메뉴 건너뛰기




Volumn 4, Issue 9, 2009, Pages

Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT

Author keywords

[No Author keywords available]

Indexed keywords

AB 1010; ABELSON KINASE; FIBROBLAST GROWTH FACTOR RECEPTOR 1; FIBROBLAST GROWTH FACTOR RECEPTOR 3; IMATINIB; MASITINIB; PLACEBO; PLATELET DERIVED GROWTH FACTOR RECEPTOR; PROTEIN KINASE LYN; PROTEIN SERINE THREONINE KINASE; PROTEIN TYROSINE KINASE; PROTEIN TYROSINE KINASE INHIBITOR; STEM CELL FACTOR RECEPTOR; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG; PROTEIN KINASE INHIBITOR; RECOMBINANT PROTEIN; THIAZOLE DERIVATIVE;

EID: 70349658639     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0007258     Document Type: Article
Times cited : (347)

References (37)
  • 1
    • 25844507795 scopus 로고    scopus 로고
    • Signaling by Kit protein-tyrosine kinase - the stem cell factor receptor
    • Roskoski R Jr (2005) Signaling by Kit protein-tyrosine kinase - the stem cell factor receptor. Biochem Biophys Res Commun 337: 1-13.
    • (2005) Biochem Biophys Res Commun , vol.337 , pp. 1-13
    • Roskoski Jr, R.1
  • 2
    • 0030846533 scopus 로고    scopus 로고
    • Stem cell factor and hematopoiesis
    • Broudy VC (1997) Stem cell factor and hematopoiesis. Blood 90: 1345-64.
    • (1997) Blood , vol.90 , pp. 1345-1364
    • Broudy, V.C.1
  • 3
    • 33644752698 scopus 로고    scopus 로고
    • Stem cell factor and its receptor c-Kit as targets for inflammatory diseases
    • Reber L, Da Silva CA, Frossard N (2006) Stem cell factor and its receptor c-Kit as targets for inflammatory diseases. Eur J Pharmacol 533: 327-40.
    • (2006) Eur J Pharmacol , vol.533 , pp. 327-340
    • Reber, L.1    Da Silva, C.A.2    Frossard, N.3
  • 4
    • 41549085995 scopus 로고    scopus 로고
    • Kit mutations in cancer and their treatment with protein kinase inhibitors
    • Tests U (2008) Kit mutations in cancer and their treatment with protein kinase inhibitors. Drugs Fut 33: 161-174.
    • (2008) Drugs Fut , vol.33 , pp. 161-174
    • Tests, U.1
  • 5
    • 12144278434 scopus 로고    scopus 로고
    • Normal and Oncogenic Forms of the Receptor Tyrosine Kinase Kit
    • Lennarttson J, Jelacic T, Linnekin D, Shivakrupa R (2005) Normal and Oncogenic Forms of the Receptor Tyrosine Kinase Kit. Stem Cells 23: 16-43.
    • (2005) Stem Cells , vol.23 , pp. 16-43
    • Lennarttson, J.1    Jelacic, T.2    Linnekin, D.3    Shivakrupa, R.4
  • 6
    • 34250024319 scopus 로고    scopus 로고
    • Recent advances in the understanding of mastocytosis: The role of KIT mutations
    • Orfao A, Garcia-Montero AC, Sanchez L, Escribano L (2007) Recent advances in the understanding of mastocytosis: the role of KIT mutations. Br J Haematol 138: 12-30.
    • (2007) Br J Haematol , vol.138 , pp. 12-30
    • Orfao, A.1    Garcia-Montero, A.C.2    Sanchez, L.3    Escribano, L.4
  • 7
    • 27544479318 scopus 로고    scopus 로고
    • Role of tyrosine kinase inhibitors in cancer therapy
    • Arora A, Scholar EM (2005) Role of tyrosine kinase inhibitors in cancer therapy. J Pharmacol Exp Ther 315: 971-9.
    • (2005) J Pharmacol Exp Ther , vol.315 , pp. 971-979
    • Arora, A.1    Scholar, E.M.2
  • 8
    • 0028968622 scopus 로고
    • Selective inhibition of the platelet-derived growth factor signal transduction pathway by a protein-tyrosine kinase inhibitor of the 2-phenylaminopyrimidine class
    • Buchdunger E, Zimmermann J, Mett H, Meyer T, Muller M, et al. (1995) Selective inhibition of the platelet-derived growth factor signal transduction pathway by a protein-tyrosine kinase inhibitor of the 2-phenylaminopyrimidine class. Proc Natl Acad Sci USA 92: 2558-62.
    • (1995) Proc Natl Acad Sci USA , vol.92 , pp. 2558-2562
    • Buchdunger, E.1    Zimmermann, J.2    Mett, H.3    Meyer, T.4    Muller, M.5
  • 9
    • 0030031766 scopus 로고    scopus 로고
    • Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative
    • Buchdunger E, Zimmermann J, Mett H, Meyer T, Muller M, et al. (1996) Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative. Cancer Res 56: 100-4.
    • (1996) Cancer Res , vol.56 , pp. 100-104
    • Buchdunger, E.1    Zimmermann, J.2    Mett, H.3    Meyer, T.4    Muller, M.5
  • 10
    • 17044403497 scopus 로고    scopus 로고
    • Macrophage colony-stimulating factor receptor c-fms is a novel target of imatinib
    • Dewar AL, Cambareri AC, Zannettino AC, Miller BL, Doherty KV, et al. (2005) Macrophage colony-stimulating factor receptor c-fms is a novel target of imatinib. Blood 105: 3127-32.
    • (2005) Blood , vol.105 , pp. 3127-3132
    • Dewar, A.L.1    Cambareri, A.C.2    Zannettino, A.C.3    Miller, B.L.4    Doherty, K.V.5
  • 11
    • 19944429284 scopus 로고    scopus 로고
    • A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase
    • Atwell S, Adams JM, Badger J, Buchanan MD, Feil IK, et al. (2004) A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase. J Biol Chem 279: 55827-32.
    • (2004) J Biol Chem , vol.279 , pp. 55827-55832
    • Atwell, S.1    Adams, J.M.2    Badger, J.3    Buchanan, M.D.4    Feil, I.K.5
  • 12
    • 33748861663 scopus 로고    scopus 로고
    • Mechanisms of resistance to small molecule kinase inhibition in the treatment of solid tumours
    • Rubin BP, Duensing A (2006) Mechanisms of resistance to small molecule kinase inhibition in the treatment of solid tumours. Lab Invest 86: 981-6.
    • (2006) Lab Invest , vol.86 , pp. 981-986
    • Rubin, B.P.1    Duensing, A.2
  • 13
    • 0036493872 scopus 로고    scopus 로고
    • The c-KIT mutation causing human mastocytosis is resistant to STI571 and other KIT kinase inhibitors; kinases with enzymatic site mutations show different inhibitor sensitivity profiles than wild-type kinases and those with regulatory-type mutations
    • Ma Y, Zeng S, Metcalfe DD, Akin C, Dimitrijevic S, et al. (2002) The c-KIT mutation causing human mastocytosis is resistant to STI571 and other KIT kinase inhibitors; kinases with enzymatic site mutations show different inhibitor sensitivity profiles than wild-type kinases and those with regulatory-type mutations. Blood 99: 1741-4.
    • (2002) Blood , vol.99 , pp. 1741-1744
    • Ma, Y.1    Zeng, S.2    Metcalfe, D.D.3    Akin, C.4    Dimitrijevic, S.5
  • 14
    • 18544398712 scopus 로고    scopus 로고
    • Constitutive activation of c-kit by the juxtamembrane but not the catalytic domain mutations is inhibited selectively by tyrosine kinase inhibitors STI571 and AG1296
    • Ueda S, Ikeda H, Mizuki M, Ishiko J, Matsumura I, et al. (2002) Constitutive activation of c-kit by the juxtamembrane but not the catalytic domain mutations is inhibited selectively by tyrosine kinase inhibitors STI571 and AG1296. Int J Hematol 76: 427-35.
    • (2002) Int J Hematol , vol.76 , pp. 427-435
    • Ueda, S.1    Ikeda, H.2    Mizuki, M.3    Ishiko, J.4    Matsumura, I.5
  • 15
    • 33746845181 scopus 로고    scopus 로고
    • Cardiotoxicity of the cancer therapeutic agent imatinib mesylate
    • Kerkela R, Grazette L, Yacobi R, Iliescu C, Patten R, et al. (2006) Cardiotoxicity of the cancer therapeutic agent imatinib mesylate. Nat Med 12: 908-16.
    • (2006) Nat Med , vol.12 , pp. 908-916
    • Kerkela, R.1    Grazette, L.2    Yacobi, R.3    Iliescu, C.4    Patten, R.5
  • 16
    • 36849056267 scopus 로고    scopus 로고
    • An anticancer C-Kit kinase inhibitor is reengineered to make it more active and less cardiotoxic
    • Fernandez A, Sanguino A, Peng Z, Ozturk E, Chen J, et al. (2007) An anticancer C-Kit kinase inhibitor is reengineered to make it more active and less cardiotoxic. J Clin Invest 117: 4044-54.
    • (2007) J Clin Invest , vol.117 , pp. 4044-4054
    • Fernandez, A.1    Sanguino, A.2    Peng, Z.3    Ozturk, E.4    Chen, J.5
  • 17
    • 0028959163 scopus 로고
    • Constitutively activating mutations of c-kit receptor tyrosine kinase confer factor-independent growth and tumourigenicity of factor-dependent hematopoietic cell lines
    • Kitayama H, Kanakura Y, Furitsu T, Tsujimura T, Oritani K, et al. (1995) Constitutively activating mutations of c-kit receptor tyrosine kinase confer factor-independent growth and tumourigenicity of factor-dependent hematopoietic cell lines. Blood 85: 790-8.
    • (1995) Blood , vol.85 , pp. 790-798
    • Kitayama, H.1    Kanakura, Y.2    Furitsu, T.3    Tsujimura, T.4    Oritani, K.5
  • 18
    • 0026584159 scopus 로고
    • The c-kit receptor ligand functions as a mast cell chemoattractant
    • Meininger CJ, Yano H, Rottapel R, Bernstein A, Zsebo KM, et al. (1992) The c-kit receptor ligand functions as a mast cell chemoattractant. Blood 79: 958-63.
    • (1992) Blood , vol.79 , pp. 958-963
    • Meininger, C.J.1    Yano, H.2    Rottapel, R.3    Bernstein, A.4    Zsebo, K.M.5
  • 19
    • 0042090223 scopus 로고    scopus 로고
    • Signal transduction by several KIT juxtamembrane domain mutations
    • Casteran N, De Sepulveda P, Beslu N, Aoubala M, Letard S, et al. (2003) Signal transduction by several KIT juxtamembrane domain mutations. Oncogene 22: 4710-22.
    • (2003) Oncogene , vol.22 , pp. 4710-4722
    • Casteran, N.1    De Sepulveda, P.2    Beslu, N.3    Aoubala, M.4    Letard, S.5
  • 20
    • 0030032943 scopus 로고    scopus 로고
    • Constitutive activation of c-kit in FMA3 murine mastocytoma cells caused by deletion of seven amino acids at the juxtamembrane domain
    • Tsujimura T, Morimoto M, Hashimoto K, Moriyama Y, Kitayama H, et al. (1996) Constitutive activation of c-kit in FMA3 murine mastocytoma cells caused by deletion of seven amino acids at the juxtamembrane domain. Blood 87: 273-83.
    • (1996) Blood , vol.87 , pp. 273-283
    • Tsujimura, T.1    Morimoto, M.2    Hashimoto, K.3    Moriyama, Y.4    Kitayama, H.5
  • 22
    • 0036682301 scopus 로고    scopus 로고
    • Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571)
    • Nagar B, Bornmann WG, Pellicena P, Schindler T, Veach DR, et al. (2002) Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571). Cancer Res 62: 4236-43.
    • (2002) Cancer Res , vol.62 , pp. 4236-4243
    • Nagar, B.1    Bornmann, W.G.2    Pellicena, P.3    Schindler, T.4    Veach, D.R.5
  • 23
    • 2942542387 scopus 로고    scopus 로고
    • Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase
    • Mol CD, Dougan DR, Schneider TR, Skene RJ, Kraus ML, et al. (2004) Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase. J Biol Chem 279: 31655-63.
    • (2004) J Biol Chem , vol.279 , pp. 31655-31663
    • Mol, C.D.1    Dougan, D.R.2    Schneider, T.R.3    Skene, R.J.4    Kraus, M.L.5
  • 24
    • 4944249117 scopus 로고    scopus 로고
    • BAY 43-9006 exhibits broad spectrum oral antitumour activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumour progression and angiogenesis
    • Wilhelm SM, Carter C, Tang L, Wilkie D, McNabola A, et al. (2004) BAY 43-9006 exhibits broad spectrum oral antitumour activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumour progression and angiogenesis. Cancer Res 64: 7099-109.
    • (2004) Cancer Res , vol.64 , pp. 7099-7109
    • Wilhelm, S.M.1    Carter, C.2    Tang, L.3    Wilkie, D.4    McNabola, A.5
  • 25
    • 12244301581 scopus 로고    scopus 로고
    • In vivo antitumour activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: Determination of a pharmacokinetic/pharmacodynamic relationship
    • Mendel DB, Laird AD, Xin X, Louie SG, Christensen JG, et al. (2003) In vivo antitumour activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res 9: 327-37.
    • (2003) Clin Cancer Res , vol.9 , pp. 327-337
    • Mendel, D.B.1    Laird, A.D.2    Xin, X.3    Louie, S.G.4    Christensen, J.G.5
  • 27
    • 70349677227 scopus 로고    scopus 로고
    • Imatinib new drug application #21-335 Gleevec Pharmacology Review http://www.fda.gov/cder/foi/nda/2001/21-335_Gleevec_pharmr_P1.pdf.
    • Imatinib new drug application #21-335 Gleevec Pharmacology Review http://www.fda.gov/cder/foi/nda/2001/21-335_Gleevec_pharmr_P1.pdf.
  • 28
    • 0344987886 scopus 로고    scopus 로고
    • Effect of tyrosine kinase inhibitor STI571 on the kinase activity of wild-type and various mutated c-kit receptors found in mast cell neoplasms
    • Zermati Y, De Sepulveda P, Feger F, Letard S, Kersual J, et al. (2003) Effect of tyrosine kinase inhibitor STI571 on the kinase activity of wild-type and various mutated c-kit receptors found in mast cell neoplasms. Oncogene 22: 660-4.
    • (2003) Oncogene , vol.22 , pp. 660-664
    • Zermati, Y.1    De Sepulveda, P.2    Feger, F.3    Letard, S.4    Kersual, J.5
  • 29
    • 0038731316 scopus 로고    scopus 로고
    • Juxtamembrane mutant V560GKit is more sensitive to Imatinib (STI571) compared with wild-type c-kit whereas the kinase domain mutant D816VKit is resistant
    • Frost MJ, Ferrao PT, Hughes TP, Ashman LK (2002) Juxtamembrane mutant V560GKit is more sensitive to Imatinib (STI571) compared with wild-type c-kit whereas the kinase domain mutant D816VKit is resistant. Mol Cancer Ther 1: 1115-24.
    • (2002) Mol Cancer Ther , vol.1 , pp. 1115-1124
    • Frost, M.J.1    Ferrao, P.T.2    Hughes, T.P.3    Ashman, L.K.4
  • 30
    • 0344987881 scopus 로고    scopus 로고
    • A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome
    • Cools J, DeAngelo DJ, Gotlib J, Stover EH, Legare RD, et al. (2003) A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome. N Engl J Med 348: 1201-14.
    • (2003) N Engl J Med , vol.348 , pp. 1201-1214
    • Cools, J.1    DeAngelo, D.J.2    Gotlib, J.3    Stover, E.H.4    Legare, R.D.5
  • 31
    • 57149112342 scopus 로고    scopus 로고
    • Masitinib is Safe and Effective for the Treatment of Canine Mast Cell Tumors
    • Hahn KA, Oglivie G, Rusk T, Devauchelle P, Leblanc A, et al. (2008) Masitinib is Safe and Effective for the Treatment of Canine Mast Cell Tumors. J Vet Intern Med 22: 1301-1309.
    • (2008) J Vet Intern Med , vol.22 , pp. 1301-1309
    • Hahn, K.A.1    Oglivie, G.2    Rusk, T.3    Devauchelle, P.4    Leblanc, A.5
  • 34
    • 0020660264 scopus 로고
    • IgE mediated release of leukotriene C4, chondroitin sulfate E proteoglycan, beta-hexosaminidase, and histamine from cultured bone marrow-derived mouse mast cells
    • Razin E, Mencia-Huerta JM, Stevens RL, Lewis RA, Liu FT, et al. (1983) IgE mediated release of leukotriene C4, chondroitin sulfate E proteoglycan, beta-hexosaminidase, and histamine from cultured bone marrow-derived mouse mast cells. J Exp Med 157: 189-201.
    • (1983) J Exp Med , vol.157 , pp. 189-201
    • Razin, E.1    Mencia-Huerta, J.M.2    Stevens, R.L.3    Lewis, R.A.4    Liu, F.T.5
  • 35
    • 0032507962 scopus 로고    scopus 로고
    • Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development
    • Zou YR, Kottmann AH, Kuroda M, Taniuchi I, Littman DR (1998) Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development. Nature 393: 595-9.
    • (1998) Nature , vol.393 , pp. 595-599
    • Zou, Y.R.1    Kottmann, A.H.2    Kuroda, M.3    Taniuchi, I.4    Littman, D.R.5
  • 36
    • 0037763817 scopus 로고    scopus 로고
    • Comparative evaluation of 11 scoring functions for molecular docking
    • Wang R, Lu Y, Wang S (2003) Comparative evaluation of 11 scoring functions for molecular docking. J Med Chem 46: 2287-303.
    • (2003) J Med Chem , vol.46 , pp. 2287-2303
    • Wang, R.1    Lu, Y.2    Wang, S.3
  • 37
    • 70349655145 scopus 로고    scopus 로고
    • Circulaire ministérielle du 16 avril 1996 relative aux expérimentations confinées d'organismes génétiquement modifiés à des fins de recherche, développement ou d'enseignement. Journal Officiel du 2 juin 1996, pp.8167.
    • Circulaire ministérielle du 16 avril 1996 relative aux expérimentations confinées d'organismes génétiquement modifiés à des fins de recherche, développement ou d'enseignement. Journal Officiel du 2 juin 1996, pp.8167.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.