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Summary
Body_ID: HC005025
Most metabolism is catalyzed by biological catalysts - enzymes. Their catalytic activities are apparent at body temperature, and they are strictly regulated by several mechanisms. Both covalent and noncovalent modifications are involved in this regulation and allow for efficient metabolic control. Enzyme activity can be inhibited (or activated) by synthetic compounds (drugs), exogenous compounds (toxins), as well as endogenous compounds (allosteric effectors). Kinetic analyses of enzymatic reaction are beneficial for evaluating the biological role of enzymes and for elucidating their reaction mechanisms. In addition, assays of enzymes in blood are useful for diagnosis of some diseases. Uncontrolled enzymatic activity, however, sometimes causes serious diseases. In such cases, appropriate inhibitors are quite useful for therapeutic purposes.
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ACTIVE LEARNING
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  1. In a multi-step sequence of enzymatic reactions, where is the most effective site for controlling the flux of substrate through the pathway. What effect will an inhibitor of a rate-limiting enzyme have on the concentration of substrates in a multi-step pathway?
  2. Most drugs are designed to inhibit specific enzymes in biological systems. The drug, Prozac, has had a profound effect on the medical treatment of depression. Review the history of development of Prozac, illustrating the importance of specificity in the mechanism of drug action.
  3. Discuss some examples of reversible and irreversible enzyme inhibitors used in medical practice.
  4. Knock-out mice are mice that lack a specific gene. Discuss the impact of KO-mice on the direction of drug development in the pharmaceutical industry.
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Further reading
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Hammes GG. Multiple conformational changes in enzyme catalysis. Biochem 2002;41:8221-8. Full articleGo to this article on the publisher's site
Body_ID: R005001
Andersson I, van Scheltinga AC, Valegard K. Towards new beta-lactam antibiotics. Cell Mol Life Sci 2001;58:1897-906.
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Christen P, Mehta PK. From cofactor to enzymes. The molecular evolution of pyridoxal-5'-phosphate-dependent enzymes. Chem Re. 2001;1:436-447. Full articleGo to this article on the publisher's site
Body_ID: R005003
Piliero PJ. Atazanavir: a novel HIV-1 protease inhibitor. Expert Opin Investig Drugs 2002;11:1295-1301.
Body_ID: R005004
Matschinsky FM. Regulation of pancreatic beta-cell glucokinase: from basics to therapeutics. Diabetes 2002;51(Suppl 3):S394-S404.
Body_ID: R005005
Michaelis ML. Drugs targeting Alzheimer's disease: some things old and some things new. J Pharmacol Exp Ther 2003;304:897-904.
Body_ID: R005006
Malasky BR, Alpert JS. Diagnosis of myocardial injury by biochemical markers: problems and promises. Cardiol Rev 2002;10:306-317. Full articleGo to this article on the publisher's site
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Relevant websites
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Case Studies, many employing clinical enzyme analysis: http://path.upmc.edu/cases/index.htmlOpen this link in a new window Full articleGo to this article on the publisher's site
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Clinical Enzymology: http://www.qub.ac.uk/cm/cb/text/studgide;Open this link in a new window http://www.labtestsonline.org/Open this link in a new window Full articleGo to this article on the publisher's site
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Enzyme Kinetics: http://www.indstate.edu/thcme/mwking/enzyme-kinetics.html;Open this link in a new window Full articleGo to this article on the publisher's site
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http://www-biol.paisley.ac.uk/kinetics/contents.htmlOpen this link in a new window Full articleGo to this article on the publisher's site
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International Federation of Clinical Chemistry and Laboratory Medicine: http://www.ifcc.org/ifcc.aspOpen this link in a new window Full articleGo to this article on the publisher's site
Body_ID: R005012
Body_ID: P0063
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