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Allosteric inhibition of JAK2 with lysine-reactive compounds that bind the pseudokinase domain.

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Title: Allosteric inhibition of JAK2 with lysine-reactive compounds that bind the pseudokinase domain.
Authors: Primi MC; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States., Tavares MT; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States., Hatcher JM; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States., Kang H; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States., Kresina TAC; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States., Chakraborty S; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States., Leroy E; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States., Schmoker AM; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States., Jeon H; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States., Weisberg EL; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Medicine, Harvard Medical School, Boston, MA, 02215, United States., Akatsu T; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States., Griffin JD; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Medicine, Harvard Medical School, Boston, MA, 02215, United States., Scott DA; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States., Eck MJ; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States. Electronic address: michael_eck@dfci.harvard.edu.
Source: European journal of medicinal chemistry [Eur J Med Chem] 2026 Jan 15; Vol. 302 (Pt 1), pp. 118274. Date of Electronic Publication: 2025 Oct 21.
Publication Type: Journal Article
Journal Info: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
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  Data: Allosteric inhibition of JAK2 with lysine-reactive compounds that bind the pseudokinase domain.
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  Data: <searchLink fieldCode="AU" term="%22Primi+MC%22">Primi MC</searchLink>; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States.<br /><searchLink fieldCode="AU" term="%22Tavares+MT%22">Tavares MT</searchLink>; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States.<br /><searchLink fieldCode="AU" term="%22Hatcher+JM%22">Hatcher JM</searchLink>; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States.<br /><searchLink fieldCode="AU" term="%22Kang+H%22">Kang H</searchLink>; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States.<br /><searchLink fieldCode="AU" term="%22Kresina+TAC%22">Kresina TAC</searchLink>; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States.<br /><searchLink fieldCode="AU" term="%22Chakraborty+S%22">Chakraborty S</searchLink>; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States.<br /><searchLink fieldCode="AU" term="%22Leroy+E%22">Leroy E</searchLink>; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States.<br /><searchLink fieldCode="AU" term="%22Schmoker+AM%22">Schmoker AM</searchLink>; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States.<br /><searchLink fieldCode="AU" term="%22Jeon+H%22">Jeon H</searchLink>; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States.<br /><searchLink fieldCode="AU" term="%22Weisberg+EL%22">Weisberg EL</searchLink>; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Medicine, Harvard Medical School, Boston, MA, 02215, United States.<br /><searchLink fieldCode="AU" term="%22Akatsu+T%22">Akatsu T</searchLink>; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States.<br /><searchLink fieldCode="AU" term="%22Griffin+JD%22">Griffin JD</searchLink>; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Medicine, Harvard Medical School, Boston, MA, 02215, United States.<br /><searchLink fieldCode="AU" term="%22Scott+DA%22">Scott DA</searchLink>; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States.<br /><searchLink fieldCode="AU" term="%22Eck+MJ%22">Eck MJ</searchLink>; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, 02215, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, 02215, United States. Electronic address: michael_eck@dfci.harvard.edu.
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  Data: <searchLink fieldCode="JN" term="%220420510%22">European journal of medicinal chemistry</searchLink> [Eur J Med Chem] 2026 Jan 15; Vol. 302 (Pt 1), pp. 118274. <i>Date of Electronic Publication: </i>2025 Oct 21.
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        Value: 10.1016/j.ejmech.2025.118274
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