PCL102H1 Lecture 3: Target Identification and Validation

• School: UTSG
• Department: Pharmacology and Toxicology
• Course: PCL102H1
• Professor: Rebecca Laposa

Document Summary

Target identification and validation: fits in the discover/preclinical testing section of the drug discovery pipeline. Intro to drug targets: 96% of targets are proteins, most drugs bind to proteins, modifying their activity. What is a receptor: a biological molecule (protein) to which a drug binds in order to produce an effect, bind to chemicals messengers (such as hormones) called ligands. Types of receptors: there are different types of receptors to which drugs bind, effects are generated by different mechanisms. Signal transduction: extracellular signaling molecule activates cell surface receptor -> receptor alters intracellular molecules to generate a response, ofte(cid:374) a (cid:862)se(cid:272)o(cid:374)d (cid:373)esse(cid:374)ger(cid:863) (cid:373)ediates sig(cid:374)ali(cid:374)g i(cid:374)side the (cid:272)ell (cid:449)hi(cid:272)h is ge(cid:374)erated (cid:271)y (cid:862)effe(cid:272)tor(cid:863) proteins. Enzyme-linked receptors: cell surface receptors, bind ligand on the extracellular side and have enzymatic activity on the intracellular side. Example: insulin receptor: the insulin receptor responds to insulin and related growth factors, regulates glucose balance, decreased insulin sensitivity is a feature of type 2 diabetes.