4r3m

From Proteopedia

(Difference between revisions)

Revision as of 09:39, 1 May 2019

Crystal structure of Human Hsp90 with JR9

Structural highlights

4r3m is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
Gene:	HSP90A, HSP90AA1, HSPC1, HSPCA (HUMAN)
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[HS90A_HUMAN] Molecular chaperone that promotes the maturation, structural maintenance and proper regulation of specific target proteins involved for instance in cell cycle control and signal transduction. Undergoes a functional cycle that is linked to its ATPase activity. This cycle probably induces conformational changes in the client proteins, thereby causing their activation. Interacts dynamically with various co-chaperones that modulate its substrate recognition, ATPase cycle and chaperone function.^[1] ^[2]

Publication Abstract from PubMed

Using a 2,3-diamino pyrazine substrate and yttrium triflate catalyst, various 2-alkyl and aryl substituted 3,8-diaminoimidazo[1,2-a]pyrazines were efficiently prepared through Groebke-Blackburn-Bienayme MCR. In particular, a novel 2-piperonyl 3,8-diaminoimidazo[1,2-a]pyrazine structure was prepared exclusively with this new method and was found to have moderate Hsp90 inhibitory activity. A crystalline complex with N-terminus ATP domain of Hsp90 and one of the new Hsp90 inhibitors was also obtained to elucidate the origin of activity of 2-piperonyl 3,8-diaminoimidazo[1,2-a]pyrazines.

Multi-substituted 8-aminoimidazo[1,2-a]pyrazines by Groebke-Blackburn-Bienayme reaction and their Hsp90 inhibitory activity.,Ren J, Yang M, Liu H, Cao D, Chen D, Li J, Tang L, He J, Chen YL, Geng M, Xiong B, Shen J Org Biomol Chem. 2015 Feb 7;13(5):1531-5. doi: 10.1039/c4ob01865f. PMID:25490978^[3]

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

References

↑ Martinez-Ruiz A, Villanueva L, Gonzalez de Orduna C, Lopez-Ferrer D, Higueras MA, Tarin C, Rodriguez-Crespo I, Vazquez J, Lamas S. S-nitrosylation of Hsp90 promotes the inhibition of its ATPase and endothelial nitric oxide synthase regulatory activities. Proc Natl Acad Sci U S A. 2005 Jun 14;102(24):8525-30. Epub 2005 Jun 3. PMID:15937123 doi:10.1073/pnas.0407294102
↑ Forsythe HL, Jarvis JL, Turner JW, Elmore LW, Holt SE. Stable association of hsp90 and p23, but Not hsp70, with active human telomerase. J Biol Chem. 2001 May 11;276(19):15571-4. Epub 2001 Mar 23. PMID:11274138 doi:10.1074/jbc.C100055200
↑ Ren J, Yang M, Liu H, Cao D, Chen D, Li J, Tang L, He J, Chen YL, Geng M, Xiong B, Shen J. Multi-substituted 8-aminoimidazo[1,2-a]pyrazines by Groebke-Blackburn-Bienayme reaction and their Hsp90 inhibitory activity. Org Biomol Chem. 2015 Feb 7;13(5):1531-5. doi: 10.1039/c4ob01865f. PMID:25490978 doi:http://dx.doi.org/10.1039/c4ob01865f

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/4r3m"

@@ Line 1: / Line 1: @@
 ==Crystal structure of Human Hsp90 with JR9==
-<StructureSection load='4r3m' size='340' side='right' caption='[[4r3m]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
+<StructureSection load='4r3m' size='340' side='right'caption='[[4r3m]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[4r3m]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4R3M OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4R3M FirstGlance]. <br>
+<table><tr><td colspan='2'>[[4r3m]] 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=4R3M OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4R3M FirstGlance]. <br>
 </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=JR9:N~3~-BENZYL-2-[(6-BROMO-1,3-BENZODIOXOL-5-YL)METHYL]IMIDAZO[1,2-A]PYRAZINE-3,8-DIAMINE'>JR9</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=4r3m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4r3m OCA], [http://pdbe.org/4r3m PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4r3m RCSB], [http://www.ebi.ac.uk/pdbsum/4r3m PDBsum]</span></td></tr>
+<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">HSP90A, HSP90AA1, HSPC1, HSPCA ([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=4r3m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4r3m OCA], [http://pdbe.org/4r3m PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4r3m RCSB], [http://www.ebi.ac.uk/pdbsum/4r3m PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4r3m ProSAT]</span></td></tr>
 </table>
 == Function ==
@@ Line 24: / Line 26: @@
 __TOC__
 </StructureSection>
+[[Category: Human]]
+[[Category: Large Structures]]
 [[Category: He, J]]
 [[Category: Li, J]]

4r3m

From Proteopedia

Revision as of 09:39, 1 May 2019

Crystal structure of Human Hsp90 with JR9

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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