ABT-199 selectively inhibits BCL2 but not BCL2L1 and efficiently induces apoptosis of chronic lymphocytic leukaemic cells but not platelets

British Journal of Haematology

Volumn 163, Issue 1, 2013, Pages 139-142

  Vogler, Meike ^a   Dinsdale, David ^a   Dyer, Martin J S ^a   Cohen, Gerald M ^a  

^a UNIVERSITY OF LEICESTER   (United Kingdom)

Author keywords

ABT 199; Apoptosis; BCL XL (BCL2L1); BCL2; Chronic lymphocytic leukaemia

Indexed keywords

4 [4 (4' CHLORO 2 BIPHENYLYLMETHYL) 1 PIPERAZINYL] N [4 [3 DIMETHYLAMINO 1 (PHENYLTHIOMETHYL)PROPYLAMINO] 3 NITROBENZENESULFONYL]BENZAMIDE; ABT 199; ANTINEOPLASTIC AGENT; CASPASE 3; CASPASE 9; CELL PROTEIN; NAVITOCLAX; PROTEIN BAK1; PROTEIN BAX; PROTEIN BCL 2; PROTEIN BCL2L1; UNCLASSIFIED DRUG;

ADVERSE OUTCOME; ANTINEOPLASTIC ACTIVITY; APOPTOSIS; CHRONIC LYMPHATIC LEUKEMIA; CONCENTRATION RESPONSE; DRUG EFFECT; DRUG EFFICACY; DRUG SELECTIVITY; DRUG STRUCTURE; ENZYME ACTIVATION; LETTER; LEUKEMIA CELL; PRIORITY JOURNAL; PROTEIN CLEAVAGE; PROTEIN EXPRESSION; PROTEIN TARGETING; THROMBOCYTE; THROMBOCYTOPENIA;

ABT-199; APOPTOSIS; BCL-XL (BCL2L1); BCL2; CHRONIC LYMPHOCYTIC LEUKAEMIA;

APOPTOSIS; BCL-X PROTEIN; BICYCLO COMPOUNDS, HETEROCYCLIC; BLOOD PLATELETS; CELL LINE, TUMOR; HUMANS; LEUKEMIA, LYMPHOCYTIC, CHRONIC, B-CELL; PROTO-ONCOGENE PROTEINS C-BCL-2; SULFONAMIDES;

EID: 84883767136     PISSN: 00071048     EISSN: 13652141     Source Type: Journal    
DOI: 10.1111/bjh.12457     Document Type: Letter

References (10)

1. Cory, S. & Adams, J.M. (2002) The Bcl2 family: regulators of the cellular life-or-death switch. Nature Reviews Cancer, 2, 647-656.
2. Del Gaizo Moore, V., Brown, J.R., Certo, M., Love, T.M., Novina, C.D. & Letai, A. (2007) Chronic lymphocytic leukemia requires BCL2 to sequester prodeath BIM, explaining sensitivity to BCL2 antagonist ABT-737. The Journal of Clinical Investigation, 117, 112-121.
3. Gottschalk, A.R., Boise, L.H., Oltvai, Z.N., Accavitti, M.A., Korsmeyer, S.J., Quintans, J. & Thompson, C.B. (1996) The ability of Bcl-x(L) and Bcl-2 to prevent apoptosis can be differentially regulated. Cell Death and Differentiation, 3, 113-118.
4. Mason, K.D., Carpinelli, M.R., Fletcher, J.I., Collinge, J.E., Hilton, A.A., Ellis, S., Kelly, P.N., Ekert, P.G., Metcalf, D., Roberts, A.W., Huang, D.C. & Kile, B.T. (2007) Programmed anuclear cell death delimits platelet life span. Cell, 128, 1173-1186.
5. Oltersdorf, T., Elmore, S.W., Shoemaker, A.R., Armstrong, R.C., Augeri, D.J., Belli, B.A., Bruncko, M., Deckwerth, T.L., Dinges, J., Hajduk, P.J., Joseph, M.K., Kitada, S., Korsmeyer, S.J., Kunzer, A.R., Letai, A., Li, C., Mitten, M.J., Nettesheim, D.G., Ng, S., Nimmer, P.M., O'Connor, J.M., Oleksijew, A., Petros, A.M., Reed, J.C., Shen, W., Tahir, S.K., Thompson, C.B., Tomaselli, K.J., Wang, B., Wendt, M.D., Zhang, H., Fesik, S.W. & Rosenberg, S.H. (2005) An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature, 435, 677-681.
6. Park, C.M., Bruncko, M., Adickes, J., Bauch, J., Ding, H., Kunzer, A., Marsh, K.C., Nimmer, P., Shoemaker, A.R., Song, X., Tahir, S.K., Tse, C., Wang, X., Wendt, M.D., Yang, X., Zhang, H., Fesik, S.W., Rosenberg, S.H. & Elmore, S.W. (2008) Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. Journal of Medicinal Chemistry, 51, 6902-6915.
7. Roberts, A.W., Seymour, J.F., Brown, J.R., Wierda, W.G., Kipps, T.J., Khaw, S.L., Carney, D.A., He, S.Z., Huang, D.C., Xiong, H., Cui, Y., Busman, T.A., McKeegan, E.M., Krivoshik, A.P., Enschede, S.H. & Humerickhouse, R. (2012) Substantial susceptibility of chronic lymphocytic leukemia to BCL2 inhibition: results of a phase I study of navitoclax in patients with relapsed or refractory disease. Journal of Clinical Oncology, 30, 488-496.
8. Souers, A.J., Leverson, J.D., Boghaert, E.R., Ackler, S.L., Catron, N.D., Chen, J., Dayton, B.D., Ding, H., Enschede, S.H., Fairbrother, W.J., Huang, D.C., Hymowitz, S.G., Jin, S., Khaw, S.L., Kovar, P.J., Lam, L.T., Lee, J., Maecker, H.L., Marsh, K.C., Mason, K.D., Mitten, M.J., Nimmer, P.M., Oleksijew, A., Park, C.H., Park, C.M., Phillips, D.C., Roberts, A.W., Sampath, D., Seymour, J.F., Smith, M.L., Sullivan, G.M., Tahir, S.K., Tse, C., Wendt, M.D., Xiao, Y., Xue, J.C., Zhang, H., Humerickhouse, R.A., Rosenberg, S.H. & Elmore, S.W. (2013) ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nature Medicine, 19, 202-208.
9. Vogler, M., Dinsdale, D., Sun, X.M., Young, K.W., Butterworth, M., Nicotera, P., Dyer, M.J. & Cohen, G.M. (2008) A novel paradigm for rapid ABT-737-induced apoptosis involving outer mitochondrial membrane rupture in primary leukemia and lymphoma cells. Cell Death and Differentiation, 15, 820-830.
10. Vogler, M., Furdas, S.D., Jung, M., Kuwana, T., Dyer, M.J. & Cohen, G.M. (2010) Diminished sensitivity of chronic lymphocytic leukemia cells to ABT-737 and ABT-263 due to albumin binding in blood. Clinical Cancer Research, 16, 4217-4225.