Therapeutic targeting of Bcl-2 family for treatment of B-cell malignancies

Sabutoclax (BI97C1) and BI112D1, Putative Inhibitors of MCL-1, Induce Mitochondrial Fragmentation Either Upstream of or Independent of Apoptosis

(2015) Shankar Varadarajan et al.   NEOPLASIA

Mechanism-based pharmacokinetic/pharmacodynamic meta-analysis of navitoclax (ABT-263) induced thrombocytopenia

(2014) Aksana Kaefer et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Pan-Bcl-2 Inhibitor, GX15-070 (Obatoclax), Decreases Human T Regulatory Lymphocytes while Preserving Effector T Lymphocytes: A Rationale for Its Use in Combination Immunotherapy

(2014) P. S. Kim et al.   JOURNAL OF IMMUNOLOGY

Hydrocarbon-Stapled Peptides: Principles, Practice, and Progress

(2014) Loren D. Walensky et al.   JOURNAL OF MEDICINAL CHEMISTRY

Evaluation of Apoptosis Induction by Concomitant Inhibition of MEK, mTOR, and Bcl-2 in Human Acute Myelogenous Leukemia Cells

(2014) W. Zhang et al.   MOLECULAR CANCER THERAPEUTICS

Inhibition of the MDM2 E3 Ligase Induces Apoptosis and Autophagy in Wild-Type and Mutant p53 Models of Multiple Myeloma, and Acts Synergistically with ABT-737

(2014) Dongmin Gu et al.   PLoS One

Small-molecule Bax agonists for cancer therapy

(2014) Meiguo Xin et al.   Nature Communications

Crosstalk between apoptosis, necrosis and autophagy

(2013) Vassiliki Nikoletopoulou et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

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

MYC/BCL2 protein coexpression contributes to the inferior survival of activated B-cell subtype of diffuse large B-cell lymphoma and demonstrates high-risk gene expression signatures: a report from The International DLBCL Rituximab-CHOP Consortium Program

(2013) S. Hu et al.   BLOOD

Evaluation and critical assessment of putative MCL-1 inhibitors

(2013) S Varadarajan et al.   CELL DEATH AND DIFFERENTIATION

Obatoclax (GX15-070) triggers necroptosis by promoting the assembly of the necrosome on autophagosomal membranes

(2013) F Basit et al.   CELL DEATH AND DIFFERENTIATION

A phase I study of AT-101 with cisplatin and etoposide in patients with advanced solid tumors with an expanded cohort in extensive-stage small cell lung cancer

(2013) William R. Schelman et al.   INVESTIGATIONAL NEW DRUGS

Bcl-2/Bcl-xL Inhibition Increases the Efficacy of MEK Inhibition Alone and in Combination with PI3 Kinase Inhibition in Lung and Pancreatic Tumor Models

(2013) N. Tan et al.   MOLECULAR CANCER THERAPEUTICS

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

(2013) Andrew J Souers et al.   NATURE MEDICINE

Molecular Pathways: The Role of NR4A Orphan Nuclear Receptors in Cancer

(2012) H. M. Mohan et al.   CLINICAL CANCER RESEARCH

Late-phase investigational approaches for the treatment of relapsed/refractory acute myeloid leukemia

(2012) Katarzyna Jamieson et al.   EXPERT OPINION ON PHARMACOTHERAPY

Anti-apoptotic MCL-1 localizes to the mitochondrial matrix and couples mitochondrial fusion to respiration

(2012) Rhonda M. Perciavalle et al.   NATURE CELL BIOLOGY

Direct and selective small-molecule activation of proapoptotic BAX

(2012) Evripidis Gavathiotis et al.   Nature Chemical Biology

Bcl-2 is a better ABT-737 target than Bcl-xL or Bcl-w and only Noxa overcomes resistance mediated by Mcl-1, Bfl-1, or Bcl-B

(2012) R W Rooswinkel et al.   Cell Death & Disease

Bcl-xL-inhibitory BH3 mimetics can induce a transient thrombocytopathy that undermines the hemostatic function of platelets

(2011) S. M. Schoenwaelder et al.   BLOOD

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

BCL2 Predicts Survival in Germinal Center B-cell-like Diffuse Large B-cell Lymphoma Treated with CHOP-like Therapy and Rituximab

(2011) J. Iqbal et al.   CLINICAL CANCER RESEARCH

Targeting Mcl-1 for the therapy of cancer

(2011) Bridget A Quinn et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Apoptotic cell signaling in cancer progression and therapy

(2011) Jessica Plati et al.   Integrative Biology

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

MEK inhibition enhances ABT-737-induced leukemia cell apoptosis via prevention of ERK-activated MCL-1 induction and modulation of MCL-1/BIM complex

(2011) M Konopleva et al.   LEUKEMIA

The novel antisense Bcl-2 inhibitor SPC2996 causes rapid leukemic cell clearance and immune activation in chronic lymphocytic leukemia

(2011) J Dürig et al.   LEUKEMIA

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

Acquired resistance to ABT-737 in lymphoma cells that up-regulate MCL-1 and BFL-1

(2010) D. Yecies et al.   BLOOD

Apogossypolone, a nonpeptidic small molecule inhibitor targeting Bcl-2 family proteins, effectively inhibits growth of diffuse large cell lymphoma cells in vitro and in vivo

(2010) Yuan Sun et al.   CANCER BIOLOGY & THERAPY

Phase I Dose Finding Studies of Obatoclax (GX15-070), a Small Molecule Pan-BCL-2 Family Antagonist, in Patients with Advanced Solid Tumors or Lymphoma

(2010) J. J. Hwang et al.   CLINICAL CANCER RESEARCH

Tyrosine dephosphorylation is required for Bak activation in apoptosis

(2010) Joanna L Fox et al.   EMBO JOURNAL

The BH3 α-Helical Mimic BH3-M6 Disrupts Bcl-XL, Bcl-2, and MCL-1 Protein-Protein Interactions with Bax, Bak, Bad, or Bim and Induces Apoptosis in a Bax- and Bim-dependent Manner

(2010) Aslamuzzaman Kazi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

BI-97C1, an Optically Pure Apogossypol Derivative as Pan-Active Inhibitor of Antiapoptotic B-Cell Lymphoma/Leukemia-2 (Bcl-2) Family Proteins

(2010) Jun Wei et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

An Open-Label, Multicenter, Phase I/II Study of Single-Agent AT-101 in Men with Castrate-Resistant Prostate Cancer

(2009) G. Liu et al.   CLINICAL CANCER RESEARCH

5-Year Survival in Patients With Relapsed or Refractory Chronic Lymphocytic Leukemia in a Randomized, Phase III Trial of Fludarabine Plus Cyclophosphamide With or Without Oblimersen

(2009) Susan O'Brien et al.   JOURNAL OF CLINICAL ONCOLOGY

Gossypol, a BH3 mimetic, induces apoptosis in chronic lymphocytic leukemia cells

(2008) K. Balakrishnan et al.   BLOOD

Mcl-1 expression has in vitro and in vivo significance in chronic lymphocytic leukemia and is associated with other poor prognostic markers

(2008) C. Pepper et al.   BLOOD

Targeting Bcl-2 family members with the BH3 mimetic AT-101 markedly enhances the therapeutic effects of chemotherapeutic agents in in vitro and in vivo models of B-cell lymphoma

(2008) L. Paoluzzi et al.   BLOOD

Phase I study of obatoclax mesylate (GX15-070), a small molecule pan-Bcl-2 family antagonist, in patients with advanced chronic lymphocytic leukemia

(2008) S. M. O'Brien et al.   BLOOD

Phase II multicenter study of oblimersen sodium, a Bcl-2 antisense oligonucleotide, in combination with rituximab in patients with recurrent B-cell non-Hodgkin lymphoma

(2008) Barbara Pro et al.   BRITISH JOURNAL OF HAEMATOLOGY

Mechanisms of Antileukemic Activity of the Novel Bcl-2 Homology Domain-3 Mimetic GX15-070 (Obatoclax)

(2008) M. Konopleva et al.   CANCER RESEARCH

To kill a tumor cell: the potential of proapoptotic receptor agonists

(2008) Avi Ashkenazi et al.   JOURNAL OF CLINICAL INVESTIGATION

Discovery of an Orally Bioavailable Small Molecule Inhibitor of Prosurvival B-Cell Lymphoma 2 Proteins

(2008) Cheol-Min Park et al.   JOURNAL OF MEDICINAL CHEMISTRY

BCL-2 phosphorylation modulates sensitivity to the BH3 mimetic GX15-070 (Obatoclax) and reduces its synergistic interaction with bortezomib in chronic lymphocytic leukemia cells

(2008) P Pérez-Galán et al.   LEUKEMIA