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)

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

Regulating cell death at, on, and in membranes

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

Fragment-based discovery of potent inhibitors of the anti-apoptotic MCL-1 protein

(2014) Andrew M. Petros et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting of MCL-1 kills MYC-driven mouse and human lymphomas even when they bear mutations in p53

(2014) G. L. Kelly et al.   GENES & DEVELOPMENT

Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL

(2014) Michael F. T. Koehler et al.   ACS Medicinal Chemistry Letters

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

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

Hydroxyquinoline-derived compounds and analoguing of selective Mcl-1 inhibitors using a functional biomarker

(2013) David J. Richard et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Evaluation and critical assessment of putative MCL-1 inhibitors

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

Structure-Guided Rational Design of α/β-Peptide Foldamers with High Affinity for BCL-2 Family Prosurvival Proteins

(2013) Brian J. Smith et al.   CHEMBIOCHEM

Loss of MCL-1 leads to impaired autophagy and rapid development of heart failure

(2013) R. L. Thomas et al.   GENES & DEVELOPMENT

Deletion of MCL-1 causes lethal cardiac failure and mitochondrial dysfunction

(2013) X. Wang et al.   GENES & DEVELOPMENT

Discovery of Potent and Selective Benzothiazole Hydrazone Inhibitors of Bcl-XL

(2013) Brad E. Sleebs et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Novel Small-Molecule Inhibitor of Mcl-1 Blocks Pancreatic Cancer Growth In Vitro and In Vivo

(2013) F. Abulwerdi et al.   MOLECULAR CANCER THERAPEUTICS

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

Purported Mcl-1 inhibitor marinopyrrole A fails to show selective cytotoxicity for Mcl-1-dependent cell lines

(2013) J M Eichhorn et al.   Cell Death & Disease

Chemical Genomics Identifies Small-Molecule MCL1 Repressors and BCL-xL as a Predictor of MCL1 Dependency

(2012) Guo Wei et al.   CANCER CELL

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

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

A Competitive Stapled Peptide Screen Identifies a Selective Small Molecule that Overcomes MCL-1-Dependent Leukemia Cell Survival

(2012) Nicole A. Cohen et al.   CHEMISTRY & BIOLOGY

Suppression of myeloid cell leukemia-1 (Mcl-1) enhances chemotherapy-associated apoptosis in gastric cancer cells

(2012) Hideko Akagi et al.   Gastric Cancer

Anti-apoptotic Mcl-1 is essential for the development and sustained growth of acute myeloid leukemia

(2012) S. P. Glaser et al.   GENES & DEVELOPMENT

Discovery of Marinopyrrole A (Maritoclax) as a Selective Mcl-1 Antagonist that Overcomes ABT-737 Resistance by Binding to and Targeting Mcl-1 for Proteasomal Degradation

(2012) Kenichiro Doi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of Potent Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods and Structure-Based Design

(2012) Anders Friberg et al.   JOURNAL OF MEDICINAL CHEMISTRY

Rational Design of Proteolytically Stable, Cell-Permeable Peptide-Based Selective Mcl-1 Inhibitors

(2012) Avinash Muppidi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

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

Delving deeper: MCL-1's contributions to normal and cancer biology

(2012) Rhonda M. Perciavalle et al.   TRENDS IN CELL BIOLOGY

Direct visualization of Bcl-2 family protein interactions using live cell fluorescent protein redistribution assays

(2012) C Wong et al.   Cell Death & Disease

Identification of a Novel Mcl-1 Protein Binding Motif

(2011) William J. Placzek et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Multiple BH3 Mimetics Antagonize Antiapoptotic MCL1 Protein by Inducing the Endoplasmic Reticulum Stress Response and Up-regulating BH3-only Protein NOXA

(2011) Tina C. Albershardt et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Sensitivity to antitubulin chemotherapeutics is regulated by MCL1 and FBW7

(2011) Ingrid E. Wertz et al.   NATURE

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

Probing the Probes: Fitness Factors For Small Molecule Tools

(2010) Paul Workman et al.   CHEMISTRY & BIOLOGY

The Bcl-xL inhibitor, ABT-737, efficiently induces apoptosis and suppresses growth of hepatoma cells in combination with sorafenib

(2010) Hayato Hikita et al.   HEPATOLOGY

Mcl1 haploinsufficiency protects mice from Myc-induced acute myeloid leukemia

(2010) Zhifu Xiang et al.   JOURNAL OF CLINICAL INVESTIGATION

Structural Insights into the Design of Small Molecule Inhibitors That Selectively Antagonize Mcl-1

(2010) Paul H. Bernardo et al.   JOURNAL OF MEDICINAL CHEMISTRY

The BCL-2 Family Reunion

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

The landscape of somatic copy-number alteration across human cancers

(2010) Rameen Beroukhim et al.   NATURE

The MCL-1 BH3 helix is an exclusive MCL-1 inhibitor and apoptosis sensitizer

(2010) Michelle L Stewart et al.   Nature Chemical Biology

Mcl-1 is critical for survival in a subgroup of non-small-cell lung cancer cell lines

(2010) H Zhang et al.   ONCOGENE

Mcl-1 and Bcl-xL cooperatively maintain integrity of hepatocytes in developing and adult murine liver

(2009) Hayato Hikita et al.   HEPATOLOGY

Inducing apoptosis and enhancing chemosensitivity to Gemcitabine via RNA interference targeting Mcl-1 gene in pancreatic carcinoma cell

(2008) San-Hua Wei et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

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

Knockout of myeloid cell leukemia-1 induces liver damage and increases apoptosis susceptibility of murine hepatocytes

(2008) Binje Vick et al.   HEPATOLOGY

A novel BH3 ligand that selectively targets Mcl-1 reveals that apoptosis can proceed without Mcl-1 degradation

(2008) Erinna F. Lee et al.   JOURNAL OF CELL BIOLOGY