期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 17, 页码 5023-5026出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.07.051
关键词
Crystal structure; Human carbonic anhydrase VII; Inhibitors; Protein-inhibitor complex; Rational drug design
资金
- European Union
Human carbonic anhydrase VII (hCA VII) is a cytosolic member of the alpha-CA family. This enzyme is mainly localized in a number of brain tissues such as the cortex, hippocampus and thalamus and has been noted for its contribution in generating neuronal excitation and seizures. Recently, it has been also proposed that hCA VII may be involved in the control of neuropathic pain, thus its inhibition may offer a new approach in designing pain killers useful for combating neuropathic pain. We report here the X-ray crystallographic structure of a mutated form of human CA VII in complex with acetazolamide, a classical sulfonamide inhibitor. These crystallographic studies provide important implications for the rational drug design of selective CA inhibitors with clinical applications. (C) 2010 Elsevier Ltd. All rights reserved.
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