5di1

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'''Unreleased structure'''
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==MAP4K4 in complex with an inhibitor==
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<StructureSection load='5di1' size='340' side='right' caption='[[5di1]], [[Resolution|resolution]] 2.90&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5di1]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5DI1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5DI1 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5DF:4-{6-AMINO-5-[4-(METHYLSULFONYL)PHENYL]PYRIDIN-3-YL}PHENOL'>5DF</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4zp5|4zp5]]</td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span></td></tr>
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<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=5di1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5di1 OCA], [http://pdbe.org/5di1 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5di1 RCSB], [http://www.ebi.ac.uk/pdbsum/5di1 PDBsum]</span></td></tr>
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/M4K4_HUMAN M4K4_HUMAN]] Serine/threonine kinase that may play a role in the response to environmental stress and cytokines such as TNF-alpha. Appears to act upstream of the JUN N-terminal pathway. Phosphorylates SMAD1 on Thr-322.<ref>PMID:9890973</ref> <ref>PMID:21690388</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Recent studies in adipose tissue, pancreas, muscle, and macrophages suggest that MAP4K4, a serine/threonine protein kinase may be a viable target for antidiabetic drugs. As part of the evaluation of MAP4K4 as a novel antidiabetic target, a tool compound, 16 (PF-6260933) and a lead 17 possessing excellent kinome selectivity and suitable properties were delivered to establish proof of concept in vivo. The medicinal chemistry effort that led to the discovery of these lead compounds is described herein together with in vivo pharmacokinetic properties and activity in a model of insulin resistance.
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The entry 5di1 is ON HOLD
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Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment.,Ammirati M, Bagley SW, Bhattacharya SK, Buckbinder L, Carlo AA, Conrad R, Cortes C, Dow RL, Dowling MS, El-Kattan A, Ford K, Guimaraes CR, Hepworth D, Jiao W, LaPerle J, Liu S, Londregan A, Loria PM, Mathiowetz AM, Munchhof M, Orr ST, Petersen DN, Price DA, Skoura A, Smith AC, Wang J ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33. doi: 10.1021/acsmedchemlett.5b00215., eCollection 2015 Nov 12. PMID:26617966<ref>PMID:26617966</ref>
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Authors: Liu, S.
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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Description: MAP4K4 in complex with an inhibitor
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<div class="pdbe-citations 5di1" style="background-color:#fffaf0;"></div>
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[[Category: Unreleased Structures]]
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Non-specific serine/threonine protein kinase]]
[[Category: Liu, S]]
[[Category: Liu, S]]
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[[Category: Complex]]
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[[Category: Inhibitor]]
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[[Category: Kinase]]
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[[Category: Medicinal chemistry]]
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[[Category: Transferase-inhibitor complex]]

Revision as of 20:14, 13 January 2016

MAP4K4 in complex with an inhibitor

5di1, resolution 2.90Å

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