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

Discovery of HIV fusion inhibitors targeting gp41 using a comprehensive α-helix mimetic library

(2012) Landon R. Whitby et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2012) Sachin Surade et al.   CHEMISTRY & BIOLOGY

Design of Bcl-2 and Bcl-xL Inhibitors with Subnanomolar Binding Affinities Based upon a New Scaffold

(2012) Haibin Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design of Novel Inhibitors of the MDM2–p53 Interaction

(2012) Yosup Rew et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design of Potent Bcl-2/Bcl-xL Inhibitors with Strong in Vivo Antitumor Activity

(2012) Haibin Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Enhancement of α-Helix Mimicry by an α/β-Peptide Foldamer via Incorporation of a Dense Ionic Side-Chain Array

(2012) Lisa M. Johnson et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Nucleation Effects in Peptide Foldamers

(2012) Anupam Patgiri 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

Rational Design of Proteolytically Stable, Cell-Permeable Peptide-Based Selective Mcl-1 Inhibitors

(2012) Avinash Muppidi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Development of α-Helical Calpain Probes by Mimicking a Natural Protein–Protein Interaction

(2012) Hyunil Jo et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Relaxation of the rigid backbone of an oligoamide-foldamer-based α-helix mimetic: identification of potent Bcl-xL inhibitors

(2012) Jeremy L. Yap et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

2-O-Alkylated para-benzamide α-helix mimetics: the role of scaffold curvature

(2012) Valeria Azzarito et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Helix-mediated protein–protein interactions as targets for intervention using foldamers

(2011) Thomas A. Edwards et al.   AMINO ACIDS

Structural Basis of Bcl-xL Recognition by a BH3-Mimetic α/β-Peptide Generated by Sequence-Based Design

(2011) Erinna F. Lee et al.   CHEMBIOCHEM

Assessing Helical Protein Interfaces for Inhibitor Design

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

Structure of the Stapled p53 Peptide Bound to Mdm2

(2011) Sohee Baek et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Evaluation of Diverse α/β-Backbone Patterns for Functional α-Helix Mimicry: Analogues of the Bim BH3 Domain

(2011) Melissa D. Boersma et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Structural Mimicry of the α-Helix in Aqueous Solution with an Isoatomic α/β/γ-Peptide Backbone

(2011) Tomohisa Sawada 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

An orthosteric inhibitor of the Ras-Sos interaction

(2011) Anupam Patgiri et al.   Nature Chemical Biology

A Stapled p53 Helix Overcomes HDMX-Mediated Suppression of p53

(2010) Federico Bernal et al.   CANCER CELL

High Specificity in Protein Recognition by Hydrogen-Bond-Surrogate α-Helices: Selective Inhibition of the p53/MDM2 Complex

(2010) Laura K. Henchey et al.   CHEMBIOCHEM

Phage display selection of miniprotein binders of the Estrogen Receptor

(2010) Trang Phan et al.   CHEMICAL COMMUNICATIONS

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

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

Disrupting protein–protein interactions with non-peptidic, small molecule α-helix mimetics

(2010) Christopher G Cummings et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

The BH3 α-Helical Mimic BH3-M6 Disrupts Bcl-XL, Bcl-2, and MCL-1 Protein-Protein Interactions with Bax, Bak, Bad, or Bim and Induces Apoptosis in a Bax- and Bim-dependent Manner

(2010) Aslamuzzaman Kazi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Novel Pyrrolopyrimidine-Based α-Helix Mimetics: Cell-Permeable Inhibitors of Protein−Protein Interactions

(2010) Ji Hoon Lee et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Coupling of receptor conformation and ligand orientation determine graded activity

(2010) John B Bruning et al.   Nature Chemical Biology

The MCL-1 BH3 helix is an exclusive MCL-1 inhibitor and apoptosis sensitizer

(2010) Michelle L Stewart et al.   Nature Chemical Biology

N-alkylated oligoamide α-helical proteomimetics

(2010) Frederick Campbell et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Oligooxopiperazines as Nonpeptidic α-Helix Mimetics

(2010) Petra Tošovská et al.   ORGANIC LETTERS

Downsizing human, bacterial, and viral proteins to short water-stable alpha helices that maintain biological potency

(2010) R. S. Harrison et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Hydrocarbon double-stapling remedies the proteolytic instability of a lengthy peptide therapeutic

(2010) G. H. Bird et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Synthetic α-Helix Mimetics as Agonists and Antagonists of Islet Amyloid Polypeptide Aggregation

(2009) Ishu Saraogi et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

High-Resolution Structural Characterization of a Helical α/β-Peptide Foldamer Bound to the Anti-Apoptotic Protein Bcl-xL

(2009) Erinna F. Lee et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

N-Acylpolyamine inhibitors of HDM2 and HDMX binding to p53

(2009) Ryo Hayashi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

β-Peptides with improved affinity for hDM2 and hDMX

(2009) Elizabeth A. Harker et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A Highly Potent and Cellularly Active β-Peptidic Inhibitor of the p53/hDM2 Interaction

(2009) Martin Hintersteiner et al.   CHEMBIOCHEM

Synthetic Inhibitors of Extended Helix-Protein Interactions Based on a Biphenyl 4,4′-Dicarboxamide Scaffold

(2009) Johanna M. Rodriguez et al.   CHEMBIOCHEM

Inhibition of protein–protein interactions using designed molecules

(2009) Andrew J. Wilson   CHEMICAL SOCIETY REVIEWS

Structure and Function of Benzoylurea-Derived α-Helix Mimetics Targeting the Bcl-xL/Bak Binding Interface

(2009) Johanna M. Rodriguez et al.   ChemMedChem

Design, Synthesis, and Evaluation of an α-Helix Mimetic Library Targeting Protein−Protein Interactions

(2009) Alex Shaginian et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Inhibition of Hypoxia Inducible Factor 1—Transcription Coactivator Interaction by a Hydrogen Bond Surrogate α-Helix

(2009) Laura K. Henchey et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Direct inhibition of the NOTCH transcription factor complex

(2009) Raymond E. Moellering et al.   NATURE

Inhibition of a viral enzyme by a small-molecule dimer disruptor

(2009) Tina Shahian et al.   Nature Chemical Biology

Novel Amphiphilic α-Helix Mimetics Based on a Bis-benzamide Scaffold

(2009) Srinivasa Marimganti et al.   ORGANIC LETTERS

Structural and biological mimicry of protein surface recognition by  / -peptide foldamers

(2009) W. S. Horne et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A Hydrogen Bond Surrogate Approach for Stabilization of Short Peptide Sequences in α-Helical Conformation

(2008) Anupam Patgiri et al.   ACCOUNTS OF CHEMICAL RESEARCH

Controlling Curvature in a Family of Oligoamide α-Helix Mimetics

(2008) Ishu Saraogi et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Sequence-Based Design of α/β-Peptide Foldamers That Mimic BH3 Domains

(2008) W. Seth Horne et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Inhibition of HIV-1 Fusion by Hydrogen-Bond-Surrogate-Based α Helices

(2008) Deyun Wang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

(2008) C. Tse et al.   CANCER RESEARCH

Photocontrollable Peptide-Based Switches Target the Anti-Apoptotic Protein Bcl-xL

(2008) Sabine Kneissl et al.   CHEMBIOCHEM

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

(2008) Ozlem Keskin et al.   CHEMICAL REVIEWS

Contemporary strategies for the stabilization of peptides in the α-helical conformation

(2008) Laura K Henchey et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Synthesis and Biological Evaluation of a 5-6-5 Imidazole-Phenyl-Thiazole Based α-Helix Mimetic

(2008) Christopher G. Cummings et al.   ORGANIC LETTERS

Temporal activation of p53 by a specific MDM2 inhibitor is selectively toxic to tumors and leads to complete tumor growth inhibition

(2008) S. Shangary et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Estimating the size of the human interactome

(2008) M. P. H. Stumpf et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Protein therapeutics: a summary and pharmacological classification

(2007) Benjamin Leader et al.   NATURE REVIEWS DRUG DISCOVERY

Synthesis of functionalised aromatic oligamide rods

(2007) Jeffrey Plante et al.   ORGANIC & BIOMOLECULAR CHEMISTRY