氨肽酶 N（CD13）作为癌症化疗的靶点。
Aminopeptidase N (CD13) as a target for cancer chemotherapy.
机构信息
Department of Medical Sciences, Division of Clinical Pharmacology, Uppsala University Hospital, Uppsala, Sweden.
出版信息
Cancer Sci. 2011 Mar;102(3):501-8. doi: 10.1111/j.1349-7006.2010.01826.x. Epub 2011 Jan 30.
Abstract
The enzyme aminopeptidase N (APN, also known as CD13) is a Zn(2+) dependent membrane-bound ectopeptidase that degrades preferentially proteins and peptides with a N-terminal neutral amino acid. Aminopeptidase N has been associated with the growth of different human cancers and suggested as a suitable target for anti-cancerous therapy. Different approaches have been used to develop new drugs directed to this target, including enzyme inhibitors as well as APN-targeted carrier constructs. This review discusses the prevalence and possible function of APN in malignant diseases, mainly solid tumors, as well as its "drugability" evaluated in preclinical in vivo models, and also provides a brief overview of current clinical trials focused on APN.
摘要
酶氨基肽酶 N（APN，也称为 CD13）是一种 Zn(2+) 依赖性膜结合外肽酶，优先降解具有 N 端中性氨基酸的蛋白质和肽。氨基肽酶 N 与不同人类癌症的生长有关，并被认为是抗癌治疗的合适靶点。已经使用了不同的方法来开发针对该靶点的新药，包括酶抑制剂以及 APN 靶向载体构建体。本文综述了 APN 在恶性疾病（主要是实体瘤）中的流行情况和可能的功能，以及在临床前体内模型中评估的“可成药性”，并简要概述了目前针对 APN 的临床试验。
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