Drug Design Flashcards
1
Q
Uptake transporter for methotrexate
A
Reduced folate carrier RFC
2
Q
How can we retain metho in cells
A
Polyglutamylated
3
Q
Metho is given with another drug when used in high dose
A
Leucovorin (folate) rescure
4
Q
What are the lipopholic anti folates
What is the advantage compare to metho
A
Pyrimethamine Nolatrexed (DHFR TS) Piritrexim Methylbenzoprim (exp) Don’t rely on RFC Can passive diffuse
5
Q
Name two TS inhibitors from the same class and how they act on rec
A
Pemetrexed and raltitrexed
Competitive inhibitor of TS at 5 10 ch2 THF binding site
Reversible binding
6
Q
What’s the name of the type of rxn when dUMP react w TS w THF(CH2)? How does it occur
A
Thiolate group (RS-) from cysteine on active site of TS
Enolate intermediate formed
Enolate is NU
THF change conformation to imime- N+=CH2 EL
Form covalent bond complex
B elimination of TS
7
Q
Explain the MOA of azacytidine
A
Weak inhibitor of TS Pyrimidine inhibitor Tri Pi Incorporate into RNA Unstable and decompose Mimics C in RNA
