ACUTE GRANULOCYTIC LEUKEMIA;
ANTINEOPLASTIC ACTIVITY;
APOPTOSIS;
CANCER SURVIVAL;
CELL PROLIFERATION;
CELL SURVIVAL;
DRUG EFFICACY;
DRUG INDUSTRY;
DRUG POTENCY;
DRUG SAFETY;
DRUG STRUCTURE;
HUMAN;
IC 50;
MEDICAL LITERATURE;
PATENT;
REVIEW;
ANIMALS;
ANTINEOPLASTIC AGENTS;
APOPTOSIS;
CELL PROLIFERATION;
CELL SURVIVAL;
DRUG DESIGN;
HUMANS;
LEGISLATION, DRUG;
MOLECULAR STRUCTURE;
MOLECULAR TARGETED THERAPY;
NEOPLASMS;
PATENTS AS TOPIC;
PROTEIN KINASE INHIBITORS;
PROTO-ONCOGENE PROTEINS C-PIM-1;
SIGNAL TRANSDUCTION;
STRUCTURE-ACTIVITY RELATIONSHIP;
Second generation PIM inhibitor exhibits potent activity in tumor models
Inc., Salt Lake City, UT USA
Jason MF, Yong X, Anna S, et al. Second generation PIM inhibitor exhibits potent activity in tumor models. Tolero Pharmaceuticals, Inc., Salt Lake City, UT USA .
PIM serine/threonine kinases in the pathogenesis and therapy of hematologic malignancies and solid cancers
Brault L, Gasser C, Bracher F, et al. PIM serine/threonine kinases in the pathogenesis and therapy of hematologic malignancies and solid cancers. Haematologica 2010;95:1004-15
Identification and structure-Activity relationship of 8-hydroxy-quinoline-7- carboxylic acid derivatives as inhibitors of PIM1 kinase
Sliman F, Blairvacq M, Durieu E, et al. Identification and structure-Activity relationship of 8-hydroxy-quinoline-7- carboxylic acid derivatives as inhibitors of PIM1 kinase. Bioorg Med Chem Lett 2010;20:2801-5
Pim-3, a proto-oncogene with serine/ threonine kinase activity, is aberrantly expressed in human pancreatic cancer and phosphorylates bad to block bad-mediated apoptosis in human pancreatic cancer cell lines
Li YY, Popivanova BK, Nagai Y, et al. Pim-3, a proto-oncogene with serine/ threonine kinase activity, is aberrantly expressed in human pancreatic cancer and phosphorylates bad to block bad-mediated apoptosis in human pancreatic cancer cell lines. Cancer Res 2006;66:6741-7
PIM kinase isoform specific regulation of MIG6 expression and EGFR signaling in prostate cancer cells
Siu A, Virtanen C, Jongstra J. PIM kinase isoform specific regulation of MIG6 expression and EGFR signaling in prostate cancer cells. Oncotarget 2011;2:1134-44
Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition
Blanco-Aparicio C, Collazo AM, Oyarzabal J, et al. Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition. Cancer Lett 2011;300:145-53
Pim kinases phosphorylate multiple sites on Bad and promote 14-3-3 binding and dissociation from Bcl-XL
Macdonald A, Campbell DG, Toth R, et al. Pim kinases phosphorylate multiple sites on Bad and promote 14-3-3 binding and dissociation from Bcl-XL. BMC Cell Biol 2006;7:1
7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6] naphthyridines: A novel class of Pim kinase inhibitors with potent cell antiproliferative activity
Pierre F, Stefan E, Nedellec AS, et al. 7-(4H-1,2,4-Triazol-3-yl)benzo[c] [2,6] naphthyridines: A novel class of Pim kinase inhibitors with potent cell antiproliferative activity. Bioorg Med Chem Lett 2011;21:6687-92
Rational evolution of a novel type of potent and selective proviral integration site in Moloney murine leukemia virus kinase 1 (PIM1) inhibitor from a screening-hit compound
Nakano H, Saito N, Parker L, et al. Rational evolution of a novel type of potent and selective proviral integration site in Moloney murine leukemia virus kinase 1 (PIM1) inhibitor from a screening-hit compound. J Med Chem 2012;55:5151-64
Structural basis of constitutive activity and a unique nucleotide binding mode of human pim-1 kinase
Qian KC, Wang L, Hickey ER, et al. Structural basis of constitutive activity and a unique nucleotide binding mode of human pim-1 kinase. J Biol Chem 2005;280:6130-7
Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002
Jacobs MD, Black J, Futer O, et al. Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002. J Biol Chem 2005;280:13728-34
PIM as a rational target for B-cell lymphomas. CNIO Frontiers Meetings; 8 - 10 March 2010; Molecular Cancer Therapeutics 22. Centro Nacional de Investigaciones Oncologicas (CNIO)
WO004984
Gomez-Abad C, Pisonero H, Blanco-Aparicio C, et al. PIM as a rational target for B-cell lymphomas. CNIO Frontiers Meetings; 8 - 10 March 2010; Molecular Cancer Therapeutics 22. Centro Nacional de Investigaciones Oncologicas (CNIO). Tricyclic compounds for use as kinase inhibitors. WO004984; 2013
Hit to lead evaluation of 1 ,2,3-Triazolo [4,5-b]pyridines as PIM kinase inhibitors
Pastor J, Oyarzabal J, Saluste G, et al. Hit to lead evaluation of 1,2,3-Triazolo [4,5-b]pyridines as PIM kinase inhibitors. Bioorg Med Chem Lett 2012;22:1591-7
Novel benzylidene-Thiazolidine- 2,4-diones inhibit Pim protein kinase activity and induce cell cycle arrest in leukemia and prostate cancer cells
Beharry Z, Zemskova M, Mahajan S, et al. Novel benzylidene-Thiazolidine- 2,4-diones inhibit Pim protein kinase activity and induce cell cycle arrest in leukemia and prostate cancer cells. Mol Cancer Ther 2009;8:1473-83
Keeton E, Palakurthi S, Alimzhanov M, et al. 1540 AZD1208, a novel, potent and selective pan pim kinase inhibitor, demonstrates efficacy in models of acute myeloid leukemia. 53rd ASH Annual Meeting & Exposition; 10 - 13 December 2011
PIM2 inhibitor as a targeted therapy for the treatment of multiple myeloma patients with specific genetic signatures
7 April 2013; Jasco Pharmaceuticals, LLC & Roswell Park Cancer Institute, Buffalo, NY 62. Macquarie University. Synthesis of ageladine a and analogs thereof WO152584
Carmen MB. PIM2 inhibitor as a targeted therapy for the treatment of multiple myeloma patients with specific genetic signatures. AACR Annual Meeting; 7 April 2013; Jasco Pharmaceuticals, LLC & Roswell Park Cancer Institute, Buffalo, NY 62. Macquarie University. Synthesis of ageladine a and analogs thereof. WO152584; 2009
Characterization of a potent and selective small-molecule inhibitor of the PIM1 kinase
Holder S, Zemskova M, Zhang C, et al. Characterization of a potent and selective small-molecule inhibitor of the PIM1 kinase. Mol Cancer Ther 2007;6:163-72
Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases
Nishiguchi GA, Atallah G, Bellamacina C, et al. Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases. Bioorg Med Chem Lett 2011;21:6366-9
A small molecule inhibitor of Pim protein kinases blocks the growth of precursor T-cell lymphoblastic leukemia/ lymphoma
Lin YW, Beharry ZM, Hill EG, et al. A small molecule inhibitor of Pim protein kinases blocks the growth of precursor T-cell lymphoblastic leukemia/ lymphoma. Blood 2010;115:824-33
PIM1 gene cooperates with human BCL6 gene to promote the development of lymphomas
Baron BW, Anastasi J, Hyjek EM, et al. PIM1 gene cooperates with human BCL6 gene to promote the development of lymphomas. Proc Natl Acad Sci USA 2012;109:5735-9
Discovery of novel benzylidene-1,3- Thiazolidine-2,4-diones as potent and selective inhibitors of the PIM1, PIM2, and PIM3 protein kinases
Dakin LA, Block MH, Chen H, et al. Discovery of novel benzylidene-1,3- Thiazolidine-2,4-diones as potent and selective inhibitors of the PIM1, PIM2, and PIM3 protein kinases. Bioorg Med Chem Lett 2012;22:4599-604
Expression, purification, crystallization and preliminary crystallographic analysis of human Pim-1 kinase
Qian KC, Studts J, Wang L, et al. Expression, purification, crystallization and preliminary crystallographic analysis of human Pim-1 kinase. Acta Crystallogr Sect F Struct Biol Cryst Commun 2005;61:96-9
Crystal structures of proto-oncogene kinase Pim1: A target of aberrant somatic hypermutations in diffuse large cell lymphoma
Kumar A, Mandiyan V, Suzuki Y, et al. Crystal structures of proto-oncogene kinase Pim1: A target of aberrant somatic hypermutations in diffuse large cell lymphoma. J Mol Biol 2005;348:183-93
Identification and structure-Activity relationships of substituted pyridones as inhibitors of Pim-1 kinase
Cheney IW, Yan S, Appleby T, et al. Identification and structure-Activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg Med Chem Lett 2007;17:1679-83
Similar biological activities of two isostructural ruthenium and osmium complexes
Maksimoska J, Williams DS, Atilla-Gokcumen GE, et al. Similar biological activities of two isostructural ruthenium and osmium complexes. E Chem Eur J 2008;14:4816-22
Hit to lead account of the discovery of a new class of inhibitors of Pim kinases and crystallographic studies revealing an unusual kinase binding mode
Qian K, Wang L, Cywin CL, et al. Hit to lead account of the discovery of a new class of inhibitors of Pim kinases and crystallographic studies revealing an unusual kinase binding mode. J Med Chem 2009;52:1814-27
Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors
Akue-Gedu R, Rossignol E, Azzaro S, et al. Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors. J Med Chem 2009;52:6369-81