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Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
Published on: May 16, 2021
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Fragment-to-Lead Medicinal Chemistry Publications in 2021
Louise Walsh1, Daniel A Erlanson2, Iwan J P de Esch3
1Astex Pharmaceuticals, 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA, United Kingdom.
Journal of Medicinal Chemistry
|January 9, 2023
Summary
This review summarizes successful fragment-to-lead case studies from 2021, highlighting trends in fragment-based drug discovery and the increasing use of structural information for lead optimization.
Area of Science:
- Drug discovery and medicinal chemistry
- Fragment-based drug discovery (F2L)
Background:
- The annual review series focuses on successful Fragment-to-Lead (F2L) case studies.
- This installment covers publications from 2021.
Purpose of the Study:
- To summarize and analyze successful F2L case studies published in 2021.
- To identify trends and new developments in fragment-based drug discovery.
- To discuss the role of structural information in F2L.
Main Methods:
- Tabulated summary of relevant articles published in 2021.
- Analysis of features including target class, screening methods, and ligand efficiency.
- Comparison of 2021 data with combined data from 2015-2021.
Main Results:
- Detailed summary of 2021 F2L case studies.
- Analysis of screening methods and ligand efficiency trends.
- Identification of key developments in the F2L field.
Conclusions:
- Fragment-to-Lead (F2L) remains a successful strategy in drug discovery.
- Structural information plays an increasingly vital role in optimizing fragments into leads.
- Continued analysis of case studies reveals evolving trends in F2L approaches.
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