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Novel Approaches and Challenges of Discovery of Exosite Modulators of a Disintegrin and Metalloprotease 10.
Frontiers in Molecular Biosciences ( IF 3.9 ) Pub Date : 2020-05-06 , DOI: 10.3389/fmolb.2020.00075
Dmitriy Minond 1, 2
Affiliation  

A disintegrin and metaproteinase 10 is an important target for multiple therapeutic areas, however, despite drug discovery efforts by both industry and academia no compounds have reached the clinic so far. The lack of enzyme and substrate selectivity of developmental drugs is believed to be a main obstacle to the success. In this review, we will focus on novel approaches and associated challenges in discovery of ADAM10 selective modulators that can overcome shortcomings of previous generations of compounds and be translated into the clinic.

中文翻译:

发现整联蛋白和金属蛋白酶的异位调节剂的新方法和挑战10。

Disintegrin和metaproteinase 10是多个治疗领域的重要目标,但是,尽管工业界和学术界都进行了药物发现,但到目前为止,尚无化合物可用于临床。发育药物缺乏酶和底物选择性被认为是成功的主要障碍。在这篇综述中,我们将专注于发现ADAM10选择性调节剂的新方法和相关挑战,这些新方法可以克服前几代化合物的缺点,并将其转化为临床应用。
更新日期:2020-05-06
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