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

Recent encounters with atropisomerism in drug discovery

(2018) Peter W. Glunz   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Phase I First-in-Human Study of Venetoclax in Patients With Relapsed or Refractory Non-Hodgkin Lymphoma

(2017) Matthew S. Davids et al.   JOURNAL OF CLINICAL ONCOLOGY

Looking Back, Looking Forward at Halogen Bonding in Drug Discovery

(2017) Lois Mendez et al.   MOLECULES

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

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

High-content screening identifies kinase inhibitors that overcome venetoclax resistance in activated CLL cells

(2016) Sina Oppermann et al.   BLOOD

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

(2016) J.-N. Gong et al.   BLOOD

Binding of Released Bim to Mcl-1 is a Mechanism of Intrinsic Resistance to ABT-199 which can be Overcome by Combination with Daunorubicin or Cytarabine in AML Cells

(2016) X. Niu et al.   CLINICAL CANCER RESEARCH

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

BET Inhibition Induces Apoptosis in Aggressive B-Cell Lymphoma via Epigenetic Regulation of BCL-2 Family Members

(2016) S. J. Hogg et al.   MOLECULAR CANCER THERAPEUTICS

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

Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain

(2016) Gizem Akçay et al.   Nature Chemical Biology

Targeting BCL2 with Venetoclax in Relapsed Chronic Lymphocytic Leukemia

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

Emerging understanding of Bcl-2 biology: Implications for neoplastic progression and treatment

(2015) Cristina Correia et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR 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

Synergistic induction of apoptosis in high-risk DLBCL by BCL2 inhibition with ABT-199 combined with pharmacologic loss of MCL1

(2015) L Li et al.   LEUKEMIA

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

MCL-1 and BCL-xL-dependent resistance to the BCL-2 inhibitor ABT-199 can be overcome by preventing PI3K/AKT/mTOR activation in lymphoid malignancies

(2015) G S Choudhary et al.   Cell Death & Disease

Mcl-1 Ubiquitination: Unique Regulation of an Essential Survival Protein

(2014) Barbara Mojsa et al.   Cells

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

(2013) B. Koss et al.   BLOOD

MYC/BCL2 protein coexpression contributes to the inferior survival of activated B-cell subtype of diffuse large B-cell lymphoma and demonstrates high-risk gene expression signatures: a report from The International DLBCL Rituximab-CHOP Consortium Program

(2013) S. Hu et al.   BLOOD

The Bcl-2 specific BH3 mimetic ABT-199: a promising targeted therapy for t(11;14) multiple myeloma

(2013) C Touzeau et al.   LEUKEMIA

Pan-cancer patterns of somatic copy number alteration

(2013) Travis I Zack et al.   NATURE GENETICS

Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

(2013) D. M. Molina et al.   SCIENCE

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 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

Distribution of Bim determines Mcl-1 dependence or codependence with Bcl-xL/Bcl-2 in Mcl-1-expressing myeloma cells

(2011) A. A. Morales et al.   BLOOD

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

Sensitivity to antitubulin chemotherapeutics is regulated by MCL1 and FBW7

(2011) Ingrid E. Wertz et al.   NATURE

Mcl-1; the molecular regulation of protein function

(2010) Luke W. Thomas et al.   FEBS LETTERS

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