1v0b

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{{STRUCTURE_1v0b| PDB=1v0b | SCENE= }}
{{STRUCTURE_1v0b| PDB=1v0b | SCENE= }}
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'''CRYSTAL STRUCTURE OF THE T198A MUTANT OF PFPK5'''
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===CRYSTAL STRUCTURE OF THE T198A MUTANT OF PFPK5===
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==Overview==
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Plasmodium falciparum cell cycle regulators are promising targets for antimalarial drug design. We have determined the structure of PfPK5, the first structure of a P. falciparum protein kinase and the first of a cyclin-dependent kinase (CDK) not derived from humans. The fold and the mechanism of inactivation of monomeric CDKs are highly conserved across evolution. ATP-competitive CDK inhibitors have been developed as potential leads for cancer therapeutics. These studies have identified regions of the CDK active site that can be exploited to achieve significant gains in inhibitor potency and selectivity. We have cocrystallized PfPK5 with three inhibitors that target such regions. The sequence differences between PfPK5 and human CDKs within these inhibitor binding sites suggest that selective inhibition is an attainable goal. Such compounds will be useful tools for P. falciparum cell cycle studies, and will provide lead compounds for antimalarial drug development.
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(as it appears on PubMed at http://www.pubmed.gov), where 14604523 is the PubMed ID number.
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{{ABSTRACT_PUBMED_14604523}}
==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 Mon Jul 28 07:03:06 2008''

Revision as of 04:03, 28 July 2008

Image:1v0b.png

Template:STRUCTURE 1v0b

CRYSTAL STRUCTURE OF THE T198A MUTANT OF PFPK5

Template:ABSTRACT PUBMED 14604523

About this Structure

1V0B is a Single protein structure of sequence from Plasmodium falciparum. Full crystallographic information is available from OCA.

Reference

Structures of P. falciparum PfPK5 test the CDK regulation paradigm and suggest mechanisms of small molecule inhibition., Holton S, Merckx A, Burgess D, Doerig C, Noble M, Endicott J, Structure. 2003 Nov;11(11):1329-37. PMID:14604523

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