Fragment-based drug discovery (FBDD) has become a mainstream technology for the identification of chemical hit matter in drug discovery programs. To date, the food and drug administration has approved four drugs, and over forty compounds are in clinical studies that can trace their origins to a fragment-based screen. The challenges associated with implementing an FBDD approach are many and diverse, ranging from the library design to developing methods for identifying weak affinity compounds. In this article, we give an overview of current progress in fragment library design, fragment to lead optimisation and on the advancement in techniques used for screening. Finally, we will comment on the future opportunities and challenges in this field.
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Review Article| January 27 2020
Fragments: where are we now?
Publisher: Portland Press Ltd
Received: November 13 2019
Revision Received: December 17 2019
Accepted: December 18 2019
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© 2020 The Author(s). Published by Portland Press Limited on behalf of the Biochemical Society
James Osborne, Stanislava Panova, Magdalini Rapti, Tatsuya Urushima, Harren Jhoti; Fragments: where are we now?. Biochem Soc Trans 28 February 2020; 48 (1): 271–280. doi: https://doi.org/10.1042/BST20190694
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