CI-1040 (PD184352), a Targeted Signal Transduction Inhibitor of MEK (MAPKK)

Seminars in Oncology

Volumn 30, Issue 5 SUPPL. 16, 2003, Pages 105-116

  Allen, Lee F ^b   Sebolt Leopold, Judith ^b   Meyer, Mark B ^a  

^a PFIZER INC   (United States)

^b NONE

Author keywords

[No Author keywords available]

Indexed keywords

1,4 DIAMINO 1,4 BIS(2 AMINOPHENYLTHIO) 2,3 DICYANOBUTADIENE; 2 (2 AMINO 3 METHOXYPHENYL)CHROMONE; 2 (2 CHLORO 4 IODOANILINO) N CYCLOPROPYLMETHOXY 3,4 DIFLUOROBENZAMIDE; MITOGEN ACTIVATED PROTEIN KINASE; MITOGEN ACTIVATED PROTEIN KINASE KINASE; MITOGEN ACTIVATED PROTEIN KINASE KINASE KINASE; RAF PROTEIN; SORAFENIB; UNCLASSIFIED DRUG;

ANGIOGENESIS; ANTINEOPLASTIC ACTIVITY; BREAST CANCER; CANCER CELL CULTURE; CANCER GROWTH; CELL MATURATION; CELL PROLIFERATION; CELL SURVIVAL; CLINICAL TRIAL; COLON CANCER; CONFERENCE PAPER; DIARRHEA; DRUG EFFECT; DRUG EFFICACY; DRUG SAFETY; DRUG TOLERABILITY; ENZYME INHIBITION; FATIGUE; GENE OVEREXPRESSION; HUMAN; KIDNEY CANCER; LUNG NON SMALL CELL CANCER; NAUSEA; OVARY CANCER; PANCREAS CANCER; PRIORITY JOURNAL; PROGNOSIS; PROSTATE CANCER; PROTO ONCOGENE; RASH; SIDE EFFECT; SIGNAL TRANSDUCTION; VOMITING;

EID: 0242468891     PISSN: 00937754     EISSN: None     Source Type: Journal    
DOI: 10.1053/j.seminoncol.2003.08.012     Document Type: Conference Paper

References (100)

1. Hunter T: Oncoprotein networks. Cell 88:333-346, 1997
2. Spencer VA, Davie JR: Signal transduction pathways and chromatin structure in cancer cells. J Cell Biochem 35:27-35, 2000 (suppl)
3. McCormick F: Signalling networks that cause cancer. Trends Cell Biol 9:M53-M56, 1999
4. Hanahan D, Weinberg RA: The hallmarks of cancer. Cell 100:57-70, 2000
5. Robinson MJ, Cobb MH: Mitogen-activated protein kinase pathways. Curr Opin Cell Biol 9:180-186, 1997
6. Seger R, Krebs EG: The MAPK signaling cascade. FASEB J 9:726-735, 1995
7. Cobb MH, Goldsmith EJ: How MAP kinases are regulated. J Biol Chem 270:14843-14846, 1995
8. Pearson G, Robinson F, Beers, et al: Mitogen-activated protein (MAP) kinase pathways: Regulation and physiological functions. Endocr Rev 22:153-183, 2001
9. Lewis TS, Shapiro PS, Ahn NG: Signal transduction through MAP kinase cascades. Adv Cancer Res 74:49-139, 1998
10. Cano E, Mahadevan LC: Parallel signal processing among mammalian MAPKs. Trends Biochem Sci 20:117-122, 1995
11. Marshall CJ: Specificity of receptor tyrosine kinase signaling: Transient versus sustained extracellular signal-regulated kinase activation. Cell 80:179-185, 1995
12. Pang L, Sawada T, Decker SJ, et al: Inhibition of MAP kinase kinase blocks the differentiation of PC-12 cells induced by nerve growth factor. J Biol Chem 270:13585-13588, 1995
13. Cowley S, Paterson H, Kemp P, et al: Activation of MAP kinase kinase is necessary and sufficient for PC12 differentiation and for transformation of NIH 3T3 cells. Cell 77:841-852, 1994
14. Schaeffer HJ, Weber MJ: Mitogen-activated protein kinases: Specific messages from ubiquitous messengers. Mol Cell Biol 19:2435-2444, 1999
15. Dhanasekaran N, Premkumar Reddy E: Signaling by dual specificity kinases. Oncogene 17:1447-1455, 1998
16. Widmann C, Gibson S, Jarpe MB, et al: Mitogen-activated protein kinase: Conservation of a three-kinase module from yeast to human. Physiol Rev 79:143-180, 1999
17. Arbabi S, Maier RV: Mitogen-activated protein kinases. Crit Care Med 30:S74-S79, 2002 (suppl 1)
18. English JM, Cobb MH: Pharmacological inhibitors of MAPK pathways. Trends Pharmacol Sci 23:40-45, 2002
19. Pierce KL, Luttrell LM, Lefkowitz RJ: New mechanisms in heptahelical receptor signaling to mitogen activated protein kinase cascades. Oncogene 20:1532-1539, 2001
20. Harada J, Sugimoto M: An inhibitor of p38 and JNK MAP kinases prevents activation of caspase and apoptosis of cultured cerebellar granule neurons. Jpn J Pharmacol 79:369-378, 1999
21. Noguchi K, Yamana H, Kitanaka C, et al: Differential role of the JNK and p38 MAPK pathway in c-Myc- and s-Myc-mediated apoptosis. Biochem Biophys Res Commun 267:221-227, 2000
22. Assefa Z, Vantieghem A, Garmyn M, et al: p38 mitogen-activated protein kinase regulates a novel, caspase-independent pathway for the mitochondrial cytochrome c release in ultraviolet B radiation-induced apoptosis. J Biol Chem 275:21416-21421, 2000
23. Harper SJ, LoGrasso P: Signalling for survival and death in neurones: The role of stress- activated kinases, JNK and p38. Cell Signal 13:299-310, 2001
24. Favata MF, Horiuchi KY, Manos EJ, et al: Identification of a novel inhibitor of mitogen- activated protein kinase kinase. J Biol Chem 273:18623-18632, 1998
25. Alessi DR, Cuenda A, Cohen P, et al: PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. J Biol Chem 270:27489-27494, 1995
26. Davies SP, Reddy H, Caivano M, et al: Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J 351:95-105, 2000
27. Dudley DT, Pang L, Decker SJ, et al: A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proc Natl Acad Sci U S A 92:7686-7689, 1995
28. Sebolt-Leopold JS: Development of anticancer drugs targeting the MAP kinase pathway. Oncogene 19:6594-6599, 2000
29. Lowinger TB, Riedl B, Dumas J, et al: Design and discovery of small molecules targeting raf-1 kinase. Curr Pharm Des 8:2269-2278, 2002
30. Lyons JF, Wilhelm S, Hibner B, et al: Discovery of a novel Raf kinase inhibitor. Endocr Relat Cancer 8:219-225, 2001
31. LoRusso PM, Adjei AA, Meyer MB, et al: A phase 1 clinical and pharmacokinetic evaluation of the oral MEK inhibitor, CI-1040, administered for 21 consecutive days, repeated every 4 weeks in patients with advanced cancer. Proc Am Soc Clin Oncol 21:81a, 2002 (abstr 321)
32. Hotte SJ, Hirte HW: BAY 43-9006: Early clinical data in patients with advanced solid malignancies. Curr Pharm Des 8:2249-2253, 2002
33. Avruch J, Zhang XF, Kyriakis JM: Raf meets Ras: Completing the framework of a signal transduction pathway. Trends Biochem Sci 19:279-283, 1994
34. Daum G, Eisenmann-Tappe I, Fries HW, et al: The ins and outs of Raf kinases. Trends Biochem Sci 19:474-480, 1994
35. Blumer KJ, Johnson GL: Diversity in function and regulation of MAP kinase pathways. Trends Biochem Sci 19:236-240, 1994
36. Warne PH, Viciana PR, Downward J: Direct interaction of Ras and the amino-terminal region of Raf-1 in vitro. Nature 364:352-355, 1993
37. McCormick F: Signal transduction. How receptors turn Ras on. Nature 363:15-16, 1993
38. Batzer AG, Rotin D, Urena JM, et al: Hierarchy of binding sites for Grb2 and Shc on the epidermal growth factor receptor. Mol Cell Biol 14:5192-5201, 1994
39. Sasaoka T, Langlois WJ, Leitner JW, et al: The signaling pathway coupling epidermal growth factor receptors to activation of p21ras. J Biol Chem 269:32621-32625, 1994
40. Kolch W: Meaningful relationships: The regulation of the Ras/Raf/MEK/ERK pathway by protein interactions. Biochem J 351:289-305, 2000
41. Hunter T: Protein kinases and phosphatases: The yin and yang of protein phosphorylation and signaling. Cell 80:225-236, 1995
42. Luzi L, Confalonieri S, Di Fiore PP, et al: Evolution of Shc functions from nematode to human. Curr Opin Genet Dev 10:668-674, 2000
43. Zheng CF, Guan KL: Cloning and characterization of two distinct human extracellular signal-regulated kinase activator kinases, MEK1 and MEK2. J Biol Chem 268:11435-11439, 1993
44. Wu J, Harrison JK, Dent P, et al: Identification and characterization of a new mammalian mitogen-activated protein kinase kinase, MKK2. Mol Cell Biol 13:4539-4548, 1993
45. Brott BK, Alessandrini A, Largaespada DA, et al: MEK2 is a kinase related to MEK1 and is differentially expressed in murine tissues. Cell Growth Diff 4:921-929, 1996
46. Hanks SK, Quinn AM: Protein kinase catalytic domain sequence database: Identification of conserved features of primary structure and classification of family members. Methods Enzymol 200:38-62, 1991
47. Dent P, Haser W, Haystead TA, et al: Activation of mitogen-activated protein kinase kinase by v-Raf in NIH 3T3 cells and in vitro. Science 257:1404-1407, 1992
48. Crews CM, Alessandrini A, Erikson RL: The primary structure of MEK, a protein kinase that phosphorylates the ERK gene product. Science 258:478-480, 1992
49. Her JH, Lakhani S, Zu K, et al: Dual phosphorylation and autophosphorylation in mitogen-activated protein (MAP) kinase activation. Biochem J 296:25-31, 1993
50. Wu J, Harrison JK, Vincent LA, et al: Molecular structure of a protein-tyrosine/threonine kinase activating p42 mitogen-activated protein (MAP) kinase: MAP kinase kinase. Proc Natl Acad Sci U S A 90:173-177, 1993
51. Seger R, Ahn NG, Posada J, et al: Purification and characterization of mitogen-activated protein kinase activator(s) from epidermal growth factor-stimulated A431 cells. J Biol Chem 267:14373-14381, 1992
52. Sivaraman VS, Wang H, Nuovo GJ, et al: Hyperexpression of mitogen-activated protein kinase in human breast cancer. J Clin Invest 99:1478-1483, 1997
53. Mandell JW, Hussaini IM, Zecevic M, et al: In situ visualization of intratumor growth factor signaling: Immunohistochemical localization of activated ERK/MAP kinase in glial neoplasms. Am J Pathol 153:1411-1423, 1998
54. Hoshino R, Chatani Y, Yamori T, et al: Constitutive activation of the 41-/43-kDa mitogen- activated protein kinase signaling pathway in human tumors. Oncogene 18:813-822, 1999
55. Johnson GL, Vaillancourt RR: Sequential protein kinase reactions controlling cell growth and differentiation. Curr Opin Cell Biol 6:230-238, 1994
56. Lazar DF, Wiese RJ, Brady MJ, et al: Mitogen-activated protein kinase kinase inhibition does not block the stimulation of glucose utilization by insulin. J Biol Chem 270:20801-20807, 1995
57. Boulton TG, Nye SH, Robbins DJ, et al: ERKs: A family of protein-serine/threonine kinases that are activated and tyrosine phosphorylated in response to insulin and NGF. Cell 65:663-675, 1991
58. Davis RJ: Signal transduction by the JNK group of MAP kinases. Cell 103:239-252, 2000
59. Zhang J, Zhang F, Ebert D, et al: Activity of the MAP kinase ERK2 is controlled by a flexible surface loop. Structure 3:299-307, 1995
60. Doza YN, Cuenda A, Thomas GM, et al: Activation of the MAP kinase homologue RK requires the phosphorylation of Thr-180 and Tyr-182 and both residues are phosphorylated in chemically stressed KB cells. FEBS Lett 364:223-228, 1995
61. Alessandrini A, Crews CM, Erikson RL: Phorbol ester stimulates a protein-tyrosine/threonine kinase that phosphorylates and activates the Erk-1 gene product. Proc Natl Acad Sci U S A 89:8200-8204, 1992
62. Cox S, Radzio-Andzelm E, Taylor SS: Domain movements in protein kinases. Curr Opin Struct Biol 4:893-901, 1994
63. Robbins DJ, Zhen E, Owaki H, et al: Regulation and properties of extracellular signal- regulated protein kinases 1 and 2 in vitro. J Biol Chem 268:5097-5106, 1993
64. Kyriakis JM, Avruch J: Mammalian mitogen-activated protein kinase signal transduction pathways activated by stress and inflammation. Physiol Rev 81:807-869, 2001
65. Waskiewicz AJ, Flynn A, Proud CG, et al: Mitogen-activated protein kinases activate the serine/threonine kinases MNK1 and MNK2. EMBO J 16:1909-1920, 1997
66. Janknecht R, Ernst WH, Pingoud V, et al: Activation of ternary complex factor Elk-1 by MAP kinases. EMBO J 12:5097-5104, 1993
67. Whitmarsh AJ, Davis RJ: Transcription factor AP-1 regulation by mitogen-activated protein kinase signal transduction pathways. J Mol Med 74:589-607, 1996
68. Hill CS, Treisman R: Transcriptional regulation by extracellular signals: Mechanisms and specificity. Cell 80:199-211, 1995
69. Gille H, Sharrocks AD, Shaw PE: Phosphorylation of transcription factor p62TCF by MAP kinase stimulates ternary complex formation at c-fos promoter. Nature 358:414-417, 1992
70. Kurokawa H, Lenferink AE, Simpson JF, et al: Inhibition of HER2/neu (erbB-2) and mitogen-activated protein kinases enhances tamoxifen action against HER2-ovorexpresessing tamoxifen-resistant breast cancer cells. Cancer Res 60:5887-5894, 2000
71. Timms JF, White SL, O'Hare MJ, et al: Effects of ErbB-2 overexpression on mitogenic signalling and cell cycle progression in human breast luminal epithelial cells. Oncogene 21:6573-6586, 2002
72. Bucci B, D'Agnano I, Botti C, et al: EGF-R expression in ductal breast cancer: Proliferation and prognostic implications. Anticancer Res 17:769-774, 1997
73. Zwick E, Bange J, Ullrich A: Receptor tyrosine kinases as targets for anticancer drugs. Trends Mol Med 8:17-23, 2002
74. Kim H, Muller WJ: The role of the epidermal growth factor receptor family in mammary tumorigenesis and metastasis. Exp Cell Res 253:78-87, 1999
75. Huang SM, Harari PM: Epidermal growth factor receptor inhibition in cancer therapy: Biology, rationale and preliminary clinical results. Invest New Drugs 17:259-269, 1999
76. Mansour SJ, Matten WT, Hermann AS, et al: Transformation of mammalian cells by constitutively active MAP kinase kinase. Science 265:966-970, 1994
77. Salh B, Maroota A, Matthewson C, et al: Investigation of the Mek-MAP kinase-Rsk pathway in human breast cancer. Anticancer Res 19:731-740, 1999
78. Maemura M, Iino Y, Koibuchi Y, et al: Mitogen-activated protein kinase cascade in breast cancer. Oncology 57:37-44, 1999 (suppl 2)
79. Hori M, Inagawa S, Shimazaki J, et al: Overexpression of mitogen-activated protein kinase superfamily proteins unrelated to Ras and AF-1 of estrogen receptor alpha mutation in advanced stage human breast cancer. Pathol Res Pract 196:817-826, 2000
80. Mueller H, Flury N, Eppenberger-Castori S, et al: Potential prognostic value of mitogen- activated protein kinase activity for disease-free survival of primary breast cancer patients. Int J Cancer 89:384-388, 2000
81. Santen RJ, Song RX, McPherson R, et al: The role of mitogen-activated protein (MAP) kinase in breast cancer. J Steroid Biochem Mol Biol 80:239-256, 2002
82. Das R, Vonderhaar BK: Activation of raf-1, MEK, and MAP kinase in prolactin responsive mammary cells. Breast Cancer Res Treat 40:141-149, 1996
83. Janes PW, Daly RJ, deFazio A, et al: Activation of the Ras signalling pathway in human breast cancer cells overexpressing erbB-2. Oncogene 9:3601-3608, 1994
84. Fiddes RJ, Janes PW, Sivertsen SP, et al: Inhibition of the MAP kinase cascade blocks heregulin-induced cell cycle progression in T-47D human breast cancer cells. Oncogene 16:2803-2813, 1998
85. Kannan S, De Santis M, Lohmeyer M, et al: Cripto enhances the tyrosine phosphorylation of Shc and activates mitogen-activated protein kinase (MAPK) in mammary epithelial cells. J Biol Chem 272:3330-3335, 1997
86. von Lintig FC, Dreilinger AD, Varki NM, et al: Ras activation in human breast cancer. Breast Cancer Res Treat 62:51-62, 2000
87. Kato S, Endoh H, Masuhiro Y, et al: Activation of the estrogen receptor through phosphorylation by mitogen-activated protein kinase. Science 270:1491-1494, 1995
88. Donovan JC, Milic A, Slingerland JM: Constitutive MEK/MAPK activation leads to p27(Kip1) deregulation and antiestrogen resistance in human breast cancer cells. J Biol Chem 276:40888-40895, 2001
89. Coutts AS, Murphy LC: Elevated mitogen-activated protein kinase activity in estrogen- nonresponsive human breast cancer cells. Cancer Res 58:4071-4074, 1998
90. El-Ashry D, Miller DL, Kharbanda S, et al: Constitutive Raf-1 kinase activity in breast cancer cells induces both estrogen-independent growth and apoptosis. Oncogene 15:423-435, 1997
91. Cohen P: The development and therapeutic potential of protein kinase inhibitors. Curr Opin Chem Biol 3:459-465, 1999
92. Wilhelm S, Chien DJ: BAY 43-9006: Preclinical data. Curr Pharm Des 8:2255-2257, 2002
93. Strumberg D, Voliotis D, Moeller JG, et al: Results of phase I pharmacokinetic and pharmacodynamic studies of the Raf kinase inhibitor BAY 43-9006 in patients with solid tumors. Int J Clin Pharm Ther 40:580-581, 2002
94. Sebolt Leopold JS, Dudley DT, Herrera R, et al: Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo. Nat Med 5:810-816, 1999
95. Mitchell DY, Reid JM, Parchment RE, et al: Pharmacokinetics (PK) and pharmacodynamics (PD) of the oral MEK inhibitor, CI-1040, following multiple dose administration to patients with advanced cancer. Proc Am Soc Clin Oncol 21:81, 2002 (abstr 320)
96. Delaney AM, Printen JA, Chen H, et al: Identification of a novel mitogen-activated protein kinase kinase activation domain recognized by the inhibitor PD 184352. Mol Cell Biol 22:7593-7602, 2002
97. Milella M, Kornblau SM, Estrov Z, et al: Therapeutic targeting of the MEK/MAPK signal transduction module in acute myeloid leukemia. J Clin Invest 108:851-859, 2001
98. Herrera R, Sebolt-Leopold JS: Unraveling the complexities of the Raf/MAP kinase pathway for pharmacological intervention. Trends Mol Med 8:S27-S31[erratum appears in Trends Mol Med 8:243, 2002], 2002 (suppl 4)
99. Herrera R, Sebolt-Leopold JS: Unraveling the complexities of the Raf/MAP kinase pathway for pharmacological intervention. Trends Mol Med 8:S27-S31[erratum appears in Trends Mol Med 8:243, 2002], 2002 (suppl 4)
100. Burton A: What went wrong with Iressa? Lancet Oncol 3:708, 2002