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Academic Journal

Discovery of Dual MER/AXL Kinase Inhibitors as Bifunctional Small Molecules for Inhibiting Tumor Growth and Enhancing Tumor Immune Microenvironment.

  • Authors : Li MC; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County 350401, Taiwan, ROC.; Biomedical Translation Research Center (BioTReC), Academia Sinica, Taipei City 115202, Taiwan, ROC.

Subjects: Tumor Microenvironment*/Tumor Microenvironment*/Tumor Microenvironment*/drug effects ; Protein Kinase Inhibitors*/Protein Kinase Inhibitors*/Protein Kinase Inhibitors*/pharmacology ; Protein Kinase Inhibitors*/Protein Kinase Inhibitors*/Protein Kinase Inhibitors*/chemistry

  • Source: Journal of medicinal chemistry [J Med Chem] 2024 Jul 11; Vol. 67 (13), pp. 10906-10927. Date of Electronic Publication: 2024 Jun 24.Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic

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Academic Journal

Preliminary Study of Radionuclide-Labeled MerTK-Targeting PET Imaging Agents for the Diagnosis of Melanoma.

  • Authors : Wang C; Department of Nuclear Medicine, Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, The Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, China.; School of Pharmacy, Southwest Medical University, Luzhou, Sichuan 646000, China.

Subjects: c-Mer Tyrosine Kinase*/c-Mer Tyrosine Kinase*/c-Mer Tyrosine Kinase*/metabolism ; Positron-Emission Tomography*/Positron-Emission Tomography*/Positron-Emission Tomography*/methods ; Radiopharmaceuticals*/Radiopharmaceuticals*/Radiopharmaceuticals*/chemistry

  • Source: Journal of medicinal chemistry [J Med Chem] 2024 Nov 14; Vol. 67 (21), pp. 19813-19825. Date of Electronic Publication: 2024 Nov 01.Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic

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Academic Journal

Discovery of Potent Azetidine-Benzoxazole MerTK Inhibitors with In Vivo Target Engagement.

  • Authors : Frey RR; Research and Development, AbbVie Inc., 1 North Waukegan Road, North Chicago, Illinois 60064, United States.; Jana N

Subjects: Azetidines*/Azetidines*/Azetidines*/pharmacology ; Azetidines*/Azetidines*/Azetidines*/chemistry ; Azetidines*/Azetidines*/Azetidines*/pharmacokinetics

  • Source: Journal of medicinal chemistry [J Med Chem] 2024 Oct 10; Vol. 67 (19), pp. 17033-17052. Date of Electronic Publication: 2024 Sep 30.Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic

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Academic Journal

Discovery of A-910, a Highly Potent and Orally Bioavailable Dual MerTK/Axl-Selective Tyrosine Kinase Inhibitor.

  • Authors : Yu Y; Abbvie, Inc, 1 North Waukegan Road, North Chicago, Illinois 60064, United States.; Jang M

Subjects: c-Mer Tyrosine Kinase*/c-Mer Tyrosine Kinase*/c-Mer Tyrosine Kinase*/antagonists & inhibitors ; c-Mer Tyrosine Kinase*/c-Mer Tyrosine Kinase*/c-Mer Tyrosine Kinase*/metabolism ; Proto-Oncogene Proteins*/Proto-Oncogene Proteins*/Proto-Oncogene Proteins*/antagonists & inhibitors

  • Source: Journal of medicinal chemistry [J Med Chem] 2024 Oct 10; Vol. 67 (19), pp. 17000-17032. Date of Electronic Publication: 2024 Sep 16.Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic

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Academic Journal

Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy.

  • Authors : Nissink JWM; Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.; Bazzaz S

Subjects: Protein Kinase Inhibitors/Protein Kinase Inhibitors/Protein Kinase Inhibitors/*chemistry ; Protein Kinase Inhibitors/Protein Kinase Inhibitors/Protein Kinase Inhibitors/*pharmacology ; c-Mer Tyrosine Kinase/c-Mer Tyrosine Kinase/c-Mer Tyrosine Kinase/*antagonists & inhibitors

  • Source: Journal of medicinal chemistry [J Med Chem] 2021 Mar 25; Vol. 64 (6), pp. 3165-3184. Date of Electronic Publication: 2021 Mar 08.Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic

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Academic Journal

Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.

  • Authors : Zhao J; Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry , UNC Eshelman School of Pharmacy , Chapel Hill , North Carolina 27599 , United States.; Zhang D

Subjects: Protein Kinase Inhibitors/Protein Kinase Inhibitors/Protein Kinase Inhibitors/*chemistry ; Protein Kinase Inhibitors/Protein Kinase Inhibitors/Protein Kinase Inhibitors/*pharmacology ; c-Mer Tyrosine Kinase/c-Mer Tyrosine Kinase/c-Mer Tyrosine Kinase/*antagonists & inhibitors

  • Source: Journal of medicinal chemistry [J Med Chem] 2018 Nov 21; Vol. 61 (22), pp. 10242-10254. Date of Electronic Publication: 2018 Nov 05.Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic

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