2hb2
From Proteopedia
(New page: 200px<br /> <applet load="2hb2" size="450" color="white" frame="true" align="right" spinBox="true" caption="2hb2, resolution 2.300Å" /> '''Structure of HIV p...) |
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caption="2hb2, resolution 2.300Å" /> | caption="2hb2, resolution 2.300Å" /> | ||
'''Structure of HIV protease 6X mutant in apo form'''<br /> | '''Structure of HIV protease 6X mutant in apo form'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2HB2 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]. Active as [http://en.wikipedia.org/wiki/HIV-1_retropepsin HIV-1 retropepsin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.16 3.4.23.16] Full crystallographic information is available from [http:// | + | 2HB2 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]. Active as [http://en.wikipedia.org/wiki/HIV-1_retropepsin HIV-1 retropepsin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.16 3.4.23.16] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2HB2 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: retrovirus]] | [[Category: retrovirus]] | ||
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Revision as of 11:56, 23 January 2008
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Structure of HIV protease 6X mutant in apo form
Overview
The crystal structures of wild-type HIV protease (HIV PR) in the absence, of substrate or inhibitor in two related crystal forms at 1.4 and 2.15 A, resolution are reported. In one crystal form HIV PR adopts an 'open', conformation with a 7.7 A separation between the tips of the flaps in the, homodimer. In the other crystal form the tips of the flaps are 'curled', towards the 80s loop, forming contacts across the local twofold axis. The, 2.3 A resolution crystal structure of a sixfold mutant of HIV PR in the, absence of substrate or inhibitor is also reported. The mutant HIV PR, which evolved in response to treatment with the potent inhibitor TL-3, contains six point mutations relative to the wild-type enzyme (L24I, M46I, F53L, L63P, V77I, V82A). In this structure the flaps also adopt a 'curled', conformation, but are separated and not in contact. Comparison of the apo, structures to those with TL-3 bound demonstrates the extent of, conformational change induced by inhibitor binding, which includes, reorganization of the packing between twofold-related flaps. Further, comparison with six other apo HIV PR structures reveals that the 'open', and 'curled' conformations define two distinct families in HIV PR. These, conformational states include hinge motion of residues at either end of, the flaps, opening and closing the entire beta-loop, and translational, motion of the flap normal to the dimer twofold axis and relative to the, 80s loop. The alternate conformations also entail changes in the beta-turn, at the tip of the flap. These observations provide insight into the, plasticity of the flap domains, the nature of their motions and their, critical role in binding substrates and inhibitors.
About this Structure
2HB2 is a Single protein structure of sequence from Human immunodeficiency virus 1. Active as HIV-1 retropepsin, with EC number 3.4.23.16 Full crystallographic information is available from OCA.
Reference
Conformational flexibility in the flap domains of ligand-free HIV protease., Heaslet H, Rosenfeld R, Giffin M, Lin YC, Tam K, Torbett BE, Elder JH, McRee DE, Stout CD, Acta Crystallogr D Biol Crystallogr. 2007 Aug;63(Pt 8):866-75. Epub 2007, Jul 17. PMID:17642513
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