5agw - Revision history

OCA at 07:21, 1 May 2024

OCA — Wed, 01 May 2024 07:21:22 GMT

←Older revision		Revision as of 07:21, 1 May 2024
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	== Function ==		== Function ==
	[https://www.uniprot.org/uniprot/B2CL1_HUMAN B2CL1_HUMAN] Potent inhibitor of cell death. Inhibits activation of caspases (By similarity). Appears to regulate cell death by blocking the voltage-dependent anion channel (VDAC) by binding to it and preventing the release of the caspase activator, CYC1, from the mitochondrial membrane. Also acts as a regulator of G2 checkpoint and progression to cytokinesis during mitosis.<ref>PMID:19917720</ref> <ref>PMID:21840391</ref> Isoform Bcl-X(S) promotes apoptosis.<ref>PMID:19917720</ref> <ref>PMID:21840391</ref> [https://www.uniprot.org/uniprot/BCL2_HUMAN BCL2_HUMAN] Suppresses apoptosis in a variety of cell systems including factor-dependent lymphohematopoietic and neural cells. Regulates cell death by controlling the mitochondrial membrane permeability. Appears to function in a feedback loop system with caspases. Inhibits caspase activity either by preventing the release of cytochrome c from the mitochondria and/or by binding to the apoptosis-activating factor (APAF-1).<ref>PMID:18570871</ref>		[https://www.uniprot.org/uniprot/B2CL1_HUMAN B2CL1_HUMAN] Potent inhibitor of cell death. Inhibits activation of caspases (By similarity). Appears to regulate cell death by blocking the voltage-dependent anion channel (VDAC) by binding to it and preventing the release of the caspase activator, CYC1, from the mitochondrial membrane. Also acts as a regulator of G2 checkpoint and progression to cytokinesis during mitosis.<ref>PMID:19917720</ref> <ref>PMID:21840391</ref> Isoform Bcl-X(S) promotes apoptosis.<ref>PMID:19917720</ref> <ref>PMID:21840391</ref> [https://www.uniprot.org/uniprot/BCL2_HUMAN BCL2_HUMAN] Suppresses apoptosis in a variety of cell systems including factor-dependent lymphohematopoietic and neural cells. Regulates cell death by controlling the mitochondrial membrane permeability. Appears to function in a feedback loop system with caspases. Inhibits caspase activity either by preventing the release of cytochrome c from the mitochondria and/or by binding to the apoptosis-activating factor (APAF-1).<ref>PMID:18570871</ref>
-	<div style="background-color:#fffaf0;">
-	== Publication Abstract from PubMed ==
-	Peptides can be developed as effective antagonists of protein-protein interactions, but conventional peptides (i.e., oligomers of l-alpha-amino acids) suffer from significant limitations in vivo. Short half-lives due to rapid proteolytic degradation and an inability to cross cell membranes often preclude biological applications of peptides. Oligomers that contain both alpha- and beta-amino acid residues ("alpha/beta-peptides") manifest decreased susceptibility to proteolytic degradation, and when properly designed these unnatural oligomers can mimic the protein-recognition properties of analogous "alpha-peptides". This report documents an extension of the alpha/beta-peptide approach to target intracellular protein-protein interactions. Specifically, we have generated alpha/beta-peptides based on a "stapled" Bim BH3 alpha-peptide, which contains a hydrocarbon cross-link to enhance alpha-helix stability. We show that a stapled alpha/beta-peptide can structurally and functionally mimic the parent stapled alpha-peptide in its ability to enter certain types of cells and block protein-protein interactions associated with apoptotic signaling. However, the alpha/beta-peptide is nearly 100-fold more resistant to proteolysis than is the parent stapled alpha-peptide. These results show that backbone modification, a strategy that has received relatively little attention in terms of peptide engineering for biomedical applications, can be combined with more commonly deployed peripheral modifications such as side chain cross-linking to produce synergistic benefits.
-
-	alpha/beta-Peptide Foldamers Targeting Intracellular Protein-Protein Interactions with Activity in Living Cells.,Checco JW, Lee EF, Evangelista M, Sleebs NJ, Rogers K, Pettikiriarachchi A, Kershaw NJ, Eddinger GA, Belair DG, Wilson JL, Eller CH, Raines RT, Murphy WL, Smith BJ, Gellman SH, Fairlie WD J Am Chem Soc. 2015 Aug 28. PMID:26317395<ref>PMID:26317395</ref>
-
-	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	</div>
-	<div class="pdbe-citations 5agw" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==

OCA at 09:28, 15 November 2023

OCA — Wed, 15 Nov 2023 09:28:36 GMT

←Older revision		Revision as of 09:28, 15 November 2023
Line 4:		Line 4:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[5agw]] is a 4 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=5AGW OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5AGW FirstGlance]. <br>		<table><tr><td colspan='2'>[[5agw]] is a 4 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=5AGW OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5AGW FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=AJE:(3S,4R)-4-AMINO-1-(3-CARBOXYPROPANOYL)PYRROLIDINE-3-CARBOXYLIC+ACID'>AJE</scene>, <scene name='pdbligand=MH8:(2S)-2-AMINO-2-METHYLHEPT-6-ENOIC+ACID'>MH8</scene>, <scene name='pdbligand=XCP:(1S,2S)-2-AMINOCYCLOPENTANECARBOXYLIC+ACID'>XCP</scene></td></tr>	+	</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution\|Resolution]] 2.695Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=AJE:(3S,4R)-4-AMINO-1-(3-CARBOXYPROPANOYL)PYRROLIDINE-3-CARBOXYLIC+ACID'>AJE</scene>, <scene name='pdbligand=MH8:(2S)-2-AMINO-2-METHYLHEPT-6-ENOIC+ACID'>MH8</scene>, <scene name='pdbligand=XCP:(1S,2S)-2-AMINOCYCLOPENTANECARBOXYLIC+ACID'>XCP</scene></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=5agw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5agw OCA], [https://pdbe.org/5agw PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5agw RCSB], [https://www.ebi.ac.uk/pdbsum/5agw PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5agw 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=5agw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5agw OCA], [https://pdbe.org/5agw PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5agw RCSB], [https://www.ebi.ac.uk/pdbsum/5agw PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5agw ProSAT]</span></td></tr>
	</table>		</table>

OCA at 04:58, 25 May 2023

OCA — Thu, 25 May 2023 04:58:51 GMT

←Older revision		Revision as of 04:58, 25 May 2023
Line 3:		Line 3:
	<StructureSection load='5agw' size='340' side='right'caption='[[5agw]], [[Resolution\|resolution]] 2.69Å' scene=''>		<StructureSection load='5agw' size='340' side='right'caption='[[5agw]], [[Resolution\|resolution]] 2.69Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5agw]] is a 4 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=5AGW OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5AGW FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5agw]] is a 4 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=5AGW OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5AGW FirstGlance]. <br>
-	</td></tr><tr id='~~NonStdRes~~'><td class="sblockLbl"><b>[[~~Non-Standard_Residue~~\|~~NonStd Res~~:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=AJE:(3S,4R)-4-AMINO-1-(3-CARBOXYPROPANOYL)PYRROLIDINE-3-CARBOXYLIC+ACID'>AJE</scene>, <scene name='pdbligand=MH8:(2S)-2-AMINO-2-METHYLHEPT-6-ENOIC+ACID'>MH8</scene>, <scene name='pdbligand=XCP:(1S,2S)-2-AMINOCYCLOPENTANECARBOXYLIC+ACID'>XCP</scene>~~</td></tr>~~	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=AJE:(3S,4R)-4-AMINO-1-(3-CARBOXYPROPANOYL)PYRROLIDINE-3-CARBOXYLIC+ACID'>AJE</scene>, <scene name='pdbligand=MH8:(2S)-2-AMINO-2-METHYLHEPT-6-ENOIC+ACID'>MH8</scene>, <scene name='pdbligand=XCP:(1S,2S)-2-AMINOCYCLOPENTANECARBOXYLIC+ACID'>XCP</scene></td></tr>
-	~~<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5agx\|5agx]]~~</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=5agw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5agw OCA], [https://pdbe.org/5agw PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5agw RCSB], [https://www.ebi.ac.uk/pdbsum/5agw PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5agw 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=5agw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5agw OCA], [~~http~~://pdbe.org/5agw PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5agw RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5agw PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5agw ProSAT]</span></td></tr>	+
	</table>		</table>
	== Disease ==		== Disease ==
-	[~~[http~~://www.uniprot.org/uniprot/BCL2_HUMAN BCL2_HUMAN]] Note=A chromosomal aberration involving BCL2 has been found in chronic lymphatic leukemia. Translocation t(14;18)(q32;q21) with immunoglobulin gene regions. BCL2 mutations found in non-Hodgkin lymphomas carrying the chromosomal translocation could be attributed to the Ig somatic hypermutation mechanism resulting in nucleotide transitions.	+	[https://www.uniprot.org/uniprot/BCL2_HUMAN BCL2_HUMAN] Note=A chromosomal aberration involving BCL2 has been found in chronic lymphatic leukemia. Translocation t(14;18)(q32;q21) with immunoglobulin gene regions. BCL2 mutations found in non-Hodgkin lymphomas carrying the chromosomal translocation could be attributed to the Ig somatic hypermutation mechanism resulting in nucleotide transitions.
	== Function ==		== Function ==
-	[[~~http~~://www.uniprot.org/uniprot/BCL2_HUMAN BCL2_HUMAN]] Suppresses apoptosis in a variety of cell systems including factor-dependent lymphohematopoietic and neural cells. Regulates cell death by controlling the mitochondrial membrane permeability. Appears to function in a feedback loop system with caspases. Inhibits caspase activity either by preventing the release of cytochrome c from the mitochondria and/or by binding to the apoptosis-activating factor (APAF-1).<ref>PMID:18570871</ref> [[http://www.uniprot.org/uniprot/B2L11_HUMAN B2L11_HUMAN]] Induces apoptosis and anoikis. Isoform BimL is more potent than isoform BimEL. Isoform Bim-alpha1, isoform Bim-alpha2 and isoform Bim-alpha3 induce apoptosis, although less potent than isoform BimEL, isoform BimL and isoform BimS. Isoform Bim-gamma induces apoptosis. Isoform Bim-alpha3 induces apoptosis possibly through a caspase-mediated pathway. Isoform BimAC and isoform BimABC lack the ability to induce apoptosis.<ref>PMID:9430630</ref> <ref>PMID:11734221</ref> <ref>PMID:12019181</ref> <ref>PMID:11997495</ref> <ref>PMID:15147734</ref> <ref>PMID:15486195</ref>	+	[https://www.uniprot.org/uniprot/B2CL1_HUMAN B2CL1_HUMAN] Potent inhibitor of cell death. Inhibits activation of caspases (By similarity). Appears to regulate cell death by blocking the voltage-dependent anion channel (VDAC) by binding to it and preventing the release of the caspase activator, CYC1, from the mitochondrial membrane. Also acts as a regulator of G2 checkpoint and progression to cytokinesis during mitosis.<ref>PMID:19917720</ref> <ref>PMID:21840391</ref> Isoform Bcl-X(S) promotes apoptosis.<ref>PMID:19917720</ref> <ref>PMID:21840391</ref> [https://www.uniprot.org/uniprot/BCL2_HUMAN BCL2_HUMAN] Suppresses apoptosis in a variety of cell systems including factor-dependent lymphohematopoietic and neural cells. Regulates cell death by controlling the mitochondrial membrane permeability. Appears to function in a feedback loop system with caspases. Inhibits caspase activity either by preventing the release of cytochrome c from the mitochondria and/or by binding to the apoptosis-activating factor (APAF-1).<ref>PMID:18570871</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 28:		Line 27:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Checco~~, J W]]~~	+	[[Category: Checco JW]]
-	~~[[Category: Fairlie, W D]]~~	+	[[Category: F Lee E]]
-	~~[[Category: Gellman, S H~~]]	+	[[Category: Fairlie WD]]
-	[[Category: Lee, E F]]	+	[[Category: Gellman SH]]
-	[[Category: ~~Smith, B J~~]]	+	[[Category: Smith BJ]]
-	[[Category: ~~Apoptosis~~]]	+
-	[[Category: ~~Bcl-2]]~~	+
-	~~[[Category: Bim]]~~	+
-	~~[[Category: Foldamer~~]]	+

OCA at 07:31, 23 October 2019

OCA — Wed, 23 Oct 2019 07:31:53 GMT

←Older revision		Revision as of 07:31, 23 October 2019
Line 1:		Line 1:

	==Bcl-2 alpha beta-1 complex==		==Bcl-2 alpha beta-1 complex==
-	<StructureSection load='5agw' size='340' side='right' caption='[[5agw]], [[Resolution\|resolution]] 2.69Å' scene=''>	+	<StructureSection load='5agw' size='340' side='right'caption='[[5agw]], [[Resolution\|resolution]] 2.69Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[5agw]] is a 4 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=5AGW OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5AGW FirstGlance]. <br>		<table><tr><td colspan='2'>[[5agw]] is a 4 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=5AGW OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5AGW FirstGlance]. <br>
Line 21:		Line 21:
	</div>		</div>
	<div class="pdbe-citations 5agw" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 5agw" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[B-cell lymphoma proteins 3D structures\|B-cell lymphoma proteins 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
Line 26:		Line 29:
	</StructureSection>		</StructureSection>
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Checco, J W]]		[[Category: Checco, J W]]
	[[Category: Fairlie, W D]]		[[Category: Fairlie, W D]]

OCA at 16:29, 16 November 2017

OCA — Thu, 16 Nov 2017 16:29:05 GMT

←Older revision		Revision as of 16:29, 16 November 2017
Line 1:		Line 1:
		+
	==Bcl-2 alpha beta-1 complex==		==Bcl-2 alpha beta-1 complex==
	<StructureSection load='5agw' size='340' side='right' caption='[[5agw]], [[Resolution\|resolution]] 2.69Å' scene=''>		<StructureSection load='5agw' size='340' side='right' caption='[[5agw]], [[Resolution\|resolution]] 2.69Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5agw]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5AGW OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5AGW FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5agw]] is a 4 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=5AGW OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5AGW FirstGlance]. <br>
	</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=AJE:(3S,4R)-4-AMINO-1-(3-CARBOXYPROPANOYL)PYRROLIDINE-3-CARBOXYLIC+ACID'>AJE</scene>, <scene name='pdbligand=MH8:(2S)-2-AMINO-2-METHYLHEPT-6-ENOIC+ACID'>MH8</scene>, <scene name='pdbligand=XCP:(1S,2S)-2-AMINOCYCLOPENTANECARBOXYLIC+ACID'>XCP</scene></td></tr>		</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=AJE:(3S,4R)-4-AMINO-1-(3-CARBOXYPROPANOYL)PYRROLIDINE-3-CARBOXYLIC+ACID'>AJE</scene>, <scene name='pdbligand=MH8:(2S)-2-AMINO-2-METHYLHEPT-6-ENOIC+ACID'>MH8</scene>, <scene name='pdbligand=XCP:(1S,2S)-2-AMINOCYCLOPENTANECARBOXYLIC+ACID'>XCP</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5agx\|5agx]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5agx\|5agx]]</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=5agw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5agw OCA], [http://pdbe.org/5agw PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5agw RCSB], [http://www.ebi.ac.uk/pdbsum/5agw 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=5agw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5agw OCA], [http://pdbe.org/5agw PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5agw RCSB], [http://www.ebi.ac.uk/pdbsum/5agw PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5agw ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
Line 24:		Line 25:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Checco, J W]]		[[Category: Checco, J W]]
	[[Category: Fairlie, W D]]		[[Category: Fairlie, W D]]

OCA at 06:30, 30 September 2015

OCA — Wed, 30 Sep 2015 06:30:16 GMT

←Older revision		Revision as of 06:30, 30 September 2015
Line 5:		Line 5:
	</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=AJE:(3S,4R)-4-AMINO-1-(3-CARBOXYPROPANOYL)PYRROLIDINE-3-CARBOXYLIC+ACID'>AJE</scene>, <scene name='pdbligand=MH8:(2S)-2-AMINO-2-METHYLHEPT-6-ENOIC+ACID'>MH8</scene>, <scene name='pdbligand=XCP:(1S,2S)-2-AMINOCYCLOPENTANECARBOXYLIC+ACID'>XCP</scene></td></tr>		</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=AJE:(3S,4R)-4-AMINO-1-(3-CARBOXYPROPANOYL)PYRROLIDINE-3-CARBOXYLIC+ACID'>AJE</scene>, <scene name='pdbligand=MH8:(2S)-2-AMINO-2-METHYLHEPT-6-ENOIC+ACID'>MH8</scene>, <scene name='pdbligand=XCP:(1S,2S)-2-AMINOCYCLOPENTANECARBOXYLIC+ACID'>XCP</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5agx\|5agx]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5agx\|5agx]]</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=5agw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5agw OCA], [http://www.rcsb.org/pdb/explore.do?structureId=5agw RCSB], [http://www.ebi.ac.uk/pdbsum/5agw 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=5agw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5agw OCA], [http://pdbe.org/5agw PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5agw RCSB], [http://www.ebi.ac.uk/pdbsum/5agw PDBsum]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
Line 19:		Line 19:
	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>
		+	<div class="pdbe-citations 5agw" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 11:15, 9 September 2015

OCA — Wed, 09 Sep 2015 11:15:26 GMT

←Older revision		Revision as of 11:15, 9 September 2015
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-	'''~~Unreleased~~ structure'''	+	==Bcl-2 alpha beta-1 complex==
		+	<StructureSection load='5agw' size='340' side='right' caption='[[5agw]], [[Resolution\|resolution]] 2.69Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5agw]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5AGW OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5AGW FirstGlance]. <br>
		+	</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=AJE:(3S,4R)-4-AMINO-1-(3-CARBOXYPROPANOYL)PYRROLIDINE-3-CARBOXYLIC+ACID'>AJE</scene>, <scene name='pdbligand=MH8:(2S)-2-AMINO-2-METHYLHEPT-6-ENOIC+ACID'>MH8</scene>, <scene name='pdbligand=XCP:(1S,2S)-2-AMINOCYCLOPENTANECARBOXYLIC+ACID'>XCP</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5agx\|5agx]]</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=5agw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5agw OCA], [http://www.rcsb.org/pdb/explore.do?structureId=5agw RCSB], [http://www.ebi.ac.uk/pdbsum/5agw PDBsum]</span></td></tr>
		+	</table>
		+	== Disease ==
		+	[[http://www.uniprot.org/uniprot/BCL2_HUMAN BCL2_HUMAN]] Note=A chromosomal aberration involving BCL2 has been found in chronic lymphatic leukemia. Translocation t(14;18)(q32;q21) with immunoglobulin gene regions. BCL2 mutations found in non-Hodgkin lymphomas carrying the chromosomal translocation could be attributed to the Ig somatic hypermutation mechanism resulting in nucleotide transitions.
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/BCL2_HUMAN BCL2_HUMAN]] Suppresses apoptosis in a variety of cell systems including factor-dependent lymphohematopoietic and neural cells. Regulates cell death by controlling the mitochondrial membrane permeability. Appears to function in a feedback loop system with caspases. Inhibits caspase activity either by preventing the release of cytochrome c from the mitochondria and/or by binding to the apoptosis-activating factor (APAF-1).<ref>PMID:18570871</ref> [[http://www.uniprot.org/uniprot/B2L11_HUMAN B2L11_HUMAN]] Induces apoptosis and anoikis. Isoform BimL is more potent than isoform BimEL. Isoform Bim-alpha1, isoform Bim-alpha2 and isoform Bim-alpha3 induce apoptosis, although less potent than isoform BimEL, isoform BimL and isoform BimS. Isoform Bim-gamma induces apoptosis. Isoform Bim-alpha3 induces apoptosis possibly through a caspase-mediated pathway. Isoform BimAC and isoform BimABC lack the ability to induce apoptosis.<ref>PMID:9430630</ref> <ref>PMID:11734221</ref> <ref>PMID:12019181</ref> <ref>PMID:11997495</ref> <ref>PMID:15147734</ref> <ref>PMID:15486195</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Peptides can be developed as effective antagonists of protein-protein interactions, but conventional peptides (i.e., oligomers of l-alpha-amino acids) suffer from significant limitations in vivo. Short half-lives due to rapid proteolytic degradation and an inability to cross cell membranes often preclude biological applications of peptides. Oligomers that contain both alpha- and beta-amino acid residues ("alpha/beta-peptides") manifest decreased susceptibility to proteolytic degradation, and when properly designed these unnatural oligomers can mimic the protein-recognition properties of analogous "alpha-peptides". This report documents an extension of the alpha/beta-peptide approach to target intracellular protein-protein interactions. Specifically, we have generated alpha/beta-peptides based on a "stapled" Bim BH3 alpha-peptide, which contains a hydrocarbon cross-link to enhance alpha-helix stability. We show that a stapled alpha/beta-peptide can structurally and functionally mimic the parent stapled alpha-peptide in its ability to enter certain types of cells and block protein-protein interactions associated with apoptotic signaling. However, the alpha/beta-peptide is nearly 100-fold more resistant to proteolysis than is the parent stapled alpha-peptide. These results show that backbone modification, a strategy that has received relatively little attention in terms of peptide engineering for biomedical applications, can be combined with more commonly deployed peripheral modifications such as side chain cross-linking to produce synergistic benefits.

-	~~The entry 5agw is ON HOLD until Paper Publication~~	+	alpha/beta-Peptide Foldamers Targeting Intracellular Protein-Protein Interactions with Activity in Living Cells.,Checco JW, Lee EF, Evangelista M, Sleebs NJ, Rogers K, Pettikiriarachchi A, Kershaw NJ, Eddinger GA, Belair DG, Wilson JL, Eller CH, Raines RT, Murphy WL, Smith BJ, Gellman SH, Fairlie WD J Am Chem Soc. 2015 Aug 28. PMID:26317395<ref>PMID:26317395</ref>

-	~~Authors: Smith~~, B.~~J., F Lee, E., Checco, J.W., Gellman,~~ S.~~H., Fairlie, W.D~~.	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-		+	</div>
-	~~Description: Bcl-2 alpha beta-1 complex~~	+	== References ==
-	[[Category: ~~Unreleased Structures~~]]	+	<references/>
-	[[Category: Fairlie, W.D]]	+	__TOC__
-	[[Category: ~~Checco~~, ~~J.W~~]]	+	</StructureSection>
-	[[Category: F Lee, E]]	+	[[Category: Checco, J W]]
-	[[Category: ~~Gellman~~, ~~S.H~~]]	+	[[Category: Fairlie, W D]]
-	[[Category: ~~Smith, B.J~~]]	+	[[Category: Gellman, S H]]
		+	[[Category: Lee, E F]]
		+	[[Category: Smith, B J]]
		+	[[Category: Apoptosis]]
		+	[[Category: Bcl-2]]
		+	[[Category: Bim]]
		+	[[Category: Foldamer]]

OCA at 10:35, 4 March 2015

OCA — Wed, 04 Mar 2015 10:35:27 GMT

←Older revision		Revision as of 10:35, 4 March 2015
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 5agw is ON HOLD	+	The entry 5agw is ON HOLD until Paper Publication

	Authors: Smith, B.J., F Lee, E., Checco, J.W., Gellman, S.H., Fairlie, W.D.		Authors: Smith, B.J., F Lee, E., Checco, J.W., Gellman, S.H., Fairlie, W.D.

OCA: Protected "5agw" [edit=sysop:move=sysop]

OCA — Thu, 12 Feb 2015 11:03:46 GMT

Protected "5agw" [edit=sysop:move=sysop]

←Older revision

Revision as of 11:03, 12 February 2015

OCA: New page: '''Unreleased structure''' The entry 5agw is ON HOLD Authors: Smith, B.J., F Lee, E., Checco, J.W., Gellman, S.H., Fairlie, W.D. Description: Bcl-2 alpha beta-1 complex [[Category: Unr...

OCA — Thu, 12 Feb 2015 11:03:45 GMT

New page: '''Unreleased structure''' The entry 5agw is ON HOLD Authors: Smith, B.J., F Lee, E., Checco, J.W., Gellman, S.H., Fairlie, W.D. Description: Bcl-2 alpha beta-1 complex [[Category: Unr...

New page

'''Unreleased structure'''

The entry 5agw is ON HOLD

Authors: Smith, B.J., F Lee, E., Checco, J.W., Gellman, S.H., Fairlie, W.D.

Description: Bcl-2 alpha beta-1 complex
[[Category: Unreleased Structures]]
[[Category: Fairlie, W.D]]
[[Category: Checco, J.W]]
[[Category: F Lee, E]]
[[Category: Gellman, S.H]]
[[Category: Smith, B.J]]