ArticleACS medicinal chemistry letters2013
Probing the binding site of abl tyrosine kinase using in situ click chemistry.
Article in ACS medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed.
- Click Reactions in Kinetic Target-Guided Synthesis: Progress in the Discovery of Inhibitors for Biological Targets.Methods and protocols · 2026Review
- Pharmacological Evaluation of Bioisosterically Replaced and Triazole- Tethered Derivatives for Anticancer Therapy.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025Review
- Shotgun Kinetic Target-Guided Synthesis Approach Enables the Discovery of Small-Molecule Inhibitors against Pathogenic Free-Living Amoeba Glucokinases.ACS infectious diseases · 2023Article
- Going beyond Binary: Rapid Identification of Protein-Protein Interaction Modulators Using a Multifragment Kinetic Target-Guided Synthesis Approach.Journal of medicinal chemistry · 2023Article
- CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review.RSC advances · 2020Review
- Tailored therapeutics based on 1,2,3-1MedChemComm · 2019Review
- Evaluation of 1,2,3-Triazoles as Amide Bioisosteres In Cystic Fibrosis Transmembrane Conductance Regulator Modulators VX-770 and VX-809.Chemistry (Weinheim an der Bergstrasse, Germany) · 2019Article
- Proteintemplat-gesteuerte Fragmentligationen - von der molekularen Erkennung zur Wirkstofffindung.Angewandte Chemie (Weinheim an der Bergstrasse, Germany) · 2017Article
- Protein-Templated Fragment Ligations-From Molecular Recognition to Drug Discovery.Angewandte Chemie (International ed. in English) · 2017Review
- The application of click chemistry in the synthesis of agents with anticancer activity.Drug design, development and therapy · 2015Review
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Authors and funding
12 authors.
Funding
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Abstract
Modern combinatorial chemistry is used to discover compounds with desired function by an alternative strategy, in which the biological target is directly involved in the choice of ligands assembled from a pool of smaller fragments. Herein, we present the first experimental result where the use of in situ click chemistry has been successfully applied to probe the ligand-binding site of Abl and the ability of this enzyme to form its inhibitor. Docking studies show that Abl is able to allow the in situ click chemistry between specific azide and alkyne fragments by binding to Abl-active sites. This report allows medicinal chemists to use protein-directed in situ click chemistry for exploring the conformational space of a ligand-binding pocket and the ability of the protein to guide its inhibitor. This approach can be a novel, valuable tool to guide drug design synthesis in the field of tyrosine kinases.
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