Peptidomimetics: A Synthetic Tool for Inhibiting Protein–Protein Interactions in Cancer

High-throughput screen for inhibitors of protein–protein interactions in a reconstituted heat shock protein 70 (Hsp70) complex

(2018) Isabelle R. Taylor et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Using Peptidomimetics and Constrained Peptides as Valuable Tools for Inhibiting Protein–Protein Interactions

(2018) Naomi Robertson et al.   MOLECULES

Utilization of peptide phage display to investigate hotspots on IL-17A and what it means for drug discovery

(2018) Joey P. Ting et al.   PLoS One

Peptidomimetics for Targeting Protein–Protein Interactions between DOT1L and MLL Oncofusion Proteins AF9 and ENL

(2018) Lei Du et al.   ACS Medicinal Chemistry Letters

Peptidomimetics Targeting Protein-Protein Interactions for Therapeutic Development

(2018) Gan Zhang et al.   PROTEIN AND PEPTIDE LETTERS

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

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

Carbonylation as a novel method for the assembly of pyrazine based oligoamide alpha-helix mimetics

(2017) Seger Van Mileghem et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Cheminformatics-aided discovery of small-molecule Protein-Protein Interaction (PPI) dual inhibitors of Tumor Necrosis Factor (TNF) and Receptor Activator of NF-κB Ligand (RANKL)

(2017) Georgia Melagraki et al.   PLoS Computational Biology

Chronic lymphocytic leukaemia

(2017) Thomas J. Kipps et al.   Nature Reviews Disease Primers

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

(2016) András Kotschy et al.   NATURE

Structure-Based Design of Inhibitors of Protein-Protein Interactions: Mimicking Peptide Binding Epitopes

(2015) Marta Pelay-Gimeno et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The Contribution of Missense Mutations in Core and Rim Residues of Protein–Protein Interfaces to Human Disease

(2015) Alessia David et al.   JOURNAL OF MOLECULAR BIOLOGY

Multivalent helix mimetics for PPI-inhibition

(2015) Anna Barnard et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Towards more drug-like proteomimetics: two-faced, synthetic α-helix mimetics based on a purine scaffold

(2015) M. E. Lanning et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Inhibiting EGFR Dimerization Using Triazolyl-Bridged Dimerization Arm Mimics

(2015) Laura E. Hanold et al.   PLoS One

Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy

(2015) Joel D. Leverson et al.   Science Translational Medicine

Stereocontrolled protein surface recognition using chiral oligoamide proteomimetic foldamers

(2015) Valeria Azzarito et al.   Chemical Science

Anatomy of β-Strands at Protein–Protein Interfaces

(2014) Andrew M. Watkins et al.   ACS Chemical Biology

Direct Targeting of Rab-GTPase-Effector Interactions

(2014) Jochen Spiegel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

MCL-1 but not BCL-XL is critical for the development and sustained expansion of thymic lymphoma in p53-deficient mice

(2014) S. Grabow et al.   BLOOD

Two-Face, Two-Turn α-Helix Mimetics Based on a Cross-Acridine Scaffold: Analogues of the Bim BH3 Domain

(2014) Xiangqian Li et al.   CHEMBIOCHEM

The Cyclic Cystine Ladder of Theta-Defensins as a Stable, Bifunctional Scaffold: A Proof-of-Concept Study Using the Integrin-Binding RGD Motif.

(2014) Anne C. Conibear et al.   CHEMBIOCHEM

Small-Molecule Proteomimetic Inhibitors of the HIF-1α-p300 Protein-Protein Interaction

(2014) George M. Burslem et al.   CHEMBIOCHEM

Linear Aliphatic Dialkynes as Alternative Linkers for Double-Click Stapling of p53-Derived Peptides

(2014) Yu Heng Lau et al.   CHEMBIOCHEM

Modulators of Protein–Protein Interactions

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

Discovery of a Potent Stapled Helix Peptide That Binds to the 70N Domain of Replication Protein A

(2014) Andreas O. Frank 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

Backbone modification of a polypeptide drug alters duration of action in vivo

(2014) Ross W Cheloha et al.   NATURE BIOTECHNOLOGY

Small-molecule modulation of Ras signaling

(2014) Jochen Spiegel et al.   Nature Chemical Biology

Orthogonal functionalisation of α-helix mimetics

(2014) Anna Barnard et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

In vivo modulation of hypoxia-inducible signaling by topographical helix mimetics

(2014) B. B. Lao et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Many players in BCL-2 family affairs

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

Functionalised staple linkages for modulating the cellular activity of stapled peptides

(2014) Yu Heng Lau et al.   Chemical Science

Design, Solid-Phase Synthesis, and Evaluation of a Phenyl-Piperazine-Triazine Scaffold as α-Helix Mimetics

(2014) Heejo Moon et al.   ACS Combinatorial Science

The structure of an MDM2–Nutlin-3a complex solved by the use of a validated MDM2 surface-entropy reduction mutant

(2013) Burcu Anil et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Direct targeting of β-catenin: Inhibition of protein–protein interactions for the inactivation of Wnt signaling

(2013) Gernot Hahne et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design of stapled α-helical peptides to specifically activate Wnt/β-catenin signaling

(2013) Hong-Kui Cui et al.   CELL RESEARCH

Structure-Guided Rational Design of α/β-Peptide Foldamers with High Affinity for BCL-2 Family Prosurvival Proteins

(2013) Brian J. Smith et al.   CHEMBIOCHEM

Aromatic Oligoamide Foldamers with a “Wet Edge” as Inhibitors of the α-Helix-Mediated p53-hDM2 Protein-Protein Interaction

(2013) Panchami Prabhakaran et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

The novel BH3 α-helix mimetic JY-1-106 induces apoptosis in a subset of cancer cells (lung cancer, colon cancer and mesothelioma) by disrupting Bcl-xL and Mcl-1 protein–protein interactions with Bak

(2013) Xiaobo Cao et al.   Molecular Cancer

Targeted disruption of the EZH2–EED complex inhibits EZH2-dependent cancer

(2013) Woojin Kim et al.   Nature Chemical Biology

Structure-guided design of a selective BCL-XL inhibitor

(2013) Guillaume Lessene et al.   Nature Chemical Biology

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

(2013) Valeria Azzarito et al.   Nature Chemistry

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

(2013) Andrew J Souers et al.   NATURE MEDICINE

Inhibition of Nutlin-Resistant HDM2 Mutants by Stapled Peptides

(2013) Siau Jia Wei et al.   PLoS One

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

Protein domain mimetics as in vivo modulators of hypoxia-inducible factor signaling

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

Mechanisms of Action of Bcl-2 Family Proteins

(2013) A. Shamas-Din et al.   Cold Spring Harbor Perspectives in Biology

Stapled Vasoactive Intestinal Peptide (VIP) Derivatives Improve VPAC2 Agonism and Glucose-Dependent Insulin Secretion

(2013) Fabrizio Giordanetto et al.   ACS Medicinal Chemistry Letters

Rational Optimization of Conformational Effects Induced By Hydrocarbon Staples in Peptides and their Binding Interfaces

(2013) Dilraj Lama et al.   Scientific Reports

ABT-737, a small molecule Bcl-2/Bcl-xL antagonist, increases antimitotic-mediated apoptosis in human prostate cancer cells

(2013) Ricardo Parrondo et al.   PeerJ

Comprehensive Peptidomimetic Libraries Targeting Protein–Protein Interactions

(2012) Landon R. Whitby et al.   ACCOUNTS OF CHEMICAL RESEARCH

Stapled Peptides with Improved Potency and Specificity That Activate p53

(2012) Christopher J. Brown et al.   ACS Chemical Biology

Plucking the high hanging fruit: A systematic approach for targeting protein–protein interactions

(2012) Monika Raj et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Microwave assisted solid phase synthesis of highly functionalized N-alkylated oligobenzamide α-helix mimetics

(2012) Kérya Long et al.   BIOORGANIC & MEDICINAL CHEMISTRY

BH3 profiling – Measuring integrated function of the mitochondrial apoptotic pathway to predict cell fate decisions

(2012) Victoria Del Gaizo Moore et al.   CANCER LETTERS

Enaminone-Based Mimics of Extended and Hydrophilic α-Helices

(2012) Marc J. Adler et al.   CHEMISTRY-A EUROPEAN JOURNAL

An Ultrahigh Affinity d-Peptide Antagonist Of MDM2

(2012) Changyou Zhan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cyclic Aza-peptide Integrin Ligand Synthesis and Biological Activity

(2012) Jochen Spiegel et al.   JOURNAL OF ORGANIC CHEMISTRY

Extending Foldamer Design beyond α-Helix Mimicry: α/β-Peptide Inhibitors of Vascular Endothelial Growth Factor Signaling

(2012) Holly S. Haase et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Nucleation Effects in Peptide Foldamers

(2012) Anupam Patgiri 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

Amphiphilic α-helix mimetics based on a benzoylurea scaffold

(2012) Sam Thompson et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

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

A Spiroligomer α-Helix Mimic That Binds HDM2, Penetrates Human Cells and Stabilizes HDM2 in Cell Culture

(2012) Zachary Z. Brown et al.   PLoS One

Inhibition of oncogenic Wnt signaling through direct targeting of  -catenin

(2012) T. N. Grossmann et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeted Disruption of the BCL9/ -Catenin Complex Inhibits Oncogenic Wnt Signaling

(2012) K. Takada et al.   Science Translational Medicine

Chapter 4: Protein Interactions and Disease

(2012) Mileidy W. Gonzalez et al.   PLoS Computational Biology

Synthesis of cell-permeable stapled peptide dual inhibitors of the p53-Mdm2/Mdmx interactions via photoinduced cycloaddition

(2011) Michael M. Madden et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A general synthesis of dirhodium metallopeptides as MDM2 ligands

(2011) Alexander N. Zaykov et al.   CHEMICAL COMMUNICATIONS

Achieving cell penetration with distance-matching cysteine cross-linkers: a facile route to cell-permeable peptide dual inhibitors of Mdm2/Mdmx

(2011) Avinash Muppidi et al.   CHEMICAL COMMUNICATIONS

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

Design, Synthesis, and Validation of a β-Turn Mimetic Library Targeting Protein–Protein and Peptide–Receptor Interactions

(2011) Landon R. Whitby et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

Getting pharmaceutical R&D back on target

(2011) Mark E Bunnage   Nature Chemical Biology

An orthosteric inhibitor of the Ras-Sos interaction

(2011) Anupam Patgiri et al.   Nature Chemical Biology

mRNA Display Selection of an Optimized MDM2-Binding Peptide That Potently Inhibits MDM2-p53 Interaction

(2011) Hirokazu Shiheido et al.   PLoS One

Double-sided α-helix mimetics

(2011) Sam Thompson et al.   TETRAHEDRON

Angiotensin II, a neuropeptide at the frontier between endocrinology and neuroscience: is there a link between the angiotensin II type 2 receptor and Alzheimer’s disease?

(2011) Nicole Gallo-Payet   Frontiers in Endocrinology

Systematic Analysis of Helical Protein Interfaces Reveals Targets for Synthetic Inhibitors

(2010) Andrea L. Jochim et al.   ACS Chemical Biology

A Left-Handed Solution to Peptide Inhibition of the p53-MDM2 Interaction

(2010) Min Liu et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

Update 1 of: Over One Hundred Peptide-Activated G Protein-Coupled Receptors Recognize Ligands with Turn Structure

(2010) Gloria Ruiz-Gómez et al.   CHEMICAL REVIEWS

Discovery of Modulators of Protein-Protein Interactions: Current Approaches and Limitations

(2010) Lidio M.C. Meireles et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Drugs targeting Bcl-2 family members as an emerging strategy in cancer

(2010) Brian Leber et al.   EXPERT REVIEWS IN MOLECULAR MEDICINE

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

Mcl1 haploinsufficiency protects mice from Myc-induced acute myeloid leukemia

(2010) Zhifu Xiang et al.   JOURNAL OF CLINICAL INVESTIGATION

Bridged β3-Peptide Inhibitors of p53-hDM2 Complexation: Correlation between Affinity and Cell Permeability

(2010) Arjel D. Bautista et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

Interactome under construction

(2010) Laura Bonetta   NATURE

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

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

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

(2010) H Zhang et al.   ONCOGENE

N-alkylated oligoamide α-helical proteomimetics

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

D-peptide inhibitors of the p53-MDM2 interaction for targeted molecular therapy of malignant neoplasms

(2010) M. Liu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Mechanism for Activation of the EGF Receptor Catalytic Domain by the Juxtamembrane Segment

(2009) Natalia Jura et al.   CELL

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

(2009) Martin Hintersteiner et al.   CHEMBIOCHEM

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

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

Structure-based Design of High Affinity Peptides Inhibiting the Interaction of p53 with MDM2 and MDMX

(2009) Jason Phan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

In Silico Improvement of β3-Peptide Inhibitors of p53•hDM2 and p53•hDMX

(2009) Julien Michel 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

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

(2009) Srinivasa Marimganti et al.   ORGANIC LETTERS

Structural basis for high-affinity peptide inhibition of p53 interactions with MDM2 and MDMX

(2009) M. Pazgier et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

β-Hairpin Peptidomimetics: Design, Structures and Biological Activities

(2008) John A. Robinson   ACCOUNTS OF CHEMICAL RESEARCH

Foldamers with Heterogeneous Backbones

(2008) W. Seth Horne et al.   ACCOUNTS OF CHEMICAL RESEARCH

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

(2008) C. Tse et al.   CANCER RESEARCH

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

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

BAX activation is initiated at a novel interaction site

(2008) Evripidis Gavathiotis et al.   NATURE

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

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

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

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