Uses of Protein Structure

Question 1

NMR/X ray crystallography

Answer 1

Structure of protein/binding interactions

AND surface not used for binding

Can modify these

Question 2

Structure is important becuase

Answer 2

Used when you have lead compound

Can design structure from random protein-no lock and key

Question 3

Potential drug steps

Answer 3

screen vs target protein
lead compound
find strcuture
redisgn
synthesis
test
prelinical
clincal
drug

Question 4

surfaces not used for binding function in designing drugs

Answer 4

change solubility and other nonbonding things

Question 5

diabetes

Answer 5

muscles decrease glucose uptake

pacnrease stops making functional insulin

liver increases glucose production

MI, stroke, vision loss, etc

Question 6

GLP1/GIP

Answer 6

Produced in stomach

Regulate glucose and apetite

Degraded by DPP4 quickly

Question 7

DPP4 in mouse trials

Answer 7

great-left GLP/GIP in system to good benefits

toxic to higher order species

Question 8

Ideal drug characteristics (really 3)

Answer 8

improve binding

good pharmokinetc props (solubility/permeability)

specificity up

combat drug resistance

stabiltze vaccine

Question 9

DPP4 story

Answer 9

got 2 lead components

crsyallize binding of DPP4 with target proteins

took parts from 2 lead components that were the binding regions

final product way different but had some key structures that were initial two lead components