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Molecular Pharmacology > Respiratory > Flashcards

Flashcards in Respiratory Deck (7):
1

Number drugs in development since completion of human genome project

Approvals

Up 62%
Down 25%- phase 2 failures

2

Amiloride

ENac blocker
Diuretic
Potassium sparing

3

Benefits of reverse pharmacology (3)

Historical success
Likely to find drug-like compounds
Insight into target biology

4

Drawback of reverse pharmacology

Will target be relevant to disease

5

FSK

Toxin
Activation of AC
Increase in cAMP
CFTR phosphorylation
Channel opens

6

Genistein

Enhances CFTR activity has little effect on current at 37 but increases current at 26

Lower temperature seems to facilitate processing of F508

Still only 10% of WT

7

Frequency of F508

More than 90% patients have at least one copy

49% are homozygous