2c4g

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[[Image:2c4g.gif|left|200px]]<br /><applet load="2c4g" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2c4g.gif|left|200px]]
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caption="2c4g, resolution 2.70&Aring;" />
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'''STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514'''<br />
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{{Structure
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|PDB= 2c4g |SIZE=350|CAPTION= <scene name='initialview01'>2c4g</scene>, resolution 2.70&Aring;
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|SITE= <scene name='pdbsite=AC1:So4+Binding+Site+For+Chain+D'>AC1</scene>
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|LIGAND= <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene> and <scene name='pdbligand=514:(3Z)-5-ACETYL-3-(BENZOYLIMINO)-3,6-DIHYDROPYRROLO[3,4-C]PYRAZOL-5-IUM'>514</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37]
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|GENE=
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}}
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'''STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2C4G is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=514:'>514</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37] Known structural/functional Site: <scene name='pdbsite=AC1:So4+Binding+Site+For+Chain+D'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2C4G OCA].
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2C4G is a [[Protein complex]] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2C4G OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16290148 16290148]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/16290148 16290148]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Protein complex]]
[[Category: Protein complex]]
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:44:45 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:10:42 2008''

Revision as of 14:10, 20 March 2008

Image:2c4g.gif


PDB ID 2c4g

Drag the structure with the mouse to rotate
, resolution 2.70Å
Sites:
Ligands: and
Activity: Transferred entry: 2.7.11.1, with EC number 2.7.1.37
Coordinates: save as pdb, mmCIF, xml



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 Thu Mar 20 16:10:42 2008

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