3v5q

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<StructureSection load='3v5q' size='340' side='right'caption='[[3v5q]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
<StructureSection load='3v5q' size='340' side='right'caption='[[3v5q]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[3v5q]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3V5Q OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3V5Q FirstGlance]. <br>
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<table><tr><td colspan='2'>[[3v5q]] 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=3V5Q OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3V5Q FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0F4:1-(3-{[(3Z)-2-OXO-3-(1H-PYRROL-2-YLMETHYLIDENE)-2,3-DIHYDRO-1H-INDOL-6-YL]AMINO}PHENYL)-3-[3-(TRIFLUOROMETHYL)PHENYL]UREA'>0F4</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene></td></tr>
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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]] 2.2001&#8491;</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">NTRK3, TRKC ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=0F4:1-(3-{[(3Z)-2-OXO-3-(1H-PYRROL-2-YLMETHYLIDENE)-2,3-DIHYDRO-1H-INDOL-6-YL]AMINO}PHENYL)-3-[3-(TRIFLUOROMETHYL)PHENYL]UREA'>0F4</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene></td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] </span></td></tr>
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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=3v5q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3v5q OCA], [https://pdbe.org/3v5q PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3v5q RCSB], [https://www.ebi.ac.uk/pdbsum/3v5q PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3v5q ProSAT]</span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3v5q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3v5q OCA], [https://pdbe.org/3v5q PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3v5q RCSB], [https://www.ebi.ac.uk/pdbsum/3v5q PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3v5q ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[https://www.uniprot.org/uniprot/NTRK3_HUMAN NTRK3_HUMAN]] Receptor for neurotrophin-3 (NT-3). This is a tyrosine-protein kinase receptor. Known substrates for the trk receptors are SHC1, PI-3 kinase, and PLCG1. The different isoforms do not have identical signaling properties.
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[https://www.uniprot.org/uniprot/NTRK3_HUMAN NTRK3_HUMAN] Receptor for neurotrophin-3 (NT-3). This is a tyrosine-protein kinase receptor. Known substrates for the trk receptors are SHC1, PI-3 kinase, and PLCG1. The different isoforms do not have identical signaling properties.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Neurotrophins and their receptors (TRKs) play key roles in the development of the nervous system and the maintenance of the neural network. Accumulating evidence points to their role in malignant transformations, chemotaxis, metastasis, and survival signaling and may contribute to the pathogenesis of a variety of tumors of both neural and non-neural origin. By screening the GNF kinase collection, a series of novel oxindole inhibitors of TRKs were identified. Optimization led to the identification of GNF-5837 (22), a potent, selective, and orally bioavailable pan-TRK inhibitor that inhibited tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF. The properties of 22 make it a good tool for the elucidation of TRK biology in cancer and other nononcology indications.
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Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models.,Albaugh P, Fan Y, Mi Y, Sun F, Adrian F, Li N, Jia Y, Sarkisova Y, Kreusch A, Hood T, Lu M, Liu G, Huang S, Liu Z, Loren J, Tuntland T, Karanewsky DS, Seidel HM, Molteni V ACS Med Chem Lett. 2012 Jan 1;3(2):140-5. doi: 10.1021/ml200261d. eCollection, 2012 Feb 9. PMID:24900443<ref>PMID:24900443</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 3v5q" style="background-color:#fffaf0;"></div>
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==See Also==
==See Also==
*[[TrkB tyrosine kinase receptor|TrkB tyrosine kinase receptor]]
*[[TrkB tyrosine kinase receptor|TrkB tyrosine kinase receptor]]
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*[[Tyrosine kinase receptor|Tyrosine kinase receptor]]
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*[[Tyrosine kinase receptor 3D structures|Tyrosine kinase receptor 3D structures]]
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== References ==
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<references/>
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Receptor protein-tyrosine kinase]]
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[[Category: Kreusch A]]
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[[Category: Kreusch, A]]
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[[Category: Kinase]]
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[[Category: Kinase domain]]
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[[Category: Phosphorylation]]
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[[Category: Transferase-transferase inhibitor complex]]
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Current revision

Discovery of a selective TRK Inhibitor with efficacy in rodent cancer tumor models

PDB ID 3v5q

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Proteopedia Page Contributors and Editors (what is this?)

OCA

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