BMS-707035 729607-74-3

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Molecular Weight:

410.42 BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.

Biological Activity

BMS-707035 is a pyrimidine carboxamide similar to Raltegravir, the first
Integrase Inhibitor licensed for clinical use. BMS-707035 is a potent,
specific, and reversible HIV-I integrase (IN) inhibitor that blocks HIV
IN strand transfer activity with IC50 of 15 nM. However,
several IN mutations, including V75I, Q148R, V151I, and G163R are found
to confer resistance to HIV IN Inhibitors.


The binding of BMS-707035 and
target DNA to IN are mutually exclusive events, as revealed by the fact
that the inhibition of strand transfer catalysis by BMS-707035 is
overcome by increasing amount of target DNA. The binding affinity of
BMS-707035 to IN is also affected by the four terminal bases at the 5'
end of the pre-processed U5 long terminal repeat (LTR).


Gln148 of IN is crucial for the binding of BMS-707035 to IN. The 3' terminus of the viral LTR, on the other hand, retards the rate
of BMS-707035 association with IN, by regulating the kinetics of binding
and dissociation.

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Product Categories : Microbiology > Integrase Inhibitor