The Exploration of Chirality for Improved Druggability within the Human Kinome.

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ID: 55117
2019
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Abstract
Chirality is important in drug discovery since 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.
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saha2019thejournal Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Saha, Debasmita;Kharbanda, Anupreet;Yan, Wei;Lakkaniga, Naga Rajiv;Frett, Brendan;Li, Hong-Yu;
Journal Journal of medicinal chemistry
Year 2019
DOI
10.1021/acs.jmedchem.9b00640
URL
Keywords
industry careers government academia contract research organization environmental toxicologic pathology

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