2z4o: Difference between revisions

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[[Image:2z4o.jpg|left|200px]]
{{Seed}}
[[Image:2z4o.png|left|200px]]


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{{STRUCTURE_2z4o|  PDB=2z4o  |  SCENE=  }}  
{{STRUCTURE_2z4o|  PDB=2z4o  |  SCENE=  }}  


'''Wild Type HIV-1 Protease with potent Antiviral inhibitor GRL-98065'''
===Wild Type HIV-1 Protease with potent Antiviral inhibitor GRL-98065===




==Overview==
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The potent new antiviral inhibitor GRL-98065 (1) of HIV-1 protease (PR) has been studied with PR variants containing the single mutations D30N, I50V, V82A, and I84V that provide resistance to the major clinical inhibitors. Compound 1 had inhibition constants of 17-fold, 8-fold, 3-fold, and 3-fold, respectively, for PR(D30N), PR(I50V), PR(V82A), and PR(I84V) relative to wild type PR. The chemically related darunavir had similar relative inhibition, except for PR(D30N), where inhibitor 1 was approximately 3-fold less potent. The high resolution (1.11-1.60 Angstrom) crystal structures of PR mutant complexes with inhibitor 1 showed small changes relative to the wild type enzyme. PR(D30N) and PR(V82A) showed compensating interactions with inhibitor 1 relative to those of PR, while reduced hydrophobic contacts were observed with PR(I50V) and PR(I84V). Importantly, inhibitor 1 complexes showed fewer changes relative to wild type enzyme than reported for darunavir complexes. Therefore, inhibitor 1 is a valuable addition to the antiviral inhibitors with high potency against resistant strains of HIV.
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{{ABSTRACT_PUBMED_17696515}}


==About this Structure==
==About this Structure==
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[[Category: Protease inhibitor]]
[[Category: Protease inhibitor]]
[[Category: Wild type protease]]
[[Category: Wild type protease]]
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