人肝脏糖原磷酸化酶的吲哚 - 2 - 甲酰胺抑制剂 - Suppr

Indole-2-carboxamide inhibitors of human liver glycogen phosphorylase.

作者信息

Hoover D J, Lefkowitz-Snow S, Burgess-Henry J L, Martin W H, Armento S J, Stock I A, McPherson R K, Genereux P E, Gibbs E M, Treadway J L

机构信息

Departments of Cardiovascular and Metabolic Diseases Medicinal Chemistry, Exploratory Medicinal Biology, and Cardiovascular and Metabolic Diseases Biology, Central Research Division, Pfizer Inc., Groton, Connecticut 06340, USA.

出版信息

J Med Chem. 1998 Jul 30;41(16):2934-8. doi: 10.1021/jm980264k.

DOI:10.1021/jm980264k

PMID:9685232

Abstract

摘要

相似文献

Indole-2-carboxamide inhibitors of human liver glycogen phosphorylase.人肝脏糖原磷酸化酶的吲哚 - 2 - 甲酰胺抑制剂

J Med Chem. 1998 Jul 30;41(16):2934-8. doi: 10.1021/jm980264k.

Synthesis of 5-chloro-N-aryl-1H-indole-2-carboxamide derivatives as inhibitors of human liver glycogen phosphorylase a.5-氯-N-芳基-1H-吲哚-2-甲酰胺衍生物作为人肝糖原磷酸化酶a抑制剂的合成

Bioorg Med Chem. 2008 May 15;16(10):5452-64. doi: 10.1016/j.bmc.2008.04.010. Epub 2008 Apr 11.

Design, synthesis, and pharmacological evaluation of N-bicyclo-5-chloro-1H-indole-2-carboxamide derivatives as potent glycogen phosphorylase inhibitors.N-双环-5-氯-1H-吲哚-2-甲酰胺衍生物作为强效糖原磷酸化酶抑制剂的设计、合成及药理评价

Bioorg Med Chem. 2008 Dec 1;16(23):10001-12. doi: 10.1016/j.bmc.2008.10.021. Epub 2008 Oct 12.

Kinetic and functional characterization of 1,4-dideoxy-1, 4-imino-d-arabinitol: a potent inhibitor of glycogen phosphorylase with anti-hyperglyceamic effect in ob/ob mice.1,4-二脱氧-1,4-亚氨基-D-阿拉伯糖醇的动力学和功能特性：一种有效的糖原磷酸化酶抑制剂，对ob/ob小鼠具有抗高血糖作用。

Arch Biochem Biophys. 2000 Aug 15;380(2):274-84. doi: 10.1006/abbi.2000.1930.

Discovery of a human liver glycogen phosphorylase inhibitor that lowers blood glucose in vivo.一种可在体内降低血糖的人肝脏糖原磷酸化酶抑制剂的发现。

Proc Natl Acad Sci U S A. 1998 Feb 17;95(4):1776-81. doi: 10.1073/pnas.95.4.1776.

Endogenous effectors of human liver glycogen phosphorylase modulate effects of indole-site inhibitors.人肝糖原磷酸化酶的内源性效应物调节吲哚位点抑制剂的作用。

Am J Physiol Endocrinol Metab. 2005 Sep;289(3):E366-72. doi: 10.1152/ajpendo.00264.2004. Epub 2005 Mar 29.

Synthesis, in vitro ADME profiling and in vivo pharmacological evaluation of novel glycogen phosphorylase inhibitors.新型糖原磷酸化酶抑制剂的合成、体外 ADME 分析及体内药效学评价。

Bioorg Med Chem Lett. 2020 Jul 15;30(14):127117. doi: 10.1016/j.bmcl.2020.127117. Epub 2020 Mar 20.

Human liver glycogen phosphorylase inhibitors bind at a new allosteric site.人肝糖原磷酸化酶抑制剂在一个新的变构位点结合。

Chem Biol. 2000 Sep;7(9):677-82. doi: 10.1016/s1074-5521(00)00004-1.

Synthesis and evaluation of 3-anilino-quinoxalinones as glycogen phosphorylase inhibitors.3-苯胺基喹喔啉酮作为糖原磷酸化酶抑制剂的合成与评价

Bioorg Med Chem Lett. 2005 Nov 1;15(21):4790-3. doi: 10.1016/j.bmcl.2005.07.021.

Synthesis and biological evaluation of asiatic acid derivatives as inhibitors of glycogen phosphorylases.积雪草苷衍生物作为糖原磷酸化酶抑制剂的合成及生物学评价

Chem Biodivers. 2009 Jun;6(6):864-74. doi: 10.1002/cbdv.200800092.

引用本文的文献

Allosteric Regulation of Glycogen Phosphorylase by Order/Disorder Transition of the 250' and 280s Loops.别构调节糖原磷酸化酶通过 250' 和 280s 环的有序/无序转变。

Biochemistry. 2023 Apr 18;62(8):1360-1368. doi: 10.1021/acs.biochem.2c00671. Epub 2023 Mar 29.

The importance of glycogen molecular structure for blood glucose control.糖原分子结构对血糖控制的重要性。

iScience. 2020 Dec 16;24(1):101953. doi: 10.1016/j.isci.2020.101953. eCollection 2021 Jan 22.

Synthetic strategies, SAR studies, and computer modeling of indole 2 and 3-carboxamides as the strong enzyme inhibitors: a review.吲哚 2 和 3-羧酰胺作为强酶抑制剂的合成策略、SAR 研究和计算机模拟：综述。

Mol Divers. 2021 Feb;25(1):535-550. doi: 10.1007/s11030-020-10061-x. Epub 2020 May 12.

Glycogen metabolism has a key role in the cancer microenvironment and provides new targets for cancer therapy.糖原代谢在癌症微环境中起着关键作用，并为癌症治疗提供了新的靶点。

J Mol Med (Berl). 2016 Feb;94(2):137-54. doi: 10.1007/s00109-015-1377-9. Epub 2016 Feb 17.

Development of a quantitative 96-well method to image glycogen storage in primary rat hepatocytes.建立一种定量 96 孔板方法，用于对原代大鼠肝细胞中的糖原储存进行成像。

Mol Cell Biochem. 2010 Aug;341(1-2):73-8. doi: 10.1007/s11010-010-0438-1. Epub 2010 Mar 24.

An assessment of the in vivo efficacy of the glycogen phosphorylase inhibitor GPi688 in rat models of hyperglycaemia.糖原磷酸化酶抑制剂GPi688在大鼠高血糖模型中的体内疗效评估。

Br J Pharmacol. 2007 Dec;152(8):1239-47. doi: 10.1038/sj.bjp.0707502. Epub 2007 Oct 15.

A glycogen phosphorylase inhibitor selectively enhances local rates of glucose utilization in brain during sensory stimulation of conscious rats: implications for glycogen turnover.糖原磷酸化酶抑制剂可在有意识大鼠的感觉刺激过程中选择性提高大脑局部葡萄糖利用率：对糖原周转的影响

J Neurochem. 2007 Jul;102(2):466-78. doi: 10.1111/j.1471-4159.2007.04595.x. Epub 2007 Apr 17.

Metabolic sensitivity of pancreatic tumour cell apoptosis to glycogen phosphorylase inhibitor treatment.胰腺肿瘤细胞凋亡对糖原磷酸化酶抑制剂治疗的代谢敏感性。

Br J Cancer. 2004 Dec 13;91(12):2094-100. doi: 10.1038/sj.bjc.6602243.

Regulation of glycogen metabolism in cultured human muscles by the glycogen phosphorylase inhibitor CP-91149.糖原磷酸化酶抑制剂CP-91149对培养的人体肌肉中糖原代谢的调节作用

Biochem J. 2004 Mar 15;378(Pt 3):1073-7. doi: 10.1042/BJ20030971.

Inhibition of autophagic proteolysis by inhibitors of phosphoinositide 3-kinase can interfere with the regulation of glycogen synthesis in isolated hepatocytes.磷酸肌醇3激酶抑制剂对自噬蛋白水解作用的抑制会干扰离体肝细胞中糖原合成的调节。

Biochem J. 2002 Dec 15;368(Pt 3):827-33. doi: 10.1042/BJ20021340.

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Indole-2-carboxamide inhibitors of human liver glycogen phosphorylase.

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