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首页> 外文期刊>Acta crystallographica.Section D. Biological crystallography >Human glutamate carboxypeptidase II inhibition: structures of GCPII in complex with two potent inhibitors, quisqualate and 2-PMPA
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Human glutamate carboxypeptidase II inhibition: structures of GCPII in complex with two potent inhibitors, quisqualate and 2-PMPA

机译：人类谷氨酸羧肽酶II抑制:GCPII结构在复杂的有两个强大的抑制剂,quisqualate 2-PMPA

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摘要

Human glutamate carboxypeptidase II (GCPII) occurs in the central nervous system as well as in human prostate (where it is called prostate-specific membrane antigen; PSMA). Inhibitors of the enzyme have been shown to provide neuroprotection, but may also be useful for the detection, imaging and treatment of prostate cancer. Crystal structures were determined of the extracellular part of GCPII (amino-acid residues 44-750) in complex with two potent inhibitors, quisqualate and 2-PMPA (the strongest GCPII inhibitor to date), at resolutions of 3.0 and 2.2 angstrom, respectively. In addition, models were constructed for binding of the inhibitors willardiine, homoibotenate, L-2-amino-4-phosphonobutanoic acid and L-serine-O-sulfate to the S1' site of the enzyme. The common denominator for high-affinity binding to the S1' site is the formation of two strong salt bridges.
机译：人类谷氨酸羧肽酶II (GCPII)发生在中枢神经系统以及在人类前列腺癌(称为前列腺特异性膜抗原;已被证明提供神经保护,但也可能是有用的检测、成像和治疗前列腺癌。测定细胞外的一部分吗GCPII(氨基酸残基44 - 750)在复杂有两个强有力的抑制剂,quisqualate和2-PMPA(迄今为止最强的GCPII抑制剂),在3.0和2.2埃分辨率,分别。构建绑定的抑制剂L-2-amino-4-phosphonobutanoic酸和L-serine-O-sulfate S1 '站点的酶。高亲和性结合的公分母S1的网站是两个强大的形成盐桥。

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