2qp6

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{{STRUCTURE_2qp6| PDB=2qp6 | SCENE= }}
{{STRUCTURE_2qp6| PDB=2qp6 | SCENE= }}
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'''The crystal structure of the complex of hcaII with a bioreductive antitumor derivative'''
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===The crystal structure of the complex of hcaII with a bioreductive antitumor derivative===
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==Overview==
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2-Substituted-5-nitro-benzenesulfonamides incorporating a large variety of secondary/tertiary amines were explored as inhibitors of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), with the aim of designing bioreductive inhibitors targeting the hypoxia overexpressed, tumor-associated isozymes. The compounds were ineffective inhibitors of the cytosolic isoform I, showed a better inhibition of the physiologically relevant CA II ( K Is of 8.8-4975 nM), and strongly inhibited the tumor-associated CA IX and XII ( K Is of 5.4-653 nM). Some of these compounds showed excellent selectivity ratios for the inhibition of the tumor-associated isozymes over the cytosolic ones (in the range of 10-1395). The X-ray crystal structure of the adduct of hCA II with the lead molecule 2-chloro-5-nitro-benzenesulfonamide as well as molecular modeling studies for interaction with hCA IX afforded a better understanding of factors governing the discrimination of the two isoforms for this type of bioreductive compound targeting specifically hypoxic tumors.
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(as it appears on PubMed at http://www.pubmed.gov), where 18481843 is the PubMed ID number.
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{{ABSTRACT_PUBMED_18481843}}
==About this Structure==
==About this Structure==
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[[Category: Carbonic anhydrase ii]]
[[Category: Carbonic anhydrase ii]]
[[Category: Lyase]]
[[Category: Lyase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jun 4 09:52:02 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 2 21:32:45 2008''

Revision as of 18:32, 2 July 2008

Image:2qp6.png

Template:STRUCTURE 2qp6

The crystal structure of the complex of hcaII with a bioreductive antitumor derivative

Template:ABSTRACT PUBMED 18481843

About this Structure

2QP6 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Carbonic Anhydrase Inhibitors: Bioreductive Nitro-Containing Sulfonamides with Selectivity for Targeting the Tumor Associated Isoforms IX and XII., D'Ambrosio K, Vitale RM, Dogne JM, Masereel B, Innocenti A, Scozzafava A, De Simone G, Supuran CT, J Med Chem. 2008 May 16;. PMID:18481843

Page seeded by OCA on Wed Jul 2 21:32:45 2008

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