6e4l

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<StructureSection load='6e4l' size='340' side='right'caption='[[6e4l]], [[Resolution|resolution]] 1.60&Aring;' scene=''>
<StructureSection load='6e4l' size='340' side='right'caption='[[6e4l]], [[Resolution|resolution]] 1.60&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[6e4l]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6E4L OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6E4L FirstGlance]. <br>
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<table><tr><td colspan='2'>[[6e4l]] is a 1 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=6E4L OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6E4L FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=HRS:5-bromo-N-(4-nitrophenyl)thiophene-2-sulfonamide'>HRS</scene></td></tr>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=HRS:5-bromo-N-(4-nitrophenyl)thiophene-2-sulfonamide'>HRS</scene></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CLTC, CLH17, CLTCL2, KIAA0034 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=6e4l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6e4l OCA], [http://pdbe.org/6e4l PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6e4l RCSB], [http://www.ebi.ac.uk/pdbsum/6e4l PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6e4l 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=6e4l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6e4l OCA], [http://pdbe.org/6e4l PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6e4l RCSB], [http://www.ebi.ac.uk/pdbsum/6e4l PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6e4l ProSAT]</span></td></tr>
</table>
</table>
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== Function ==
== Function ==
[[http://www.uniprot.org/uniprot/CLH1_HUMAN CLH1_HUMAN]] Clathrin is the major protein of the polyhedral coat of coated pits and vesicles. Two different adapter protein complexes link the clathrin lattice either to the plasma membrane or to the trans-Golgi network.
[[http://www.uniprot.org/uniprot/CLH1_HUMAN CLH1_HUMAN]] Clathrin is the major protein of the polyhedral coat of coated pits and vesicles. Two different adapter protein complexes link the clathrin lattice either to the plasma membrane or to the trans-Golgi network.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Clathrin-mediated endocytosis (CME) is a highly conserved and essential cellular process in eukaryotic cells, but its dynamic and vital nature makes it challenging to study using classical genetics tools. In contrast, although small molecules can acutely and reversibly perturb CME, the few chemical CME inhibitors that have been applied to plants are either ineffective or show undesirable side effects. Here, we identify the previously described endosidin9 (ES9) as an inhibitor of clathrin heavy chain (CHC) function in both Arabidopsis and human cells through affinity-based target isolation, in vitro binding studies and X-ray crystallography. Moreover, we present a chemically improved ES9 analog, ES9-17, which lacks the undesirable side effects of ES9 while retaining the ability to target CHC. ES9 and ES9-17 have expanded the chemical toolbox used to probe CHC function, and present chemical scaffolds for further design of more specific and potent CHC inhibitors across different systems.
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Disruption of endocytosis through chemical inhibition of clathrin heavy chain function.,Dejonghe W, Sharma I, Denoo B, De Munck S, Lu Q, Mishev K, Bulut H, Mylle E, De Rycke R, Vasileva M, Savatin DV, Nerinckx W, Staes A, Drozdzecki A, Audenaert D, Yperman K, Madder A, Friml J, Van Damme D, Gevaert K, Haucke V, Savvides SN, Winne J, Russinova E Nat Chem Biol. 2019 Apr 22. pii: 10.1038/s41589-019-0262-1. doi:, 10.1038/s41589-019-0262-1. PMID:31011214<ref>PMID:31011214</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 6e4l" style="background-color:#fffaf0;"></div>
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== References ==
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<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
[[Category: Large Structures]]
[[Category: Large Structures]]
[[Category: Audenaert, D]]
[[Category: Audenaert, D]]

Revision as of 13:23, 10 May 2019

The structure of the N-terminal domain of human clathrin heavy chain 1 (nTD) in complex with ES9

PDB ID 6e4l

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