PCL102H1 Lecture 4: Identification and Validation
31 Jan 2019
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Document Summary
Target identification and target validation fits in the drug discovery pipeline. Macromolecules are possible drug targets although, most come with complications (e. g. carbs = toxicity, lipids = low specificity, and nucleic acids = hard ot find potent compounds), however, proteins are good targets (96% of targets are proteins) Receptor is a biological molecule to which a drug binds in order to produce an effect. Involved in cellular communication: mostly cell surface proteins, can be inside cell. Receptors bind chemical messengers (e. g. hormones) and these are called ligands from there the binding relays the message to the cell and the cell might change its function. Signal transduction is when extracellular signalling molecules activates cell surface receptor: receptors alters intracellular molecules to generate a response, often a second messenger mediates signaling inside the cell. Substrates fit into active sites and the reaction occurs between the enzyme-substrate complex. Products do not fit as well into the active site and therefore dissociate spontaneously.
