6knm
From Proteopedia
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<StructureSection load='6knm' size='340' side='right'caption='[[6knm]], [[Resolution|resolution]] 3.20Å' scene=''> | <StructureSection load='6knm' size='340' side='right'caption='[[6knm]], [[Resolution|resolution]] 3.20Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[6knm]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6KNM OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6KNM FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[6knm]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/"bacillus_pasteurianus"_(winogradsky_1895)_lehmann_and_neumann_1907 "bacillus pasteurianus" (winogradsky 1895) lehmann and neumann 1907] and [http://en.wikipedia.org/wiki/Bactrian_camel Bactrian camel]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6KNM OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6KNM FirstGlance]. <br> |
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">APLNR, AGTRL1, APJ ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=1501 "Bacillus pasteurianus" (Winogradsky 1895) Lehmann and Neumann 1907])</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=6knm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6knm OCA], [http://pdbe.org/6knm PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6knm RCSB], [http://www.ebi.ac.uk/pdbsum/6knm PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6knm 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=6knm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6knm OCA], [http://pdbe.org/6knm PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6knm RCSB], [http://www.ebi.ac.uk/pdbsum/6knm PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6knm ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
[[http://www.uniprot.org/uniprot/APJ_HUMAN APJ_HUMAN]] Receptor for apelin coupled to G proteins that inhibit adenylate cyclase activity. Alternative coreceptor with CD4 for HIV-1 infection; may be involved in the development of AIDS dementia. | [[http://www.uniprot.org/uniprot/APJ_HUMAN APJ_HUMAN]] Receptor for apelin coupled to G proteins that inhibit adenylate cyclase activity. Alternative coreceptor with CD4 for HIV-1 infection; may be involved in the development of AIDS dementia. | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Developing antibody agonists targeting the human apelin receptor (APJ) is a promising therapeutic approach for the treatment of chronic heart failure. Here, we report the structure-guided discovery of a single-domain antibody (sdAb) agonist JN241-9, based on the cocrystal structure of APJ with an sdAb antagonist JN241, the first cocrystal structure of a class A G protein-coupled receptor (GPCR) with a functional antibody. As revealed by the structure, JN241 binds to the extracellular side of APJ, makes critical contacts with the second extracellular loop, and inserts the CDR3 into the ligand-binding pocket. We converted JN241 into a full agonist JN241-9 by inserting a tyrosine into the CDR3. Modeling and molecular dynamics simulation shed light on JN241-9-stimulated receptor activation, providing structural insights for finding agonistic antibodies against class A GPCRs. | ||
| + | |||
| + | Structure-guided discovery of a single-domain antibody agonist against human apelin receptor.,Ma Y, Ding Y, Song X, Ma X, Li X, Zhang N, Song Y, Sun Y, Shen Y, Zhong W, Hu LA, Ma Y, Zhang MY Sci Adv. 2020 Jan 15;6(3):eaax7379. doi: 10.1126/sciadv.aax7379. eCollection 2020, Jan. PMID:31998837<ref>PMID:31998837</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 6knm" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| + | [[Category: Bactrian camel]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
[[Category: Ding, Y]] | [[Category: Ding, Y]] | ||
Revision as of 04:38, 13 February 2020
Apelin receptor in complex with single domain antibody
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Categories: Bactrian camel | Large Structures | Ding, Y | Hu, L A | Li, X | Ma, X | Ma, Y B | Ma, Y L | Shen, Y | Song, X | Song, Y | Sun, Y | Zhang, M Y | Zhang, N | Zhong, W | Agonist | Antagonist | Gpcr | Membrane protein | Single-domain antibody
