2c4g

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[[Image:2c4g.gif|left|200px]]
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{{STRUCTURE_2c4g| PDB=2c4g | SCENE= }}
{{STRUCTURE_2c4g| PDB=2c4g | SCENE= }}
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'''STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514'''
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===STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514===
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==Overview==
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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.
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{{ABSTRACT_PUBMED_16290148}}
==About this Structure==
==About this Structure==
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[[Category: Serine/threonine-protein kinase]]
[[Category: Serine/threonine-protein kinase]]
[[Category: Transferase]]
[[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 Jul 28 10:57:32 2008''

Revision as of 07:57, 28 July 2008

Image:2c4g.png

Template:STRUCTURE 2c4g

STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514

Template:ABSTRACT PUBMED 16290148

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

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