Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy

A phase I safety and pharmacokinetic (PK) study of navitoclax (N) in combination with docetaxel (D) in patients (pts) with solid tumors.

(2017) M. Puglisi et al.   JOURNAL OF CLINICAL ONCOLOGY

Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax)

(2015) J D Leverson et al.   Cell Death & Disease

Regulating cell death at, on, and in membranes

(2014) Xiaoke Chi et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Elimination of quiescent/slow-proliferating cancer stem cells by Bcl-XL inhibition in non-small cell lung cancer

(2014) A Zeuner et al.   CELL DEATH AND DIFFERENTIATION

Acute myeloid leukemia cells harboring MLL fusion genes or with the acute promyelocytic leukemia phenotype are sensitive to the Bcl-2-selective inhibitor ABT-199

(2014) X Niu et al.   LEUKEMIA

Both leukaemic and normal peripheral B lymphoid cells are highly sensitive to the selective pharmacological inhibition of prosurvival Bcl-2 with ABT-199

(2014) S L Khaw et al.   LEUKEMIA

Ex vivoactivity of BCL-2 family inhibitors ABT-199 and ABT-737 combined with 5-azacytidine in myeloid malignancies

(2014) James M. Bogenberger et al.   LEUKEMIA & LYMPHOMA

Clinical development success rates for investigational drugs

(2014) Michael Hay et al.   NATURE BIOTECHNOLOGY

Bcl-xL controls a switch between cell death modes during mitotic arrest

(2014) N Bah et al.   Cell Death & Disease

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity

(2014) Zhi-Fu Tao et al.   ACS Medicinal Chemistry Letters

Maturation Stage of T-cell Acute Lymphoblastic Leukemia Determines BCL-2 versus BCL-XL Dependence and Sensitivity to ABT-199

(2014) T. N. Chonghaile et al.   Cancer Discovery

ABT-199, a new Bcl-2-specific BH3 mimetic, has in vivo efficacy against aggressive Myc-driven mouse lymphomas without provoking thrombocytopenia

(2013) C. J. Vandenberg et al.   BLOOD

Targeting BCL-2 with the BH3 Mimetic ABT-199 in Estrogen Receptor-Positive Breast Cancer

(2013) François Vaillant et al.   CANCER CELL

An Interactive Resource to Identify Cancer Genetic and Lineage Dependencies Targeted by Small Molecules

(2013) Amrita Basu et al.   CELL

The Bcl-2 specific BH3 mimetic ABT-199: a promising targeted therapy for t(11;14) multiple myeloma

(2013) C Touzeau et al.   LEUKEMIA

BCL2-specific inhibitor ABT-199 synergizes strongly with cytarabine against the early immature LOUCY cell line but not more-differentiated T-ALL cell lines

(2013) N M Anderson et al.   LEUKEMIA

Structure-guided design of a selective BCL-XL inhibitor

(2013) Guillaume Lessene et al.   Nature Chemical Biology

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

(2013) Andrew J Souers et al.   NATURE MEDICINE

Control of apoptosis by the BCL-2 protein family: implications for physiology and therapy

(2013) Peter E. Czabotar et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Selective BCL-2 Inhibition by ABT-199 Causes On-Target Cell Death in Acute Myeloid Leukemia

(2013) R. Pan et al.   Cancer Discovery

BH3 profiling – Measuring integrated function of the mitochondrial apoptotic pathway to predict cell fate decisions

(2012) Victoria Del Gaizo Moore et al.   CANCER LETTERS

Navitoclax (ABT-263) Reduces Bcl-xL-Mediated Chemoresistance in Ovarian Cancer Models

(2012) M. Wong et al.   MOLECULAR CANCER THERAPEUTICS

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

Navitoclax Enhances the Efficacy of Taxanes in Non–Small Cell Lung Cancer Models

(2011) Nguyen Tan et al.   CLINICAL CANCER RESEARCH

Phase I Study of Navitoclax (ABT-263), a Novel Bcl-2 Family Inhibitor, in Patients With Small-Cell Lung Cancer and Other Solid Tumors

(2011) Leena Gandhi et al.   JOURNAL OF CLINICAL ONCOLOGY

Substantial Susceptibility of Chronic Lymphocytic Leukemia to BCL2 Inhibition: Results of a Phase I Study of Navitoclax in Patients With Relapsed or Refractory Disease

(2011) Andrew W. Roberts et al.   JOURNAL OF CLINICAL ONCOLOGY

The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

(2011) J. Chen et al.   MOLECULAR CANCER THERAPEUTICS

Sensitization of BCL-2-expressing breast tumors to chemotherapy by the BH3 mimetic ABT-737

(2011) S. R. Oakes et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Bcl-2 inhibitor ABT-263 enhances the response of multiple chemotherapeutic regimens in hematologic tumors in vivo

(2010) Scott Ackler et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

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

(2010) Wyndham H Wilson et al.   LANCET ONCOLOGY

The BCL-2 Family Reunion

(2010) Jerry E. Chipuk et al.   MOLECULAR CELL

ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor

(2008) C. Tse et al.   CANCER RESEARCH

Activity of the Bcl-2 Family Inhibitor ABT-263 in a Panel of Small Cell Lung Cancer Xenograft Models

(2008) A. R. Shoemaker et al.   CLINICAL CANCER RESEARCH