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5whi

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Revision as of 08:52, 30 September 2020

Crystal Structure of Bcl-2-related protein A1

Structural highlights

5whi is a 1 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[B2LA1_HUMAN] Retards apoptosis induced by IL-3 deprivation. May function in the response of hemopoietic cells to external signals and in maintaining endothelial survival during infection (By similarity).

Publication Abstract from PubMed

BCL-2 family proteins are high-priority cancer targets whose structures provide essential blueprints for drug design. Whereas numerous structures of anti-apoptotic BCL-2 protein complexes with alpha-helical BH3 peptides have been reported, the corresponding panel of apo structures remains incomplete. Here, we report the crystal structure of apo BFL-1 at 1.69-A resolution, revealing similarities and key differences among unliganded anti-apoptotic proteins. Unlike all other BCL-2 proteins, apo BFL-1 contains a surface-accessible cysteine within its BH3-binding groove, allowing for selective covalent targeting by a NOXA BH3-based stapled peptide inhibitor. The crystal structure of this complex demonstrated the sulfhydryl bond and fortuitous interactions between the acrylamide-bearing moiety and a newly formed hydrophobic cavity. Comparison of the apo and BH3-liganded structures further revealed an induced conformational change. The two BFL-1 structures expand our understanding of the surface landscapes available for therapeutic targeting so that the apoptotic blockades of BFL-1-dependent cancers can be overcome.

Crystal Structures of Anti-apoptotic BFL-1 and Its Complex with a Covalent Stapled Peptide Inhibitor.,Harvey EP, Seo HS, Guerra RM, Bird GH, Dhe-Paganon S, Walensky LD Structure. 2018 Jan 2;26(1):153-160.e4. doi: 10.1016/j.str.2017.11.016. Epub 2017, Dec 21. PMID:29276033^[1]

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

References

↑ Harvey EP, Seo HS, Guerra RM, Bird GH, Dhe-Paganon S, Walensky LD. Crystal Structures of Anti-apoptotic BFL-1 and Its Complex with a Covalent Stapled Peptide Inhibitor. Structure. 2018 Jan 2;26(1):153-160.e4. doi: 10.1016/j.str.2017.11.016. Epub 2017, Dec 21. PMID:29276033 doi:http://dx.doi.org/10.1016/j.str.2017.11.016

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

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/5whi"

Categories: Large Structures | Dhe-Paganon, S | Seo, H S | Apoptosis

@@ Line 1: / Line 1: @@
 ==Crystal Structure of Bcl-2-related protein A1==
-<StructureSection load='5whi' size='340' side='right' caption='[[5whi]], [[Resolution|resolution]] 1.69&Aring;' scene=''>
+<StructureSection load='5whi' size='340' side='right'caption='[[5whi]], [[Resolution|resolution]] 1.69&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[5whi]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5WHI OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5WHI FirstGlance]. <br>
+<table><tr><td colspan='2'>[[5whi]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5WHI OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5WHI FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CAD:CACODYLIC+ACID'>CAD</scene></td></tr>
+</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CAD:CACODYLIC+ACID'>CAD</scene></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=5whi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5whi OCA], [http://pdbe.org/5whi PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5whi RCSB], [http://www.ebi.ac.uk/pdbsum/5whi PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5whi ProSAT]</span></td></tr>
+<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=5whi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5whi OCA], [http://pdbe.org/5whi PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5whi RCSB], [http://www.ebi.ac.uk/pdbsum/5whi PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5whi ProSAT]</span></td></tr>
 </table>
 == Function ==
@@ Line 18: / Line 18: @@
 </div>
 <div class="pdbe-citations 5whi" style="background-color:#fffaf0;"></div>
+==See Also==
+*[[B-cell lymphoma proteins 3D structures|B-cell lymphoma proteins 3D structures]]
 == References ==
 <references/>
 __TOC__
 </StructureSection>
+[[Category: Large Structures]]
 [[Category: Dhe-Paganon, S]]
 [[Category: Seo, H S]]
 [[Category: Apoptosis]]

5whi

From Proteopedia

Revision as of 08:52, 30 September 2020

Crystal Structure of Bcl-2-related protein A1

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

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