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NR5A2发现可阻断胰腺导管腺癌肿瘤生长的化合物。

NR5A2 discovering compounds that block tumor growth in PDAC.

作者信息

Fletterick Robert

机构信息

Department of Biochemistry, School of Medicine, UCSF, San Francisco, California.

出版信息

J Surg Oncol. 2017 Jul;116(1):89-93. doi: 10.1002/jso.24639. Epub 2017 Apr 26.

DOI:10.1002/jso.24639
PMID:28445593
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5519325/
Abstract

Pancreatic cancers depend on driver molecules, oncogene proteins such as RAS. NR5A2 protein is a transcription factor and either activates or inhibits transcription through actions at hundreds of enhancers. It has unusual properties with effects appearing in multiple signaling networks. NR5A2 is a pluripotency reprogramming factor in the class nuclear receptor. Its controlling hormone is PIP3. Experiments suggest NR5A2 activation drives PDAC and inhibitors blunt cancer cell proliferation.

摘要

胰腺癌依赖于驱动分子,如RAS等致癌基因蛋白。NR5A2蛋白是一种转录因子,通过作用于数百个增强子来激活或抑制转录。它具有不同寻常的特性,其效应出现在多个信号网络中。NR5A2是核受体类中的一种多能性重编程因子。其调控激素是PIP3。实验表明,NR5A2的激活会驱动胰腺导管腺癌(PDAC),而抑制剂会抑制癌细胞增殖。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4d3c/5519325/79d4e7d22081/nihms865722f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4d3c/5519325/79d4e7d22081/nihms865722f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4d3c/5519325/79d4e7d22081/nihms865722f1.jpg

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Structure of Liver Receptor Homolog-1 (NR5A2) with PIP3 hormone bound in the ligand binding pocket.肝脏受体同源物-1(NR5A2)的结构,其配体结合口袋中结合有PIP3激素。
J Struct Biol. 2015 Dec;192(3):342-348. doi: 10.1016/j.jsb.2015.09.012. Epub 2015 Sep 28.
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Molecular basis for the regulation of the nuclear receptor LRH-1.
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Nat Commun. 2022 Oct 8;13(1):5941. doi: 10.1038/s41467-022-33718-7.
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