HomeCoursesMEDSCI 204: Pharmacology and ToxicologyLecture 20 Lecture 20 1. How are drug targets discovered? Comparing genomes of cancer cells and normal cells, comparing tissue differences (mRNA/protein levels)How are drug targets discovered? == Comparing genomes of cancer cells and normal cells, comparing tissue differences (mRNA/protein levels) 2. How is genetic characterisation for determining if a particular gene is relevant to a disease? Remove gene product, replace gene product with an inactive form, increase the levels of the gene productHow is genetic characterisation for determining if a particular gene is relevant to a disease?== Remove gene product, replace gene product with an inactive form, increase the levels of the gene product 3. What is parmacological characterisation to determine disease relevance? Modulate product activityWhat is parmacological characterisation to determine disease relevance? ==Modulate product activity 4. What are examples of serendipitous discoveries? Penicillin, nitrogen mustards for chemotherapyWhat are examples of serendipitous discoveries?== Penicillin, nitrogen mustards for chemotherapy 5. What is a hit? When a molecule binds target and modulates activityWhat is a hit?== When a molecule binds target and modulates activity 6. What links biological research to correct compounds/chemistry? AssaysWhat links biological research to correct compounds/chemistry?== Assays 7. What are phenotypes of cancer? Unrestrained proliferation, evasion of growth suppresion genesWhat are phenotypes of cancer?== Unrestrained proliferation, evasion of growth suppresion genes 8. What is phenotype screening? Many compounds assayed with cells to discern if an effect is produced on disease trait (phenotype)What is phenotype screening?== Many compounds assayed with cells to discern if an effect is produced on disease trait (phenotype) 9. What are some drug binding sites? substrate binding sites, orthosteric sites, allosteric sites, protein-protein interactionsWhat are some drug binding sites?== substrate binding sites, orthosteric sites, allosteric sites, protein-protein interactions 10. What is an analogue? Compounds closely related to a ligandWhat is an analogue? ==Compounds closely related to a ligand 11. What are compound sources? Plants, hormones, synthetic, drug repurposingWhat are compound sources?== Plants, hormones, synthetic, drug repurposing 12. How is binding detected? Inhibition of enzyme activityHow is binding detected?== Inhibition of enzyme activity 13. Where do kinase inhibitors usually bind? ATP sitesWhere do kinase inhibitors usually bind?== ATP sites 14. What kind of interaction binds kinase inhibitors? Ionic, hydrophobic, H-bondsWhat kind of interaction binds kinase inhibitors?== Ionic, hydrophobic, H-bonds Loading...