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Potential clinical applications of matrix metalloproteinase inhibitors and their future prospects

机译:基质金属蛋白酶抑制剂的潜在临床应用及其未来前景

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摘要

Matrix metalloproteinases (MMPs) are endopeptidases that are involved in extracellular matrix degradation. They are also implicated in a number of abnormal bioprocesses, such as tumor growth, invasion, and metastasis. Therefore, controlling MMP activities has generated considerable interest as a possible therapeutic target. The tissue inhibitors of metalloproteinases (TIMPs) are the major naturally occurring proteins that specifically inhibit MMPs and assist in maintaining the balance between extracellular matrix destruction and formation. However, TIMPs are probably not suitable for pharmacological applications due to their short half-lives in vivo. During the last few decades, synthetic MMP inhibitors (MMPIs) have undergone rapid clinical development in attempts to control MMP enzymatic activities in abnormal bioprocesses. Although studies with these agents have met with limited clinical success, the field of MMPIs is still expanding, and generation of highly effective and selective MMPIs might be a promising direction of this research area.
机译:基质金属蛋白酶(MMP)是内肽酶,参与细胞外基质降解。它们也与许多异常的生物过程有关,例如肿瘤生长,侵袭和转移。因此,控制MMP活性已引起人们极大的兴趣,将其作为一种可能的治疗靶标。金属蛋白酶(TIMPs)的组织抑制剂是主要的天然存在的蛋白,其特异性抑制MMP并帮助维持细胞外基质破坏和形成之间的平衡。但是,TIMP由于其体内半衰期短,可能不适合药理应用。在过去的几十年中,合成MMP抑制剂(MMPI)经历了快速的临床开发,试图控制异常生物过程中的MMP酶活性。尽管用这些药物进行的研究在临床上取得了有限的成功,但是MMPI的领域仍在扩展,并且高效,选择性的MMPI的产生可能是该研究领域的一个有希望的方向。

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