IAP antagonists Birinapant and AT-406 efficiently synergise with either TRAIL, BRAF, or BCL-2 inhibitors to sensitise BRAFV600E colorectal tumour cells to apoptosis

Patient-derived glioblastoma cells show significant heterogeneity in treatment responses to the inhibitor-of-apoptosis-protein antagonist birinapant

(2015) Z Zakaria et al.   BRITISH JOURNAL OF CANCER

Safety, pharmacokinetics, and pharmacodynamic properties of oral DEBIO1143 (AT-406) in patients with advanced cancer: results of a first-in-man study

(2015) Herbert I. Hurwitz et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Molecular Pathways: Leveraging the BCL-2 Interactome to Kill Cancer Cells--Mitochondrial Outer Membrane Permeabilization and Beyond

(2015) H. Brahmbhatt et al.   CLINICAL CANCER RESEARCH

Effect of a Smac Mimetic (TL32711, Birinapant) on the Apoptotic Program and Apoptosis Biomarkers Examined with Validated Multiplex Immunoassays Fit for Clinical Use

(2015) A. K. Srivastava et al.   CLINICAL CANCER RESEARCH

5-Fluorouracil preferentially sensitizes mutant KRAS non-small cell lung carcinoma cells to TRAIL-induced apoptosis

(2015) Haizhen Wang et al.   Molecular Oncology

An apoptosis-enhancing drug overcomes platinum resistance in a tumour-initiating subpopulation of ovarian cancer

(2015) D. M. Janzen et al.   Nature Communications

Combining TRAIL with PI3 kinase or HSP90 inhibitors enhances apoptosis in colorectal cancer cells via suppression of survival signaling

(2015) Grazia Saturno et al.   Oncotarget

BRAF vs RAS oncogenes: Are mutations of the same pathway equal? Differential signalling and therapeutic implications

(2015) Eftychia Oikonomou et al.   Oncotarget

Birinapant, a Smac-Mimetic with Improved Tolerability for the Treatment of Solid Tumors and Hematological Malignancies

(2014) Stephen M. Condon et al.   JOURNAL OF MEDICINAL CHEMISTRY

AT-406, an IAP Inhibitor, Activates Apoptosis and Induces Radiosensitization of Normoxic and Hypoxic Cervical Cancer Cells

(2014) Jing Lu et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

Synergistic Targeting of AML Stem/Progenitor Cells With IAP Antagonist Birinapant and Demethylating Agents

(2014) Bing Z. Carter et al.   JNCI-Journal of the National Cancer Institute

Birinapant (TL32711), a Bivalent SMAC Mimetic, Targets TRAF2-Associated cIAPs, Abrogates TNF-Induced NF- B Activation, and Is Active in Patient-Derived Xenograft Models

(2014) C. A. Benetatos et al.   MOLECULAR CANCER THERAPEUTICS

TRAIL-R2-specific antibodies and recombinant TRAIL can synergise to kill cancer cells

(2014) M H Tuthill et al.   ONCOGENE

Temporal and Spatial Evolution of Therapy-Induced Tumor Apoptosis Detected by Caspase-3-Selective Molecular Imaging

(2013) Q.-D. Nguyen et al.   CLINICAL CANCER RESEARCH

The Novel SMAC Mimetic Birinapant Exhibits Potent Activity against Human Melanoma Cells

(2013) C. Krepler et al.   CLINICAL CANCER RESEARCH

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

(2013) Andrew J Souers et al.   NATURE MEDICINE

IAPs on the move: role of inhibitors of apoptosis proteins in cell migration

(2013) T K Oberoi-Khanuja et al.   Cell Death & Disease

Smac mimetic Birinapant induces apoptosis and enhances TRAIL potency in inflammatory breast cancer cells in an IAP-dependent and TNF-α-independent mechanism

(2012) Jennifer L. Allensworth et al.   BREAST CANCER RESEARCH AND TREATMENT

AT-406, an orally active antagonist of multiple inhibitor of apoptosis proteins, inhibits progression of human ovarian cancer

(2012) Melissa K. Brunckhorst et al.   CANCER BIOLOGY & THERAPY

TRAIL Signaling and Synergy Mechanisms Used in TRAIL-Based Combination Therapies

(2012) C. T. Hellwig et al.   MOLECULAR CANCER THERAPEUTICS

Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR

(2012) Anirudh Prahallad et al.   NATURE

Vemurafenib: the first drug approved for BRAF-mutant cancer

(2012) Gideon Bollag et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting IAP proteins for therapeutic intervention in cancer

(2012) Simone Fulda et al.   NATURE REVIEWS DRUG DISCOVERY

A Potent and Orally Active Antagonist (SM-406/AT-406) of Multiple Inhibitor of Apoptosis Proteins (IAPs) in Clinical Development for Cancer Treatment

(2011) Qian Cai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective BRAFV600E Inhibitor PLX4720, Requires TRAIL Assistance to Overcome Oncogenic PIK3CA Resistance

(2011) Eftychia Oikonomou et al.   PLoS One

Ceramide synthase 6 modulates TRAIL sensitivity and nuclear translocation of active caspase-3 in colon cancer cells

(2009) S White-Gilbertson et al.   ONCOGENE

Preclinicalversusclinical drug combination studies

(2008) Ting-Chao Chou   LEUKEMIA & LYMPHOMA

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

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