Interdiction at a protein-protein interface: MCL-1 inhibitors for oncology

Recent advances in the development of Mcl-1 inhibitors for cancer therapy

(2019) Alexander W. Hird et al.   PHARMACOLOGY & THERAPEUTICS

Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer

(2019) Taekyu Lee et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecular Comprehension of Mcl-1: From Gene Structure to Cancer Therapy

(2019) Viacheslav V. Senichkin et al.   TRENDS IN CELL BIOLOGY

Structure-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity

(2019) Zoltan Szlávik et al.   JOURNAL OF MEDICINAL CHEMISTRY

MCL-1 inhibitors – where are we now (2019)?

(2019) Steven Fletcher   EXPERT OPINION ON THERAPEUTIC PATENTS

Discovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an α-Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere

(2019) Gwenaella Rescourio et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small-molecule Mcl-1 inhibitors: Emerging anti-tumor agents

(2018) Yichao Wan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design

(2018) Subrata Shaw et al.   JOURNAL OF MEDICINAL CHEMISTRY

The MCL1-specific inhibitor S63845 acts synergistically with venetoclax/ABT-199 to induce apoptosis in T-cell acute lymphoblastic leukemia cells

(2018) Zhaodong Li et al.   LEUKEMIA

Selective targeting of antiapoptotic BCL-2 proteins in cancer

(2018) Ahmet Can Timucin et al.   MEDICINAL RESEARCH REVIEWS

Combining BH3-mimetics to target both BCL-2 and MCL1 has potent activity in pre-clinical models of acute myeloid leukemia

(2018) Donia M. Moujalled et al.   LEUKEMIA

Gene essentiality landscape and druggable oncogenic dependencies in herpesviral primary effusion lymphoma

(2018) Mark Manzano et al.   Nature Communications

A Novel MCL-1 Inhibitor Combined with Venetoclax Rescues Venetoclax Resistant Acute Myelogenous Leukemia

(2018) Haley E. Ramsey et al.   Cancer Discovery

Exploiting MCL-1 dependency with combination MEK + MCL-1 inhibitors leads to induction of apoptosis and tumor regression in KRAS mutant non-small cell lung cancer

(2018) Varuna Nangia et al.   Cancer Discovery

BH3-Mimetic Drugs: Blazing the Trail for New Cancer Medicines

(2018) Delphine Merino et al.   CANCER CELL

Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia

(2018) Adriana E. Tron et al.   Nature Communications

Pathways and mechanisms of venetoclax resistance

(2017) Prithviraj Bose et al.   LEUKEMIA & LYMPHOMA

From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors

(2017) Avi Ashkenazi et al.   NATURE REVIEWS DRUG DISCOVERY

Structure Based Design of Non-Natural Peptidic Macrocyclic Mcl-1 Inhibitors

(2017) Jeffrey W. Johannes et al.   ACS Medicinal Chemistry Letters

Hierarchy for targeting prosurvival BCL2 family proteins in multiple myeloma: pivotal role of MCL1

(2016) J.-N. Gong et al.   BLOOD

Mcl-1 inhibitors: a patent review

(2016) Lijia Chen et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Discovery and biological characterization of potent myeloid cell leukemia-1 inhibitors

(2016) Taekyu Lee et al.   FEBS LETTERS

Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods

(2016) Nicholas F. Pelz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules

(2016) Jeremy L. Yap et al.   JOURNAL OF MEDICINAL CHEMISTRY

Venetoclax in relapsed or refractory chronic lymphocytic leukaemia with 17p deletion: a multicentre, open-label, phase 2 study

(2016) Stephan Stilgenbauer et al.   LANCET ONCOLOGY

BCL2 Inhibitors as Anticancer Drugs: A Plethora of Misleading BH3 Mimetics

(2016) R. S. Soderquist et al.   MOLECULAR CANCER THERAPEUTICS

The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models

(2016) András Kotschy et al.   NATURE

Targeting BCL2 with Venetoclax in Relapsed Chronic Lymphocytic Leukemia

(2016) Andrew W. Roberts et al.   NEW ENGLAND JOURNAL OF MEDICINE

Efficacy and Biological Correlates of Response in a Phase II Study of Venetoclax Monotherapy in Patients with Acute Myelogenous Leukemia

(2016) M. Konopleva et al.   Cancer Discovery

Targeting MCL-1/BCL-XL Forestalls the Acquisition of Resistance to ABT-199 in Acute Myeloid Leukemia

(2016) Kevin H. Lin et al.   Scientific Reports

Loss of a Single Mcl-1 Allele Inhibits MYC-Driven Lymphomagenesis by Sensitizing Pro-B Cells to Apoptosis

(2016) Stephanie Grabow et al.   Cell Reports

A CRISPR Dropout Screen Identifies Genetic Vulnerabilities and Therapeutic Targets in Acute Myeloid Leukemia

(2016) Konstantinos Tzelepis et al.   Cell Reports

The BCL-2 protein family, BH3-mimetics and cancer therapy

(2015) A R D Delbridge et al.   CELL DEATH AND DIFFERENTIATION

Discovery of Tricyclic Indoles That Potently Inhibit Mcl-1 Using Fragment-Based Methods and Structure-Based Design

(2015) Jason P. Burke et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

An interconnected hierarchical model of cell death regulation by the BCL-2 family

(2015) Hui-Chen Chen et al.   NATURE CELL BIOLOGY

Small molecule Mcl-1 inhibitors for the treatment of cancer

(2015) Johannes Belmar et al.   PHARMACOLOGY & THERAPEUTICS

Cell Death Signaling

(2015) Douglas R. Green et al.   Cold Spring Harbor Perspectives in Biology

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

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

Many players in BCL-2 family affairs

(2014) Tudor Moldoveanu et al.   TRENDS IN BIOCHEMICAL SCIENCES

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

Mcl-1 is essential for the survival of plasma cells

(2013) Victor Peperzak 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

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 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

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

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

Identification of Molecular Vulnerabilities in Human Multiple Myeloma Cells by RNA Interference Lethality Screening of the Druggable Genome

(2011) R. E. Tiedemann et al.   CANCER RESEARCH

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

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

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

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

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

(2011) Fabien Llambi et al.   MOLECULAR CELL

Sensitivity to antitubulin chemotherapeutics is regulated by MCL1 and FBW7

(2011) Ingrid E. Wertz et al.   NATURE

Thermodynamic analysis of water molecules at the surface of proteins and applications to binding site prediction and characterization

(2011) Thijs Beuming et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

Targeting Apoptosis Signaling Pathways for Anticancer Therapy

(2011) Simone Fulda   Frontiers in Oncology

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

(2010) D. Yecies et al.   BLOOD

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

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

(2010) H Zhang et al.   ONCOGENE

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

Therapeutic Efficacy of ABT-737, a Selective Inhibitor of BCL-2, in Small Cell Lung Cancer

(2008) C. L. Hann 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

The BCL-2 protein family: opposing activities that mediate cell death

(2007) Richard J. Youle et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY