Search Results - "CUI, Jean"
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Targeting Receptor Tyrosine Kinase MET in Cancer: Small Molecule Inhibitors and Clinical Progress
Published in Journal of medicinal chemistry (12-06-2014)“…The HGF/MET signaling pathway is critical in mediating a wide range of normal physiological functions including embryological development, wound healing, and…”
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Repotrectinib Exhibits Potent Antitumor Activity in Treatment-Naïve and Solvent-Front-Mutant ROS1-Rearranged Non-Small Cell Lung Cancer
Published in Clinical cancer research (01-07-2020)“…Although first-line crizotinib treatment leads to clinical benefit in lung cancer, high prevalence of crizotinib-resistant ROS1-G2032R (ROS1 ) mutation and…”
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Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal–Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Kinase (ALK)
Published in Journal of medicinal chemistry (22-09-2011)“…Because of the critical roles of aberrant signaling in cancer, both c-MET and ALK receptor tyrosine kinases are attractive oncology targets for therapeutic…”
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Crizotinib for the Treatment of ALK‐Rearranged Non‐Small Cell Lung Cancer: A Success Story to Usher in the Second Decade of Molecular Targeted Therapy in Oncology
Published in The oncologist (Dayton, Ohio) (01-11-2012)“…Crizotinib, an ALK/MET/ROS1 inhibitor, was approved by the U.S. Food and Drug Administration for the treatment of anaplastic lymphoma kinase (ALK)‐rearranged…”
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Discovery of a Novel Class of Exquisitely Selective Mesenchymal-Epithelial Transition Factor (c-MET) Protein Kinase Inhibitors and Identification of the Clinical Candidate 2‑(4-(1-(Quinolin-6-ylmethyl)‑1H‑[1,2,3]triazolo[4,5‑b]pyrazin-6-yl)‑1H‑pyrazol-1-yl)ethanol (PF-04217903) for the Treatment of Cancer
Published in Journal of medicinal chemistry (27-09-2012)“…The c-MET receptor tyrosine kinase is an attractive oncology target because of its critical role in human oncogenesis and tumor progression. An oxindole…”
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A Novel Sequentially Evolved EML4-ALK Variant 3 G1202R/S1206Y Double Mutation In Cis Confers Resistance to Lorlatinib: A Brief Report and Literature Review
Published in JTO clinical and research reports (01-01-2021)“…Lorlatinib is a third-generation ALK inhibitor that can overcome the largest number of acquired ALK resistance mutations, including the solvent-front mutation…”
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Common Co-activation of AXL and CDCP1 in EGFR-mutation-positive Non-smallcell Lung Cancer Associated With Poor Prognosis
Published in EBioMedicine (01-03-2018)“…Epidermal growth factor receptor (EGFR)-mutation-positive non-smallcell lung cancer (NSCLC) is incurable, despite high rates of response to EGFR tyrosine…”
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Discovery of 5-[5-Fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic Acid (2-Diethylaminoethyl)amide, a Novel Tyrosine Kinase Inhibitor Targeting Vascular Endothelial and Platelet-Derived Growth Factor Receptor Tyrosine Kinase
Published in Journal of medicinal chemistry (27-03-2003)“…To improve the antitumor properties and optimize the pharmaceutical properties including solubility and protein binding of indolin-2-ones, a number of…”
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Synthesis of Aryl Ethers via a Sulfonyl Transfer Reaction
Published in Organic letters (03-08-2012)“…A general synthesis of aryl ethers from primary and secondary alcohols and aryl mesylates is presented. The reaction proceeds via a sulfonyl-transfer…”
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Crystal Structure of the Tyrosine Kinase Domain of the Hepatocyte Growth Factor Receptor c-Met and Its Complex with the Microbial Alkaloid K-252a
Published in Proceedings of the National Academy of Sciences - PNAS (28-10-2003)“…The protooncogene c-met codes for the hepatocyte growth factor receptor tyrosine kinase. Binding of its ligand, hepatocyte growth factor/scatter factor,…”
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Design of Potent and Selective Inhibitors to Overcome Clinical Anaplastic Lymphoma Kinase Mutations Resistant to Crizotinib
Published in Journal of medicinal chemistry (27-02-2014)“…Crizotinib (1), an anaplastic lymphoma kinase (ALK) receptor tyrosine kinase inhibitor approved by the U.S. Food and Drug Administration in 2011, is…”
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Abstract 2132: The novel, rationally-designed, ALK/SRC inhibitor TPX-0005 overcomes multiple acquired resistance mechanisms to current ALK inhibitors
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…Non-small cell lung cancers harboring rearrangements involving the ALK gene are sensitive to treatment with the ALK inhibitor crizotinib. However, the…”
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Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations
Published in Journal of medicinal chemistry (12-06-2014)“…Although crizotinib demonstrates robust efficacy in anaplastic lymphoma kinase (ALK)-positive non-small-cell lung carcinoma patients, progression during…”
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Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor
Published in Molecular cancer therapeutics (01-04-2012)“…The c-Met pathway has been implicated in a variety of human cancers for its critical role in tumor growth, invasion, and metastasis. PF-04217903 is a novel…”
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A New Challenging and Promising Era of Tyrosine Kinase Inhibitors
Published in ACS medicinal chemistry letters (10-04-2014)“…Protein kinases are key regulators that govern complex cellular processes. Dysregulation of kinase signaling is associated in many human diseases, particularly…”
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Discovery of Allosteric, Potent, Subtype Selective, and Peripherally Restricted TrkA Kinase Inhibitors
Published in Journal of medicinal chemistry (10-01-2019)“…Tropomyosin receptor kinases (TrkA, TrkB, TrkC) are activated by hormones of the neurotrophin family: nerve growth factor (NGF), brain derived neurotrophic…”
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High Levels of HER-2 Expression Alter the Ability of Epidermal Growth Factor Receptor (EGFR) Family Tyrosine Kinase Inhibitors to Inhibit EGFR Phosphorylation in Vivo
Published in Clinical cancer research (01-12-2001)“…The epidermal growth factor receptor (EGFR) and HER-2 tyrosine kinases have been implicated in the development, progression, and severity of several human…”
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Identification of a novel T1151K ALK mutation in a patient with ALK -rearranged NSCLC with prior exposure to crizotinib and ceritinib
Published in Lung cancer (Amsterdam, Netherlands) (01-08-2017)“…Highlights • Novel T1151 K ALK mutation confers resistance to ceritinib. • Co-crystal structure shows a strong interaction between ceritinib and the P-loop. •…”
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Lessons from (S)‑6-(1-(6-(1-Methyl‑1H‑pyrazol-4-yl)-[1,2,4]triazolo[4,3‑b]pyridazin-3-yl)ethyl)quinoline (PF-04254644), an Inhibitor of Receptor Tyrosine Kinase c‑Met with High Protein Kinase Selectivity but Broad Phosphodiesterase Family Inhibition Leading to Myocardial Degeneration in Rats
Published in Journal of medicinal chemistry (12-09-2013)“…The hepatocyte growth factor (HGF)/c-Met signaling axis is deregulated in many cancers and plays important roles in tumor invasive growth and metastasis. An…”
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Rational design of 4,5-disubstituted-5,7-dihydro-pyrrolo[2,3- d]pyrimidin-6-ones as a novel class of inhibitors of epidermal growth factor receptor (EGF-R) and Her2(p185 erbB) tyrosine kinases
Published in Bioorganic & medicinal chemistry letters (19-08-2002)“…A novel class of 4,5-disubstituted-5,7-dihydro-pyrrolo[2,3- d]pyrimidin-6-ones has been discovered as potent and selective inhibitors of the EGF-R tyrosine…”
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