The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

Proceedings of the National Academy of Sciences of the United States of America

Volumn 107, Issue 29, 2010, Pages 13075-13080

  Honigberg, Lee A ^a,g   Smith, Ashley M ^a,g   Sirisawad, Mint ^a   Verner, Erik ^a   Loury, David ^a   Chang, Betty ^a   Li, Shyr ^b,c   Pan, Zhengying ^b,d   Thamm, Douglas H ^e   Miller, Richard A ^a,f   Buggy, Joseph J ^a  

^a PHARMACYCLICS INC   (United States)

^b CELERA   (United States)

^c EXELIXIS INC   (United States)

^d PEKING UNIVERSITY   (China)

^e Department of Environmental and Radiological Health Sciences   (United States)

^f STANFORD UNIVERSITY MEDICAL CENTER   (United States)

^g GENENTECH INC   (United States)

Author keywords

Lymphoma; X linked agammaglobulinemia

Indexed keywords

AUTOANTIBODY; BRUTON TYROSINE KINASE; CYCLOPHOSPHAMIDE; DEXAMETHASONE; DOXORUBICIN; PCI 29732; PCI 32765; PCI 33380; PREDNISOLONE; PREDNISONE; PROTEIN TYROSINE KINASE INHIBITOR; T LYMPHOCYTE RECEPTOR; UNCLASSIFIED DRUG; VINCRISTINE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTHRITIS; ARTICLE; AUTOIMMUNE DISEASE; B CELL LYMPHOMA; B LYMPHOCYTE; B LYMPHOCYTE ACTIVATION; CONTROLLED STUDY; DRUG EFFICACY; ENZYME INHIBITION; EXPERIMENTAL DOG; HUMAN; HUMAN CELL; LUPUS LIKE SYNDROME; LYMPHOCYTE FUNCTION; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; SIGNAL TRANSDUCTION; TREATMENT RESPONSE;

ADMINISTRATION, ORAL; ANIMALS; ARTHRITIS, EXPERIMENTAL; AUTOANTIBODIES; AUTOIMMUNE DISEASES; B-LYMPHOCYTES; BENZOFURANS; DISEASE MODELS, ANIMAL; DOGS; HUMANS; LYMPHOCYTE ACTIVATION; LYMPHOMA, B-CELL; MICE; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; PYRAZOLES; PYRIMIDINES; RECEPTORS, ANTIGEN, B-CELL; SIGNAL TRANSDUCTION; TREATMENT OUTCOME;

CANIS FAMILIARIS; MUS;

EID: 77955625479     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.1004594107     Document Type: Article

References (28)

1. Satterthwaite AB, Witte ON (2000) The role of Bruton's tyrosine kinase in B-cell development and function: A genetic perspective. Immunol Rev 175:120-127.
2. Khan WN (2001) Regulation of B lymphocyte development and activation by Bruton's tyrosine kinase. Immunol Res 23:147-156.
3. Afar DE, et al. (1996) Regulation of Btk by Src family tyrosine kinases. Mol Cell Biol 16: 3465-3471.
4. Cheng G, Ye ZS (1994) Baltimore D binding of Bruton's tyrosine kinase to Fyn, Lyn, or Hck through a Src homology 3 domain-mediated interaction. Proc Natl Acad Sci USA 91:8152-8155.
5. Humphries LA, et al. (2004) Tec kinases mediate sustained calcium influx via site-specific tyrosine phosphorylation of the phospholipase Cgamma Src homology 2-Src homology 3 linker. J Biol Chem 279:37651-37661.
6. Conley ME, et al. (2009) Primary B cell immunodeficiencies: Comparisons and contrasts. Annu Rev Immunol 27:199-227.
7. Tsukada S, Rawlings DJ, Witte ON (1994) Role of Bruton's tyrosine kinase in immunodeficiency. Curr Opin Immunol 6:623-630. (Pubitemid 24249522)
8. Rawlings DJ, et al. (1993) Mutation of unique region of Bruton's tyrosine kinase in immunodeficient XID mice. Science 261:358-361.
9. Satterthwaite AB, Cheroutre H, Khan WN, Sideras P, Witte ON (1997) Btk dosage determines sensitivity to B cell antigen receptor cross-linking. Proc Natl Acad Sci USA 94:13152-13157.
10. Texido G, et al. (2000) The B-cell-specific Src-family kinase Blk is dispensable for B-cell development and activation. Mol Cell Biol 20:1227-1233.
11. Lowell CA (2004) Src-family kinases: Rheostats of immune cell signaling. Mol Immunol 41:631-643.
12. Edwards JC, et al. (2004) Efficacy of B-cell-targeted therapy with rituximab in patients with rheumatoid arthritis. N Engl J Med 350:2572-2581.
13. Favas C, Isenberg DA (2009) B-cell-depletion therapy in SLE - what are the current prospects for its acceptance? Nat Rev Rheumatol 5:711-716.
14. Hauser SL, et al.; HERMES Trial Group (2008) B-cell depletion with rituximab in relapsing-remitting multiple sclerosis. N Engl J Med 358:676-688.
15. Küppers R (2005) Mechanisms of B-cell lymphoma pathogenesis. Nat Rev Cancer 5: 251-262.
16. Davis RE, et al. (2010) Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma. Nature 463:88-92.
17. Pan Z, et al. (2007) Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase. ChemMedChem 2:58-61.
18. Marcotte DJ, et al. (2010) Structures of human Bruton's tyrosine kinase in active and inactive conformations suggest a mechanism of activation for TEC family kinases. Protein Sci 19:429-439.
19. Jansson L, Holmdahl R (1993) Genes on the X chromosome affect development of collagen-induced arthritis in mice. Clin Exp Immunol 94:459-465.
20. Shlomchik MJ, Madaio MP, Ni D, Trounstein M, Huszar D (1994) The role of B cells in lpr/lpr-induced autoimmunity. J Exp Med 180:1295-1306.
21. Breen M, Modiano JF (2008) Evolutionarily conserved cytogenetic changes in hematological malignancies of dogs and humans - man and his best friend share more than companionship. Chromosome Res 16:145-154.
22. Fry DW, et al. (1998) Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor. Proc Natl Acad Sci USA 95:12022-12027.
23. Cohen MS, Zhang C, Shokat KM, Taunton J (2005) Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Science 308:1318-1321.
24. Yanaba K, et al. (2007) B cell depletion delays collagen-induced arthritis in mice: Arthritis induction requires synergy between humoral and cell-mediated immunity. J Immunol 179:1369-1380.
25. Chen L, et al. (2008) SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Blood 111:2230-2237.
26. Chan O, Madaio MP, Shlomchik MJ (1997) The roles of B cells in MRL/lpr murine lupus. Ann N Y Acad Sci 815:75-87.
27. Vail DM (2004) Veterinary Co-operative Oncology Group - Common Terminology Criteria for Adverse Events following chemotherapy or biological antineoplastic therapy in dogs and cats. Vet Comp Oncol 2:194-213.
28. Vail DM, Michels GM, Khanna C, Selting KA, London CA; Veterinary Cooperative Oncology Group (2010) Response evaluation criteria for peripheral nodal lymphoma in dogs (v1.0) - a Veterinary Cooperative Oncology Group (VCOG) consensus document. Vet Comp Oncol 8:28-37.