ArticleBioorganic & medicinal chemistry letters2008
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.
Article in Bioorganic & medicinal chemistry letters, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
What it found
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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.
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Who cites it
15 citing papers in PubMed.
- New targets for therapy: antigen identification in adults with B-cell acute lymphoblastic leukaemia.Cancer immunology, immunotherapy : CII · 2020Review
- The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry · 2020Review
- A non-covalent inhibitor XMU-MP-3 overrides ibrutinib-resistant BtkBritish journal of pharmacology · 2019Article
- Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent.ACS medicinal chemistry letters · 2017Article
- Antitumor Activity of HM781-36B, alone or in Combination with Chemotherapeutic Agents, in Colorectal Cancer Cells.Cancer research and treatment · 2016Article
- Endothelial Bmx tyrosine kinase activity is essential for myocardial hypertrophy and remodeling.Proceedings of the National Academy of Sciences of the United States of America · 2015Article
- BMX Negatively Regulates BAK Function, Thereby Increasing Apoptotic Resistance to Chemotherapeutic Drugs.Cancer research · 2015Article
- Tricyclic covalent inhibitors selectively target Jak3 through an active site thiol.The Journal of biological chemistry · 2015Article
- Ibrutinib (ImbruvicaTM) potently inhibits ErbB receptor phosphorylation and cell viability of ErbB2-positive breast cancer cells.Investigational new drugs · 2014Article
- Targeting Btk/Etk of prostate cancer cells by a novel dual inhibitor.Cell death & disease · 2014Article
- A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors.Nature chemical biology · 2014Article
- Developing irreversible inhibitors of the protein kinase cysteinome.Chemistry & biology · 2013Review
- RAF1-MEK1-ERK/AKT axis may confer NSCLC cell lines resistance to erlotinib.International journal of clinical and experimental pathology · 2013Article
- A structure-guided approach to creating covalent FGFR inhibitors.Chemistry & biology · 2010Article
- Article
Corrections and comments
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Authors and funding
17 authors.
Funding
Abstract
Irreversible HER/erbB inhibitors selectively inhibit HER-family kinases by targeting a unique cysteine residue located within the ATP-binding pocket. Sequence alignment reveals that this rare cysteine is also present in ten other protein kinases including all five Tec-family members. We demonstrate that the Tec-family kinase Bmx is potently inhibited by irreversible modification at Cys496 by clinical stage EGFR inhibitors such as CI-1033. This cross-reactivity may have significant clinical implications.
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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.