ReviewAngewandte Chemie (International ed. in English)2017
Protein-Templated Fragment Ligations-From Molecular Recognition to Drug Discovery.
Review in Angewandte Chemie (International ed. in English), 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
30 citing papers in PubMed, 68 citations in OpenAlex.
- Toward Precision Bioconjugation: Chemical Strategies for Site-Selective Cysteine Conjugation.Precision chemistry · 2026Review
- Discovery of SHANK1-PDZ Peptide-Fragment Inhibitors Using a Dynamic Ligation Screening Strategy.Biochemistry · 2026Article
- Click Reactions in Kinetic Target-Guided Synthesis: Progress in the Discovery of Inhibitors for Biological Targets.Methods and protocols · 2026Review
- Chemically Induced Dimerization via Nanobody Binding Facilitates in Situ Ligand Assembly and On-Demand GPCR Activation.JACS Au · 2024Article
- Targeted small molecule inhibitors blocking the cytolytic effects of pneumolysin and homologous toxins.Nature communications · 2024Article
- Isomerization of bioactive acylhydrazones triggered by light or thiols.Nature chemistry · 2023Article
- Identification of specific carbonic anhydrase inhibitorsRSC medicinal chemistry · 2023Article
- Templated Generation of a Bcl-xChemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Implications of Fragment-Based Drug Discovery in Tuberculosis and HIV.Pharmaceuticals (Basel, Switzerland) · 2022Review
- In Situ Inhibitor Synthesis and Screening by Fluorescence Polarization: An Efficient Approach for Accelerating Drug Discovery.Angewandte Chemie (Weinheim an der Bergstrasse, Germany) · 2022Article
- In Situ Inhibitor Synthesis and Screening by Fluorescence Polarization: An Efficient Approach for Accelerating Drug Discovery.Angewandte Chemie (International ed. in English) · 2022Article
- A Formylglycine-Peptide for the Site-Directed Identification of Phosphotyrosine-Mimetic Fragments.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Article
- Recent advances in DNA-encoded dynamic libraries.RSC chemical biology · 2022Review
- Chemical Evolution of Antivirals Against Enterovirus D68 through Protein-Templated Knoevenagel Reactions.Angewandte Chemie (International ed. in English) · 2021Article
- Fragment-based covalent ligand discovery.RSC chemical biology · 2021Review
- Identification of β-strand mediated protein-protein interaction inhibitors using ligand-directed fragment ligation.Chemical science · 2021Article
- Protein-Templated Hit Identification through an Ugi Four-Component Reaction*.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Article
- Enhancing native chemical ligation for challenging chemical protein syntheses.Current opinion in chemical biology · 2020Review
- Optimized Inhibitors of MDM2 via an Attempted Protein-Templated Reductive Amination.ChemMedChem · 2020Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Protein-templated fragment ligation is a novel concept to support drug discovery and can help to improve the efficacy of protein ligands. Protein-templated fragment ligations are chemical reactions between small molecules ("fragments") utilizing a protein's surface as a reaction vessel to catalyze the formation of a protein ligand with increased binding affinity. The approach exploits the molecular recognition of reactive small-molecule fragments by proteins both for ligand assembly and for the identification of bioactive fragment combinations. In this way, chemical synthesis and bioassay are integrated in one single step. This Review discusses the biophysical basis of reversible and irreversible fragment ligations and gives an overview of the available methods to detect protein-templated ligation products. The chemical scope and recent applications as well as future potential of the concept in drug discovery are reviewed.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.