前列腺特异性膜抗原（PSMA）抑制剂的蜕变
Metamorphosis of prostate specific membrane antigen (PSMA) inhibitors.
作者信息
Nikfarjam Zahra, Zargari Farshid, Nowroozi Alireza, Bavi Omid
机构信息
Department of Physical and Computational Chemistry, Chemistry and Chemical Engineering Research Center of Iran, 1496813151 Tehran, Iran.
Pharmacology Research Center, Zahedan University of Medical Sciences, Zahedan, 9816743463 Iran.
出版信息
Biophys Rev. 2022 Jan 13;14(1):303-315. doi: 10.1007/s12551-021-00919-1. eCollection 2022 Feb.
Abstract
Prostate-specific membrane antigen (PSMA), also called glutamate carboxypeptidase II (GCP(II)), is a Zn-dependent metalloprotease that is known as a well prostate cancer indication and a potential targeting towards anti-cancer medicines and drug delivery. Because of its centrality in the diagnostics and treatment of prostate cancer, several types of inhibitors are designed with particular scaffolds. In this study, important groups of related inhibitors as well as reported experimental and computational studies are being reviewed, in which we examined three functional groups on each group of structures. The importance of computational biochemistry and the necessity of extensive research in this area on PSMA and its effective ligands are recommended.
摘要
前列腺特异性膜抗原（PSMA），也称为谷氨酸羧肽酶II（GCP(II)），是一种锌依赖性金属蛋白酶，是一种公认的前列腺癌指标，也是抗癌药物和药物递送的潜在靶点。由于其在前列腺癌诊断和治疗中的核心地位，人们设计了几种具有特定支架的抑制剂。在本研究中，我们对相关抑制剂的重要类别以及已报道的实验和计算研究进行了综述，其中我们检查了每组结构上的三个官能团。推荐了计算生物化学的重要性以及在该领域对PSMA及其有效配体进行广泛研究的必要性。
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