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MPET2008-HI - 1 - DRUG DEVELOPMENT Next to diagnostic tests, drug development is the major area where biotechnology (in the broadest sense, so including molecular life sciences) contributes to health care. This contribution not only consists of the production of therapeutic proteins or (in the future) approaches such as gene therapy and stem cell therapy, but became also very important in the development of classical (organic chemical) drugs. In the quest for the pathogenic mechanisms of diseases, the identification and validation of targets for drug development and in the screening of candidate drugs, applications of biotechnology nowadays form an essential part. Drugs can be developed in different ways: direct identification (e.g. insulin, erythropoietin), by serendipity (the faculty of making happy and unexpected discoveries by accident, e.g. penicillin) and through rational screening. In drug development different stages can be identified: 1. Discovery Research 2. Preclinical testing 3. Clinical testing 4. Registration and marketing 5. Post-marketing surveillance I. Discovery Research The deliverable of discovery research is the isolation or synthesis of a new substance having biological activity and potential therapeutic value. Using direct identification or serendipity the new substance is isolated immediately. Most discovery processes, however, use a rational screening. To
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MPET2008-HI - 2 - be able to perform a rational screening, one needs targets. Every drug exerts its activity by interacting with a molecule and by modulating the activity of that molecule (increase, inhibit, modify). This molecule was classically called a receptor” in pharmacology (not to be confounded with the term receptor in signal transduction), but more recently the term target is used. Depending on the modulation exerted by the drug terms as agonists (mimic an activity) and antagonists (inhibits an activity) are used. These can be competitive/non- competitive, complete or partial, and allosteric. Discovery research using screening consists of a number of stages: Ia. Target identification Ib. Target validation Ic. Assay development Id. High throughput screening and lead-identification Ie. Lead optimization/candidate selection Ia. Target identification In principle, every molecule involved in the pathogenesis is a (candidate) target. Molecules of which the quantity or activation state (e.g. phosphorylation) changes in the disease process relative to the healthy situation, and which changes correlate with the effect under study are commonly considered as potential targets. Targets can be identified by molecular analysis. Nowadays more and more use is made of the possibilities of the “omics” (genomics, proteomics,… ) to identify targets, not only analytical but also by interference screening (e.g. RNAi). Within the targets one sometimes uses the concept drugable target . It is indeed so that experience has learned that some targets result more easily in modulating drugs than others. So, e.g. enzymes and
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This note was uploaded on 05/28/2010 for the course WE BIBI000000 taught by Professor Johangrooten during the Spring '10 term at Ghent University.

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