The diamond anniversary of tissue transglutaminase: a protein of many talents.

The diamond anniversary of tissue transglutaminase: a protein of many talents.
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DOI:
10.1016/j.drudis.2018.01.037
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发表时间:
2018-03
影响因子:
7.4
通讯作者:
Cerione RA
Cerione RA
中科院分区:
医学2区
文献类型:
--
作者:
Katt WP;Antonyak MA;Cerione RA

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组织转氨酶(tTG)能够结合和水解GTP,以及催化将伯胺交联至谷氨酰胺残基的酶促转酰胺反应。tTG采用两种截然不同的构象,这取决于它是作为GTP结合蛋白还是交联酶发挥作用。它已被证明在癌症进展的几个不同方面具有重要作用,使其成为治疗干预的有吸引力的靶点。在这里,我们强调了许多主要的发现涉及tTG自60年前发现,并描述了最近的药物发现的努力,针对这种独特的蛋白质的特定活动或构象。
Tissue transglutaminase (tTG) is capable of binding and hydrolyzing GTP, as well as catalyzing an enzymatic transamidation reaction that crosslinks primary amines to glutamine residues. tTG adopts two vastly different conformations, depending on whether it is functioning as a GTP-binding protein or a crosslinking enzyme. It has been shown to have important roles in several different aspects of cancer progression, making it an attractive target for therapeutic intervention. Here, we highlight many of the major findings involving tTG since its discovery 60 years ago, and describe recent drug discovery efforts that target specific activities or conformations of this unique protein.
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