The Exploration of Chirality for Improved Druggability within the Human Kinome

Debasmita Saha, Anupreet Kharbanda, Wei Yan, Naga Rajiv Lakkaniga, Brendan Frett, Hong Yu Li

Research output: Contribution to journalArticlepeer-review

26 Scopus citations


Chirality is important in drug discovery because stereoselective drugs can ameliorate therapeutic difficulties including adverse toxicity and poor pharmacokinetic profiles. The human kinome, a major druggable enzyme class has been exploited to treat a wide range of diseases. However, many kinase inhibitors are planar and overlap in chemical space, which leads to selectivity and toxicity issues. By exploring chirality within the kinome, a new iteration of kinase inhibitors is being developed to better utilize the three-dimensional nature of the kinase active site. Exploration into novel chemical space, in turn, will also improve drug solubility and pharmacokinetic profiles. This perspective explores the role of chirality to improve kinome druggability and will serve as a resource for pioneering kinase inhibitor development to address current therapeutic needs.

Original languageEnglish (US)
Pages (from-to)441-469
Number of pages29
JournalJournal of Medicinal Chemistry
Issue number2
StatePublished - Jan 23 2020
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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