9hvp
From Proteopedia
(New page: 200px<br /> <applet load="9hvp" size="450" color="white" frame="true" align="right" spinBox="true" caption="9hvp, resolution 2.8Å" /> '''DESIGN, ACTIVITY AND...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:9hvp.gif|left|200px]]<br /> | + | [[Image:9hvp.gif|left|200px]]<br /><applet load="9hvp" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="9hvp" size=" | + | |
caption="9hvp, resolution 2.8Å" /> | caption="9hvp, resolution 2.8Å" /> | ||
'''DESIGN, ACTIVITY AND 2.8 ANGSTROMS CRYSTAL STRUCTURE OF A C2 SYMMETRIC INHIBITOR COMPLEXED TO HIV-1 PROTEASE'''<br /> | '''DESIGN, ACTIVITY AND 2.8 ANGSTROMS CRYSTAL STRUCTURE OF A C2 SYMMETRIC INHIBITOR COMPLEXED TO HIV-1 PROTEASE'''<br /> | ||
==Overview== | ==Overview== | ||
| - | A two-fold (C2) symmetric inhibitor of the protease of human | + | A two-fold (C2) symmetric inhibitor of the protease of human immunodeficiency virus type-1 (HIV-1) has been designed on the basis of the three-dimensional symmetry of the enzyme active site. The symmetric molecule inhibited both protease activity and acute HIV-1 infection in vitro, was at least 10,000-fold more potent against HIV-1 protease than against related enzymes, and appeared to be stable to degradative enzymes. The 2.8 angstrom crystal structure of the inhibitor-enzyme complex demonstrated that the inhibitor binds to the enzyme in a highly symmetric fashion. |
==About this Structure== | ==About this Structure== | ||
| - | 9HVP is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1] with PHQ as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 9HVP is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1] with <scene name='pdbligand=PHQ:'>PHQ</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=9HVP OCA]. |
==Reference== | ==Reference== | ||
| Line 15: | Line 14: | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Erickson, J.]] | [[Category: Erickson, J.]] | ||
| - | [[Category: Neidhart, D | + | [[Category: Neidhart, D J.]] |
[[Category: PHQ]] | [[Category: PHQ]] | ||
[[Category: hydrolase(acid proteinase)]] | [[Category: hydrolase(acid proteinase)]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 19:18:34 2008'' |
Revision as of 17:18, 21 February 2008
|
DESIGN, ACTIVITY AND 2.8 ANGSTROMS CRYSTAL STRUCTURE OF A C2 SYMMETRIC INHIBITOR COMPLEXED TO HIV-1 PROTEASE
Overview
A two-fold (C2) symmetric inhibitor of the protease of human immunodeficiency virus type-1 (HIV-1) has been designed on the basis of the three-dimensional symmetry of the enzyme active site. The symmetric molecule inhibited both protease activity and acute HIV-1 infection in vitro, was at least 10,000-fold more potent against HIV-1 protease than against related enzymes, and appeared to be stable to degradative enzymes. The 2.8 angstrom crystal structure of the inhibitor-enzyme complex demonstrated that the inhibitor binds to the enzyme in a highly symmetric fashion.
About this Structure
9HVP is a Single protein structure of sequence from Human immunodeficiency virus 1 with as ligand. Full crystallographic information is available from OCA.
Reference
Design, activity, and 2.8 A crystal structure of a C2 symmetric inhibitor complexed to HIV-1 protease., Erickson J, Neidhart DJ, VanDrie J, Kempf DJ, Wang XC, Norbeck DW, Plattner JJ, Rittenhouse JW, Turon M, Wideburg N, et al., Science. 1990 Aug 3;249(4968):527-33. PMID:2200122
Page seeded by OCA on Thu Feb 21 19:18:34 2008
