ArticleACS chemical biology2012
Irreversible inhibitors of c-Src kinase that target a nonconserved cysteine.
Article in ACS chemical biology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
21 citing papers in PubMed, 44 citations in OpenAlex.
- Click Reactions in Kinetic Target-Guided Synthesis: Progress in the Discovery of Inhibitors for Biological Targets.Methods and protocols · 2026Review
- Affinity-Based Kinase-Catalyzed Crosslinking to Study Kinase-Substrate Pairs.Bioconjugate chemistry · 2023Article
- Design, Synthesis, and Biological Evaluation of Proteolysis Targeting Chimeras (PROTACs) for the Dual Degradation of IGF-1R and Src.Molecules (Basel, Switzerland) · 2020Article
- Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine.Journal of medicinal chemistry · 2020Article
- Structure and Characterization of a Covalent Inhibitor of Src Kinase.Frontiers in molecular biosciences · 2020Article
- Selective Proteolysis to Study the Global Conformation and Regulatory Mechanisms of c-Src Kinase.ACS chemical biology · 2019Article
- Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome.Cell chemical biology · 2019Article
- A Near-IR Fluorescent Dasatinib Derivative That Localizes in Cancer Cells.Bioconjugate chemistry · 2019Article
- Acrolein and thiol-reactive electrophiles suppress allergen-induced innate airway epithelial responses by inhibition of DUOX1 and EGFR.American journal of physiology. Lung cellular and molecular physiology · 2016Article
- The NADPH Oxidases DUOX1 and NOX2 Play Distinct Roles in Redox Regulation of Epidermal Growth Factor Receptor Signaling.The Journal of biological chemistry · 2016Article
- Structural and Biochemical Basis for Intracellular Kinase Inhibition by Src-specific Peptidic Macrocycles.Cell chemical biology · 2016Article
- Bivalent Inhibitors of c-Src Tyrosine Kinase That Bind a Regulatory Domain.Bioconjugate chemistry · 2016Article
- Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility.Bioorganic & medicinal chemistry letters · 2015Article
- Discovery of Bivalent Kinase Inhibitors via Enzyme-Templated Fragment Elaboration.ACS medicinal chemistry letters · 2015Article
- 5'-β,γ-CHF-ATP diastereomers: synthesis and fluorine-mediated selective binding by c-Src protein kinase.Organic letters · 2015Article
- Irreversible inhibition of DNA polymerase β by small-molecule mimics of a DNA lesion.Journal of the American Chemical Society · 2014Article
- Targeting protein kinases with selective and semipromiscuous covalent inhibitors.Methods in enzymology · 2014Review
- Conformation-selective inhibitors reveal differences in the activation and phosphate-binding loops of the tyrosine kinases Abl and Src.ACS chemical biology · 2013Article
- Selective targeting of distinct active site nucleophiles by irreversible SRC-family kinase inhibitors.Journal of the American Chemical Society · 2012Article
- Selective targeting of the inactive state of hematopoietic cell kinase (Hck) with a stable curcumin derivative.The Journal of biological chemistryArticle
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
We have developed the first irreversible inhibitors of wild-type c-Src kinase. We demonstrate that our irreversible inhibitors display improved potency and selectivity relative to that of their reversible counterparts. Our strategy involves modifying a promiscuous kinase inhibitor with an electrophile to generate covalent inhibitors of c-Src. We applied this methodology to two inhibitor scaffolds that exhibit increased cellular efficacy when rendered irreversible. In addition, we have demonstrated the utility of irreversible inhibitors in studying the conformation of an important loop in kinases that can control inhibitor selectivity and cause drug resistance. Together, we have developed a general and robust framework for generating selective irreversible inhibitors from reversible, promiscuous inhibitor scaffolds.
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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.