Small molecules targeting Mcl-1: the search for a silver bullet in cancer therapy

Design, synthesis and evaluation of marinopyrrole derivatives as selective inhibitors of Mcl-1 binding to pro-apoptotic Bim and dual Mcl-1/Bcl-xL inhibitors

(2015) Rongshi Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Mcl-1 antagonism is a potential therapeutic strategy in a subset of solid cancers

(2015) Michele Modugno et al.   EXPERIMENTAL CELL RESEARCH

Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity

(2015) Milan Bruncko et al.   JOURNAL OF MEDICINAL CHEMISTRY

Marinopyrroles: Unique Drug Discoveries Based on Marine Natural Products

(2015) Rongshi Li   MEDICINAL RESEARCH REVIEWS

The promise and peril of chemical probes

(2015) Cheryl H Arrowsmith et al.   Nature Chemical Biology

Small molecule Mcl-1 inhibitors for the treatment of cancer

(2015) Johannes Belmar et al.   PHARMACOLOGY & THERAPEUTICS

Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy

(2015) Joel D. Leverson et al.   Science Translational Medicine

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)

(2015) J D Leverson et al.   Cell Death & Disease

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

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

MCL-1 but not BCL-XL is critical for the development and sustained expansion of thymic lymphoma in p53-deficient mice

(2014) S. Grabow et al.   BLOOD

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

3-Substituted-N-(4-Hydroxynaphthalen-1-yl)arylsulfonamides as a Novel Class of Selective Mcl-1 Inhibitors: Structure-Based Design, Synthesis, SAR, and Biological Evaluation

(2014) Fardokht A. Abulwerdi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identifying local co-regulation relationships in gene expression data

(2014) Yonggang Pei et al.   JOURNAL OF THEORETICAL BIOLOGY

Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-xL Binding to Bim

(2014) Chunwei Cheng et al.   Marine Drugs

The Bcl-2/xL inhibitor ABT-263 increases the stability of Mcl-1 mRNA and protein in hepatocellular carcinoma cells

(2014) Bin Wang et al.   Molecular Cancer

Chemistry: Chemical con artists foil drug discovery

(2014) Jonathan Baell et al.   NATURE

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

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

Modulation of Mcl-1 sensitizes glioblastoma to TRAIL-induced apoptosis

(2013) Á. C. Murphy et al.   APOPTOSIS

Simultaneous knock-down of Bcl-xL and Mcl-1 induces apoptosis through Bax activation in pancreatic cancer cells

(2013) Hiroki Takahashi et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

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

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

Requirement for antiapoptotic MCL-1 in the survival of BCR-ABL B-lineage acute lymphoblastic leukemia

(2013) B. Koss et al.   BLOOD

Cell death and the mitochondria: therapeutic targeting of the BCL-2 family-driven pathway

(2013) M J Roy et al.   BRITISH JOURNAL OF PHARMACOLOGY

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

Characterization of the Stereochemical Structures of 2H-Thiazolo[3,2-a]pyrimidine Compounds and Their Binding Affinities for Anti-apoptotic Bcl-2 Family Proteins

(2013) Yaochun Xu et al.   ChemMedChem

De Novo Design, Synthesis and Evaluation of Benzylpiperazine Derivatives as Highly Selective Binders of Mcl-1

(2013) Xiao Ding et al.   ChemMedChem

Cyclin-dependent kinase inhibitor therapy for hematologic malignancies

(2013) Prithviraj Bose et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

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 Mcl-1/Bcl-xL Dual Inhibitors by Using a Hybridization Strategy Based on Structural Analysis of Target Proteins

(2013) Yuta Tanaka et al.   JOURNAL OF MEDICINAL CHEMISTRY

The novel BH3 α-helix mimetic JY-1-106 induces apoptosis in a subset of cancer cells (lung cancer, colon cancer and mesothelioma) by disrupting Bcl-xL and Mcl-1 protein–protein interactions with Bak

(2013) Xiaobo Cao et al.   Molecular Cancer

Structure-guided design of a selective BCL-XL inhibitor

(2013) Guillaume Lessene et al.   Nature Chemical Biology

Antiapoptotic Mcl-1 is critical for the survival and niche-filling capacity of Foxp3+ regulatory T cells

(2013) Wim Pierson et al.   NATURE IMMUNOLOGY

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

Proteasomal Degradation of Mcl-1 by Maritoclax Induces Apoptosis and Enhances the Efficacy of ABT-737 in Melanoma Cells

(2013) Manoj K. Pandey et al.   PLoS One

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

8-Hydroxyquinolines: a review of their metal chelating properties and medicinal applications

(2013) Virapong Prachayasittikul et al.   Drug Design Development and Therapy

Stabilizing the Pro-Apoptotic BimBH3 Helix (BimSAHB) Does Not Necessarily Enhance Affinity or Biological Activity

(2012) Toru Okamoto et al.   ACS Chemical Biology

3-Thiomorpholin-8-oxo-8H-acenaphtho [1,2-b] pyrrole-9-carbonitrile (S1) derivatives as pan-Bcl-2-inhibitors of Bcl-2, Bcl-xL and Mcl-1

(2012) Ting Song et al.   BIOORGANIC & MEDICINAL CHEMISTRY

The downregulation of Mcl-1 via USP9X inhibition sensitizes solid tumors to Bcl-xl inhibition

(2012) Chander Peddaboina et al.   BMC CANCER

Myeloid cell leukemia-1 is a key molecular target for mithramycin A-induced apoptosis in androgen-independent prostate cancer cells and a tumor xenograft animal model

(2012) Eun-Sun Choi et al.   CANCER LETTERS

Mcl-1 Phosphorylation Defines ABT-737 Resistance That Can Be Overcome by Increased NOXA Expression in Leukemic B cells

(2012) S. Mazumder et al.   CANCER RESEARCH

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

Novel soluble myeloid cell leukemia sequence 1 (Mcl-1) inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (4g) developed using a fragment-based approach

(2012) Zhichao Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Rhodanine as a scaffold in drug discovery: a critical review of its biological activities and mechanisms of target modulation

(2012) Tihomir Tomašić et al.   Expert Opinion on Drug Discovery

Targeting the Bcl-2 family for cancer therapy

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

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

Inhibition of Mcl-1 Promotes Senescence in Cancer Cells: Implications for Preventing Tumor Growth and Chemotherapy Resistance

(2012) E. Bolesta et al.   MOLECULAR AND CELLULAR BIOLOGY

Hallmarks of cancer: of all cancer cells, all the time?

(2012) Sébastien L. Floor et al.   TRENDS IN MOLECULAR MEDICINE

Translation inhibitors induce cell death by multiple mechanisms and Mcl-1 reduction is only a minor contributor

(2012) L M Lindqvist et al.   Cell Death & Disease

Gambogic Acid Is a Tissue-Specific Proteasome Inhibitor In Vitro and In Vivo

(2012) Xiaofen Li et al.   Cell Reports

Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: Characteristics of broad-spectrum protein binding and its effects on anti-tumor activity

(2011) Can-Hui Zheng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

Discovery and Development of Thiazolo[3,2-a]pyrimidinone Derivatives as General Inhibitors of Bcl-2 Family Proteins

(2011) Bingcheng Zhou et al.   ChemMedChem

Inhibitors of the anti-apoptotic Bcl-2 proteins: a patent review

(2011) Naval Bajwa et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

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

3-Thiomorpholin-8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile (S1) Based Molecules as Potent, Dual Inhibitors of B-Cell Lymphoma 2 (Bcl-2) and Myeloid Cell Leukemia Sequence 1 (Mcl-1): Structure-Based Design and Structure−Activity Relationship Studies

(2011) Zhichao Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of a rhodanine-based compound library targeting Bcl-XL and Mcl-1

(2011) Paul H. Bernardo et al.   PURE AND APPLIED CHEMISTRY

Targeting Apoptosis Signaling Pathways for Anticancer Therapy

(2011) Simone Fulda   Frontiers in Oncology

Bcl-2 Family Proteins as Therapeutic Targets

(2010) Peter E. Czabotar et al.   CURRENT PHARMACEUTICAL DESIGN

Emerging Bcl-2 inhibitors for the treatment of cancer

(2010) Asfar S Azmi et al.   EXPERT OPINION ON EMERGING DRUGS

Observations on screening-based research and some concerning trends in the literature

(2010) Jonathan B Baell   Future Medicinal Chemistry

A novel BH3 mimetic S1 potently induces Bax/Bak-dependent apoptosis by targeting both Bcl-2 and Mcl-1

(2010) Zhichao Zhang et al.   INTERNATIONAL JOURNAL OF CANCER

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

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

Design, Synthesis, and Interaction Study of Quinazoline-2(1H)-thione Derivatives as Novel Potential Bcl-xLInhibitors

(2010) Yu Feng et al.   JOURNAL OF MEDICINAL 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

New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

(2010) Jonathan B. Baell et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

The novel plant-derived agent silvestrol has B-cell selective activity in chronic lymphocytic leukemia and acute lymphoblastic leukemia in vitro and in vivo

(2009) David M. Lucas et al.   BLOOD

Mechanisms by which Bak and Bax permeabilise mitochondria during apoptosis

(2009) G. Dewson et al.   JOURNAL OF CELL SCIENCE

Bcl-2 antagonist apogossypol (NSC736630) displays single-agent activity in Bcl-2-transgenic mice and has superior efficacy with less toxicity compared with gossypol (NSC19048)

(2008) S. Kitada et al.   BLOOD

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

(2008) M. Konopleva et al.   CANCER RESEARCH

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

(2008) C. Tse et al.   CANCER RESEARCH

Bcl-2 inhibitors: small molecules with a big impact on cancer therapy

(2008) M Vogler et al.   CELL DEATH AND DIFFERENTIATION

Natural BH3 mimetic (-)-gossypol chemosensitizes human prostate cancer via Bcl-xL inhibition accompanied by increase of Puma and Noxa

(2008) Y. Meng et al.   MOLECULAR CANCER THERAPEUTICS

Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins

(2008) Dayong Zhai et al.   MOLECULAR CANCER THERAPEUTICS

BCL-2 family antagonists for cancer therapy

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

The Marinopyrroles, Antibiotics of an Unprecedented Structure Class from a MarineStreptomycessp.

(2008) Chambers C. Hughes et al.   ORGANIC LETTERS