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自动分泌酶的三维视图。

A 3D view of autotaxin.

机构信息

Department of Biophysics and Biochemistry, Graduate School of Science, University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.

出版信息

Trends Pharmacol Sci. 2012 Mar;33(3):138-45. doi: 10.1016/j.tips.2011.12.004. Epub 2012 Jan 23.

DOI:10.1016/j.tips.2011.12.004
PMID:22277299
Abstract

Autotaxin (ATX), also known as ectonucleotide pyrophosphatase/phosphodiesterase 2 (Enpp2), is a secreted lysophospholipase D (lysoPLD) that generates the lipid mediator lysophosphatidic acid (LPA), which in turn activates G protein-coupled receptors to evoke various cellular responses. ATX is essential for normal development, is implicated in various physiological processes, and is also associated with pathological conditions such as cancer, pain and fibrosis. Despite its importance, the molecular mechanism of ATX-catalyzed LPA production has long been elusive. Recent structural analyses have provided new insights into the mechanisms of localized and regulated LPA production by ATX. This structural information will pave the way for further biochemical, biological and medical research.

摘要

自分泌酶(ATX),也称为核苷酸焦磷酸酶/磷酸二酯酶 2(Enpp2),是一种分泌型溶血磷脂酶 D(lysoPLD),可生成脂质介质溶血磷脂酸(LPA),LPA 反过来激活 G 蛋白偶联受体,引发各种细胞反应。ATX 对正常发育至关重要,与各种生理过程有关,也与癌症、疼痛和纤维化等病理状况有关。尽管它很重要,但 ATX 催化 LPA 产生的分子机制长期以来一直难以捉摸。最近的结构分析为 ATX 局部和调节 LPA 产生的机制提供了新的见解。这些结构信息将为进一步的生化、生物学和医学研究铺平道路。

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A 3D view of autotaxin.自动分泌酶的三维视图。
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[Function and biological activities of the autotaxin-LPA axis].自分泌运动因子-溶血磷脂酸轴的功能及生物学活性
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Lysophospholipase D and its role in LPA production.溶血磷脂酶D及其在溶血磷脂酸生成中的作用。
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Discovery of potent nucleotide pyrophosphatase/phosphodiesterase3 (NPP3) inhibitors with ancillary carbonic anhydrase inhibition for cancer (immuno)therapy.发现具有辅助性碳酸酐酶抑制作用的强效核苷酸焦磷酸酶/磷酸二酯酶3(NPP3)抑制剂用于癌症(免疫)治疗。
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