Flexibility is important for inhibition of the MDM2/p53 protein–protein interaction by cyclic β-hairpins

Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?

(2016) Frauke Weber et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small molecules, big targets: drug discovery faces the protein–protein interaction challenge

(2016) Duncan E. Scott et al.   NATURE REVIEWS DRUG DISCOVERY

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

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

Peptide stapling techniques based on different macrocyclisation chemistries

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

State-of-the-art strategies for targeting protein–protein interactions by small-molecule inhibitors

(2015) Chunquan Sheng et al.   CHEMICAL SOCIETY REVIEWS

Peptide therapeutics: Targeting the undruggable space

(2015) Natia Tsomaia   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

How Beyond Rule of 5 Drugs and Clinical Candidates Bind to Their Targets

(2015) Bradley C. Doak et al.   JOURNAL OF MEDICINAL CHEMISTRY

Macrocycles: lessons from the distant past, recent developments, and future directions

(2015) Andrei K. Yudin   Chemical Science

Constraining Cyclic Peptides To Mimic Protein Structure Motifs

(2014) Timothy A. Hill et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Hot spot-based design of small-molecule inhibitors for protein–protein interactions

(2014) Wenxing Guo et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Mutant p53 in Cancer: New Functions and Therapeutic Opportunities

(2014) Patricia A.J. Muller et al.   CANCER CELL

Small Molecule Modulators of Protein–Protein Interactions: Selected Case Studies

(2014) Madhu Aeluri et al.   CHEMICAL REVIEWS

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

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

Promiscuity and the Conformational Rearrangement of Drug-Like Molecules: Insight from the Protein Data Bank

(2014) Michael W. He et al.   ChemMedChem

Antiviral Atropisomers: Conformational Energy Surfaces by NMR for Host-Directed Myxovirus Blockers

(2014) Craig Grimmer et al.   Journal of Chemical Information and Modeling

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

Drugging the p53 pathway: understanding the route to clinical efficacy

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

Druggable protein–protein interactions – from hot spots to hot segments

(2013) Nir London et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

A Potent Small-Molecule Inhibitor of the MDM2–p53 Interaction (MI-888) Achieved Complete and Durable Tumor Regression in Mice

(2013) Yujun Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Handles for Fmoc Solid-Phase Synthesis of Protected Peptides

(2013) Miriam Góngora-Benítez et al.   ACS Combinatorial Science

The paradox of conformational constraint in the design of Cbl(TKB)-binding peptides

(2013) Eric A. Kumar et al.   Scientific Reports

Getting in Shape: Controlling Peptide Bioactivity and Bioavailability Using Conformational Constraints

(2012) Jonathan E. Bock et al.   ACS Chemical Biology

The Future of Peptide-based Drugs

(2012) David J. Craik et al.   Chemical Biology & Drug Design

Principles and Applications of Halogen Bonding in Medicinal Chemistry and Chemical Biology

(2012) Rainer Wilcken et al.   JOURNAL OF MEDICINAL CHEMISTRY

Proline-mediated formation of novel chroman-4-one tetrahydropyrimidines

(2012) Maria Fridén-Saxin et al.   TETRAHEDRON

Structure of the Stapled p53 Peptide Bound to Mdm2

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

β-hairpin-forming peptides; models of early stages of protein folding

(2010) Agnieszka Lewandowska et al.   BIOPHYSICAL CHEMISTRY

A Stapled p53 Helix Overcomes HDMX-Mediated Suppression of p53

(2010) Federico Bernal et al.   CANCER CELL

Identification and Characterization of the First Small Molecule Inhibitor of MDMX

(2010) Damon Reed et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Disulfide Cyclized Tripeptide Analogues of Angiotensin IV as Potent and Selective Inhibitors of Insulin-Regulated Aminopeptidase (IRAP)

(2010) Hanna Andersson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Conformational ensembles of flexible β-turn mimetics in DMSO-d6

(2010) Jari J. Koivisto et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Thermodynamic and Structural Effects of Macrocyclic Constraints in Protein−Ligand Interactions

(2010) John E. DeLorbe et al.   ACS Medicinal Chemistry Letters

Amino Acid-Protecting Groups

(2009) Albert Isidro-Llobet et al.   CHEMICAL REVIEWS

Synthetic therapeutic peptides: science and market

(2009) Patrick Vlieghe et al.   DRUG DISCOVERY TODAY

β-Hairpin Peptidomimetics: Design, Structures and Biological Activities

(2008) John A. Robinson   ACCOUNTS OF CHEMICAL RESEARCH

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

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