Abstract
The hallmark of chronic myelogenous leukemia (CML) is the expression of Bcr-Abl, a constitutivelyactive form of the Abl tyrosine kinase. Imatinib, a 2-phenyl aminopyrimidine Bcr-Abl inhibitor developedby Novartis and marketed under the tradename of Gleevec (Glivec), is highly effective in treating CML patientswith early stage disease. However, patients with advanced disease often become resistant to imatinib. Thepredominant form of this resistance is the development of mutations in the Bcr-Abl protein. These pointmutations can be amino acid residues that make direct contact with imatinib or residues that do not allowBcr-Abl to adopt the inactive conformation. Since imatinib can only bind to the inactive conformation ofthe protein, both types of mutations prevent this inhibitor from binding. Several approaches have beentaken to identify additional Bcr-Abl inhibitors including: (1) more potent analogs of imatinib; (2) non-ATPcompetitive inhibitors of Bcr-Abl; and (3) dual inhibitors of both Bcr-Abl and members of the Src familyof kinases (SFKs) that bind to the active form of Bcr-Abl. The progress made on the development of thesenew agents, including compounds with activity against the highly resistant T315I mutation of Bcr-Abl, willbe discussed.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
Abbreviations
- CML:
-
chronic myelogenous leukemia
- ALL:
-
acute lymphoblastic leukemia
- SFK:
-
Src family kinase
- GST:
-
gastrointestinal stromal tumors
- ASH:
-
American Society of Hematology
- AACR:
-
American Association for Cancer Research
- ASCO:
-
American Society of Clinical Oncology
References
Goldman JM, Melo JV (2003) N Eng J Med 349:1451
Thijsen SFT, Schuurhuis GJ, Van Oostveen JW, Ossenkoppele GJ (1999) Leukemia 13:1646
Kalidas M, Kantarjian H, Talpaz M (2001) JAMA 286:895
Goldman JM, Druker BJ (2001) Blood 98:2039
Salesse S, Verfaillie CM (2002) Oncogene 21:8547
Faderl S, Talpaz M, Estrov Z, O'Brien S, Kurzrock R, Kantarjian HM (1999) N Engl J Med 341:164
Ribeiro R, Abromowitch M, Raimondi S, Murphy S, Behm F, Williams D (1987) Blood 70:948
Bloomfield C, Goldman A, Alimena G, Berger R, Borgstrom G, Brandt L, Catovsky D, de la Chapelle A, Dewald G, Garson (1986) Blood 67:415
Westbrook C, Hooberman A, Spino C, Dodge R, Larson R, Davey F, Wurster-Hill D, Sobol R, Schiffer C, Bloomfield C (1992) Blood 80:2983
Faderl S, Jeha S, M. KH (2003) Cancer 98:1337
Buchdunger E, Zimmermann J, Mett H, Meyer T, Mueller M, Druker BJ, Lydon NB (1996) Cancer Res 56:100
Zimmermann J, Buchdunger E, Mett H, Meyer T, Lydon NB (1997) Bioorg Med Chem Lett 7:187
Buchdunger E, Cioffi CL, Law N, Stover D, Ohno-Jones S, Druker BJ, Lydon NB (2000) J Pharmacol Exp Ther 295:139
Boggon TJ, Eck MJ (2004) Oncogene 23:7918
Superti-Furga G, Courtneidge SA (1995) BioEssays 17:321
Druker BJ, Tamura S, Buchdunger E, Ohno S, Segal GM, Fanning S, Zimmermann J, Lydon NB (1996) Nat Med 2:561
Carroll M, Ohno-Jones S, Tamura S, Buchdunger E, Zimmermann J, Lydon NB, Gilliland DG, Druker BJ (1997) Blood 90:4947
Gambacorti-Passerini C, Le Coutre P, Mologni L, Fanelli M, Bertazzoli C, Marchesi E, Di Nicola M, Biondi A, Corneo GM, Belotti D, Pogliani E, Lydon NB (1997) Blood Cells Mol Dis 23:380
Deininger MWN, Goldman JM, Lydon N, Melo JV (1997) Blood 90:3691
Le Coutre P, Mologni L, Cleris L, Marchesi E, Buchdunger E, Giardini R, Formelli F, Gambacorti-Passerini C (1999) J Natl Cancer Inst 91:163
Druker BJ, Talpaz M, Resta DJ, Peng B, Buchdunger E, Ford JM, Lydon NB, Kantarjian H, Capdeville R, Ohno-Jones S, Sawyers CL (2001) N Engl J Med 344:1031
Druker BJ, Sawyers CL, Kantarjian H, Resta DJ, Reese SF, Ford JM, Capdeville R, Talpaz M (2001) N Engl J Med 344:1038
Lydon NB, Druker BJ (2004) Leukemia Res 28:S29
Cowan-Jacob SW, Guez V, Fendrich G, Griffin JD, Fabbro D, Furet P, Liebetanz J, Mestan J, Manley PW (2004) Mini-Reviews Med Chem 4:285
Crossman LC, O'Brien S (2004) Leukemia Res 28:S3
Deininger M, Buchdunger E, Druker BJ (2005) Blood 105:2640
Capdeville R, Buchdunger E, Zimmermann J, Matter A (2002) Nat Rev Drug Disc 1:493
Vasella D, Slater R (2003) Magic Cancer Bullet. Harper Business, New York
Tuveson DA, Willis NA, Jacks T, Griffin JD, Singer S, Fletcher CDM, Fletcher JA, Demetri GD (2001) Oncogene 20:5054
Demetri GD, von Mehren M, Blanke CD, Van den Abbeele AD, Eisenberg B, Roberts PJ, Heinrich MC, Tuveson DA, Singer S, Janicek M, Fletcher JA, Silverman SG, Silberman SL, Capdeville R, Kiese B, Peng B, Dimitrijevic S, Druker BJ, Corless C, Fletcher CD, Joensuu H (2002) N Engl J Med 347:472
Wiedmann MW, Caca K (2005) Curr Cancer Drug Targets 5:171
Gorre ME, Mohammed M, Ellwood K, Hsu N, Paquette R, Rao PN, Sawyers CL (2001) Science 293:876
Shah N, Sawyers CL (2003) Oncogene 22:7389
Corbin AS, La Rosee P, Stoffregen EP, Druker BJ, Deininger MW (2003) Blood 101:4611
von Bubnoff N, Peschel C, Duyster J (2003) Leukemia 17:829
Schindler T, Bornmann W, Pellicena P, Miller WT, Clarkson B, Kuriyan J (2000) Science 289:1938
Nagar B, Bornmann WG, Pellicena P, Schindler T, Veach DR, Miller WT, Clarkson B, Kuriyan J (2002) Cancer Res 62:4236
Manley PW, Breitenstein W, Brueggen J, Cowan-Jacob SW, Furet P, Mestan J, Meyer T (2004) Bioorg Med Chem Lett 14:5793
Mestan J, Ellen W, Sandra C-J, Doriano F, Pascal F, Gabriele F, Gerard G, Dominique K, Markus G, James GD, Manley PW (2004) Annu Meeting Am Soc Hematol, Abstract 1978
Weisberg E, Manley PW, Breitenstein W, Brueggen J, Cowan-Jacob SW, Ray A, Huntly B, Fabbro D, Fendrich G, Hall-Meyers E, Kung AL, Mestan J, Daley GQ, Callahan L, Catley L, Cavazza C, Mohammed A, Neuberg D, Wright RD, Gilliland DG, Griffin JD (2005) Cancer Cell 7:129
Manley P, Cowan-Jacob SW, Fendrich G, Mestan J (2005) Annu Meeting Am Soc Hematol, Abstract 3365
Golemovic M, Verstovsek S, Giles F, Cortes J, Manshouri T, Manley PW, Mestan J, Dugan M, Alland L, Griffin JD, Arlinghaus RB, Sun T, Kantarjian H, Beran M (2005) Clin Cancer Res 11:4941
Martinelli G, Martelli AM, Grafone T, Mantovani I, Cappellini A, Tazzari PL, Ottaviani E, Soverini S, Amabile M, Renzulli M, Terragna C, Colarossi S, Iacobucci I, Poerio A, Baccarani M (2005) Annu Meeting Am Soc Hematol, Abstract 2004
Martinelli G, Martelli AM, Grafone T, Rosti G, Mantovani I, Cappellini A, Tazzari PL, Ottaviani E, Renzulli M, Amabile M, Poerio A, Soverini S, Terragna C, Taccioli C, Bassi S, Baccarani M (2004) Annu Meeting Am Soc Hematol, Abstract 4687
Ma G, Lu D, Wu Y, Liu J, Arlinghaus RB (1997) Oncogene 14:2367
Van Etten RA (2004) Leukemia Res 28:S21
Ottmann OG, Druker BJ, Sawyers CL, Goldman JM, Reiffers J, Silver RT, Tura S, Fischer T, Deininger MW, Schiffer CA, Baccarani M, Gratwohl A, Hochhaus A, Hoelzer D, Fernandes-Reese S, Gathmann I, Capdeville R, O'Brien SG (2002) Blood 100:1965
Verstovsek S, Golemovic M, Kantarjian H, Manshouri T, Estrov Z, Manley P, Sun T, Arlinghaus RB, Alland L, Dugan M, Cortes J, Giles F, Beran M (2005) Cancer 104:1230
Giles F, Kantarjian H, Wassmann B, Cortes J, O'Brien S, Tanaka C, Rae P, Mietlowski W, Romano A, Alland L, Dugan M, Albitar M, Ottmann O (2004) Annu Meeting Am Soc Hematol, Abstract 22
Ottman O, Giles F, Wassman B, Hochhaus A, Rae P, Beran M, Albitar M, Dugan M, Kantarjian H (2005) Annu Meeting Am Soc Clin Oncol, Abstract 3015
Kantarjian H, Ottman O, Cortes J, Wassman B, Hochhaus A, Alland L, Dugan M, Albitar M, Giles F (2005) Annu Meeting Am Soc Clin Oncol, Abstract 3014A
Giles F, Ottman O, Cortes J, Wassman B, Wunderle S, O'Brien S, Jones D, Hochhaus A, Verstovsek S, Rae P, Rose K, Alland L, Dugan M, Manley P, Beran M, Albitar M, Kantarjian H (2005) Annu Meeting Am Assoc Cancer Res, Abstract 3971
Kantarjian H, M., Ottman O, Cortes J, Wassman M, Wunderle S, Bhalla K, Jones D, Hochhaus A, Rae P, Alland L, Dugan M, Albitar M, Giles F (2005) Annu Meeting Am Soc Hematol, Abstract 37
La Rosee P, Holm-Eriksen S, Ernst T, Konig H, Erben P, Mueller M, Schenk Y, Emig M, Binckebanck A, Wunderle S, Alland L, Schuld P, Hehlmann R, Ottman OG, Hochhaus A (2005) Annu Meeting Am Soc Hematol, Abstract 497
Von Bubnoff N, Veach DR, Van der Kuip H, Aulitzky WE, Saenger J, Seipel P, Bornmann WG, Peschel C, Clarkson B, Duyster J (2005) Blood 105:1652
von Bubnoff N, Saenger J, Manley PW, Mestan J, Peschel C, Duyster J (2005) Annu Meeting Am Soc Hematol, Abstract 1983
Ray A, Cowan-Jacob S, Manley PW, Mestan J, Griffin JD (2005) Annu Meeting Am Soc Hematol, Abstract 494
Kimura S, Naito H, Segawa H, Kuroda J, Yuasa T, Sato K, Yokota A, Kamitsuji Y, Kawata E, Ashihara E, Nakaya Y, Naruoka H, Wakayama T, Nasu K, Asaki T, Niwa T, Hirabayashi K, Maekawa T (2005) Blood 106:3948
Naito H, Kimura S, Nakaya Y, Naruoka H, Wakayama T, Kimura S, Ito S, Ashihara E, Maekawa T, Hirabayashi K (2005) Annu Meeting Am Soc Hematol, Abstract 1518
Asaki T, Sugiyama Y, Hamamoto T, Higashioka M, Umehara M, Naito H, Niwa T (2006) Bioorg Med Chem Lett 16:1421
Gumireddy K, Baker SJ, Cosenza SC, John P, Kang AD, Robell KA, Reddy MVR, Reddy EP (2005) Proc Natl Acad Sci USA 102:1992
http://www.onconova.com , (Last visited on: Jan 05, 2006)
Gumireddy K, Reddy MVR, Cosenza SC, Nathan RB, Baker SJ, Papathi N, Jiang J, Holland J, Reddy EP (2005) Cancer Cell 7:275
Kaur G, Gazit A, Levitzki A, Stowe E, Cooney DA, Sausville EA (1994) Anti-Cancer Drug 5:213
Kaur G, Narayanan VL, Risbood PA, Hollingshead MG, Stinson SF, Varma RK, Sausville EA (2005) Bioorg Med Chem 13:1749
Svingen PA, Tefferi A, Kottke TJ, Kaur G, Narayanan VL, Sausville EA, Kaufmann SH (2000) Clin Cancer Res 6:237
Mow BMF, Chandra J, Svingen PA, Hallgren CG, Weisberg E, Kottke TJ, Narayanan VL, Litzow MR, Griffin JD, Sausville EA, Tefferi A, Kaufmann SH (2002) Blood 99:664
Avramis IA, Laug WE, Sausville EA, Avramis VI (2003) Cancer Chemother Pharmacol 52:307
Deutsch E, Maggiorella L, Wen B, Bonnet ML, Khanfir K, Frascogna V, Turhan AG, Bourhis J (2004) Br J Cancer 91:1735
Camirand A, Zakikhani M, Young F, Pollak M (2005) Breast Cancer Res 7:R465
Blum G, Gazit A, Levitzki A (2000) Biochemistry 39:15705
Camirand A, Pollak M (2004) Br J Cancer 90:1825
Dorsey JF, Jove R, Kraker AJ, Wu J (2000) Cancer Res 60:3127
Wisniewski D, Lambek CL, Liu C, Strife A, Veach DR, Nagar B, Young MA, Schindler T, Bornmann WG, Bertino JR, Kuriyan J, Clarkson B (2002) Cancer Res 62:4244
Courtneidge SA (2002) Biochem Soc Trans 30:11
Ito H, Gardner-Thorpe J, Zinner MJ, Ashley SW, Whang EE (2003) Surgery 134:221
Wiener JR, Windham TC, Estrella VC, Parikh NU, Thall PF, Deavers MT, Bast RC, Mills GB, Gallick GE (2003) Gynecol Oncol 88:73
Myoui A, Nishimura R, Williams PJ, Hiraga T, Tamura D, Michigami T, Mundy GR, Yoneda T (2003) Cancer Res 63:5028
Danhauser-Riedl S, Warmuth M, Druker BJ, Emmerich B, Hallek M (1996) Cancer Res 56:3589
Warmuth M, Bergmann M, Priess A, Hauslmann K, Emmerich B, Hallek M (1997) J Biol Chem 272:33260
Roginskaya V, Zuo S, Caudell E, Nambudiri G, Kraker AJ, Corey SJ (1999) Leukemia 13:855
Lionberger JM, Wilson MB, Smithgall TE (2000) J Biol Chem 275:18581
Donato NJ, Wu JY, Stapley J, Gallick G, Lin H, Arlinghaus R, Talpaz M (2003) Blood 101:690
Klutchko SR, Hamby JM, Boschelli DH, Wu Z, Kraker AJ, Amar AM, Hartl BG, Shen C, Klohs WD, Steinkampf RW, Driscoll DL, Nelson JM, Elliott WL, Roberts BJ, Stoner CL, Vincent PW, Dykes DJ, Panek RL, Lu GH, Major TC, Dahring TK, Hallak H, Bradford LA, Showalter HDH, Doherty AM (1998) J Med Chem 41:3276
Kraker AJ, Hartl BG, Amar AM, Barvian MR, Showalter HDH, Moore CW (2000) Biochem Pharmacol 60:885
La Rosee P, Corbin AS, Stoffregen EP, Deininger MW, Druker BJ (2002) Cancer Res 62:7149
Huron DR, Gorre ME, Kraker AJ, Sawyers CL, Rosen N, Moasser MM (2003) Clin Cancer Res 9:1267
von Bubnoff N, Veach DR, Miller WT, Li W, Saenger J, Peschel C, Bornmann WG, Clarkson B, Duyster J (2003) Cancer Res 63:6395
Veach DR, Lambek C, Liu C-Y, Duyster J, Beresten T, Li W, Wolff NC, Ilaria RL, Gelovani J, Miller WT, von Bubnoff N, Bornmann WG, Clarkson BD (2003) 226th Nat Meeting Am Chem Soc, Abstract MEDI-067
Tipping AJ, Baluch S, Barnes DJ, Veach DR, Clarkson BM, Bornmann WG, Mahon FX, Goldman JM, Melo JV (2004) Leukemia 18:1352
Wolff NC, Veach DR, Tong WP, Bornmann WG, Clarkson B, Ilaria RL Jr (2005) Blood 105:3995
http://www.medicalnewstoday.com , (Last visited on: Jan 05, 2006)
Missbach M, Jeschke M, Feyen J, Muller K, Glatt M, Green J, Susa M (1999) Bone 24:437
Li B, Boast S, De los Santos K, Schieren I, Quiroz M, Teitelbaum SL, Tondravi MM, Goff SP (2000) Nat Genet 24:304
Missbach M, Altmann E, Widler L, Susa M, Buchdunger E, Mett H, Meyer T, Green J (2000) Bioorg Med Chem Lett 10:945
Widler L, Green J, Missbach M, Susa M, Altmann E (2001) Bioorg Med Chem Lett 11:849
Altmann E, Missbach M, Green J, Susa M, Wagenknecht HA, Widler L (2001) Bioorg Med Chem Lett 11:853
Altmann E, Widler L, Missbach M (2002) Mini-Reviews Med Chem 2:201
Warmuth M, Simon N, Mitina O, Mathes R, Fabbro D, Manley PW, Buchdunger E, Forster K, Moarefi I, Hallek M (2003) Blood 101:664
Hu Y, Liu Y, Pelletier S, Buchdunger E, Warmuth M, Fabbro D, Hallek M, Van Etten RA, Li S (2004) Nat Genet 36:453
Shakespeare WC, Metcalf CA III, Wang Y, Sundaramoorthi R, Keenan T, Weigele M, Bohacek RS, Dalgarno DC, Sawyer TK (2003) Curr Opin Drug Dis Dev 6:729
Wang Y, Metcalf CA III, Shakespeare WC, Sundaramoorthi R, Keenan TP, Bohacek RS, Van Schravendijk MR, Violette SM, Narula SS, Dalgarno DC, Haraldson C, Keats J, Liou S, Mani U, Pradeepan S, Ram M, Adams S, Weigele M, Sawyer TK (2003) Bioorg Med Chem Lett 13:3067
Metcalf C III, Wang Y, Shakespeare W, Sundaramoorthi R, Keenan T, Dalgarno D, Bohacek R, Burns K, Roses J, van Schravendijk MR, Ram M, Keats J, Liou S, Adams S, Snodgrass J, Rivera V, Weigele M, Iuliucci J, Clackson T, Frame M, Brunton V, Sawyer T (2003) 226th Nat Meeting Am Chem Soc, Abstract COMP-079
Dalgarno D, Bohacek R, Stehle T, Narula S, Metcalf C III, Shakespeare W, Sundaramoorthi R, Keenan T, Wang Y, Keats J, Ram M, Adams S, Van Schravandijk MR, Weigele M, Sawyer T (2003) AACR-NCI-EORTC Int Conf Mol Targets Cancer Ther, Abstract A5
Dalgarno D, Stehle T, Narula S, Schelling P, Van Schravandijk MR, Adams S, Andrade L, Keats J, Ram M, Jin L, Grossman T, MacNeil I, Metcalf C III, Shakespeare W, Wang Y, Keenan T, Sundaramoorthi R, Bohacek R, Weigele M, Sawyer T (2006) Chem Biol Drug Des 67:46
O'Hare T, Pollock R, Stoffregen EP, Keats JA, Abdullah OM, Moseson EM, Rivera VM, Tang H, Metcalf CA III, Bohacek RS, Wang Y, Sundaramoorthi R, Shakespeare WC, Dalgarno D, Clackson T, Sawyer TK, Deininger MW, Druker BJ (2004) Blood 104:2532
O'Hare T, Walters DK, Stoffregen EP, Sherbenou DW, Heinrich MC, Deininger MWN, Druker BJ (2005) Clin Cancer Res 11:6987
Corbin AS, Demehri S, Griswold IJ, Wang Y, Metcalf CA III, Sundaramoorthi R, Shakespeare WC, Snodgrass J, Wardwell S, Dalgarno D, Iuliucci J, Sawyer TK, Heinrich MC, Druker BJ, Deininger MWN (2005) Blood 106:227
Azam M, Nardi V, Shakespeare WC, Latek RR, Veach DR, Clarckson B, Bohacek R, Sawyer TK, Daley GQ (2005) Annu Meeting Am Soc Hematol, Abstract 1996
http://www.ariad.com , (Last visited on: Jan 05, 2006)
Boschelli DH, Wang YD, Ye F, Wu B, Zhang N, Dutia M, Powell DW, Wissner A, Arndt K, Weber JM, Boschelli F (2001) J Med Chem 44:822
Boschelli DH, Ye F, Wang YD, Dutia M, Johnson SL, Wu B, Miller K, Powell DW, Yaczko D, Young M, Tischler M, Arndt K, Discafani C, Etienne C, Gibbons J, Grod J, Lucas J, Weber JM, Boschelli F (2001) J Med Chem 44:3965
Golas JM, Arndt K, Etienne C, Lucas J, Nardin D, Gibbons J, Frost P, Ye F, Boschelli DH, Boschelli F (2003) Cancer Res 63:375
Donato NJ, Wu JY, Talpaz M, Dutia M, Ye F, Boschelli D, Boschelli F (2002) Annu Meeting Am Soc Hematol, Abstract 1434
Grafone T, Mancini M, Ottaviani E, Renzulli M, Boschelli F, Ferraretti L, Santucci MA, Amabile M, Soverini S, Terragna C, Poerio A, Rosti G, Taccioli C, Baccarani M, Martinelli G (2004) Annu Meeting Am Soc Hematol, Abstract 1991
Grafone T, Mancini M, Ottaviani E, Renzulli M, Boschelli F, Ferraretti L, Santucci MA, Soverini S, Amabile M, Terragna C, Poerio A, Rosti G, Taccioli C, Palmerini E, Baccarani M, Martinelli G (2005) Annu Meeting Am Assoc Cancer Res, Abstract 5984
Boschelli DH, Boschelli F, Wu B, Ye F, Wang Y, Golas JM, Young T, Lucas J (2005) Haematologica Rep 1(8):28
Renzulli M, Grafone T, Taccioli C, Terragna C, Boschelli F, Mancini M, Creo P, Ottaviani E, Colarossi S, Amabile M, Soverini S, Poerio A, Iacobucci I, Baccarani M, Martinelli G (2005) Annu Meeting Am Soc Hematol, Abstract 4870
Boschelli DH, Wang YD, Johnson S, Wu B, Ye F, Barrios Sosa AC, Golas JM, Boschelli F (2004) J Med Chem 47:1599
Boschelli DH, Wu B, Barrios Sosa AC, Durutlic H, Ye F, Raifeld Y, Golas JM, Boschelli F (2004) J Med Chem 47:6666
Boschelli DH, Wu B, Barrios Sosa AC, Chen JJ, Golas JM, Boschelli F (2005) Bioorg Med Chem Lett 15:4681
Golas JM, Lucas J, Etienne C, Golas J, Discafani C, Sridharan L, Boghaert E, Arndt K, Ye F, Boschelli DH, Li F, Titsch C, Huselton C, Chaudhary I, Boschelli F (2005) Cancer Res 65:5358
http://www.cmlsupport.com/cml/newletters.html (2003) CML Update 2:1, (Last visited on: Jan 05, 2006)
MD Anderson (2003) Cancer Center Leukemia Insights Newsletter 8(2), http://www.mdanderson.org/publications/insights , (Last visited on: Jan 05, 2006)
Lee FY, Lombardo L, Borzilleri R, Camuso A, Castaneda S, Donato N, Fager K, Flefleh C, Gray h, Inigo I, Kan D, Luo R, Pang S, Wen M-L, Wild R, Wong TW, Talpaz M, Kramer R (2004) Annu Meeting Am Assoc Cancer Res, Abstract 3987
Shah NP, Tran C, Lee FY, Sawyers CL (2004) Annu Meeting Am Assoc Cancer Res, Abstract 5624
Wu JY, Donato NJ, Hong DS, Lee FY, Talpaz M (2004) Annu Meeting Am Assoc Cancer Res, Abstract 3850
Shah NP, Tran C, Lee FY, Chen P, Norris D, Sawyers CL (2004) Science 305:399
Wityak J, Das J, Moquin RV, Shen Z, Lin J, Chen P, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, Schieven GL, Kanner SB, Barrish JC (2003) Bioorg Med Chem Lett 13:4007
Lombardo LJ, Lee FY, Chen P, Norris D, Barrish JC, Behnia K, Castaneda S, Cornelius LAM, Das J, Doweyko AM, Fairchild C, Hunt JT, Inigo I, Johnston K, Kamath A, Kan D, Klei H, Marathe P, Pang S, Peterson R, Pitt S, Schieven GL, Schmidt RJ, Tokarski J, Wen M-L, Wityak J, Borzilleri RM (2004) J Med Chem 47:6658
Tokarski JS, Newitt J, Lee FY, Lombardo L, Borzilleri R, Kish K, Xie D, Zhang Y, Cheng JD, Kiefer SE, Chang CYJ, Klei HE (2004) Annu Meeting Am Soc Hematol, Abstract 553
Azam M, Latek RR, Daley GQ (2003) Cell 112:831
Burgess MR, Skaggs BJ, Shah NP, Lee FY, Sawyers CL (2005) Proc Natl Acad Sci USA 102:3395
Luo FR, Yang Z, Camuso A, Smykla R, Castenada S, Flefleh C, Fager K, Inigo I, Kan D, McGlinchey K, Wen M-L, Wild R, Borzilleri R, Lombardo L, Kramer R, Lee FY (2004) Annu Meeting Am Soc Hematol, Abstract 1987
Lee FY, Wen M-L, Bhide R, Camuso A, Castaneda S, Fager K, Flefleh C, Inigo I, Kan D, Luo R, McGlinchey K, Smykla R, Wild R, Borzilleri R, Lombardo L (2005) Annu Meeting Am Soc Hematol, Abstract 1994
Dai H, Marbach P, Lemaire M, Hayes M, Elmquist WF (2003) J Pharmacol Exp Ther 304:1085
Wild R, Castaneda S, Flefleh C, Fager K, Inigo I, Kan D, Smykla R, Camuso A, McGlinchey K, Wen M-L, Luo FR, Borzilleri R, Lombardo L, Kramer R, Lee FY (2004) Annu Meeting Am Soc Hematol, Abstract 1988
Sawyers CL, Shah NP, Kantarjian HM, Donato N, Nicoll J, Bai SA, Huang F, Clark E, DeCillis AP, Talpaz M (2004) Annu Meeting Am Soc Hematol, Abstract 1
Talpaz M, Kantarjian H, Shah NP, Donato N, Nicoll J, Bai SA, Huang F, Clark E, DeCillis AP, Sawyers C (2004) Annu Meeting Am Soc Hematol, Abstract 20
Talpaz M, Kantarjian HM, Paquette R, Shah N, Cortes J, Nicoll J, Bai SA, Huang F, Decillis AP, Sawyers CL (2005) Annu Meeting Am Soc Clin Oncol, Abstract 6519
Sawyers CL, Shah NP, Kantarjian HM, Cortes J, Paquette R, Nicoll J, Bai SA, Clark E, Decillis AP, Talpaz M (2005) Annu Meeting Am Soc Clin Oncol, Abstract 6520
Sawyers CL, Kantarjian H, Shah N, Cortes J, Paquette R, Donato N, Nicoll J, Bleickardt E, Chen T-T, Talpaz M (2005) Annu Meeting Am Soc Hematol, Abstract 38
Gao H, Talpaz M, Lee BN, Donato N, Cortes JE, Kantarjian HM, Reuben JM (2005) Annu Meeting Am Soc Clin Oncol, Abstract 6619
Guilhot F, Apperley JF, Shah N, Kim DW, Grigg A, Cheng S, Iyer M, Cortes J (2005) Annu Meeting Am Soc Hematol, Abstract 39
Talpaz M, Rousselot P, Kim DW, Guilhot F, Corm S, Bleickardt E, Zink R, Rosti G, Coutre S, Sawyers C (2005) Annu Meeting Am Soc Hematol, Abstract 40
Hochhaus A, Baccarani M, Sawyers C, Nagler A, Facon T, Goldberg SL, Cervantes F, Larson RA, Voi M, Ezzeddine R, Kantarjian H (2005) Annu Meeting Am Soc Hematol, Abstract 41
Ottman O, Martinelli G, Dombret H, Kantarjian H, Hochhaus A, Simonsson B, Aloe A, Apanovitch A, Shah N (2005) Annu Meeting Am Soc Hematol, Abstract 42
Shah N, Nicoll J, Branford S, Hughes TP, Paquette RL, Talpaz M, Nicaise C, Huang F, Sawyers CL (2005) Annu Meeting Am Soc Hematol, Abstract 1093
Jabbour E, Cortes J, Talpaz M, Jones D, O'Brien S, Nicaise C, Kantarjian H (2005) Annu Meeting Am Soc Hematol, Abstract 1091
Donato N, Wu J, Kong LY, Meng F, Lee F, Talpaz M (2005) Annu Meeting Am Soc Hematol, Abstract 1087
Johnson FM, Saigal B, Talpaz M, Donato NJ (2005) Clin Cancer Res 11:6924
http://www.fda.gov/bbs/topics/NEWS/2006/NEW01400.html , (Last visited on: Jan 05, 2006)
Ple PA, Green TP, Hennequin LF, Curwen J, Fennell M, Allen J, Lambert-van der Brempt C, Costello G (2004) J Med Chem 47:871
Yezhelyev MV, Koehl G, Guba M, Brabletz T, Jauch KW, Ryan A, Barge A, Green T, Fennell M, Bruns CJ (2004) Clin Cancer Res 10:8028
Hennequin LF, Allen J, Costello GF, Fennell M, Green TP, Jacobs V, Morgentin R, Olivier A, Ple PA (2005) Annu Meeting Am Assoc Cancer Res, Abstract 2537
Lockton JA, Smethurst D, Macpherson M, Tootell R, Marshall AL, Clack G, Gallagher NJ (2005) Annu Meeting Am Soc Clin Oncol, Abstract 3125
Gallagher NJ, Lockton AJ, Macpherson M, Marshall A, Clack G (2005) Annu Meeting Am Assoc for Cancer Res, Abstract 3972
O'Hare T, Walters DK, Stoffregen EP, Jia T, Manley PW, Mestan J, Cowan-Jacob SW, Lee FY, Heinrich MC, Deininger MWN, Druker BJ (2005) Cancer Res 65:4500
Deininger MWN, Bradeen H, Jia T, O'Hare T, Willis SG, Lee F, Druker BJ (2005) Annu Meeting Am Soc Hematol, Abstract 691
Griffin JD, Weisberg EL (2005) Annu Meeting Am Soc Hematol, Abstract 694
Fabian MA, Biggs WH, Treiber DK, Atteridge CE, Azimioara MD, Benedetti MG, Carter TA, Ciceri P, Edeen PT, Floyd M, Ford JM, Galvin M, Gerlach JL, Grotzfeld RM, Herrgard S, Insko DE, Insko MA, Lai AG, Lelias J-M, Mehta SA, Milanov ZV, Velasco AM, Wodicka LM, Patel HK, Zarrinkar PP, Lockhart DJ (2005) Nat Biotechnol 23:329
Carter TA, Wodicka LM, Shah NP, Velasco AM, Fabian MA, Treiber DK, Milanov ZV, Atteridge CE, Biggs WH III, Edeen PT, Floyd M, Ford JM, Grotzfeld RM, Herrgard S, Insko DE, Mehta SA, Patel HK, Pao W, Sawyers CL, Varmus H, Zarrinkar PP, Lockhart DJ (2005) Proc Natl Acad Sci USA 102:11011
O'Hare T, Druker BJ (2005) Nat Biotechnol 23:1209
http://www.vrtx.com , (Last visited on: Jan 05, 2006)
Burley SK (2005) Annu Meeting Am Soc Hematol, Abstract 698
http://www.sgxpharma.com , (Last visited on: Jan 05, 2006)
http://www.newcmldrug.com , (Last visited on: Jan 05, 2006)
Cortes J, Garcia-Manero G, O'Brien S, Hernandez I, Rackoff W, Faderl S, Thomas D, Ferrajoli A, Talpaz M, Kantarjian H (2004) Annu Meeting Am Soc Hematol, Abstract 1011
Cortes J, O'Brien S, Verstovsek S, Daley G, Koller C, Ferrajoli A, Pate O, Faderl S, Ravandi-Kashani F, Talpaz M, Zhu Y, Statkevich P, Sugrue M, Kantarjian H (2004) Annu Meeting Am Soc Hematol, Abstract 1009
Kobayashi S, Boggon TJ, Dayaram T, Janne PA, Kocher O, Meyerson M, Johnson BE, Eck MJ, Tenen DG, Halmos B (2005) N Engl J Med 352:786
Pao W, Miller VA, Politi KA, Riely GJ, Somwar R, Zakowski MF, Kris MG, Varmus H (2005) PLoS Med 2:e73, http://www.plosmedicine.org , (Last visited on: Jan 05, 2006)
Kwak EL, Sordella R, Bell DW, Godin-Heymann N, Okimoto RA, Brannigan BW, Harris PL, Driscoll DR, Fidias P, Lynch TJ, Rabindran SK, McGinnis JP, Wissner A, Sharma SV, Isselbacher KJ, Settleman J, Haber DA (2005) Proc Natl Acad Sci USA 102:7665
Acknowledgments
I thank Frank Boschelli, Janis Upeslacis and Dennis Powell for their critical review of this manuscript.
Author information
Authors and Affiliations
Corresponding author
Editor information
Rights and permissions
Copyright information
© 2006 Springer-Verlag Berlin Heidelberg
About this chapter
Cite this chapter
Boschelli, D.H. (2006). Bcr-Abl Kinase Inhibitors. In: Bradbury, R.H. (eds) Cancer. Topics in Medicinal Chemistry, vol 1. Springer, Berlin, Heidelberg. https://doi.org/10.1007/7355_2006_008
Download citation
DOI: https://doi.org/10.1007/7355_2006_008
Published:
Publisher Name: Springer, Berlin, Heidelberg
Print ISBN: 978-3-540-33119-3
Online ISBN: 978-3-540-33120-9
eBook Packages: Chemistry and Materials ScienceChemistry and Material Science (R0)