6n0m
From Proteopedia
(Difference between revisions)
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<StructureSection load='6n0m' size='340' side='right'caption='[[6n0m]], [[Resolution|resolution]] 3.30Å' scene=''> | <StructureSection load='6n0m' size='340' side='right'caption='[[6n0m]], [[Resolution|resolution]] 3.30Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[6n0m]] is a 5 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6N0M OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6N0M FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[6n0m]] is a 5 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6N0M OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6N0M FirstGlance]. <br> |
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=K94:4-(difluoromethyl)-L-leucine'>K94</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=K94:4-(difluoromethyl)-L-leucine'>K94</scene></td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">SESN2, Hi95, SEST2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr> | ||
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Peroxiredoxin Peroxiredoxin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.11.1.15 1.11.1.15] </span></td></tr> | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Peroxiredoxin Peroxiredoxin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.11.1.15 1.11.1.15] </span></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=6n0m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6n0m OCA], [http://pdbe.org/6n0m PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6n0m RCSB], [http://www.ebi.ac.uk/pdbsum/6n0m PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6n0m ProSAT]</span></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=6n0m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6n0m OCA], [http://pdbe.org/6n0m PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6n0m RCSB], [http://www.ebi.ac.uk/pdbsum/6n0m PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6n0m ProSAT]</span></td></tr> | ||
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== Function == | == Function == | ||
[[http://www.uniprot.org/uniprot/SESN2_HUMAN SESN2_HUMAN]] Involved in the reduction of peroxiredoxins.<ref>PMID:15105503</ref> | [[http://www.uniprot.org/uniprot/SESN2_HUMAN SESN2_HUMAN]] Involved in the reduction of peroxiredoxins.<ref>PMID:15105503</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | The mechanistic target of rapamycin complex 1 (mTORC1) has been linked to several important chronic medical conditions many of which are associated with advancing age. A variety of inputs including the amino acid leucine are required for full mTORC1 activation. The cytoplasmic proteins Sestrin1 and Sestrin2 specifically bind to the multiprotein complex GATOR2 and communicate leucine sufficiency to the mTORC1 pathway activation complex. Herein, we report NV-5138, a novel orally bioavailable compound that binds to Sestrin2 and activates mTORC1 both in vitro and in vivo. NV-5138 like leucine transiently activates mTORC1 in several peripheral tissues, but in contrast to leucine uniquely activates this complex in the brain due lack of metabolism and utilization in protein synthesis. As such, NV-5138 will permit the exploration in areas of unmet medical need including neuropsychiatric conditions and cognition which have been linked to the activation status of mTORC1. | ||
| + | |||
| + | Discovery of NV-5138, the first selective Brain mTORC1 activator.,Sengupta S, Giaime E, Narayan S, Hahm S, Howell J, O'Neill D, Vlasuk GP, Saiah E Sci Rep. 2019 Mar 11;9(1):4107. doi: 10.1038/s41598-019-40693-5. PMID:30858438<ref>PMID:30858438</ref> | ||
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| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 6n0m" style="background-color:#fffaf0;"></div> | ||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| + | [[Category: Human]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
[[Category: Peroxiredoxin]] | [[Category: Peroxiredoxin]] | ||
Revision as of 07:02, 17 April 2019
CRYSTAL STRUCTURE OF SESTRIN2 IN COMPLEX WITH NV-0005138
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Categories: Human | Large Structures | Peroxiredoxin | Neill, D O | Amino-acid | Leucine | Mtor | Sensing | Signaling protein
