ArticleJournal of medicinal chemistry2020
Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine.
Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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The trial behind it
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Who cites it
15 citing papers in PubMed, 36 citations in OpenAlex.
- Discovery of Covalent Ligands with AlphaFold3.Journal of the American Chemical Society · 2026Article
- Subtimizer: Computational Workflow for Structure-Guided Design of Potent and Selective Kinase Peptide Substrates.Journal of chemical information and modeling · 2026Article
- Drug resistance and tumor heterogeneity: cells and ensembles.Biophysical reviews · 2025Review
- SRC kinase drives multidrug resistance induced by KRAS-G12C inhibition.Science advances · 2024Article
- Green SeaweedMarine drugs · 2024Article
- Emerging Roles of YES1 in Cancer: The Putative Target in Drug Resistance.International journal of molecular sciences · 2024Review
- A renaissance for YES in cancer.Oncogene · 2023Review
- LIMS-Kinase provides sensitive and generalizable label-freeCell reports. Physical science · 2023Article
- Elucidation of Pharmacological Mechanism Underlying the Anti-Alzheimer's Disease Effects ofMolecules (Basel, Switzerland) · 2023Article
- Oxidation-Dependent Activation of Src Kinase Mediates Epithelial IL-33 Production and Signaling during Acute Airway Allergen Challenge.Journal of immunology (Baltimore, Md. : 1950) · 2021Article
- Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries.Nature biotechnology · 2021Article
- Discovery of Aminopyrazole Derivatives as Potent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2 and 3.ACS medicinal chemistry letters · 2021Article
- Identification of Novel Src Inhibitors: Pharmacophore-Based Virtual Screening, Molecular Docking and Molecular Dynamics Simulations.Molecules (Basel, Switzerland) · 2020Article
- Protein Binding and Stability of Drug Candidates: The Achilles' Heel in In Vitro Potency Assays.European journal of drug metabolism and pharmacokinetics · 2020Article
- Structure and Characterization of a Covalent Inhibitor of Src Kinase.Frontiers in molecular biosciences · 2020Article
Corrections and comments
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Authors and funding
14 authors at 3 institutions in 1 country.
Funding
Abstract
SRC is a major regulator of many signaling pathways and contributes to cancer development. However, development of a selective SRC inhibitor has been challenging, and FDA-approved SRC inhibitors, dasatinib and bosutinib, are multitargeted kinase inhibitors. Here, we describe our efforts to develop a selective SRC covalent inhibitor by targeting cysteine 277 on the P-loop of SRC. Using a promiscuous covalent kinase inhibitor (CKI)
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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.