Kenny Paraic A
Life Sciences Division, Lawrence Berkeley National Laboratory, 1 Cyclotron Road, MS977-225A, University of California, Berkeley, CA 94720, USA.
Expert Opin Ther Targets. 2007 Oct;11(10):1287-98. doi: 10.1517/14728222.11.10.1287.
TNF-alpha converting enzyme (TACE/ADAM17) is a transmembrane metalloprotease that plays a key role in the cleavage and mobilization of receptor ligands that are initially synthesized as membrane-tethered precursors. For many years, attention has focused on the role of TACE-dependent TNF-alpha cleavage in arthritis and, more recently, it has become apparent that TACE also plays an important role in regulating epidermal growth factor receptor activity in several tumor types. This review presents the background to these findings and a rationale for the continued development of TACE inhibitors for the treatment of epidermal growth factor receptor-dependent epithelial tumors.
肿瘤坏死因子-α转换酶(TACE/ADAM17)是一种跨膜金属蛋白酶,在最初作为膜结合前体合成的受体配体的切割和释放过程中起关键作用。多年来,人们一直关注TACE依赖性肿瘤坏死因子-α切割在关节炎中的作用,最近,很明显TACE在调节几种肿瘤类型的表皮生长因子受体活性方面也起着重要作用。本文综述了这些发现的背景以及继续开发TACE抑制剂用于治疗表皮生长因子受体依赖性上皮肿瘤的理论依据。