Single cell imaging of Bruton's Tyrosine Kinase using an irreversible inhibitor

Scientific Reports

Volumn 4, Issue , 2014, Pages

  Turetsky, Anna ^a   Kim, Eunha ^a   Kohler, Rainer H ^a   Miller, Miles A ^a   Weissleder, Ralph ^a,b  

^a MASSACHUSETTS GENERAL HOSPITAL   (United States)

^b HARVARD MEDICAL SCHOOL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AGAMMAGLOBULINAEMIA TYROSINE KINASE; IBRUTINIB; PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE; PYRAZOLE DERIVATIVE; PYRIMIDINE DERIVATIVE;

ANIMAL; ARTICLE; BINDING SITE; CHEMICAL STRUCTURE; CHEMISTRY; CONFORMATION; DRUG ANTAGONISM; GENE EXPRESSION; HUMAN; LYMPHOMA; METABOLISM; MOLECULAR IMAGING; MOUSE; PROTEIN BINDING; REPORTER GENE; SINGLE CELL ANALYSIS; TUMOR CELL LINE; XENOGRAFT;

ANIMALS; BINDING SITES; CELL LINE, TUMOR; GENE EXPRESSION; GENES, REPORTER; HETEROGRAFTS; HUMANS; LYMPHOMA; MICE; MODELS, MOLECULAR; MOLECULAR CONFORMATION; MOLECULAR IMAGING; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; PYRAZOLES; PYRIMIDINES; SINGLE-CELL ANALYSIS;

EID: 84899472363     PISSN: None     EISSN: 20452322     Source Type: Journal    
DOI: 10.1038/srep04782     Document Type: Article

References (48)

1. Vetrie,D. et al. The gene involved in X-linked agammaglobulinaemia is amember of the src family of protein-tyrosine kinases. Nature 361, 226-233 (1993
2. Tsukada, S. et al. Deficient expression of a B cell cytoplasmic tyrosine kinase in human X-linked agammaglobulinemia. Cell 72, 279-290 (1993
3. Mangla, A. et al. Pleiotropic consequences of Bruton tyrosine kinase deficiency in myeloid lineages lead to poor inflammatory responses. Blood 104, 1191-1197 (2004
4. Eifert, C. et al. A novel isoform of the B cell tyrosine kinase BTK protects breast cancer cells from apoptosis. Gene Chromosom Canc 52, 961-975 (2013
5. Rawlings, D. J. et al. Mutation of unique region of Bruton?s tyrosine kinase in immunodeficient XID mice. Science 261, 358-361 (1993
6. de Weers, M. et al. B-cell antigen receptor stimulation activates the human Bruton?s tyrosine kinase, which is deficient in X-linked agammaglobulinemia. J Biol Chem 269, 23857-23860 (1994
7. Fruman, D. A. et al. Phosphoinositide 3-kinase and Bruton?s tyrosine kinase regulate overlapping sets of genes in B lymphocytes. Proc Natl Acad Sci U S A 99, 359-364 (2002
8. Mahajan, S. et al. Transcription factor STAT5A is a substrate of Bruton?s tyrosine kinase in B cells. J Biol Chem 276, 31216-31228 (2001
9. Petro, J. B., Rahman, S. M., Ballard, D. W. & Khan, W. N. Bruton?s tyrosine kinase is required for activation of IkappaB kinase and nuclear factor kappaB in response to B cell receptor engagement. J Exp Med 191, 1745-1754 (2000
10. Bajpai, U. D., Zhang, K., Teutsch, M., Sen, R. & Wortis, H. H. Bruton?s tyrosine kinase links the B cell receptor to nuclear factor kappaB activation. J Exp Med 191, 1735-1744 (2000
11. Tai, Y. T. et al. Bruton tyrosine kinase inhibition is a novel therapeutic strategy targeting tumor in the bone marrow microenvironment in multiple myeloma. Blood 120, 1877-1887 (2012
12. Rushworth, S. A., Murray, M. Y., Zaitseva, L., Bowles, K. M. & Macewan, D. J. Identification of Bruton?s tyrosine kinase as a therapeutic target in acute myeloid leukemia. Blood (2013
13. Woyach, J. A. et al. Bruton?s tyrosine kinase (BTK) function is important to the development and expansion of chronic lymphocytic leukemia (CLL). Blood (2013
14. Bogusz, A. M. et al. Quantitative immunofluorescence reveals the signature of active B-cell receptor signaling in diffuse large B-cell lymphoma. Clin Cancer Res 18, 6122-6135 (2012
15. Cinar, M. et al. Bruton tyrosine kinase is commonly overexpressed in mantle cell lymphoma and its attenuation by Ibrutinib induces apoptosis. Leuk Res 37, 1271-1277 (2013
16. Advani, R. H. et al. Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) has significant activity in patients with relapsed/refractory B-cell malignancies. J Clin Oncol 31, 88-94 (2013
17. O?Brien, S. et al. Ibrutinib as initial therapy for elderly patients with chronic lymphocytic leukaemia or small lymphocytic lymphoma: An open-label, multicentre, phase 1b/2 trial. Lancet Oncol 15, 48-58 (2014
18. Byrd, J. C. et al. Targeting BTK with ibrutinib in relapsed chronic lymphocytic leukemia. N Engl J Med 369, 32-42 (2013
19. Evans, E. K. et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J Pharmacol Exp Ther 346, 219-228 (2013
20. Wang, M. L. et al. Targeting BTK with ibrutinib in relapsed or refractory mantlecell lymphoma. N Engl J Med 369, 507-516 (2013
21. Honigberg, L. A. et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks Bcell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci U S A 107, 13075-13080 (2010
22. Liu, Q. et al. Developing irreversible inhibitors of the protein kinase cysteinome. Chem Biol 20, 146-159 (2013
23. Lou, Y., Owens, T. D., Kuglstatter, A., Kondru, R. K. & Goldstein, D. M. Bruton?s tyrosine kinase inhibitors: Approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. J Med Chem 55, 4539-4550 (2012
24. Younes, A. & Berry, D. A. From drug discovery to biomarker-driven clinical trials in lymphoma. Nat Rev Clin Oncol 9, 643-653 (2012
25. Pan, Z. et al. Discovery of selective irreversible inhibitors for Bruton?s tyrosine kinase. ChemMedChem 2, 58-61 (2007
26. Akinleye, A., Chen, Y., Mukhi, N., Song, Y. & Liu, D. Ibrutinib and novel BTK inhibitors in clinical development. J Hematol Oncol 6, 59 (2013
27. Fallahi-Sichani, M., Honarnejad, S., Heiser, L. M., Gray, J. W. & Sorger, P. K. Metrics other than potency reveal systematic variation in responses to cancer drugs. Nat Chem Biol 9, 708-714 (2013
28. Davis, R. E. et al. Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma. Nature 463, 88-92 (2010
29. Rickert, R. C. New insights into pre-BCR and BCR signalling with relevance to B cell malignancies. Nat Rev Immunol 13, 578-591 (2013
30. Mohamed, A. J. et al. Nucleocytoplasmic shuttling of Bruton?s tyrosine kinase. J Biol Chem 275, 40614-40619 (2000
31. Lowry, W. E. & Huang, X. Y. G Protein beta gamma subunits act on the catalytic domain to stimulate Bruton?s agammaglobulinemia tyrosine kinase. J Biol Chem 277, 1488-1492 (2002
32. Gustafsson, M. O. et al. Regulation of nucleocytoplasmic shuttling of Bruton?s tyrosine kinase (Btk) through a novel SH3-dependent interaction with ankyrin repeat domain 54 (ANKRD54). Mol Cell Biol 32, 2440-2453 (2012
33. Su, Q., Zhou, Y. & Johns, R. A. Bruton?s tyrosine kinase (BTK) is a binding partner for hypoxia induced mitogenic factor (HIMF/FIZZ1) and mediates myeloid cell chemotaxis. FASEB J 21, 1376-1382 (2007
34. Dragoi, A. M., Talman, A. M. & Agaisse, H. Bruton?s tyrosine kinase regulates Shigella flexneri dissemination in HT-29 intestinal cells. Infect Immun 81, 598-607 (2013
35. Strijbis, K. et al. Bruton?s Tyrosine Kinase (BTK) and Vav1 contribute to Dectin1-dependent phagocytosis of Candida albicans in macrophages. PLoS Pathog 9, e1003446 (2013
36. Keliher, E. J., Reiner, T., Turetsky, A., Hilderbrand, S. A. & Weissleder, R. Highyielding, two-step 18F labeling strategy for 18F-PARP1 inhibitors. ChemMedChem 6, 424-427 (2011
37. Reiner, T., Keliher, E. J., Earley, S., Marinelli, B. &Weissleder, R. Synthesis and in vivo imaging of a 18F-labeled PARP1 inhibitor using a chemically orthogonal scavenger-assisted high-performance method. Angew Chem Int Ed Engl 50, 1922-1925 (2011
38. Reiner, T. et al. Imaging therapeutic PARP inhibition in vivo through bioorthogonally developed companion imaging agents. Neoplasia 14, 169-177 (2012
39. Zeglis, B. M. et al. A pretargeted PET imaging strategy based on bioorthogonal Diels-Alder click chemistry. J Nucl Med 54, 1389-1396 (2013
40. Borjesson, P. K. et al. Radiation dosimetry of 89Zr-labeled chimeric monoclonal antibody U36 as used for immuno-PET in head and neck cancer patients. J Nucl Med 50, 1828-1836 (2009
41. Holland, J. P. et al. 89Zr-DFO-J591 for immunoPET of prostate-specific membrane antigen expression in vivo. J Nucl Med 51, 1293-1300 (2010
42. Keliher, E. J. et al. 89Zr-labeled dextran nanoparticles allow in vivo macrophage imaging. Bioconjug Chem 22, 2383-2389 (2011
43. Natarajan, A., Habte, F. & Gambhir, S. S. Development of a Novel Long-Lived ImmunoPET Tracer for Monitoring Lymphoma Therapy in a Humanized Transgenic Mouse Model. Bioconjug Chem (2012
44. Fischer, G., Seibold, U., Schirrmacher, R., Wangler, B. & Wangler, C. (89)Zr, a radiometal nuclide with high potential for molecular imaging with PET: Chemistry, applications and remaining challenges. Molecules 18, 6469-6490 (2013
45. Kerns, H. M. et al. B cell-specific lentiviral gene therapy leads to sustained B-cell functional recovery in a murine model of X-linked agammaglobulinemia. Blood 115, 2146-2155 (2010
46. Orth, J.D. et al. Analysis of mitosis and antimitotic drug responses in tumors by in vivo microscopy and single-cell pharmacodynamics. Cancer Res 71, 4608-4616 (2011
47. Pittet, M. J. & Weissleder, R. Intravital imaging. Cell 147, 983-991 (2011
48. Thurber, G. M. et al. Single-cell and subcellular pharmacokinetic imaging allows insight into drug action in vivo. Nat Commun 4, 1504 (2013).