5zpw: Difference between revisions

Line 1:

~~'''Unreleased structure'''~~

~~The entry~~ 5zpw is ~~ON HOLD until Paper~~ Publication

==Generation of a long-acting fusion inhibitor against HIV-1==

== Structural highlights ==

<table><tr><td colspan='2'>[[5zpw]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5ZPW OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5ZPW FirstGlance]. <br>

</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=MK8:2-METHYL-L-NORLEUCINE'>MK8</scene></td></tr>

<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5zpw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5zpw OCA], [http://pdbe.org/5zpw PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5zpw RCSB], [http://www.ebi.ac.uk/pdbsum/5zpw PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5zpw ProSAT]</span></td></tr>

</table>

== Publication Abstract from PubMed ==

AIDS has evolved from a fatal infectious disease to a manageable chronic disease under the treatment of anti-AIDS medications. HIV fusion inhibitors with high activity, low side effects and strong selectivity are promising drugs against HIV. Only one fusion inhibitor is currently approved, thereby highly active long-acting fusion inhibitors need to be developed for long-term AIDS treatment. Here, we synthesised MT-SC22EK (a small HIV fusion inhibitor) derivatives containing 1-2 staples to improve its stability. Antiviral activity studies showed that MT-SC22EK-2 with two staples exhibited potent inhibitory activity against HIV-1 standard strains and Chinese epidemic strains, and at the same time, MT-SC22EK-2 presented strong anti-T20 resistance. Surprisingly, MT-SC22EK-2 possessed excellent protease stability with a half-life of 3665 min. MT-SC22EK-2 is a potential HIV fusion inhibitor considered as a long-acting anti-HIV drug candidate.

~~Authors~~:

Generation of a long-acting fusion inhibitor against HIV-1.,Guo Y, Zhou PP, Zhang SY, Fan XW, Dou YW, Shi XL Medchemcomm. 2018 Jun 6;9(7):1226-1231. doi: 10.1039/c8md00124c. eCollection 2018, Jul 1. PMID:30109011<ref>PMID:30109011</ref>

~~Description~~:

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>

[[Category: ~~Unreleased Structures~~]]

</div>

== References ==

__TOC__

</StructureSection>

[[Category: Guo, Y]]

[[Category: Shi, X L]]

[[Category: Complex]]

[[Category: Inhibitor]]

[[Category: Virus]]

[[Category: Virus like particle]]

Navigation menu

Page actions

Page actions

Personal tools

Navigation

Search

Tools

@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
-The entry 5zpw is ON HOLD  until Paper Publication
+==Generation of a long-acting fusion inhibitor against HIV-1==
+<StructureSection load='5zpw' size='340' side='right'  caption='[[5zpw]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
+== Structural highlights ==
+<table><tr><td colspan='2'>[[5zpw]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5ZPW OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5ZPW FirstGlance]. <br>
+</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=MK8:2-METHYL-L-NORLEUCINE'>MK8</scene></td></tr>
+<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5zpw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5zpw OCA], [http://pdbe.org/5zpw PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5zpw RCSB], [http://www.ebi.ac.uk/pdbsum/5zpw PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5zpw ProSAT]</span></td></tr>
+</table>
+<div style="background-color:#fffaf0;">
+== Publication Abstract from PubMed ==
+AIDS has evolved from a fatal infectious disease to a manageable chronic disease under the treatment of anti-AIDS medications. HIV fusion inhibitors with high activity, low side effects and strong selectivity are promising drugs against HIV. Only one fusion inhibitor is currently approved, thereby highly active long-acting fusion inhibitors need to be developed for long-term AIDS treatment. Here, we synthesised MT-SC22EK (a small HIV fusion inhibitor) derivatives containing 1-2 staples to improve its stability. Antiviral activity studies showed that MT-SC22EK-2 with two staples exhibited potent inhibitory activity against HIV-1 standard strains and Chinese epidemic strains, and at the same time, MT-SC22EK-2 presented strong anti-T20 resistance. Surprisingly, MT-SC22EK-2 possessed excellent protease stability with a half-life of 3665 min. MT-SC22EK-2 is a potential HIV fusion inhibitor considered as a long-acting anti-HIV drug candidate.
-Authors:
+Generation of a long-acting fusion inhibitor against HIV-1.,Guo Y, Zhou PP, Zhang SY, Fan XW, Dou YW, Shi XL Medchemcomm. 2018 Jun 6;9(7):1226-1231. doi: 10.1039/c8md00124c. eCollection 2018, Jul 1. PMID:30109011<ref>PMID:30109011</ref>
-Description:
+From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-[[Category: Unreleased Structures]]
+</div>
+<div class="pdbe-citations 5zpw" style="background-color:#fffaf0;"></div>
+== References ==
+<references/>
+__TOC__
+</StructureSection>
+[[Category: Guo, Y]]
+[[Category: Shi, X L]]
+[[Category: Complex]]
+[[Category: Inhibitor]]
+[[Category: Virus]]
+[[Category: Virus like particle]]