Types of inhibtors Med Chem Ch. 7
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| Does Rev. Inhibitor under go rxn with active site? | No
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| Rev. inhibition depends on what factors? | Binding strength and [Inhibitor]
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| Rev. inhibitor is likely similar to... | substrate, product, or cofactor
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| For Rev. Inhibitor, increase [substrate] results in... | lowering inhibition
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| Ex. of Rev. Inhibitors | Diuretics
ACE inhibitors
Statins
Sulfonamides
Protease inhibitors
Kinase inhibitors
antidepressants
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| What bonding occurs between Irrev. inhibitor and active site? | Covalent
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| For Irrev. inhibitor, increase[substrate].... | does not affect inhibition
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| Irrev. inhibitor likely similar to... | substrate
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| Ex. of Irrev. inhibitors | Nerve gases
Penicillins
Disulfuram
Cephalosporins
Proton pump inhibitors
Orlistat
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| Orlistat (anti-obesity drug) inhibits.... | pancreatic lipase (digests fats)
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| Orlistat is a ______ inhibitor | Irreversible
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| Irrev. inhibitor binds to _____ site of enzyme | active site
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| Rev. inhibitor binds to _____ site of enzyme | active site
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| Allo. inhibitor binds to ____ site of enzyme | allosteric site
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| Allo. inhibitor binds rev. or irrev. to enzyme? | reversible binding
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| For Allo. inhibitor, increase [substrate]... | does not reverse inhibition
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| Is Allo. inhibitor similar to substrate? | not similar to substrate
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| How does Allo. inhibitor inhibit enzyme? | Binds to allosteric site, alters shape of enzyme (and active site), substrate can't bind
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| Ex. of Allo. inhibitor | 6-Mercaptopurine
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| 6-Mercaptopurine blocks synthesis of ____ and ____ | purines and DNA
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| 6-Mercaptopurine used to treat... | leukemia
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| Transition-state inhibitors bind rev or irrev. to enzyme? | reversible inhibition
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| Transition-state inhibitors are similar to... | transition state of catalyzed rxn
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| Transition-state inhibitors bond to ____ site of enzyme | active site
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| Transition-state inhibitors bind more strongly than drugs that mimic ____ or ____ | substrate or products
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| Renin inhibitor blocks synthesis of... | angiotensin I & II
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| Renin inhibitor produces what effect in body? | lowers blood pressure (anti-hypertensive)
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| Ho does Renin inhibitor work? | Mimics one -OH binding group and tetrahedral geometry
Binds to actives site but has to leaving group
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| Ex. Tansition-state inhibitors | ACE inhibitors
Protease inhibitors
Statins
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| Suicide inhibitors bind rev. or irrev. to enzyme? | Irreversible binding
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| Suicide inhibitors bind to ____ site of enzyme | active site
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| Ex. Suicide inhibitors | Trifluoroalanine
Tienilic Acid
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| Trifluoroalanine blocks | alanine transaminase
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| Trifluoroalanine similar to... | rxn substrate
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| How does Trifluoroalanine work? | has -CF3 (base removes 1 F) group that resembles -CH3 rxn binding group
Enzyme Nu covalently binds to -CF2
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| Tienilic Acid covalently binds to ____ (amino acid) | cyctein (-CH2-SH)
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| Tienilic Acid inhibits _______ enzymes | cytochrome P450
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| Useful Antibacterial targets: ______ and _______ | Dihydropteroate synthetase and transpeptidase
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| Useful Antiviral targets: _____ , ______ and ______ | HIV reverse transcriptase , HIV protease and viral DNA polymerase
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| Useful Anti-inflammatory target: _____ | Cyclooxygenase
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| Usefule Cholesterol-lowering target: _____ | HMG-CoA reductase
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| Useful Antidepressant target: _____ | Monoamine oxidase
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| Useful Anti-cancer targets: _____ , _____ , ______ and _______ , ect. | Tyrosine kinase , Dihydrofolate reductase , thymidylate synthase and aromatase
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