Liras Spiros, Mcclure Kim F
Biogen Inc., 225 Binney Street, Cambridge, Massachusetts 02142, United States.
Pinteon Therapeutics, 1188 Centre Street, Newton Centre, Massachusetts 02549, United States.
ACS Med Chem Lett. 2019 Jun 14;10(7):1026-1032. doi: 10.1021/acsmedchemlett.9b00149. eCollection 2019 Jul 11.
Macrocycles have emerged as a viable approach for the modulation of tough targets in drug discovery. In this Innovations article we discuss recent progress toward the design of cell permeable and orally bioavailable peptide macrocycles and cyclotides and provide a perspective for their potential as therapeutics. We highlight design concepts that may be broadly relevant to drug discovery efforts beyond the rule of five.
大环化合物已成为药物研发中调控棘手靶点的一种可行方法。在这篇创新文章中，我们讨论了在设计可穿透细胞且口服生物利用的肽大环化合物和环肽方面的最新进展，并展望了它们作为治疗药物的潜力。我们强调了一些设计理念，这些理念可能广泛适用于超出“五规则”的药物研发工作。
