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Title: ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

Journal Article · · Nature Medicine
DOI:https://doi.org/10.1038/nm.3048· OSTI ID:1247361

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
INDUSTRY
OSTI ID:
1247361
Journal Information:
Nature Medicine, Vol. 19, Issue 01, 2013; ISSN 1078-8956
Publisher:
Nature Publishing Group
Country of Publication:
United States
Language:
ENGLISH

References (43)

Bcl-2 inhibitors induce apoptosis in chronic lymphocytic leukemia cells journal December 2006
MiR-15a and miR-16-1 cluster functions in human leukemia journal March 2008
Activity of the Bcl-2 Family Inhibitor ABT-263 in a Panel of Small Cell Lung Cancer Xenograft Models journal June 2008
Bax and the mitochondrial permeability transition cooperate in the release of cytochrome c during endoplasmic reticulum-stress-induced apoptosis journal December 2006
bcl-x, a bcl-2-related gene that functions as a dominant regulator of apoptotic cell death journal August 1993
Hedgehog signaling pathway is activated in diffuse large B-cell lymphoma and contributes to tumor cell survival and proliferation journal March 2010
Structural Plasticity in a Remodeled Protein-Protein Interface journal November 1997
Crystal structure of ABT-737 complexed with Bcl-xL: implications for selectivity of antagonists of the Bcl-2 family journal June 2007
Development of a high-throughput fluorescence polarization assay for Bcl-xL journal August 2002
Discovery of ABT-263, a Bcl-family protein inhibitor: observations on targeting a large protein–protein interaction journal August 2008
Flt3 Y591 duplication and Bcl-2 overexpression are detected in acute myeloid leukemia cells with high levels of phosphorylated wild-type p53 journal November 2006
Predictive biomarkers: a paradigm shift towards personalized cancer medicine journal August 2011
Studies Leading to Potent, Dual Inhibitors of Bcl-2 and Bcl-xL journal February 2007
Cloning and structural analysis of cDNAs for bcl-2 and a hybrid bcl-2/immunoglobulin transcript resulting from the t(14;18) translocation journal October 1986
The BH3 mimetic compound, ABT-737, synergizes with a range of cytotoxic chemotherapy agents in chronic lymphocytic leukemia journal July 2009
Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity journal December 2010
Phase I Study of Navitoclax (ABT-263), a Novel Bcl-2 Family Inhibitor, in Patients With Small-Cell Lung Cancer and Other Solid Tumors journal March 2011
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 February 2012
The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo journal September 2011
Discovery of an Orally Bioavailable Small Molecule Inhibitor of Prosurvival B-Cell Lymphoma 2 Proteins journal November 2008
Navitoclax (ABT-263) and bendamustine ± rituximab induce enhanced killing of non-Hodgkin's lymphoma tumours in vivo : Navitoclax and bendamustine in lymphoma journal September 2012
Survival factor-induced extracellular signal-regulated kinase phosphorylates BIM, inhibiting its association with BAX and proapoptotic activity journal October 2004
X-ray and NMR structure of human Bcl-xL, an inhibitor of programmed cell death journal May 1996
Bcl-2 gene promotes haemopoietic cell survival and cooperates with c-myc to immortalize pre-B cells journal September 1988
An inhibitor of Bcl-2 family proteins induces regression of solid tumours journal May 2005
mRNA display selection of a high-affinity, Bcl-X L -specific binding peptide journal July 2010
The Bcl-2 apoptotic switch in cancer development and therapy journal February 2007
Structure of Bcl-x L -Bak Peptide Complex: Recognition Between Regulators of Apoptosis journal February 1997
Involvement of the bcl-2 gene in human follicular lymphoma journal June 1985
Discovery and Structure−Activity Relationship of Antagonists of B-Cell Lymphoma 2 Family Proteins with Chemopotentiation Activity in Vitro and in Vivo journal February 2006
Analysis of Bcl-2 Protein Expression in Chronic Lymphocytic Leukemia journal February 2000
The management of tumor lysis syndrome journal August 2006
The t(14;18) defines a unique subset of diffuse large B-cell lymphoma with a germinal center B-cell gene expression profile journal April 2002
VSV Oncolysis in Combination With the BCL-2 Inhibitor Obatoclax Overcomes Apoptosis Resistance in Chronic Lymphocytic Leukemia journal December 2010
Diffuse large B-cell lymphoma subgroups have distinct genetic profiles that influence tumor biology and improve gene-expression-based survival prediction journal November 2005
miR-15 and miR-16 induce apoptosis by targeting BCL2 journal September 2005
Solution structure of the antiapoptotic protein bcl-2 journal February 2001
The Hallmarks of Cancer journal January 2000
The BCL-2 protein family: opposing activities that mediate cell death journal January 2008
Programmed Anuclear Cell Death Delimits Platelet Life Span journal March 2007
ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor journal May 2008
BCL2 Expression Is a Prognostic Marker for the Activated B-Cell–Like Type of Diffuse Large B-Cell Lymphoma journal February 2006
BCL-2 dependence and ABT-737 sensitivity in acute lymphoblastic leukemia journal February 2008