PHAR 435 Lecture Notes - Lecture 4: Idiopathic Pulmonary Fibrosis, Protein Kinase Inhibitor, Sh2 Domain

• School: UBC
• Department: Pharmaceutical Sciences
• Course: PHAR 435
• Professor: Stelvio Bandiera

Document Summary

Identification of (cid:862)(cid:272)o(cid:373)ple(cid:373)e(cid:374)tary(cid:863) (cid:271)i(cid:374)di(cid:374)g sites not used by atp. Kinase inhibitors were developed to target cancer cells more efficiently than conventional chemotherapy, so that the function of normal cells remain intact. 28 kinase inhibitors have been approved (28 = cancer, tofacitinib for ra, nintedanib for idiopathic pulmonary fibrosis: >20 other small molecules are in trials for anti-inflammatory treatment, and others for cns/cv diseases. There are >500 kinases + 900 other proteins with kinase domains. A group of enzymes (sub-group of phosphotransferases) that catalyze the transfer of the -phosphate group from the bound co-factor atp to the hydroxyl group of a substrate molecule. Substrates = lipids, inositols, carbohydrates, nucleosides/ nucleotides, proteins. Protein kinases: substrates = tyrosine, serine, or threonine. ~600 protein kinases are encoded in the human genome (about 2% of all human genes) Up to 30% of all proteins undergo phosphorylation (cid:373)ost of the ti(cid:373)e it"s a er residue that"s phosphor(cid:455)lated (cid:894) er 86%, thr (cid:1005)(cid:1006)%, t(cid:455)r (cid:1006)%(cid:895)