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Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.
Burger MT, Han W, Lan J, Nishiguchi G, Bellamacina C, Lindval M, Atallah G, Ding Y, Mathur M, McBride C, Beans EL, Muller K, Tamez V, Zhang Y, Huh K, Feucht P, Zavorotinskaya T, Dai Y, Holash J, Castillo J, Langowski J, Wang Y, Chen MY, Garcia PD. Burger MT, et al. Among authors: langowski j. ACS Med Chem Lett. 2013 Oct 15;4(12):1193-7. doi: 10.1021/ml400307j. eCollection 2013 Dec 12. ACS Med Chem Lett. 2013. PMID: 24900629 Free PMC article.
Pan-PIM kinase inhibition provides a novel therapy for treating hematologic cancers.
Garcia PD, Langowski JL, Wang Y, Chen M, Castillo J, Fanton C, Ison M, Zavorotinskaya T, Dai Y, Lu J, Niu XH, Basham S, Chan J, Yu J, Doyle M, Feucht P, Warne R, Narberes J, Tsang T, Fritsch C, Kauffmann A, Pfister E, Drueckes P, Trappe J, Wilson C, Han W, Lan J, Nishiguchi G, Lindvall M, Bellamacina C, Aycinena JA, Zang R, Holash J, Burger MT. Garcia PD, et al. Among authors: langowski jl. Clin Cancer Res. 2014 Apr 1;20(7):1834-45. doi: 10.1158/1078-0432.CCR-13-2062. Epub 2014 Jan 28. Clin Cancer Res. 2014. PMID: 24474669
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: langowski jl. 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
Synthesis and Structure-Activity Relationship of Tetra-Substituted Cyclohexyl Diol Inhibitors of Proviral Insertion of Moloney Virus (PIM) Kinases.
Han W, Ding Y, Chen Z, Langowski JL, Bellamacina C, Rico A, Nishiguchi GA, Lan J, Atallah G, Lindvall M, Lin S, Zang R, Feucht P, Zavorotinskaya T, Dai Y, Garcia P, Burger MT. Han W, et al. Among authors: langowski jl. J Med Chem. 2020 Dec 10;63(23):14885-14904. doi: 10.1021/acs.jmedchem.0c01279. Epub 2020 Dec 1. J Med Chem. 2020. PMID: 33258605
Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.
Poddutoori R, Aardalen K, Aithal K, Barahagar SS, Belliappa C, Bock M, Chelur S, Gerken A, Gopinath S, Gruenenfelder B, Kiffe M, Krishnaswami M, Langowski J, Madapa S, Narayanan K, Pandit C, Panigrahi SK, Perrone M, Potakamuri RK, Ramachandra M, Ramanathan A, Ramos R, Sager E, Samajdar S, Subramanya HS, Thimmasandra DS, Venetsanakos E, Möbitz H. Poddutoori R, et al. Among authors: langowski j. J Med Chem. 2022 Mar 10;65(5):4350-4366. doi: 10.1021/acs.jmedchem.1c02192. Epub 2022 Feb 23. J Med Chem. 2022. PMID: 35195996
203 results