Raltegravir Mechanism

[Dr Hunter]

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Hello guys,

I'm really interested about Integrase(IN) Inhibitors and I was searching for their detailed mechanism of action and binding...

What I found is that Mg++ is an important ion for IN activation and a domain in IN binds with it and Raltegravir binds with Mg and chelates it... Here is the question; Does it bind to IN and then to Mg or just binds to Mg, and if the answer is the second, why doesn't it bind to any Mg ion in the body, why just that Mg required for IN activation?

Thanks

 

[RxMonkey]

Raltegravir binds to Mg++ in the HIV-1 IN active site. I imagine that raltegravir's specificity has to do with geometric orientation of the 2 Mg++ in the active site.

For a more verbose explaination http://www.pnas.org/content/109/7/2251.full.

 

[Dr Hunter]

The Mg++ is divalent how come it binds to IN and Raltegravir in the same time, thanks for the reply, but I need more enlightenment.