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Updated: May 31, 2026
06:26
Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
Published on: May 16, 2021
Introduction to fragment-based drug discovery.
1Carmot Therapeutics, Inc., San Francisco, CA 94158, USA. derlanson@carmot.us
Topics in Current Chemistry
|June 23, 2011
Summary
Fragment-based drug discovery (FBDD) uses small molecules to find drug leads. This method, advanced by sensitive techniques, is now widely used in research and industry.
Area of Science:
- Drug Discovery
- Medicinal Chemistry
- Structural Biology
Background:
- Fragment-based drug discovery (FBDD) is a powerful approach for identifying drug leads.
- It utilizes small molecules, approximately half the size of conventional drugs, as starting points.
- The practical application of FBDD emerged in the mid-1990s due to advancements in experimental techniques.
Purpose of the Study:
- Introduce key concepts of FBDD to readers with limited prior knowledge.
- Provide foundational information for subsequent chapters on the topic.
- Highlight the critical role of X-ray crystallography in FBDD.
Main Methods:
- Fragment identification using sensitive experimental techniques.
- Expansion and linking of identified fragments to generate drug leads.
- Utilizing X-ray crystallography for fragment screening and optimization.
Main Results:
- FBDD has become a significant field with widespread adoption in academia and industry.
- At least 18 drugs discovered using FBDD have entered clinical trials.
- Numerous reviews and books have been published, reflecting the field's growth.
Conclusions:
- FBDD is a well-established and highly successful drug discovery strategy.
- X-ray crystallography is indispensable for the initial stages of FBDD.
- The field continues to evolve, contributing significantly to modern therapeutics.
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