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Volumn 3, Issue 2, 2012, Pages 135-139

Discovery of CX-6258. A potent, selective, and orally efficacious pan-pim kinases inhibitor

Author keywords

CX 6258; MV 4 11; PC3; Pim 1; Pim 2; Pim 3

Indexed keywords

ANTINEOPLASTIC AGENT; CX 6258; DOXORUBICIN; PACLITAXEL; PIM KINASE; PROTEIN KINASE; PROTEIN SERINE THREONINE KINASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 84856853371     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml200259q     Document Type: Article
Times cited : (73)

References (35)
  • 1
    • 78650606450 scopus 로고    scopus 로고
    • For better or for worse: The role of Pim oncogenes in tumorigenesis
    • Nawijn, M. C.; Alendar, A.; Berns, A. For better or for worse: the role of Pim oncogenes in tumorigenesis Nat. Rev. Cancer 2010, 11, 23-34
    • (2010) Nat. Rev. Cancer , vol.11 , pp. 23-34
    • Nawijn, M.C.1    Alendar, A.2    Berns, A.3
  • 2
    • 26444448463 scopus 로고    scopus 로고
    • The survival kinases Akt and Pim as potential pharmacological targets
    • DOI 10.1172/JCI26273
    • Amaravadi, R.; Thompson, C. B. The survival kinases Akt and Pim as potential pharmacological targets J. Clin. Invest. 2005, 115 (10) 2618-24 (Pubitemid 41434384)
    • (2005) Journal of Clinical Investigation , vol.115 , Issue.10 , pp. 2618-2624
    • Amaravadi, R.1    Thompson, C.B.2
  • 3
    • 0034708236 scopus 로고    scopus 로고
    • Developmental expression of Pim kinases suggests functions also outside of the hematopoietic system
    • Eichmann, A.; Yuan, L.; Breant, C.; Alitalo, K.; Koskinen, P. J. Developmental expression of pim kinases suggests functions also outside of the hematopoietic system Oncogene 2000, 19 (9) 1215-24 (Pubitemid 30157552)
    • (2000) Oncogene , vol.19 , Issue.9 , pp. 1215-1224
    • Eichmann, A.1    Yuan, L.2    Breant, C.3    Alitalo, K.4    Koskinen, P.J.5
  • 4
    • 0030829781 scopus 로고    scopus 로고
    • Pim-2 transgene induces lymphoid tumors, exhibiting potent synergy with c-myc
    • Allen, J. D.; Verhoeven, E.; Domen, J.; van der Valk, M.; Berns, A. Pim-2 transgene induces lymphoid tumors, exhibiting potent synergy with c-myc Oncogene 1997, 15 (10) 1133-41 (Pubitemid 27429616)
    • (1997) Oncogene , vol.15 , Issue.10 , pp. 1133-1141
    • Allen, J.D.1    Verhoeven, E.2    Domen, J.3    Van Der Valk, M.4    Berns, A.5
  • 5
    • 0029068012 scopus 로고
    • Transcriptional induction of pim-1 protein kinase gene expression by interferon gamma and posttranscriptional effects on costimulation with steel factor
    • Yip-Schneider, M. T.; Horie, M.; Broxmeyer, H. E. Transcriptional induction of pim-1 protein kinase gene expression by interferon gamma and posttranscriptional effects on costimulation with steel factor Blood 1995, 85 (12) 3494-502
    • (1995) Blood , vol.85 , Issue.12 , pp. 3494-502
    • Yip-Schneider, M.T.1    Horie, M.2    Broxmeyer, H.E.3
  • 7
    • 49649127162 scopus 로고    scopus 로고
    • Pim kinase-dependent inhibition of c-Myc degradation
    • Zhang, Y.; Wang, Z.; Li, X.; Magnuson, N. S. Pim kinase-dependent inhibition of c-Myc degradation Oncogene 2008, 27 (35) 4809-19
    • (2008) Oncogene , vol.27 , Issue.35 , pp. 4809-19
    • Zhang, Y.1    Wang, Z.2    Li, X.3    Magnuson, N.S.4
  • 9
    • 0025986962 scopus 로고
    • Eμ N- and Eμ L-myc cooperate with Eμ pim-1 to generate lymphoid tumors at high frequency in double-transgenic mice
    • Moroy, T.; Verbeek, S.; Ma, A.; Achacoso, P.; Berns, A.; Alt, F. 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 Oncogene 1991, 6 (11) 1941-8 (Pubitemid 21924031)
    • (1991) Oncogene , vol.6 , Issue.11 , pp. 1941-1948
    • Moroy, T.1    Verbeek, S.2    Ma, A.3    Achacoso, P.4    Berns, A.5    Alt, F.6
  • 10
    • 3343007095 scopus 로고    scopus 로고
    • 112 gatekeeper site
    • DOI 10.1016/j.febslet.2004.06.050, PII S0014579304008026
    • Aho, T. L.; Sandholm, J.; Peltola, K. J.; Mankonen, H. P.; Lilly, M.; Koskinen, P. J. Pim-1 kinase promotes inactivation of the pro-apoptotic Bad protein by phosphorylating it on the Ser112 gatekeeper site FEBS Lett. 2004, 571 (1-3) 43-9 (Pubitemid 38992921)
    • (2004) FEBS Letters , vol.571 , Issue.1-3 , pp. 43-49
    • Aho, T.L.T.1    Sandholm, J.2    Peltola, K.J.3    Mankonen, H.P.4    Lilly, M.5    Koskinen, P.J.6
  • 11
    • 32944458740 scopus 로고    scopus 로고
    • Pim kinases phosphorylate multiple sites on Bad and promote 14-3-3 binding and dissociation from Bcl-XL
    • Macdonald, A.; Campbell, D. G.; Toth, R.; McLauchlan, H.; Hastie, C. J.; Arthur, J. S. Pim kinases phosphorylate multiple sites on Bad and promote 14-3-3 binding and dissociation from Bcl-XL BMC Cell Biol. 2006, 7, 1
    • (2006) BMC Cell Biol. , vol.7 , pp. 1
    • MacDonald, A.1    Campbell, D.G.2    Toth, R.3    McLauchlan, H.4    Hastie, C.J.5    Arthur, J.S.6
  • 12
    • 0242580961 scopus 로고    scopus 로고
    • The PIM-2 Kinase Phosphorylates BAD on Serine 112 and Reverses BAD-induced Cell Death
    • DOI 10.1074/jbc.M307933200
    • Yan, B.; Zemskova, M.; Holder, S.; Chin, V.; Kraft, A.; Koskinen, P. J.; Lilly, M. The PIM-2 kinase phosphorylates BAD on serine 112 and reverses BAD-induced cell death J. Biol. Chem. 2003, 278 (46) 45358-67 (Pubitemid 37432672)
    • (2003) Journal of Biological Chemistry , vol.278 , Issue.46 , pp. 45358-45367
    • Yan, B.1    Zemskova, M.2    Holder, S.3    Chin, V.4    Kraft, A.5    Koskinen, P.J.6    Lilly, M.7
  • 13
    • 0022100028 scopus 로고
    • Proviral activation of the putative oncogene Pim-1 in MuLV induced T-cell lymphomas
    • Selten, G.; Cuypers, H. T.; Berns, A. Proviral activation of the putative oncogene Pim-1 in MuLV induced T-cell lymphomas EMBO J. 1985, 4 (7) 1793-8
    • (1985) EMBO J. , vol.4 , Issue.7 , pp. 1793-8
    • Selten, G.1    Cuypers, H.T.2    Berns, A.3
  • 14
    • 33746122005 scopus 로고    scopus 로고
    • 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
    • DOI 10.1158/0008-5472.CAN-05-4272
    • Li, Y. Y.; Popivanova, B. K.; Nagai, Y.; Ishikura, H.; Fujii, C.; Mukaida, N. 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 (13) 6741-7 (Pubitemid 44085632)
    • (2006) Cancer Research , vol.66 , Issue.13 , pp. 6741-6747
    • Li, Y.-Y.1    Popivanova, B.K.2    Nagai, Y.3    Ishikura, H.4    Fujii, C.5    Mukaida, N.6
  • 16
    • 0033603454 scopus 로고    scopus 로고
    • Physical and functional interactions between Pim-1 kinase and Cdc25A phosphatase. Implications for the Pim-1-mediated activation of the c-Myc signaling pathway
    • Mochizuki, T.; Kitanaka, C.; Noguchi, K.; Muramatsu, T.; Asai, A.; Kuchino, Y. Physical and functional interactions between Pim-1 kinase and Cdc25A phosphatase. Implications for the Pim-1-mediated activation of the c-Myc signaling pathway J. Biol. Chem. 1999, 274 (26) 18659-66
    • (1999) J. Biol. Chem. , vol.274 , Issue.26 , pp. 18659-66
    • Mochizuki, T.1    Kitanaka, C.2    Noguchi, K.3    Muramatsu, T.4    Asai, A.5    Kuchino, Y.6
  • 17
    • 48549096958 scopus 로고    scopus 로고
    • Pim kinases promote cell cycle progression by phosphorylating and down-regulating p27Kip1 at the transcriptional and posttranscriptional levels
    • Morishita, D.; Katayama, R.; Sekimizu, K.; Tsuruo, T.; Fujita, N. Pim kinases promote cell cycle progression by phosphorylating and down-regulating p27Kip1 at the transcriptional and posttranscriptional levels Cancer Res. 2008, 68 (13) 5076-85
    • (2008) Cancer Res. , vol.68 , Issue.13 , pp. 5076-85
    • Morishita, D.1    Katayama, R.2    Sekimizu, K.3    Tsuruo, T.4    Fujita, N.5
  • 18
    • 29244464759 scopus 로고    scopus 로고
    • The oncogenic serine/threonine kinase Pim-1 directly phosphorylates and activates the G2/M specific phosphatase Cdc25C
    • DOI 10.1016/j.biocel.2005.10.010, PII S1357272505003092
    • Bachmann, M.; Kosan, C.; Xing, P. X.; Montenarh, M.; Hoffmann, I.; Moroy, T. The oncogenic serine/threonine kinase Pim-1 directly phosphorylates and activates the G2/M specific phosphatase Cdc25C Int. J. Biochem. Cell Biol. 2006, 38 (3) 430-43 (Pubitemid 41821890)
    • (2006) International Journal of Biochemistry and Cell Biology , vol.38 , Issue.3 , pp. 430-443
    • Bachmann, M.1    Kosan, C.2    Xing, P.X.3    Montenarh, M.4    Hoffmann, I.5    Moroy, T.6
  • 20
    • 76149130727 scopus 로고    scopus 로고
    • Pim kinase inhibitors: A survey of the patent literature
    • Morwick, T. Pim kinase inhibitors: a survey of the patent literature Expert Opin. Ther. Pat. 2010, 2, 193-212
    • (2010) Expert Opin. Ther. Pat. , vol.2 , pp. 193-212
    • Morwick, T.1
  • 21
    • 79959756890 scopus 로고    scopus 로고
    • Discovery of novel Pim-1 kinase inhibitors by a hierarchical multistage virtual screening approach based on SVM model, pharmacophore, and molecular docking
    • Ren, J. X.; Li, L. L.; Zheng, R. L.; Xie, H. Z.; Cao, Z. X.; Feng, S.; Pan, Y. L.; Chen, X.; Wei, Y. Q.; Yang, S. Y. Discovery of novel Pim-1 kinase inhibitors by a hierarchical multistage virtual screening approach based on SVM model, pharmacophore, and molecular docking J. Chem. Inf. Model. 2011, 51 (6) 1364-75
    • (2011) J. Chem. Inf. Model. , vol.51 , Issue.6 , pp. 1364-75
    • Ren, J.X.1    Li, L.L.2    Zheng, R.L.3    Xie, H.Z.4    Cao, Z.X.5    Feng, S.6    Pan, Y.L.7    Chen, X.8    Wei, Y.Q.9    Yang, S.Y.10
  • 23
    • 41149093037 scopus 로고    scopus 로고
    • Docking study yields four novel inhibitors of the protooncogene Pim-1 kinase
    • DOI 10.1021/jm701248t
    • Pierce, A. C.; Jacobs, M.; Stuver-Moody, C. Docking study yields four novel inhibitors of the protooncogene Pim-1 kinase J. Med. Chem. 2008, 51 (6) 1972-5 (Pubitemid 351438879)
    • (2008) Journal of Medicinal Chemistry , vol.51 , Issue.6 , pp. 1972-1975
    • Pierce, A.C.1    Jacobs, M.2    Stuver-Moody, C.3
  • 24
    • 34547132324 scopus 로고    scopus 로고
    • Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity
    • DOI 10.1158/0008-5472.CAN-07-0320
    • Pogacic, V.; Bullock, A. N.; Fedorov, O.; Filippakopoulos, P.; Gasser, C.; Biondi, A.; Meyer-Monard, S.; Knapp, S.; Schwaller, J. Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity Cancer Res. 2007, 67 (14) 6916-24 (Pubitemid 47105539)
    • (2007) Cancer Research , vol.67 , Issue.14 , pp. 6916-6924
    • Pogacic, V.1    Bullock, A.N.2    Fedorov, O.3    Filippakopoulos, P.4    Gasser, C.5    Biondi, A.6    Meyer-Monard, S.7    Knapp, S.8    Schwaller, J.9
  • 26
    • 28144464847 scopus 로고    scopus 로고
    • Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase
    • DOI 10.1021/jm0504858
    • Bullock, A. N.; Debreczeni, J. E.; Fedorov, O. Y.; Nelson, A.; Marsden, B. D.; Knapp, S. Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase J. Med. Chem. 2005, 48 (24) 7604-14 (Pubitemid 41698801)
    • (2005) Journal of Medicinal Chemistry , vol.48 , Issue.24 , pp. 7604-7614
    • Bullock, A.N.1    Debreczeni, J.E.2    Fedorov, O.Y.3    Nelson, A.4    Marsden, B.D.5    Knapp, S.6
  • 28
    • 33847058740 scopus 로고    scopus 로고
    • Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase
    • DOI 10.1016/j.bmcl.2006.12.086, PII S0960894X07000078
    • Cheney, I. W.; Yan, S.; Appleby, T.; Walker, H.; Vo, T.; Yao, N.; Hamatake, R.; Hong, Z.; Wu, J. Z. Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase Bioorg. Med. Chem. Lett. 2007, 17 (6) 1679-83 (Pubitemid 46274341)
    • (2007) Bioorganic and Medicinal Chemistry Letters , vol.17 , Issue.6 , pp. 1679-1683
    • Cheney, I.W.1    Yan, S.2    Appleby, T.3    Walker, H.4    Vo, T.5    Yao, N.6    Hamatake, R.7    Hong, Z.8    Wu, J.Z.9
  • 31
    • 0032474915 scopus 로고    scopus 로고
    • 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
    • DOI 10.1021/jm980123i
    • Sun, L.; Tran, N.; Tang, F.; App, H.; Hirth, P.; McMahon, G.; Tang, C. 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 J. Med. Chem. 1998, 41 (14) 2588-603 (Pubitemid 28321908)
    • (1998) Journal of Medicinal Chemistry , vol.41 , Issue.14 , pp. 2588-2603
    • Sun, L.1    Tran, N.2    Tang, F.3    App, H.4    Hirth, P.5    McMahon, G.6    Tang, C.7
  • 32
    • 33746471790 scopus 로고    scopus 로고
    • Constitutively activated FLT3 phosphorylates BAD partially through Pim-1
    • DOI 10.1111/j.1365-2141.2006.06225.x
    • Kim, K. T.; Levis, M.; Small, D. Constitutively activated FLT3 phosphorylates BAD partially through pim-1 Br. J. Hamaetol. 2006, 134 (5) 500-9 (Pubitemid 44141716)
    • (2006) British Journal of Haematology , vol.134 , Issue.5 , pp. 500-509
    • Kim, K.-T.1    Levis, M.2    Small, D.3
  • 33
    • 13544268345 scopus 로고    scopus 로고
    • Pim-1 is up-regulated by constitutively activated FLT3 and plays a role in FLT3-mediated cell survival
    • DOI 10.1182/blood-2004-05-2006
    • Kim, K. T.; Baird, K.; Ahn, J. Y.; Meltzer, P.; Lilly, M.; Levis, M.; Small, D. Pim-1 is up-regulated by constitutively activated FLT3 and plays a role in FLT3-mediated cell survival Blood 2005, 105 (4) 1759-67 (Pubitemid 40223700)
    • (2005) Blood , vol.105 , Issue.4 , pp. 1759-1767
    • Kim, K.-T.1    Baird, K.2    Ahn, J.-Y.3    Meltzer, P.4    Lilly, M.5    Levis, M.6    Small, D.7
  • 35
    • 33846701190 scopus 로고    scopus 로고
    • Proto-oncogene, Pim-3 with serine/threonine kinase activity, is aberrantly expressed in human colon cancer cells and can prevent Bad-mediated apoptosis
    • DOI 10.1111/j.1349-7006.2007.00390.x
    • Popivanova, B. K.; Li, Y. Y.; Zheng, H.; Omura, K.; Fujii, C.; Tsuneyama, K.; Mukaida, N. Proto-oncogene, Pim-3 with serine/threonine kinase activity, is aberrantly expressed in human colon cancer cells and can prevent Bad-mediated apoptosis Cancer Sci. 2007, 98 (3) 321-8 (Pubitemid 46195601)
    • (2007) Cancer Science , vol.98 , Issue.3 , pp. 321-328
    • Popivanova, B.K.1    Li, Y.-Y.2    Zheng, H.3    Omura, K.4    Fujii, C.5    Tsuneyama, K.6    Mukaida, N.7


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