Rational combination strategies to enhance venetoclax activity and overcome resistance in hematologic malignancies

Bruton’s tyrosine kinase inhibition increases BCL-2 dependence and enhances sensitivity to venetoclax in chronic lymphocytic leukemia

(2017) J Deng et al.   LEUKEMIA

Targeting BET proteins improves the therapeutic efficacy of BCL-2 inhibition in T-cell acute lymphoblastic leukemia

(2017) S Peirs et al.   LEUKEMIA

The potential combination of BCL-2 inhibitors and ibrutinib as frontline therapy in chronic lymphocytic leukemia

(2017) Andrew Aw et al.   LEUKEMIA & LYMPHOMA

Pathways and mechanisms of venetoclax resistance

(2017) Prithviraj Bose et al.   LEUKEMIA & LYMPHOMA

Combination of galectin inhibitor GCS-100 and BH3 mimetics eliminates both p53 wild type and p53 null AML cells

(2016) Peter P. Ruvolo et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Rational targeted therapies to overcome microenvironment-dependent expansion of mantle cell lymphoma

(2016) D. Chiron et al.   BLOOD

High-content screening identifies kinase inhibitors that overcome venetoclax resistance in activated CLL cells

(2016) Sina Oppermann et al.   BLOOD

BCR signaling inhibitors differ in their ability to overcome Mcl-1-mediated resistance of CLL B cells to ABT-199

(2016) K. Bojarczuk et al.   BLOOD

Venetoclax: First Global Approval

(2016) Emma D. Deeks   DRUGS

Superior anti-tumor activity of the MDM2 antagonist idasanutlin and the Bcl-2 inhibitor venetoclax in p53 wild-type acute myeloid leukemia models

(2016) Christian Lehmann et al.   Journal of Hematology & Oncology

Duvelisib treatment is associated with altered expression of apoptotic regulators that helps in sensitization of chronic lymphocytic leukemia cells to venetoclax (ABT-199)

(2016) V M Patel et al.   LEUKEMIA

Expression Profile of BCL-2, BCL-XL, and MCL-1 Predicts Pharmacological Response to the BCL-2 Selective Antagonist Venetoclax in Multiple Myeloma Models

(2016) E. A. Punnoose et al.   MOLECULAR CANCER THERAPEUTICS

Targeting BCL2 with Venetoclax in Relapsed Chronic Lymphocytic Leukemia

(2016) Andrew W. Roberts et al.   NEW ENGLAND JOURNAL OF MEDICINE

Efficacy and Biological Correlates of Response in a Phase II Study of Venetoclax Monotherapy in Patients with Acute Myelogenous Leukemia

(2016) M. Konopleva et al.   Cancer Discovery

Acquired resistance to venetoclax (ABT-199) in t(14;18) positive lymphoma cells

(2016) Juraj Bodo et al.   Oncotarget

Getting a handle on hereditary CEBPA mutations

(2015) C. D. DiNardo   BLOOD

Targeting glutaminolysis has antileukemic activity in acute myeloid leukemia and synergizes with BCL-2 inhibition

(2015) N. Jacque et al.   BLOOD

MLN4924 induces Noxa upregulation in acute myelogenous leukemia and synergizes with Bcl-2 inhibitors

(2015) K L B Knorr et al.   CELL DEATH AND DIFFERENTIATION

Pharmacological and Protein Profiling Suggests Venetoclax (ABT-199) as Optimal Partner with Ibrutinib in Chronic Lymphocytic Leukemia

(2015) F. Cervantes-Gomez et al.   CLINICAL CANCER RESEARCH

Targeting of BCL2 Family Proteins with ABT-199 and Homoharringtonine Reveals BCL2- and MCL1-Dependent Subgroups of Diffuse Large B-Cell Lymphoma

(2015) M. Klanova et al.   CLINICAL CANCER RESEARCH

BH3 profiling identifies heterogeneous dependency on Bcl-2 family members in multiple myeloma and predicts sensitivity to BH3 mimetics

(2015) C Touzeau et al.   LEUKEMIA

Synergistic induction of apoptosis in high-risk DLBCL by BCL2 inhibition with ABT-199 combined with pharmacologic loss of MCL1

(2015) L Li et al.   LEUKEMIA

Isocitrate dehydrogenase 1 and 2 mutations induce BCL-2 dependence in acute myeloid leukemia

(2015) Steven M Chan et al.   NATURE MEDICINE

Targeting glutamine metabolism in multiple myeloma enhances BIM binding to BCL-2 eliciting synthetic lethality to venetoclax

(2015) R Bajpai et al.   ONCOGENE

MCL-1 and BCL-xL-dependent resistance to the BCL-2 inhibitor ABT-199 can be overcome by preventing PI3K/AKT/mTOR activation in lymphoid malignancies

(2015) G S Choudhary et al.   Cell Death & Disease

Loss in MCL-1 function sensitizes non-Hodgkin’s lymphoma cell lines to the BCL-2-selective inhibitor venetoclax (ABT-199)

(2015) D C Phillips et al.   Blood Cancer Journal

Bcl-2high mantle cell lymphoma cells are sensitized to acadesine with ABT-199

(2015) Arnau Montraveta et al.   Oncotarget

Biological rational for sequential targeting of Bruton tyrosine kinase and Bcl-2 to overcome CD40-induced ABT-199 resistance in mantle cell lymphoma

(2015) David Chiron et al.   Oncotarget

A Bim-targeting strategy overcomes adaptive bortezomib resistance in myeloma through a novel link between autophagy and apoptosis

(2014) S. Chen et al.   BLOOD

BCL-2 family proteins as 5-Azacytidine-sensitizing targets and determinants of response in myeloid malignancies

(2014) J M Bogenberger et al.   LEUKEMIA

Targeting SQSTM1/p62 Induces Cargo Loading Failure and Converts Autophagy to Apoptosis via NBK/Bik

(2014) S. Chen et al.   MOLECULAR AND CELLULAR BIOLOGY

Targeting BCL2 for the Treatment of Lymphoid Malignancies

(2014) Mary Ann Anderson et al.   SEMINARS IN HEMATOLOGY

Targeting the mitochondrial apoptotic pathway: a preferred approach in hematologic malignancies?

(2014) K Brinkmann et al.   Cell Death & Disease

PANORAMA 2: panobinostat in combination with bortezomib and dexamethasone in patients with relapsed and bortezomib-refractory myeloma

(2013) P. G. Richardson et al.   BLOOD

Phase Ib Study of Panobinostat and Bortezomib in Relapsed or Relapsed and Refractory Multiple Myeloma

(2013) Jesús F. San-Miguel et al.   JOURNAL OF CLINICAL ONCOLOGY

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

(2013) C Touzeau et al.   LEUKEMIA

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

Death Receptor-Ligand Systems in Cancer, Cell Death, and Inflammation

(2013) H. Walczak   Cold Spring Harbor Perspectives in Biology

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

(2013) R. Pan et al.   Cancer Discovery

Dual Inhibition of Bcl-2 and Bcl-xL Strikingly Enhances PI3K Inhibition-Induced Apoptosis in Human Myeloid Leukemia Cells through a GSK3- and Bim-Dependent Mechanism

(2012) M. Rahmani et al.   CANCER RESEARCH

CDK Inhibitors Upregulate BH3-Only Proteins to Sensitize Human Myeloma Cells to BH3 Mimetic Therapies

(2012) Shuang Chen et al.   CANCER RESEARCH

Targeting MCL-1 sensitizes FLT3-ITD-positive leukemias to cytotoxic therapies

(2012) S Kasper et al.   Blood Cancer Journal

ABT-737 is highly effective against molecular subgroups of multiple myeloma

(2011) L. Bodet et al.   BLOOD

Distribution of Bim determines Mcl-1 dependence or codependence with Bcl-xL/Bcl-2 in Mcl-1-expressing myeloma cells

(2011) A. A. Morales et al.   BLOOD

Ripoptosome: a novel IAP-regulated cell death-signalling platform

(2011) G. Imre et al.   Journal of Molecular Cell Biology

The BCL-2 Family Reunion

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

FLT3-ITD up-regulates MCL-1 to promote survival of stem cells in acute myeloid leukemia via FLT3-ITD-specific STAT5 activation

(2009) G. Yoshimoto et al.   BLOOD

Proteasome inhibitors induce apoptosis in human lung cancer cells through a positive feedback mechanism and the subsequent Mcl-1 protein cleavage

(2009) B-Z Yuan et al.   ONCOGENE

Mechanism of apoptosis induction by inhibition of the anti-apoptotic BCL-2 proteins

(2008) J. E. Chipuk et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The BCL-2 protein family: opposing activities that mediate cell death

(2007) Richard J. Youle et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY