2c4g

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[[Image:2c4g.gif|left|200px]]
[[Image:2c4g.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2c4g |SIZE=350|CAPTION= <scene name='initialview01'>2c4g</scene>, resolution 2.70&Aring;
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The line below this paragraph, containing "STRUCTURE_2c4g", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:So4+Binding+Site+For+Chain+D'>AC1</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=514:(3Z)-5-ACETYL-3-(BENZOYLIMINO)-3,6-DIHYDROPYRROLO[3,4-C]PYRAZOL-5-IUM'>514</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_2c4g| PDB=2c4g | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2c4g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2c4g OCA], [http://www.ebi.ac.uk/pdbsum/2c4g PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2c4g RCSB]</span>
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}}
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'''STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514'''
'''STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514'''
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[[Category: Villa, M.]]
[[Category: Villa, M.]]
[[Category: Vulpetti, A.]]
[[Category: Vulpetti, A.]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: cell cycle]]
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[[Category: Cell cycle]]
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[[Category: cell division]]
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[[Category: Cell division]]
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[[Category: cyclin]]
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[[Category: Cyclin]]
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[[Category: mitosis]]
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[[Category: Mitosis]]
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[[Category: nucleotide-binding]]
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[[Category: Nucleotide-binding]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: polymorphism]]
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[[Category: Polymorphism]]
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[[Category: protein kinase]]
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[[Category: Protein kinase]]
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[[Category: serine/threonine-protein kinase]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 21:14:08 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:16:08 2008''
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Revision as of 18:14, 3 May 2008

Template:STRUCTURE 2c4g

STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514


Overview

We have recently reported about a new class of Aurora-A inhibitors based on a bicyclic tetrahydropyrrolo[3,4-c]pyrazole scaffold. Here we describe the synthesis and early expansion of CDK2/cyclin A-E inhibitors belonging to the same chemical class. Synthesis of the compounds was accomplished using a solution-phase protocol amenable to rapid parallel expansion. Compounds with nanomolar activity in the biochemical assay and able to efficiently inhibit CDK2-mediated tumor cell proliferation have been obtained.

About this Structure

2C4G is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors., Pevarello P, Fancelli D, Vulpetti A, Amici R, Villa M, Pittala V, Vianello P, Cameron A, Ciomei M, Mercurio C, Bischoff JR, Roletto F, Varasi M, Brasca MG, Bioorg Med Chem Lett. 2006 Feb 15;16(4):1084-90. Epub 2005 Nov 14. PMID:16290148 Page seeded by OCA on Sat May 3 21:14:08 2008

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