Lecture 20

1.
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 product
3.
What is parmacological characterisation to determine disease relevance?
Modulate product activity
4.
What are examples of serendipitous discoveries?
Penicillin, nitrogen mustards for chemotherapy
5.
What is a hit?
When a molecule binds target and modulates activity
6.
What links biological research to correct compounds/chemistry?
Assays
7.
What 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)
9.
What 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 ligand
11.
What are compound sources?
Plants, hormones, synthetic, drug repurposing
12.
How is binding detected?
Inhibition of enzyme activity
13.
Where do kinase inhibitors usually bind?
ATP sites
14.
What kind of interaction binds kinase inhibitors?
Ionic, hydrophobic, H-bonds