Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.
暂无分享,去创建一个
Adam Siddiqui-Jain | J. Bliesath | Diwata Macalino | M. Omori | Nicole Streiner | K. Anderes | C. Proffitt | S. O'Brien | D. Ryckman | W. Rice | D. Drygin | Joe A. Tran | M. Haddach | M. Schwaebe | Denis Drygin | Fabrice Pierre | Kenna Anderes | Mustapha Haddach | Jerome Michaux | Michael K Schwaebe | Sean E O'Brien | Cosmin Borsan | Joe Tran | Nicholas Raffaele | Suchitra Ravula | Adam Siddiqui-Jain | Levan Darjania | Ryan Stansfield | Chris Proffitt | Diwata Macalino | Nicole Streiner | Joshua Bliesath | May Omori | Jeffrey P Whitten | William G Rice | David M Ryckman | F. Pierre | Jérôme Michaux | J. Whitten | L. Darjania | R. Stansfield | Suchitra Ravula | N. Raffaele | Cosmin Borsan | J. Michaux
[1] A. Pierce,et al. Docking study yields four novel inhibitors of the protooncogene Pim-1 kinase. , 2008, Journal of medicinal chemistry.
[2] G. Mcmahon,et al. Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases. , 1998, Journal of medicinal chemistry.
[3] M. Lilly,et al. Characterization of a potent and selective small-molecule inhibitor of the PIM1 kinase , 2007, Molecular Cancer Therapeutics.
[4] S. Dhanasekaran,et al. Delineation of prognostic biomarkers in prostate cancer , 2001, Nature.
[5] T. Möröy,et al. The serine/threonine kinase Pim-1. , 2005, The international journal of biochemistry & cell biology.
[6] P. Koskinen,et al. Pim‐1 kinase promotes inactivation of the pro‐apoptotic Bad protein by phosphorylating it on the Ser112 gatekeeper site , 2004, FEBS letters.
[7] A. Good,et al. The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors. , 2011, Bioorganic & medicinal chemistry letters.
[8] G. Bemis,et al. Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase. , 2009, Bioorganic & medicinal chemistry letters.
[9] J. Arthur,et al. Pim kinases phosphorylate multiple sites on Bad and promote 14-3-3 binding and dissociation from Bcl-XL , 2006, BMC Cell Biology.
[10] S. Knapp,et al. Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase. , 2005, Journal of medicinal chemistry.
[11] T. Graeber,et al. Myc-driven murine prostate cancer shares molecular features with human prostate tumors. , 2003, Cancer cell.
[12] T. Möröy,et al. The oncogenic serine/threonine kinase Pim-1 directly phosphorylates and activates the G2/M specific phosphatase Cdc25C. , 2006, The international journal of biochemistry & cell biology.
[13] Mika Lindvall,et al. Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases. , 2011, Bioorganic & medicinal chemistry letters.
[14] Kyu-Tae Kim,et al. Constitutively activated FLT3 phosphorylates BAD partially through Pim‐1 , 2006, British journal of haematology.
[15] V. Stoll,et al. Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases. , 2009, Journal of medicinal chemistry.
[16] M. Nawijn,et al. For better or for worse: the role of Pim oncogenes in tumorigenesis , 2011, Nature Reviews Cancer.
[17] I. W. Cheney,et al. Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. , 2007, Bioorganic & medicinal chemistry letters.
[18] H. Broxmeyer,et al. Transcriptional induction of pim-1 protein kinase gene expression by interferon gamma and posttranscriptional effects on costimulation with steel factor. , 1995, Blood.
[19] C. Thompson,et al. The survival kinases Akt and Pim as potential pharmacological targets. , 2005, The Journal of clinical investigation.
[20] T. Morwick. Pim kinase inhibitors: a survey of the patent literature , 2010, Expert opinion on therapeutic patents.
[21] K. Tsuneyama,et al. Proto‐oncogene, Pim‐3 with serine/threonine kinase activity, is aberrantly expressed in human colon cancer cells and can prevent Bad‐mediated apoptosis , 2007, Cancer science.
[22] Xin Chen,et al. Discovery of Novel Pim-1 Kinase Inhibitors by a Hierarchical Multistage Virtual Screening Approach Based on SVM Model, Pharmacophore, and Molecular Docking , 2011, J. Chem. Inf. Model..
[23] A Ma,et al. E mu N- and E mu L-myc cooperate with E mu pim-1 to generate lymphoid tumors at high frequency in double-transgenic mice. , 1991, Oncogene.
[24] S. Knapp,et al. Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity. , 2007, Cancer research.
[25] A. Kraft,et al. The PIM-2 Kinase Phosphorylates BAD on Serine 112 and Reverses BAD-induced Cell Death* , 2003, Journal of Biological Chemistry.
[26] T. Tsuruo,et al. Pim kinases promote cell cycle progression by phosphorylating and down-regulating p27Kip1 at the transcriptional and posttranscriptional levels. , 2008, Cancer research.
[27] A. Berns,et al. Pim-2 transgene induces lymphoid tumors, exhibiting potent synergy with c-myc , 1997, Oncogene.
[28] K. Alitalo,et al. Developmental expression of Pim kinases suggests functions also outside of the hematopoietic system , 2000, Oncogene.
[29] K. Tsuneyama,et al. Aberrant Pim-3 expression is involved in gastric adenoma–adenocarcinoma sequence and cancer progression , 2008, Journal of Cancer Research and Clinical Oncology.
[30] Hiroshi Ishikura,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. , 2006, Cancer research.
[31] A. Berns,et al. Proviral activation of the putative oncogene Pim‐1 in MuLV induced T‐cell lymphomas. , 1985, The EMBO journal.
[32] Z. Wang,et al. Pim kinase-dependent inhibition of c-Myc degradation , 2008, Oncogene.
[33] Wenyi Wei,et al. Phosphorylation of the cell cycle inhibitor p21Cip1/WAF1 by Pim-1 kinase. , 2002, Biochimica et biophysica acta.
[34] P. Meltzer,et al. Pim-1 is up-regulated by constitutively activated FLT3 and plays a role in FLT3-mediated cell survival. , 2005, Blood.
[35] K. Noguchi,et al. Physical and Functional Interactions between Pim-1 Kinase and Cdc25A Phosphatase , 1999, The Journal of Biological Chemistry.