2qd8: Difference between revisions

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-[[Image:2qd8.jpg|left|200px]]
+{{Seed}}
+[[Image:2qd8.png|left|200px]]
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 {{STRUCTURE_2qd8|  PDB=2qd8  |  SCENE=  }}
-'''HIV-1 Protease Mutant I84V with potent Antiviral inhibitor GRL-98065'''
+===HIV-1 Protease Mutant I84V with potent Antiviral inhibitor GRL-98065===
-==Overview==
+<!--
-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.
+The line below this paragraph, {{ABSTRACT_PUBMED_17696515}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 17696515 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_17696515}}
 ==About this Structure==
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 [[Category: Hydrolase]]
 [[Category: Protease inhibitor]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Apr 24 09:40:52 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 20:22:41 2008''