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