2qp6: Difference between revisions

Revision as of 21:32, 2 July 2008

This article has been automatically seeded. Changes to this page should pertain to the PDB entry only and not to the protein or biomolecule in general.

File:2qp6.png

Template:STRUCTURE 2qp6

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

Template:ABSTRACT PUBMED 18481843

About this StructureAbout this Structure

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

ReferenceReference

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

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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

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-'''The crystal structure of the complex of hcaII with a bioreductive antitumor derivative'''
+===The crystal structure of the complex of hcaII with a bioreductive antitumor derivative===
-==Overview==
+<!--
--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.
+The line below this paragraph, {{ABSTRACT_PUBMED_18481843}}, adds the Publication Abstract to the page
+(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==
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 [[Category: Carbonic anhydrase ii]]
 [[Category: Lyase]]
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