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2oxy

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{{STRUCTURE_2oxy| PDB=2oxy | SCENE= }}
{{STRUCTURE_2oxy| PDB=2oxy | SCENE= }}
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'''Protein kinase CK2 in complex with tetrabromobenzoimidazole derivatives K17, K22 and K32'''
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===Protein kinase CK2 in complex with tetrabromobenzoimidazole derivatives K17, K22 and K32===
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==Overview==
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CK2 is a highly pleiotropic Ser/Thr protein kinase that is able to promote cell survival and enhance the tumour phenotype under specific circumstances. We have determined the crystal structure of three new complexes with tetrabromobenzimidazole derivatives that display K(i) values between 0.15 and 0.30 microM. A comparative analysis of these data with those of four other inhibitors of the same family revealed the presence of some highly conserved water molecules in the ATP-binding site. These waters reside near Lys68, in an area with a positive electrostatic potential that is able to attract and orient negatively charged ligands. The presence of this positive region and two unique bulky residues that are typical of CK2, Ile66 and Ile174, play a critical role in determining the ligand orientation and binding selectivity.
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{{ABSTRACT_PUBMED_17768728}}
==About this Structure==
==About this Structure==
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[[Category: Tetrabromobenzoimidazole derivative]]
[[Category: Tetrabromobenzoimidazole derivative]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 11:36:21 2008''

Revision as of 08:36, 28 July 2008

Image:2oxy.png

Template:STRUCTURE 2oxy

Protein kinase CK2 in complex with tetrabromobenzoimidazole derivatives K17, K22 and K32

Template:ABSTRACT PUBMED 17768728

About this Structure

2OXY is a Single protein structure of sequence from Zea mays. Full crystallographic information is available from OCA.

Reference

The ATP-binding site of protein kinase CK2 holds a positive electrostatic area and conserved water molecules., Battistutta R, Mazzorana M, Cendron L, Bortolato A, Sarno S, Kazimierczuk Z, Zanotti G, Moro S, Pinna LA, Chembiochem. 2007 Oct 15;8(15):1804-9. PMID:17768728

Page seeded by OCA on Mon Jul 28 11:36:21 2008

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