De novo coiled-coil peptides as scaffolds for disrupting protein–protein interactions

Iterative optimization yields Mcl-1–targeting stapled peptides with selective cytotoxicity to Mcl-1–dependent cancer cells

(2018) Raheleh Rezaei Araghi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Extreme disorder in an ultrahigh-affinity protein complex

(2018) Alessandro Borgia et al.   NATURE

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

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

Double quick, double click reversible peptide “stapling”

(2017) Claire M. Grison et al.   Chemical Science

Protease-Resistant and Cell-Permeable Double-Stapled Peptides Targeting the Rab8a GTPase

(2016) Philipp M. Cromm et al.   ACS Chemical Biology

hBfl-1/hNOXA Interaction Studies Provide New Insights on the Role of Bfl-1 in Cancer Cell Resistance and for the Design of Novel Anticancer Agents

(2016) Elisa Barile et al.   ACS Chemical Biology

An α-Helix-Mimicking 12,13-Helix: Designed α/β/γ-Foldamers as Selective Inhibitors of Protein-Protein Interactions

(2016) Claire M. Grison et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Designing helical peptide inhibitors of protein–protein interactions

(2016) Raheleh Rezaei Araghi et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

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

(2016) András Kotschy et al.   NATURE

Biophysical determinants for cellular uptake of hydrocarbon-stapled peptide helices

(2016) Gregory H Bird et al.   Nature Chemical Biology

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

Hydrocarbon constrained peptides – understanding preorganisation and binding affinity

(2016) Jennifer A. Miles et al.   Chemical Science

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

(2016) Duong Nhu et al.   MedChemComm

Computationally designed high specificity inhibitors delineate the roles of BCL2 family proteins in cancer

(2016) Stephanie Berger et al.   eLife

Hydrocarbon Stapled Peptides as Modulators of Biological Function

(2015) Philipp M. Cromm et al.   ACS Chemical Biology

Selective and Potent Proteomimetic Inhibitors of Intracellular Protein-Protein Interactions

(2015) Anna Barnard et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Peptide stapling techniques based on different macrocyclisation chemistries

(2015) Yu Heng Lau et al.   CHEMICAL SOCIETY REVIEWS

α/β-Peptide Foldamers Targeting Intracellular Protein–Protein Interactions with Activity in Living Cells

(2015) James W. Checco et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

An analysis of the attrition of drug candidates from four major pharmaceutical companies

(2015) Michael J. Waring et al.   NATURE REVIEWS DRUG DISCOVERY

The Bcl-2 family: structures, interactions and targets for drug discovery

(2014) Marc Kvansakul et al.   APOPTOSIS

A Computationally Designed Inhibitor of an Epstein-Barr Viral Bcl-2 Protein Induces Apoptosis in Infected Cells

(2014) Erik Procko et al.   CELL

GLUE That Sticks to HIV: A Helix-Grafted GLUE Protein That Selectively Binds the HIV gp41 N-Terminal Helical Region

(2014) Susanne N. Walker et al.   CHEMBIOCHEM

Modulators of Protein–Protein Interactions

(2014) Lech-Gustav Milroy et al.   CHEMICAL REVIEWS

Small-Molecule Inhibitors of Protein-Protein Interactions: Progressing toward the Reality

(2014) Michelle R. Arkin et al.   CHEMISTRY & BIOLOGY

Small-Molecule Inhibitors of the MDM2–p53 Protein–Protein Interaction (MDM2 Inhibitors) in Clinical Trials for Cancer Treatment

(2014) Yujun Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Hydrocarbon-Stapled Peptides: Principles, Practice, and Progress

(2014) Loren D. Walensky et al.   JOURNAL OF MEDICINAL CHEMISTRY

Rational Design of Topographical Helix Mimics as Potent Inhibitors of Protein–Protein Interactions

(2014) Brooke Bullock Lao et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Drugging the p53 pathway: understanding the route to clinical efficacy

(2014) Kian Hoe Khoo et al.   NATURE REVIEWS DRUG DISCOVERY

Computational design of water-soluble α-helical barrels

(2014) Andrew R. Thomson et al.   SCIENCE

Protein grafting of p53TAD onto a leucine zipper scaffold generates a potent HDM dual inhibitor

(2014) Jung-Hoon Lee et al.   Nature Communications

A Versatile Platform to Analyze Low-Affinity and Transient Protein-Protein Interactions in Living Cells in Real Time

(2014) Yao-Cheng Li et al.   Cell Reports

Anti-apoptosis Proteins Mcl-1 and Bcl-xL Have Different p53-Binding Profiles

(2013) Hongwei Yao et al.   BIOCHEMISTRY

Allostery in Disease and in Drug Discovery

(2013) Ruth Nussinov et al.   CELL

Oxime Side-Chain Cross-Links in an α-Helical Coiled-Coil Protein: Structure, Thermodynamics, and Folding-Templated Synthesis of Bicyclic Species

(2013) Conor M. Haney et al.   CHEMISTRY-A EUROPEAN JOURNAL

A Set of de Novo Designed Parallel Heterodimeric Coiled Coils with Quantified Dissociation Constants in the Micromolar to Sub-nanomolar Regime

(2013) Franziska Thomas et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Inhibition of α-helix-mediated protein–protein interactions using designed molecules

(2013) Valeria Azzarito et al.   Nature Chemistry

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

Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy

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

The Native GCN4 Leucine-Zipper Domain Does Not Uniquely Specify a Dimeric Oligomerization State

(2012) Kaylyn M. Oshaben et al.   BIOCHEMISTRY

Structural Biology and Drug Discovery of Difficult Targets: The Limits of Ligandability

(2012) Sachin Surade et al.   CHEMISTRY & BIOLOGY

Rewiring Kinase Specificity with a Synthetic Adaptor Protein

(2012) Elissa M. Hobert et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

NMR Solution Structure of a Photoswitchable Apoptosis Activating Bak Peptide Bound to Bcl-xL

(2012) Piotr Wysoczanski et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Acid-Mediated Prevention of Aspartimide Formation in Solid Phase Peptide Synthesis

(2012) Tillmann Michels et al.   ORGANIC LETTERS

A Basis Set of de Novo Coiled-Coil Peptide Oligomers for Rational Protein Design and Synthetic Biology

(2012) Jordan M. Fletcher et al.   ACS Synthetic Biology

Artificially Induced Protein-Membrane Anchorage with Cholesterol-Based Recognition Agents as a New Therapeutic Concept

(2011) Miriam Avadisian et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Assessing Helical Protein Interfaces for Inhibitor Design

(2011) Brooke N. Bullock et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Design and Structure of Stapled Peptides Binding to Estrogen Receptors

(2011) Chris Phillips et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Too many roads not taken

(2011) Aled M. Edwards et al.   NATURE

Phage display selection of miniprotein binders of the Estrogen Receptor

(2010) Trang Phan et al.   CHEMICAL COMMUNICATIONS

A Synthetic Coiled-Coil Interactome Provides Heterospecific Modules for Molecular Engineering

(2010) Aaron W. Reinke et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The art of the chemical probe

(2010) Stephen V Frye   Nature Chemical Biology

Oligobenzamide proteomimetic inhibitors of the p53–hDM2 protein–protein interaction

(2009) Jeffrey P. Plante et al.   CHEMICAL COMMUNICATIONS

Principles of Protein−Protein Interactions: What are the Preferred Ways For Proteins To Interact?

(2008) Ozlem Keskin et al.   CHEMICAL REVIEWS

Designed α-Helical Tectons for Constructing Multicomponent Synthetic Biological Systems

(2008) Elizabeth H. C. Bromley et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY