2bkz

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[[Image:2bkz.gif|left|200px]]
[[Image:2bkz.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2bkz |SIZE=350|CAPTION= <scene name='initialview01'>2bkz</scene>, resolution 2.60&Aring;
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The line below this paragraph, containing "STRUCTURE_2bkz", 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=SBC:1-[4-(AMINOSULFONYL)PHENYL]-1,6-DIHYDROPYRAZOLO[3,4-E]INDAZOLE-3-CARBOXAMIDE'>SBC</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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-->
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|DOMAIN=
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{{STRUCTURE_2bkz| PDB=2bkz | 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=2bkz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2bkz OCA], [http://www.ebi.ac.uk/pdbsum/2bkz PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2bkz RCSB]</span>
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}}
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'''STRUCTURE OF CDK2-CYCLIN A WITH PHA-404611'''
'''STRUCTURE OF CDK2-CYCLIN A WITH PHA-404611'''
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[[Category: Vazquez, M L.]]
[[Category: Vazquez, M L.]]
[[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: 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 20:26:06 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:07:55 2008''
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Revision as of 17:26, 3 May 2008

Image:2bkz.gif

Template:STRUCTURE 2bkz

STRUCTURE OF CDK2-CYCLIN A WITH PHA-404611


Overview

The synthesis and the preliminary expansion of this new class of CDK2 inhibitors are presented. The synthesis was accomplished using a solution-phase protocol amenable to rapid parallel expansion and suitable to be scaled-up in view of possible lead development. Following a medicinal chemistry program aimed at improving cell permeability and selectivity, a series of compounds with nanomolar activity in the biochemical assay and able to efficiently inhibit tumor cell proliferation has been obtained.

About this Structure

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

Reference

Benzodipyrazoles: a new class of potent CDK2 inhibitors., D'Alessio R, Bargiotti A, Metz S, Brasca MG, Cameron A, Ermoli A, Marsiglio A, Polucci P, Roletto F, Tibolla M, Vazquez ML, Vulpetti A, Pevarello P, Bioorg Med Chem Lett. 2005 Mar 1;15(5):1315-9. PMID:15713378 Page seeded by OCA on Sat May 3 20:26:06 2008

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OCA

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