The DOI matches its Crossref record; 110 of the 110 references it cites were found in a registry or an index.
Twenty years on: the impact of fragments on drug discovery
Abstract
After 20 years of sometimes quiet growth, fragment-based drug discovery (FBDD) has become mainstream. More than 30 drug candidates derived from fragments have entered the clinic, with two approved and several more in advanced trials. FBDD has been widely applied in both academia and industry, as evidenced by the large number of papers from universities, non-profit research institutions, biotechnology companies and pharmaceutical companies. Moreover, FBDD draws on a diverse range of disciplines, from biochemistry and biophysics to computational and medicinal chemistry. As the promise of FBDD strategies becomes increasingly realized, now is an opportune time to draw lessons and point the way to the future. This Review briefly discusses how to design fragment libraries, how to select screening techniques and how to make the most of information gleaned from them. It also shows how concepts from FBDD have permeated and enhanced drug discovery efforts.
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“Fragment-based ligand discovery (FBLD) has emerged as a versatile approach for the discovery of atom-efficient, small-molecule binders for a wide range of proteins10–12.”
From Expedited mapping of the ligandable proteome using fully functionalized enantiomeric probe pairs (2019) · cites this paper as [12]
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Cites
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Research works printed but not linked: 1
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Induced protein degradation: an emerging drug discovery paradigm
Lai, A. C., & Crews, C. M. (2017) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.211 · Cited by 1,486
PROteolysis TArgeting Chimeras (PROTACs) — Past, present and future
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Metadata
- Authors
- Erlanson, D. A., Fesik, S. W., Hubbard, R. E., Jahnke, W., & Jhoti, H.
- Affiliations
- Carmot Therapeutics (United States) (US)
- Vanderbilt University (US)
- Vernalis (R&D) Limited (United Kingdom) (GB)
- Novartis (Switzerland) (CH)
- Corresponding author
- Erlanson, Daniel A.
- Venue
- Nature Reviews Drug Discovery
- Published
- 2016-07-15
- Volume
- 15
- Issue
- 9
- Pages
- 605-619
- ISSN
- 1474-1776 (ISSN-L)
- 1474-1784
- OpenAlex
- W2467779447
- Cited by
- 1,000
- References
- 110
- Citations by year
- 2026: 80 · 2025: 92 · 2024: 112 · 2023: 95 · 2022: 97 · 2021: 106 · 2020: 141 · 2019: 79 · 2018: 99 · 2017: 84 · 2016: 14
- FWCI
- 7.35
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Nature Reviews Drug Discovery (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Drug Discovery › Computational Drug Discovery Methods
- Physical Sciences › Chemistry › Organic Chemistry › Chemical Synthesis and Analysis
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Keywords
- fragment-based drug discovery, fragment libraries, fragment screening
- MeSH terms
- Clinical Trials as Topic, Humans, Peptide Fragments, Protein Conformation, Peptide Library, Computational Biology, Small Molecule Libraries, Drug Discovery, High-Throughput Screening Assays
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