3q2h

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[[Image:3q2h.jpg|left|200px]]
 
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==Adamts1 in complex with N-hydroxyformamide inhibitors of ADAM-TS4==
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The line below this paragraph, containing "STRUCTURE_3q2h", creates the "Structure Box" on the page.
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<StructureSection load='3q2h' size='340' side='right'caption='[[3q2h]], [[Resolution|resolution]] 2.33&Aring;' scene=''>
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3q2h]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3Q2H OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3Q2H FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.33&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CD:CADMIUM+ION'>CD</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</scene>, <scene name='pdbligand=QHF:N-[(2S,4S)-1-({4-[2-(3,5-DIMETHYL-1,2-OXAZOL-4-YL)ETHYL]PIPERIDIN-1-YL}SULFONYL)-4-(5-FLUOROPYRIMIDIN-2-YL)-2-METHYLPENTAN-2-YL]-N-HYDROXYFORMAMIDE'>QHF</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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{{STRUCTURE_3q2h| PDB=3q2h | SCENE= }}
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3q2h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3q2h OCA], [https://pdbe.org/3q2h PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3q2h RCSB], [https://www.ebi.ac.uk/pdbsum/3q2h PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3q2h ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/ATS1_HUMAN ATS1_HUMAN] Cleaves aggrecan, a cartilage proteoglycan, and may be involved in its turnover (By similarity). Has angiogenic inhibitor activity. Active metalloprotease, which may be associated with various inflammatory processes as well as development of cancer cachexia. May play a critical role in follicular rupture.<ref>PMID:10438512</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Two series of N-hydroxyformamide inhibitors of ADAM-TS4 were identified from screening compounds previously synthesised as inhibitors of matrix metalloproteinase-13 (collagenase-3). Understanding of the binding mode of this class of compound using ADAM-TS1 as a structural surrogate has led to the discovery of potent and very selective inhibitors with favourable DMPK properties. Synthesis, structure-activity relationships, and strategies to improve selectivity and lower in vivo metabolic clearance are described.
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===Adamts1 in complex with N-hydroxyformamide inhibitors of ADAM-TS4===
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The design and synthesis of novel N-hydroxyformamide inhibitors of ADAM-TS4 for the treatment of osteoarthritis.,De Savi C, Pape A, Cumming JG, Ting A, Smith PD, Burrows JN, Mills M, Davies C, Lamont S, Milne D, Cook C, Moore P, Sawyer Y, Gerhardt S Bioorg Med Chem Lett. 2011 Mar 1;21(5):1376-81. Epub 2011 Jan 18. PMID:21300546<ref>PMID:21300546</ref>
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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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<div class="pdbe-citations 3q2h" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_21300546}}, adds the Publication Abstract to the page
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*[[A Disintegrin And Metalloproteinase 3D structures|A Disintegrin And Metalloproteinase 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 21300546 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_21300546}}
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__TOC__
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</StructureSection>
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==About this Structure==
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[[3q2h]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3Q2H OCA].
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==Reference==
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<ref group="xtra">PMID:21300546</ref><references group="xtra"/>
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Gerhardt, S.]]
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[[Category: Large Structures]]
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[[Category: Hargreaves, D.]]
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[[Category: Gerhardt S]]
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[[Category: Hargreaves D]]

Current revision

Adamts1 in complex with N-hydroxyformamide inhibitors of ADAM-TS4

PDB ID 3q2h

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