Direct Activation of Bax Protein for Cancer Therapy

Small-Molecule Bcl2 BH4 Antagonist for Lung Cancer Therapy

(2015) Bingshe Han et al.   CANCER CELL

Evolutions in fragment-based drug design: the deconstruction–reconstruction approach

(2015) Haijun Chen et al.   DRUG DISCOVERY TODAY

Peptide therapeutics: current status and future directions

(2015) Keld Fosgerau et al.   DRUG DISCOVERY TODAY

Structure-Based Lead Optimization and Biological Evaluation of BAX Direct Activators as Novel Potential Anticancer Agents

(2015) Mariano Stornaiuolo et al.   JOURNAL OF MEDICINAL CHEMISTRY

p53, a translational regulator: contribution to its tumour-suppressor activity

(2015) V Marcel et al.   ONCOGENE

Crystal structure of Bax bound to the BH3 peptide of Bim identifies important contacts for interaction

(2015) A Y Robin et al.   Cell Death & Disease

Mode of cell death induced by the HSP90 inhibitor 17-AAG (tanespimycin) is dependent on the expression of pro-apoptotic BAX

(2015) Marissa V Powers et al.   Oncotarget

Roles of the Bcl-2/Bax Ratio, Caspase-8 and 9 in Resistance of Breast Cancer Cells to Paclitaxel

(2014) Simin Sharifi et al.   Asian Pacific Journal of Cancer Prevention

Acquired mutations in BCL2 family proteins conferring resistance to the BH3 mimetic ABT-199 in lymphoma

(2014) V. Fresquet et al.   BLOOD

Activation of the Proapoptotic Bcl-2 Protein Bax by a Small Molecule Induces Tumor Cell Apoptosis

(2014) G. Zhao et al.   MOLECULAR AND CELLULAR BIOLOGY

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

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

Small-molecule Bax agonists for cancer therapy

(2014) Meiguo Xin et al.   Nature Communications

Bcl-2 Family Proteins Are Involved in the Signal Crosstalk between Endoplasmic Reticulum Stress and Mitochondrial Dysfunction in Tumor Chemotherapy Resistance

(2014) Jing Su et al.   Biomed Research International

Targeting Apoptosis Pathways for New Cancer Therapeutics

(2013) Longchuan Bai et al.   Annual Review of Medicine

Bax Crystal Structures Reveal How BH3 Domains Activate Bax and Nucleate Its Oligomerization to Induce Apoptosis

(2013) Peter E. Czabotar et al.   CELL

Loss of the proteins Bak and Bax prevents apoptosis mediated by histone deacetylase inhibitors

(2013) Caterina Ieranò et al.   CELL CYCLE

Sensitization of melanoma cells for TRAIL-induced apoptosis by activation of mitochondrial pathways via Bax

(2013) Sandra-Annika Quast et al.   EUROPEAN JOURNAL OF CELL BIOLOGY

Hsp90 Inhibitors Promote p53-Dependent Apoptosis through PUMA and Bax

(2013) Kan He et al.   MOLECULAR CANCER THERAPEUTICS

Pulling the plug on BCL-XL

(2013) Paul S Jeng 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

The 'rule of three' for fragment-based drug discovery: where are we now?

(2013) Harren Jhoti et al.   NATURE REVIEWS DRUG DISCOVERY

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

Down-Regulation of BAX Gene During Carcinogenesis and Acquisition of Resistance to 5-FU in Colorectal Cancer

(2013) Mehdi Manoochehri et al.   PATHOLOGY & ONCOLOGY RESEARCH

Sensitization of melanoma cells for TRAIL-induced apoptosis by BMS-345541 correlates with altered phosphorylation and activation of Bax

(2013) A Berger et al.   Cell Death & Disease

Wip1 suppresses apoptotic cell death through direct dephosphorylation of BAX in response to γ-radiation

(2013) J-Y Song et al.   Cell Death & Disease

The Future of Peptide-based Drugs

(2012) David J. Craik et al.   Chemical Biology & Drug Design

Unleashing a “True” pSer-Mimic in the Cell

(2012) Kaushik Panigrahi et al.   CHEMISTRY & BIOLOGY

Synthesis of a Phosphoserine Mimetic Prodrug with Potent 14-3-3 Protein Inhibitory Activity

(2012) Allison Arrendale et al.   CHEMISTRY & BIOLOGY

Targeting the Bcl-2 family for cancer therapy

(2012) Shibu Thomas et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Direct and selective small-molecule activation of proapoptotic BAX

(2012) Evripidis Gavathiotis et al.   Nature Chemical Biology

Obesity and Hepatosteatosis in Mice with Enhanced Oxidative DNA Damage Processing in Mitochondria

(2011) Haihong Zhang et al.   AMERICAN JOURNAL OF PATHOLOGY

Bortezomib Primes Glioblastoma, Including Glioblastoma Stem Cells, for TRAIL by Increasing tBid Stability and Mitochondrial Apoptosis

(2011) T. Unterkircher et al.   CLINICAL CANCER RESEARCH

A Unified Model of Mammalian BCL-2 Protein Family Interactions at the Mitochondria

(2011) Fabien Llambi et al.   MOLECULAR CELL

Integrating stress signals at the endoplasmic reticulum: The BCL-2 protein family rheostat

(2010) Diego Rodriguez et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

MiR-21 protected human glioblastoma U87MG cells from chemotherapeutic drug temozolomide induced apoptosis by decreasing Bax/Bcl-2 ratio and caspase-3 activity

(2010) Lei Shi et al.   BRAIN RESEARCH

Apoptosis: embedded in membranes

(2010) Christian Bogner et al.   CURRENT OPINION IN CELL BIOLOGY

Drugs targeting Bcl-2 family members as an emerging strategy in cancer

(2010) Brian Leber et al.   EXPERT REVIEWS IN MOLECULAR MEDICINE

Mitochondria and cell death: outer membrane permeabilization and beyond

(2010) Stephen W. G. Tait et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Still embedded together binding to membranes regulates Bcl-2 protein interactions

(2010) B Leber et al.   ONCOGENE

The Bcl-2 family in autoimmune and degenerative disorders

(2009) Delphine Mérino et al.   APOPTOSIS

Atorvastatin mediates increases in intralesional BAX and BAK expression in human end-stage abdominal aortic aneurysms

(2009) Morris Schweitzer et al.   CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY

Bax activation by Bim?

(2009) P E Czabotar et al.   CELL DEATH AND DIFFERENTIATION

Bcl-2 Inhibitors: Targeting Mitochondrial Apoptotic Pathways in Cancer Therapy

(2009) M. H. Kang et al.   CLINICAL CANCER RESEARCH

Mitochondrial cell death effectors

(2009) Dirk Brenner et al.   CURRENT OPINION IN CELL BIOLOGY

Impaired Mitochondrial Function and Insulin Resistance of Skeletal Muscle in Mitochondrial Diabetes

(2009) J. Szendroedi et al.   DIABETES CARE

Synthetic therapeutic peptides: science and market

(2009) Patrick Vlieghe et al.   DRUG DISCOVERY TODAY

Conformational changes and protein stability of the pro-apoptotic protein Bax

(2009) Stephanie Bleicken et al.   JOURNAL OF BIOENERGETICS AND BIOMEMBRANES

Puma strikes Bax: Figure 1.

(2009) Anthony Letai   JOURNAL OF CELL BIOLOGY

Bax activation by the BH3-only protein Puma promotes cell dependence on antiapoptotic Bcl-2 family members

(2009) Tristan Gallenne et al.   JOURNAL OF CELL BIOLOGY

The mitochondrial death pathway: a promising therapeutic target in diseases

(2009) Sanjeev Gupta et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Stepwise Activation of BAX and BAK by tBID, BIM, and PUMA Initiates Mitochondrial Apoptosis

(2009) Hyungjin Kim et al.   MOLECULAR CELL

Cell Death

(2009) Richard S. Hotchkiss et al.   NEW ENGLAND JOURNAL OF MEDICINE

BH3-only proteins and their roles in programmed cell death

(2009) M Giam et al.   ONCOGENE

Improving Oral Bioavailability of Peptides by Multiple N-Methylation: Somatostatin Analogues

(2008) Eric Biron et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

(2008) C. Tse et al.   CANCER RESEARCH

Mitochondrial alterations in Parkinson’s disease: new clues

(2008) Miquel Vila et al.   JOURNAL OF NEUROCHEMISTRY

Erlotinib Induces Mitochondrial-Mediated Apoptosis in Human H3255 Non-Small-Cell Lung Cancer Cells with Epidermal Growth Factor ReceptorL858R Mutation through Mitochondrial Oxidative Phosphorylation-Dependent Activation of BAX and BAK

(2008) Y.-H. Ling et al.   MOLECULAR PHARMACOLOGY

BAX activation is initiated at a novel interaction site

(2008) Evripidis Gavathiotis et al.   NATURE

BCL-2 family antagonists for cancer therapy

(2008) Guillaume Lessene et al.   NATURE REVIEWS DRUG DISCOVERY

Mitochondrial Bax translocation partially mediates synergistic cytotoxicity between histone deacetylase inhibitors and proteasome inhibitors in glioma cells

(2008) Chunrong Yu et al.   NEURO-ONCOLOGY

Bcl-2 family proteins and cancer

(2008) K W Yip et al.   ONCOGENE

How do BCL-2 proteins induce mitochondrial outer membrane permeabilization?

(2008) Jerry E. Chipuk et al.   TRENDS IN CELL BIOLOGY