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MED CHEM TERM 1 - Coggle Diagram
MED CHEM TERM 1
Drug Targets
Transmembrane Receptors
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Epidermal growth factor
- active site on each half of dimer
- EGF binds triggering dimerization which catalyzes phosphorylation of tyrosine which can then bind to other proteins and enzymes
Insulin receptors
- exists at heterotetrameric state and insulin binding causes phosphorylation
Growth hormone receptor
- tetrameric complex binds growth hormone, dimerizes and then binds kinases to do phosphorylation
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Nucleic Acids
- nucleosides: sugar + base
- nucleotide: sugar + phosphate + base
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Intracellular Receptors
- important for gene expression
- hydrophobic
- zinc ions = stabilization and conformation
- 8/9 cysteine bind zinc
- zinc finger domains bind target molecule
Enzymes
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active site:
- more hydrophobic
- induced fit model
- bond rotation can occur
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nucleophillic groups: react w substrate to form less energy using intermediates. usually cys and ser (OH and SH) are good
chymotrypsin: digestive enzyme where catalytic triad positions itself correctly for enzymatic activity (asp, his, ser)
regulation:
- allosteric inhibition: inc substrate doesn't reverse inhibition
- intermolecular bond formation
- induced fit change enzyme shape
- active site distorted
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Other
types of signaling
endocrine: hormone
paracrine: cell to other cell
autocrine: cell onto itself
plasma membrane shared cells
desolvation penalties
when a substrate wants to bind to an enzyme they must be solvated to get rid of water molecules before binding
therapeutic index: TD/ED want it to be small so that you need lots to be toxic and a little to be effective
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