Functional characterization of BTK C481S mutation that confers ibrutinib resistance: Exploration of alternative kinase inhibitors

Leukemia

Volumn 29, Issue 4, 2015, Pages 895-900

  Cheng, S ^a   Guo, A ^b   Lu, P ^b   Ma, J ^a   Coleman, M ^a   Wang, Y L ^b  

^a WEILL CORNELL MEDICAL COLLEGE   (United States)

^b UNIVERSITY OF CHICAGO   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BRUTON TYROSINE KINASE; CERDULATINIB; CYCLOPHOSPHAMIDE; CYSTEINE; DASATINIB; FLUDARABINE; IBRUTINIB; IDELALISIB; PROTEIN KINASE SYK INHIBITOR; PRT 060318; RITUXIMAB; RNA; SERINE; TOFACITINIB; UNCLASSIFIED DRUG; 2-(2-AMINOCYCLOHEXYLAMINO)-4-(M-TOLYLAMINO)PYRIMIDINE-5-CARBOXAMIDE; AGAMMAGLOBULINAEMIA TYROSINE KINASE; ANTINEOPLASTIC AGENT; CYCLOHEXYLAMINE DERIVATIVE; PIPERIDINE DERIVATIVE; PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE; PYRAZOLE DERIVATIVE; PYRIMIDINE DERIVATIVE; PYRROLE DERIVATIVE; SMALL INTERFERING RNA; THIAZOLE DERIVATIVE;

ADULT; ARTICLE; BINDING AFFINITY; CANCER CHEMOTHERAPY; CANCER COMBINATION CHEMOTHERAPY; CANCER RESISTANCE; CELL FUNCTION; CELL ISOLATION; CELL PROLIFERATION; CHEMOSENSITIVITY; CHRONIC LYMPHATIC LEUKEMIA; CLINICAL ARTICLE; CONTROLLED STUDY; COVALENT BOND; DISEASE COURSE; DISEASE MARKER; DRUG BINDING; DRUG DOSE ESCALATION; DRUG RESPONSE; ENZYME ACTIVITY; FEMALE; GENE EXPRESSION; GENE EXPRESSION PROFILING; GENE MUTATION; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; IMMUNOBLOTTING; LYMPHOMA CELL; MIDDLE AGED; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; RNA SEQUENCE; SIGNAL TRANSDUCTION; WILD TYPE; ANTAGONISTS AND INHIBITORS; B LYMPHOCYTE; CASE REPORT; CHEMISTRY; DRUG EFFECTS; DRUG RESISTANCE; ENZYMOLOGY; GENETICS; LEUKEMIA, LYMPHOCYTIC, CHRONIC, B-CELL; METABOLISM; MUTATION; PATHOLOGY; STRUCTURE ACTIVITY RELATION; TUMOR CELL LINE;

ANTINEOPLASTIC AGENTS; B-LYMPHOCYTES; CELL LINE, TUMOR; CYCLOHEXYLAMINES; DRUG RESISTANCE, NEOPLASM; FEMALE; GENE EXPRESSION; HUMANS; LEUKEMIA, LYMPHOCYTIC, CHRONIC, B-CELL; MIDDLE AGED; MUTATION; PIPERIDINES; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; PYRAZOLES; PYRIMIDINES; PYRROLES; RNA, SMALL INTERFERING; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES;

EID: 84927656208     PISSN: 08876924     EISSN: 14765551     Source Type: Journal    
DOI: 10.1038/leu.2014.263     Document Type: Article

References (24)

1. Rickert RC. New insights into pre-BCR and BCR signalling with relevance to B cell malignancies. Nat Rev Immunol 2013; 13: 578-591.
2. Dal Porto JM, Gauld SB, Merrell KT, Mills D, Pugh-Bernard AE, Cambier J. B cell antigen receptor signaling 101. Mol Immunol 2004; 41: 599-613.
3. Kurosaki T, Shinohara H, Baba Y. B cell signaling and fate decision. Annu Rev Immunol 2009; 28: 21-55.
4. Harwood NE, Batista FD. Early events in B cell activation. Annu Rev Immunol 2010; 28: 185-210.
5. Advani RH, Buggy JJ, Sharman JP, Smith SM, Boyd TE, Grant B et al. Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) has significant activity in patients with relapsed/refractory B-cell malignancies. J Clin Oncol 2013; 31: 88-94.
6. Byrd JC, Furman RR, Coutre SE, Flinn IW, Burger JA, Blum KA et al. Targeting BTK with ibrutinib in relapsed chronic lymphocytic leukemia. N Engl J Med 2013; 369: 32-42.
7. Chang BY, Furman RR, Zapatka M, Barrientos JC, Li D, Steggerda S et al. Use of tumor genomic profiling to reveal mechanisms of resistance to the BTK inhibitor ibrutinib in chronic lymphocytic leukemia (CLL). ASCO Meet Abstr 2013; 31: 7014.
8. Woyach JA, Furman RR, Liu TM, Ozer HG, Zapatka M, Ruppert AS et al. Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib. N Engl J Med 2014; 370: 2286-2294.
9. Furman RR, Cheng S, Lu P, Setty M, Perez AR, Guo A et al. Ibrutinib resistance in chronic lymphocytic leukemia. N Engl J Med 2014; 370: 2352-2354.
10. Cheng S, Ma J, Guo A, Lu P, Leonard JP, Coleman M et al. BTK inhibition targets in vivo CLL proliferation through its effects on B-cell receptor signaling activity. Leukemia 2014; 28: 649-657.
11. Song Z, Lu P, Furman RR, Leonard JP, Martin P, Tyrell L et al. Activities of SYK and PLCgamma2 predict apoptotic response of CLL cells to SRC tyrosine kinase inhibitor dasatinib. Clin Cancer Res 2010; 16: 587-599.
12. Yang C, Lu P, Lee FY, Chadburn A, Barrientos JC, Leonard JP et al. Tyrosine kinase inhibition in diffuse large B-cell lymphoma: Molecular basis for antitumor activity and drug resistance of dasatinib. Leukemia 2008; 22: 1755-1766.
13. Jo SH, Yang C, Miao Q, Marzec M, Wasik MA, Lu P et al. Peroxisome proliferatoractivated receptor gamma promotes lymphocyte survival through its actions on cellular metabolic activities. J Immunol 2006; 177: 3737-3745.
14. Lu P, Yang C, Guasparri I, Harrington W, Wang YL, Cesarman E. Early events of B-cell receptor signaling are not essential for the proliferation and viability of AIDS-related lymphoma. Leukemia 2009; 23: 807-810.
15. Herishanu Y, Perez-Galan P, Liu D, Biancotto A, Pittaluga S, Vire B et al. The lymph node microenvironment promotes B-cell receptor signaling, NF-kappaB activation, and tumor proliferation in chronic lymphocytic leukemia. Blood 2011; 117: 563-574.
16. Damle RN, Temburni S, Calissano C, Yancopoulos S, Banapour T, Sison C et al. CD38 expression labels an activated subset within chronic lymphocytic leukemia clones enriched in proliferating B cells. Blood 2007; 110: 3352-3359.
17. Cheng S, Coffey G, Zhang XH, Shaknovich R, Song Z, Lu P et al. SYK inhibition and response prediction in diffuse large B-cell lymphoma. Blood 2011; 118: 6342-6352.
18. Christopher LJ, Cui D, Wu C, Luo R, Manning JA, Bonacorsi SJ et al. Metabolism and disposition of dasatinib after oral administration to humans. Drug Metab Dispos 2008; 36: 1357-1364.
19. Dowty ME, Jesson MI, Ghosh S, Lee J, Meyer DM, Krishnaswami S et al. Preclinical to clinical translation of tofacitinib, a Janus kinase inhibitor, in rheumatoid arthritis. J Pharmacol Exp Ther 2014; 348: 165-173.
20. Hantschel O, Rix U, Schmidt U, Burckstummer T, Kneidinger M, Schutze G et al. The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. Proc Natl Acad Sci USA 2007; 104: 13283-13288.
21. Furman RR, Sharman JP, Coutre SE, Cheson BD, Pagel JM, Hillmen P et al. Idelalisib and rituximab in relapsed chronic lymphocytic leukemia. N Engl J Med 2014; 370: 997-1007.
22. Brown JR, Byrd JC, Coutre SE, Benson DM, Flinn IW, Wagner-Johnston ND et al. Idelalisib, an inhibitor of phosphatidylinositol 3-kinase p110delta, for relapsed/refractory chronic lymphocytic leukemia. Blood 2014; 123: 3390-3397.
23. Jin F, Robeson M, Zhou H, Moyer C, Ramanathan S. Pharmacokinetics and safety of idelalisib, a novel PI3K? inhibitor, in Japanese and Caucasian subjects. ASH Annu Meet Abstr 2013; abstract 5575.
24. Burger JA, Landau D, Hoellenriegel J, Sougnez C, Schlesner M, Ishaque N et al. Clonal evolution in patients with chronic lymphocytic leukemia (CLL) developing resistance to BTK inhibition. ASH Annu Meet Abstr 2013; abstract 866.