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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: lindvall mk. 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
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. 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
2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors.
Costales A, Mathur M, Ramurthy S, Lan J, Subramanian S, Jain R, Atallah G, Setti L, Lindvall M, Appleton BA, Ornelas E, Feucht P, Warne B, Doyle L, Basham SE, Aronchik I, Jefferson AB, Shafer CM. Costales A, et al. Bioorg Med Chem Lett. 2014 Mar 15;24(6):1592-6. doi: 10.1016/j.bmcl.2014.01.058. Epub 2014 Jan 30. Bioorg Med Chem Lett. 2014. PMID: 24534486
Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers.
Aronchik I, Appleton BA, Basham SE, Crawford K, Del Rosario M, Doyle LV, Estacio WF, Lan J, Lindvall MK, Luu CA, Ornelas E, Venetsanakos E, Shafer CM, Jefferson AB. Aronchik I, et al. Among authors: lindvall mk. Mol Cancer Res. 2014 May;12(5):803-12. doi: 10.1158/1541-7786.MCR-13-0595. Epub 2014 Feb 19. Mol Cancer Res. 2014. PMID: 24554780 Free article.
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.
Karpov AS, Amiri P, Bellamacina C, Bellance MH, Breitenstein W, Daniel D, Denay R, Fabbro D, Fernandez C, Galuba I, Guerro-Lagasse S, Gutmann S, Hinh L, Jahnke W, Klopp J, Lai A, Lindvall MK, Ma S, Möbitz H, Pecchi S, Rummel G, Shoemaker K, Trappe J, Voliva C, Cowan-Jacob SW, Marzinzik AL. Karpov AS, et al. Among authors: lindvall mk. ACS Med Chem Lett. 2015 May 22;6(7):776-81. doi: 10.1021/acsmedchemlett.5b00102. eCollection 2015 Jul 9. ACS Med Chem Lett. 2015. PMID: 26191365 Free PMC article.
Discovery of Potent and Selective RSK Inhibitors as Biological Probes.
Jain R, Mathur M, Lan J, Costales A, Atallah G, Ramurthy S, Subramanian S, Setti L, Feucht P, Warne B, Doyle L, Basham S, Jefferson AB, Lindvall M, Appleton BA, Shafer CM. Jain R, et al. J Med Chem. 2015 Sep 10;58(17):6766-83. doi: 10.1021/acs.jmedchem.5b00450. Epub 2015 Aug 13. J Med Chem. 2015. PMID: 26270416
35 results