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4wmr

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Revision as of 02:00, 10 March 2017

STRUCTURE OF MCL1 BOUND TO BRD inhibitor ligand 1 AT 1.7A

Structural highlights

4wmr is a 1 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	, ,
Related:	4wms, 4wmt, 4wmu, 4wmv, 4wmw, 4wmx
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[MCL1_HUMAN] Involved in the regulation of apoptosis versus cell survival, and in the maintenance of viability but not of proliferation. Mediates its effects by interactions with a number of other regulators of apoptosis. Isoform 1 inhibits apoptosis. Isoform 2 promotes apoptosis.^[1]

Publication Abstract from PubMed

Crystallization of a maltose-binding protein MCL1 fusion has yielded a robust crystallography platform that generated the first apo MCL1 crystal structure, as well as five ligand-bound structures. The ability to obtain fragment-bound structures advances structure-based drug design efforts that, despite considerable effort, had previously been intractable by crystallography. In the ligand-independent crystal form we identify inhibitor binding modes not observed in earlier crystallographic systems. This MBP-MCL1 construct dramatically improves the structural understanding of well-validated MCL1 ligands, and will likely catalyze the structure-based optimization of high affinity MCL1 inhibitors.

A Maltose-Binding Protein Fusion Construct Yields a Robust Crystallography Platform for MCL1.,Clifton MC, Dranow DM, Leed A, Fulroth B, Fairman JW, Abendroth J, Atkins KA, Wallace E, Fan D, Xu G, Ni ZJ, Daniels D, Van Drie J, Wei G, Burgin AB, Golub TR, Hubbard BK, Serrano-Wu MH PLoS One. 2015 Apr 24;10(4):e0125010. doi: 10.1371/journal.pone.0125010., eCollection 2015. PMID:25909780^[2]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Bingle CD, Craig RW, Swales BM, Singleton V, Zhou P, Whyte MK. Exon skipping in Mcl-1 results in a bcl-2 homology domain 3 only gene product that promotes cell death. J Biol Chem. 2000 Jul 21;275(29):22136-46. PMID:10766760 doi:10.1074/jbc.M909572199
↑ Clifton MC, Dranow DM, Leed A, Fulroth B, Fairman JW, Abendroth J, Atkins KA, Wallace E, Fan D, Xu G, Ni ZJ, Daniels D, Van Drie J, Wei G, Burgin AB, Golub TR, Hubbard BK, Serrano-Wu MH. A Maltose-Binding Protein Fusion Construct Yields a Robust Crystallography Platform for MCL1. PLoS One. 2015 Apr 24;10(4):e0125010. doi: 10.1371/journal.pone.0125010., eCollection 2015. PMID:25909780 doi:http://dx.doi.org/10.1371/journal.pone.0125010

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/4wmr"

Categories: CLIFTON, M C | EDWARDS, T E | Apoptosis | Protein-protein interaction

@@ Line 1: / Line 1: @@
 ==STRUCTURE OF MCL1 BOUND TO BRD inhibitor ligand 1 AT 1.7A==
 <StructureSection load='4wmr' size='340' side='right' caption='[[4wmr]], [[Resolution|resolution]] 1.70&Aring;' scene=''>
@@ Line 5: / Line 6: @@
 </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=865:7-[2-(1H-IMIDAZOL-1-YL)-4-METHYLPYRIDIN-3-YL]-3-[3-(NAPHTHALEN-1-YLOXY)PROPYL]-1-[2-OXO-2-(PIPERAZIN-1-YL)ETHYL]-1H-INDOLE-2-CARBOXYLIC+ACID'>865</scene>, <scene name='pdbligand=POP:PYROPHOSPHATE+2-'>POP</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
 <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4wms|4wms]], [[4wmt|4wmt]], [[4wmu|4wmu]], [[4wmv|4wmv]], [[4wmw|4wmw]], [[4wmx|4wmx]]</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=4wmr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4wmr OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4wmr RCSB], [http://www.ebi.ac.uk/pdbsum/4wmr PDBsum]</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=4wmr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4wmr OCA], [http://pdbe.org/4wmr PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4wmr RCSB], [http://www.ebi.ac.uk/pdbsum/4wmr PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4wmr ProSAT]</span></td></tr>
 </table>
 == Function ==
@@ Line 17: / Line 18: @@
 From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
 </div>
+<div class="pdbe-citations 4wmr" style="background-color:#fffaf0;"></div>
 == References ==
 <references/>

4wmr

From Proteopedia

Revision as of 02:00, 10 March 2017

STRUCTURE OF MCL1 BOUND TO BRD inhibitor ligand 1 AT 1.7A

Structural highlights

Function

Publication Abstract from PubMed

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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