Cyclophilin Succumbs to a Macrocyclic Chameleon

Bradley C. Doak, Jan Kihlberg

Research output: Contribution to journalReview ArticleResearchpeer-review

Abstract

Targets that have large and groove-shaped binding sites, such as cyclophilin, are difficult to drug with small molecules. Macrocycles of natural product origin can be ideal starting points for such targets as illustrated by the transformation of sanglifehrin A into an orally bioavailable potential candidate drug. Optimization benefits from development of convergent, modular synthetic routes in combination with structure and property based methods for lead optimization.

Original languageEnglish
Pages (from-to)9469-9472
Number of pages4
JournalJournal of Medicinal Chemistry
Volume61
Issue number21
DOIs
Publication statusPublished - 8 Nov 2018

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