Small Peptides as Modulators of Serine Proteases

doi:10.2174/0929867325666181016163630
摘要

丝氨酸蛋白酶在许多生理和病理过程中发挥重要作用，并在许多临床适应症中被证实为诊断和治疗靶点。抑制这些蛋白酶异常的蛋白水解活性已被临床用于相关疾病的治疗。作为丝氨酸蛋白酶的药物调节剂的10-20个残基多肽具有小分子药物和大分子药物的双重特性，倍受人们的关注。本文综述了与单克隆抗体相比具有强抑制和高特异性的抗丝氨酸蛋白酶肽抑制剂的研究进展。此外，我们还讨论了提高肽在体内的半衰期和生物利用度的策略，这是目前限制肽类药物临床转译的主要障碍。本文提出了开发有效的丝氨酸蛋白酶抑制剂的新途径，并强调了这些抑制剂的药用前景。
关键词: 丝氨酸蛋白酶，肽基抑制剂，合理设计，，癌症，血栓，晶体学。
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DOI https://dx.doi.org/10.2174/0929867325666181016163630	Print ISSN 0929-8673
Publisher Name Bentham Science Publisher	Online ISSN 1875-533X
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