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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Kinetic characterization of 4,4′-biphenylsulfonamides as selective non-zinc binding MMP inhibitors
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Kinetic characterization of 4,4′-biphenylsulfonamides as selective non-zinc binding MMP inhibitors

机译：作为选择性非锌结合MMP抑制剂的4,4'-联苯磺酰胺的动力学表征

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摘要

We describe the characterisation of a series of 4,4′-biphenylsulfonamides as selective inhibitors of matrix metalloproteases MMP-2 and -13, two enzymes involved in cell invasion and angiogenesis. Double-inhibitor studies in the presence of acetohydroxamic acid show that these molecules do not bind the catalytic zinc. Moreover, two of the characterised inhibitors (11 and 19) act as non-competitive inhibitors, whereas the para-methyl ester derivative 13 behaves as a competitive inhibitor. This finding suggests that this class of molecules binds to a catalytic subsite, possibly the S1′-pocket. Moreover, since these compounds also act as inhibitors of carbonic anhydrases (CAs), another family of enzymes involved in cell invasion, they could be potentially useful as CA/MMP dual target inhibitors with increased efficacy as anticancer agents.
机译：我们描述了一系列4,4'-联苯磺酰胺作为基质金属蛋白酶MMP-2和-13（参与细胞入侵和血管生成的两种酶）的选择性抑制剂的表征。在乙酰氧肟酸存在下的双抑制剂研究表明，这些分子不结合催化锌。此外，两个特征化的抑制剂（11和19）充当非竞争性抑制剂，而对甲基酯衍生物13充当竞争性抑制剂。这一发现表明，这类分子与催化亚位结合，可能与S1'-口袋结合。此外，由于这些化合物还充当了碳酸酐酶（CAs）的抑制剂，而碳酸酐酶（CAs）是参与细胞入侵的另一种酶，因此它们有可能作为CA / MMP双靶标抑制剂而具有作为抗癌剂增强的功效。

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