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Tethering: Fragment-Based Drug Discovery

Erlanson, Daniel A., Wells, James A., Braisted, Andrew C.·2004·Annual Review of Biophysics and Biomolecular Structure

DOI 10.1146/annurev.biophys.33.110502.140409

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Abstract

▪ Abstract The genomics revolution has provided a deluge of new targets for drug discovery. To facilitate the drug discovery process, many researchers are turning to fragment-based approaches to find lead molecules more efficiently. One such method, Tethering 1 , allows for the identification of small-molecule fragments that bind to specific regions of a protein target. These fragments can then be elaborated, combined with other molecules, or combined with one another to provide high-affinity drug leads. In this review we describe the background and theory behind Tethering and discuss its use in identifying novel inhibitors for protein targets including interleukin-2 (IL-2), thymidylate synthase (TS), protein tyrosine phosphatase 1B (PTP-1B), and caspases.

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Authors: Erlanson, D. A., Wells, J. A., & Braisted, A. C.
Affiliations: Sunesis (United States) (US)
ORCID: Erlanson, Daniel A.
Wells, James A.
Venue: Annual Review of Biophysics and Biomolecular Structure
Publisher: Annual Reviews
Published: 2004-06-09
Volume: 33
Issue: 1
Pages: 199-223
ISSN: 1056-8700 (ISSN-L)
1545-4266
DOI: 10.1146/annurev.biophys.33.110502.140409
OpenAlex: W2138958920
Cited by: 385
References: 78
Citations by year: 2026: 5 · 2025: 7 · 2024: 17 · 2023: 16 · 2022: 17 · 2021: 8 · 2020: 17 · 2019: 17 · 2018: 21 · 2017: 6 · 2016: 18 · 2015: 21 · 2014: 23 · 2013: 11 · 2012: 29
FWCI: 1.77
Type: journal article
Language: en
Open access: closed
Locations: Annual Review of Biophysics and Biomolecular Structure (publishedVersion)
PubMed (publishedVersion)
Funders: Sunesis
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 › Structural Biology › Enzyme Structure and Function
Keywords: tethering, fragment-based drug discovery, small-molecule fragments, protein-ligand binding, lead compound identification, interleukin-2, thymidylate synthase, PTP1B, caspases, protein inhibitors
MeSH terms: Binding Sites, Peptide Fragments, Protein Binding, Proteins, Drug Design, Protein Interaction Mapping, Protein Array Analysis

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Tethering: Fragment-Based Drug Discovery

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