Allosteric inhibition of antiapoptotic MCL-1

The Design of Covalent Allosteric Drugs

(2015) Ruth Nussinov et al.   Annual Review of Pharmacology and Toxicology

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

Inhibition of Pro-Apoptotic BAX by a Noncanonical Interaction Mechanism

(2015) Lauren A. Barclay et al.   MOLECULAR CELL

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

Chemistry: Chemical con artists foil drug discovery

(2014) Jonathan Baell et al.   NATURE

High-Quality NMR Structure of Human Anti-Apoptotic Protein Domain Mcl-1(171-327) for Cancer Drug Design

(2014) Gaohua Liu et al.   PLoS One

Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors

(2014) Li Tan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Hydrogen Exchange-Mass Spectrometry Measures Stapled Peptide Conformational Dynamics and Predicts Pharmacokinetic Properties

(2013) Xiangguo (Eric) Shi et al.   ANALYTICAL CHEMISTRY

Therapeutic Targeting of Oncogenic K-Ras by a Covalent Catalytic Site Inhibitor

(2013) Sang Min Lim et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Multimodal Interaction with BCL-2 Family Proteins Underlies the Proapoptotic Activity of PUMA BH3

(2013) Amanda L. Edwards et al.   CHEMISTRY & BIOLOGY

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

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

Protein and ligand preparation: parameters, protocols, and influence on virtual screening enrichments

(2013) G. Madhavi Sastry et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

(2013) Jonathan M. Ostrem et al.   NATURE

PUMA binding induces partial unfolding within BCL-xL to disrupt p53 binding and promote apoptosis

(2013) Ariele Viacava Follis 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

Direct activation of full-length proapoptotic BAK

(2013) Elizaveta S. Leshchiner et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Discovery and Synthesis of Hydronaphthoquinones as Novel Proteasome Inhibitors

(2012) Yiyu Ge et al.   JOURNAL OF MEDICINAL 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

Mcl-1 regulates the survival of adult neural precursor cells

(2012) Craig D. Malone et al.   MOLECULAR AND CELLULAR NEUROSCIENCE

Inhibition of DNA binding activity of cAMP response element-binding protein by 1,2-naphthoquinone through chemical modification of Cys-286

(2011) Akiko Endo et al.   CHEMICO-BIOLOGICAL INTERACTIONS

BAX unleashed: the biochemical transformation of an inactive cytosolic monomer into a toxic mitochondrial pore

(2011) Loren D. Walensky et al.   TRENDS IN BIOCHEMICAL SCIENCES

Probing theα-Helical Structural Stability of Stapled p53 Peptides: Molecular Dynamics Simulations and Analysis

(2010) Zuojun Guo et al.   Chemical Biology & Drug Design

Photoreactive Stapled BH3 Peptides to Dissect the BCL-2 Family Interactome

(2010) Craig R. Braun et al.   CHEMISTRY & BIOLOGY

Ubiquitin-Independent Degradation of Antiapoptotic MCL-1

(2010) D. P. Stewart et al.   MOLECULAR AND CELLULAR BIOLOGY

BH3-Triggered Structural Reorganization Drives the Activation of Proapoptotic BAX

(2010) Evripidis Gavathiotis 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

Analysis of Protein Conformation and Dynamics by Hydrogen/Deuterium Exchange MS

(2009) John R. Engen   ANALYTICAL CHEMISTRY

Conformational Changes in Bcl-2 Pro-survival Proteins Determine Their Capacity to Bind Ligands

(2009) Erinna F. Lee et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

(2009) Wenjun Zhou et al.   NATURE

BAX activation is initiated at a novel interaction site

(2008) Evripidis Gavathiotis et al.   NATURE