Alain 3

Question 1

How to obtain Enz. inhibitors?

Answer 1

1. Screening library to isolate Hits and fragment Hits.
2. Virtual screening (Docking) base on Enz. Struc.
3. Starting from substrate or product stucture

Question 2

How to improve efficiency of an inhibitor?

Answer 2

1. Synthesize hit derivatives and SAR base on biological evaluation.
2. Molecular modelling.
3. XR and NMR studies
4. Use the target Enz. mechanism.

Question 3

Understand enz. mechanism cam help

Answer 3

medicinal chemists design more powerful inhibitors.

Question 4

Wt is prodrug?

Answer 4

Is a pharmacological substance that is administered in an inactive (or less than fully active) form and is subsequently converted to an active pharmacological agent (drug) mainly through metabolic processes (bioactivation).

Question 5

TS inhibitors

Answer 5

Mimic TS in the reaction between E and S.
–> High specificity and affinity.
Usually discovered by screening natural products.

Question 6

Some note about cholesterol:

Answer 6

1. biosyn. & cell membrane
2. excess –> cardiovascular disease
3. LDL and HDL supply the traspormation of fatty acids
4. LDLs carry cholesterol to cell
5. HDLs carry cholesterol from cell to liver
6. Mortality associated with Low HDL or high LDL
7. Cause fatty plaques in arteries that cause artherosclerosis, stroke, heart attack, clot formation.