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The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1.
Nature. 2017 Mar 30;543(7647):733-737. doi: 10.1038/nature21702. Epub 2017 Mar 22.
Nature. 2017.
PMID: 28329763
Asciminib in Chronic Myeloid Leukemia after ABL Kinase Inhibitor Failure.
Hughes TP, Mauro MJ, Cortes JE, Minami H, Rea D, DeAngelo DJ, Breccia M, Goh YT, Talpaz M, Hochhaus A, le Coutre P, Ottmann O, Heinrich MC, Steegmann JL, Deininger MWN, Janssen JJWM, Mahon FX, Minami Y, Yeung D, Ross DM, Tallman MS, Park JH, Druker BJ, Hynds D, Duan Y, Meille C, Hourcade-Potelleret F, Vanasse KG, Lang F, Kim DW.
Hughes TP, et al. Among authors: vanasse kg.
N Engl J Med. 2019 Dec 12;381(24):2315-2326. doi: 10.1056/NEJMoa1902328.
N Engl J Med. 2019.
PMID: 31826340
Free PMC article.
Clinical Trial.
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Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.
Burger MT, Nishiguchi G, Han W, Lan J, Simmons R, Atallah G, Ding Y, Tamez V, Zhang Y, Mathur M, Muller K, Bellamacina C, Lindvall MK, Zang R, Huh K, Feucht P, Zavorotinskaya T, Dai Y, Basham S, Chan J, Ginn E, Aycinena A, Holash J, Castillo J, Langowski JL, Wang Y, Chen MY, Lambert A, Fritsch C, Kauffmann A, Pfister E, Vanasse KG, Garcia PD.
Burger MT, et al. Among authors: vanasse kg.
J Med Chem. 2015 Nov 12;58(21):8373-86. doi: 10.1021/acs.jmedchem.5b01275. Epub 2015 Oct 27.
J Med Chem. 2015.
PMID: 26505898
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The first-in-human study of the pan-PIM kinase inhibitor PIM447 in patients with relapsed and/or refractory multiple myeloma.
Raab MS, Thomas SK, Ocio EM, Guenther A, Goh YT, Talpaz M, Hohmann N, Zhao S, Xiang F, Simon C, Vanasse KG, Kumar SK.
Raab MS, et al. Among authors: vanasse kg.
Leukemia. 2019 Dec;33(12):2924-2933. doi: 10.1038/s41375-019-0482-0. Epub 2019 May 15.
Leukemia. 2019.
PMID: 31092894
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