Osimertinib

EGFR inhibitor

Tyrosine kinase target (catalytic receptor)

Methicillin

Transpeptidase enzyme inhibitor (cell wall synthesis)

Antibiotic

Camptothecin

Topoisomerase inhibitor

Losartan

Losartan - ARB interaction

look for biphenyl ring