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Altered regulation of metabolic pathways in human lung cancer discerned by (13)C stable isotope-resolved metabolomics (SIRM).通过(13)C 稳定同位素分辨代谢组学(SIRM)识别出人类肺癌中代谢途径的调节异常。
Mol Cancer. 2009 Jun 26;8:41. doi: 10.1186/1476-4598-8-41.
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Smaller is better for antibiotic discovery.对于抗生素发现而言,越小越好。
ACS Chem Biol. 2009 Jun 19;4(6):397-9. doi: 10.1021/cb900122j.
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A symmetrical tetramer for S. aureus pyruvate carboxylase in complex with coenzyme A.与辅酶A结合的金黄色葡萄球菌丙酮酸羧化酶的对称四聚体。
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Discovery of antibacterial biotin carboxylase inhibitors by virtual screening and fragment-based approaches.通过虚拟筛选和基于片段的方法发现抗菌生物素羧化酶抑制剂。
ACS Chem Biol. 2009 Jun 19;4(6):473-83. doi: 10.1021/cb9000102.
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Insight into the carboxyl transferase domain mechanism of pyruvate carboxylase from Rhizobium etli.对来自墨西哥根瘤菌的丙酮酸羧化酶羧基转移酶结构域机制的深入了解。
Biochemistry. 2009 May 26;48(20):4305-13. doi: 10.1021/bi9003759.
6
A class of selective antibacterials derived from a protein kinase inhibitor pharmacophore.一类源自蛋白激酶抑制剂药效团的选择性抗菌剂。
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Metabolic cycling in control of glucose-stimulated insulin secretion.代谢循环对葡萄糖刺激的胰岛素分泌的调控
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8
Impaired anaplerosis and insulin secretion in insulinoma cells caused by small interfering RNA-mediated suppression of pyruvate carboxylase.小干扰RNA介导的丙酮酸羧化酶抑制导致胰岛素瘤细胞中回补反应和胰岛素分泌受损。
J Biol Chem. 2008 Oct 17;283(42):28048-59. doi: 10.1074/jbc.M804170200. Epub 2008 Aug 12.
9
Structure, mechanism and regulation of pyruvate carboxylase.丙酮酸羧化酶的结构、机制与调控
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10
Crystal structures of human and Staphylococcus aureus pyruvate carboxylase and molecular insights into the carboxyltransfer reaction.人源和金黄色葡萄球菌丙酮酸羧化酶的晶体结构以及对羧基转移反应的分子见解
Nat Struct Mol Biol. 2008 Mar;15(3):295-302. doi: 10.1038/nsmb.1393. Epub 2008 Feb 24.

丙酮酸羧化酶抑制剂

Inhibitors of Pyruvate Carboxylase.

作者信息

Zeczycki Tonya N, Maurice Martin St, Attwood Paul V

机构信息

Department of Biochemistry, University of Wisconsin, Madison, WI 53726, USA.

出版信息

Open Enzym Inhib J. 2010;3:8-26. doi: 10.2174/1874940201003010008.

DOI:10.2174/1874940201003010008
PMID:22180764
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3238542/
Abstract

This review aims to discuss the varied types of inhibitors of biotin-dependent carboxylases, with an emphasis on the inhibitors of pyruvate carboxylase. Some of these inhibitors are physiologically relevant, in that they provide ways of regulating the cellular activities of the enzymes e.g. aspartate and prohibitin inhibition of pyruvate carboxylase. Most of the inhibitors that will be discussed have been used to probe various aspects of the structure and function of these enzymes. They target particular parts of the structure e.g. avidin - biotin, FTP - ATP binding site, oxamate - pyruvate binding site, phosphonoacetate - binding site of the putative carboxyphosphate intermediate.

摘要

本综述旨在讨论生物素依赖性羧化酶的多种抑制剂类型,重点是丙酮酸羧化酶的抑制剂。其中一些抑制剂具有生理相关性,因为它们提供了调节这些酶细胞活性的方式,例如天冬氨酸和抑制素对丙酮酸羧化酶的抑制作用。本文将讨论的大多数抑制剂已被用于探究这些酶结构和功能的各个方面。它们作用于结构的特定部位,例如抗生物素蛋白-生物素、FTP-ATP结合位点、草氨酸-丙酮酸结合位点、假定的羧基磷酸中间体的膦酰乙酸结合位点。