Fragment-to-Lead Medicinal Chemistry Publications in 2020

Iwan J.P. De Esch*, Daniel A. Erlanson, Wolfgang Jahnke, Christopher N. Johnson, Louise Walsh

*Corresponding author for this work

Research output: Contribution to JournalReview articleAcademicpeer-review

Abstract

Fragment-based drug discovery (FBDD) continues to evolve and make an impact in the pharmaceutical sciences. We summarize successful fragment-to-lead studies that were published in 2020. Having systematically analyzed annual scientific outputs since 2015, we discuss trends and best practices in terms of fragment libraries, target proteins, screening technologies, hit-optimization strategies, and the properties of hit fragments and the leads resulting from them. As well as the tabulated Fragment-to-Lead (F2L) programs, our 2020 literature review identifies several trends and innovations that promise to further increase the success of FBDD. These include developing structurally novel screening fragments, improving fragment-screening technologies, using new computer-aided design and virtual screening approaches, and combining FBDD with other innovative drug-discovery technologies.

Original languageEnglish
Pages (from-to)84-99
Number of pages16
JournalJournal of medicinal chemistry
Volume65
Issue number1
Early online date20 Dec 2021
DOIs
Publication statusPublished - 13 Jan 2022

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