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嘧啶-2,4,6-三酮:一类新型有效的选择性基质金属蛋白酶抑制剂。

Pyrimidine-2,4,6-Triones: a new effective and selective class of matrix metalloproteinase inhibitors.

作者信息

Grams F, Brandstetter H, D'Alò S, Geppert D, Krell H W, Leinert H, Livi V, Menta E, Oliva A, Zimmermann G, Gram F, Brandstetter H, D'Alò S, Geppert D, Krell H W, Leinert H, Livi VMenta E, Oliva A, Zimmermann G

机构信息

Discovery Technologies, Preclinical Research Pharma, F.Hoffmann-LaRoche AG, Basel, Switzerland.

出版信息

Biol Chem. 2001 Aug;382(8):1277-85. doi: 10.1515/BC.2001.159.

Abstract

Matrix metalloproteinases (MMPs) are a family of zinc endopeptidases that have been implicated in various disease processes. Different classes of MMP inhibitors, including hydroxamic acids, phosphinic acids and thiols, have been previously described. Most of these mimic peptides and most likely bind in a similar way to the corresponding peptide substrates. Here we describe pyrimidine-triones as a completely new class of metalloprotease inhibitors. While the pyrimidine-trione template is used as the zinc-chelating moiety, the substituents have been optimized to yield inhibitors comparable in their inhibition efficiency of matrix metalloproteinases to hydroxamic acid derivatives such as batimastat. However, they are much more specific for a small subgroup of MMPs, namely the gelatinases (MMP-2 and MMP-9).

摘要

基质金属蛋白酶(MMPs)是一类锌内肽酶,与多种疾病进程有关。此前已描述了不同类型的MMP抑制剂,包括异羟肟酸、次膦酸和硫醇。这些抑制剂大多模拟肽段,很可能以与相应肽底物相似的方式结合。在此,我们描述了嘧啶三酮作为一类全新的金属蛋白酶抑制剂。虽然嘧啶三酮模板用作锌螯合部分,但已对取代基进行了优化,以产生在基质金属蛋白酶抑制效率方面与诸如batimastat等异羟肟酸衍生物相当的抑制剂。然而,它们对MMPs的一个小亚组,即明胶酶(MMP - 2和MMP - 9)具有更高的特异性。

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