Modulating protein–protein interactions: the potential of peptides

Anatomy of hot spots in protein interfaces

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Reaching for high-hanging fruit in drug discovery at protein–protein interfaces

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Small-molecule inhibitors of protein–protein interactions: progressing towards the dream

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Phage Display

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Synthetic therapeutic peptides: science and market

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Activation of Apoptosis in Vivo by a Hydrocarbon-Stapled BH3 Helix

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Protein-binding assays in biological liquids using microscale thermophoresis

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Contemporary strategies for peptide macrocyclization

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An All-Hydrocarbon Cross-Linking System for Enhancing the Helicity and Metabolic Stability of Peptides

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Cell‐penetrating peptides: 20 years later, where do we stand?

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The rise of fragment-based drug discovery

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Hot spots—A review of the protein–protein interface determinant amino‐acid residues

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Direct inhibition of the NOTCH transcription factor complex

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Phage-encoded combinatorial chemical libraries based on bicyclic peptides

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

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β-Peptidic Peptidomimetics

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

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Isothermal Titration Calorimetry of Protein–Protein Interactions

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Highly Efficient Synthesis of Covalently Cross-Linked Peptide Helices by Ring-Closing Metathesis

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Reactivation of the p53 Tumor Suppressor Pathway by a Stapled p53 Peptide

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Modulators of Protein–Protein Interactions

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A Perfluoroaryl-Cysteine S N Ar Chemistry Approach to Unprotected Peptide Stapling

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Flexizymes for genetic code reprogramming

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Butelase 1 is an Asx-specific ligase enabling peptide macrocyclization and synthesis

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

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Perspectives on NMR in drug discovery: a technique comes of age

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Synthesis of all-hydrocarbon stapled α-helical peptides by ring-closing olefin metathesis

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

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β-Hairpin Peptidomimetics: Design, Structures and Biological Activities

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Oncogenic protein interfaces: small molecules, big challenges

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An orthosteric inhibitor of the Ras-Sos interaction

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Photo-control of helix content in a short peptide

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A Stapled p53 Helix Overcomes HDMX-Mediated Suppression of p53

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Delivery of gold nanoparticles to the brain by conjugation with a peptide that recognizes the transferrin receptor

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Inhibition of oncogenic Wnt signaling through direct targeting of β-catenin

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Design of Triazole-Stapled BCL9 α-Helical Peptides to Target the β-Catenin/B-Cell CLL/lymphoma 9 (BCL9) Protein–Protein Interaction

Kawamoto, S. A., Coleska, A., Ran, X., Yi, H., Yang, C.-Y., & Wang, S. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm201125d · Cited by 249

In Vitro Selection of Highly Modified Cyclic Peptides That Act as Tight Binding Inhibitors

Guillen Schlippe, Y. V., Hartman, M. C. T., Josephson, K., & Szostak, J. W. (2012) · Journal of the American Chemical Society · doi:10.1021/ja301017y · Cited by 239

DARPins and other repeat protein scaffolds: advances in engineering and applications

Boersma, Y. L., & Plückthun, A. (2011) · Current Opinion in Biotechnology · doi:10.1016/j.copbio.2011.06.004 · Cited by 239

In Vivo Activation of the p53 Tumor Suppressor Pathway by an Engineered Cyclotide

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

London, N., Raveh, B., & Schueler-Furman, O. (2013) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2013.10.011 · Cited by 223

Synthesis, biological activity and conformational analysis of cyclic GRF analogs

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Functionalised staple linkages for modulating the cellular activity of stapled peptides

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Stapled Peptides with Improved Potency and Specificity That Activate p53

Brown, C. J., Quah, S. T., Jong, J., Goh, A. M., Chiam, P. C., Khoo, K. H., Choong, M. L., Lee, M. A., Yurlova, L., Zolghadr, K., et al. (2013) · ACS Chemical Biology · doi:10.1021/cb3005148 · Cited by 209

Small‐Molecule Stabilization of Protein–Protein Interactions: An Underestimated Concept in Drug Discovery?

Thiel, P., Kaiser, M., & Ottmann, C. (2012) · Angewandte Chemie International Edition · doi:10.1002/anie.201107616 · Cited by 207

Comprehensive analysis of loops at protein-protein interfaces for macrocycle design

Gavenonis, J., Sheneman, B. A., Siegert, T. R., Eshelman, M. R., & Kritzer, J. A. (2014) · Nature Chemical Biology · doi:10.1038/nchembio.1580 · Cited by 198

Synthesis and Conformational Analysis of a Cyclic Peptide Obtained via i to i+4 Intramolecular Side-Chain to Side-Chain Azide−Alkyne 1,3-Dipolar Cycloaddition

Cantel, S., Le Chevalier Isaad, A., Scrima, M., Levy, J. J., DiMarchi, R. D., Rovero, P., Halperin, J. A., D’Ursi, A. M., Papini, A. M., & Chorev, M. (2008) · The Journal of Organic Chemistry · doi:10.1021/jo800142s · Cited by 190

A Cyclic Peptide Inhibitor of HIF-1 Heterodimerization That Inhibits Hypoxia Signaling in Cancer Cells

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

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Label‐Free Microscale Thermophoresis Discriminates Sites and Affinity of Protein–Ligand Binding

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Mediation of the antiapoptotic activity of Bcl-xL protein upon interaction with VDAC1 protein

Arbel, N., Ben-Hail, D., & Shoshan-Barmatz, V. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.m112.345918 · Cited by 179

Structural biology and bioinformatics in drug design: opportunities and challenges for target identification and lead discovery

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Early Endosomal Escape of a Cyclic Cell-Penetrating Peptide Allows Effective Cytosolic Cargo Delivery

Qian, Z., LaRochelle, J. R., Jiang, B., Lian, W., Hard, R. L., Selner, N. G., Luechapanichkul, R., Barrios, A. M., & Pei, D. (2014) · Biochemistry · doi:10.1021/bi5004102 · Cited by 176

Comparative α‐Helicity of Cyclic Pentapeptides in Water

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Can self‐inhibitory peptides be derived from the interfaces of globular protein–protein interactions?

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Probing the Structural Requirements of Peptoids That Inhibit HDM2−p53 Interactions

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

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Inhibition of HIV Budding by a Genetically Selected Cyclic Peptide Targeting the Gag−TSG101 Interaction

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

Horne, W. S., Boersma, M., Windsor, M. A., & Gellman, S. H. (2008) · Angewandte Chemie International Edition · doi:10.1002/anie.200705315 · Cited by 153

Constrained Peptides with Target‐Adapted Cross‐Links as Inhibitors of a Pathogenic Protein–Protein Interaction

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Applications of saturation transfer difference NMR in biological systems

Bhunia, A., Bhattacharjya, S., & Chatterjee, S. (2011) · Drug Discovery Today · doi:10.1016/j.drudis.2011.12.016 · Cited by 143

Stabilizing the Pro-Apoptotic BimBH3 Helix (BimSAHB) Does Not Necessarily Enhance Affinity or Biological Activity

Okamoto, T., Zobel, K., Fedorova, A., Quan, C., Yang, H., Fairbrother, W. J., Huang, D. C. S., Smith, B. J., Deshayes, K., & Czabotar, P. E. (2013) · ACS Chemical Biology · doi:10.1021/cb3005403 · Cited by 136

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

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Large-scale interaction profiling of PDZ domains through proteomic peptide-phage display using human and viral phage peptidomes

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Peptides And Peptide Conjugates: Therapeutics On The Upward Path

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Protein–protein interactions as druggable targets: recent technological advances

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Cell-Permeable Bicyclic Peptide Inhibitors against Intracellular Proteins

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

Bautista, A. D., Appelbaum, J., Craig, C. J., Michel, J., & Schepartz, A. (2010) · Journal of the American Chemical Society · doi:10.1021/ja910715u · Cited by 130

Screening Bicyclic Peptide Libraries for Protein–Protein Interaction Inhibitors: Discovery of a Tumor Necrosis Factor-α Antagonist

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

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Using a Fragment‐Based Approach To Target Protein–Protein Interactions

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Interplay among side chain sequence, backbone composition, and residue rigidification in polypeptide folding and assembly

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Progress towards the development of SH2 domain inhibitors

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Diketopiperazines as a Tool for the Study of Transport across the Blood−Brain Barrier (BBB) and Their Potential Use as BBB-Shuttles

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Flexizymes: Their Evolutionary History and the Origin of Catalytic Function

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Light‐Regulated Stapled Peptides to Inhibit Protein–Protein Interactions Involved in Clathrin‐Mediated Endocytosis

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Peptidic modulators of protein‐protein interactions: Progress and challenges in computational design

Rubinstein, M., & Niv, M. Y. (2009) · Biopolymers · doi:10.1002/bip.21164 · Cited by 101

Potential therapeutic applications of the cyclotides and related cystine knot mini-proteins

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Miniature Protein Inhibitors of the p53–hDM2 Interaction

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Direct Targeting of Rab‐GTPase–Effector Interactions

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

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State-of-the-Art High-Speed Atomic Force Microscopy for Investigation of Single-Molecular Dynamics of Proteins

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Stability and structural recovery of the tetramerization domain of p53-R337H mutant induced by a designed templating ligand

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A cyclic peptide inhibitor of C-terminal binding protein dimerization links metabolism with mitotic fidelity in breast cancer cells

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Shuttle‐Mediated Drug Delivery to the Brain

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Comparing experimental and computational alanine scanning techniques for probing a prototypical protein–protein interaction

Bradshaw, R. T., Patel, B. H., Tate, E. W., Leatherbarrow, R. J., & Gould, I. R. (2010) · Protein Engineering Design and Selection · doi:10.1093/protein/gzq047 · Cited by 85

Phage Selection of Photoswitchable Peptide Ligands

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Synthesis of Constrained Head‐to‐Tail Cyclic Tetrapeptides by an Imine‐Induced Ring‐Closing/Contraction Strategy

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Photochemical Regulation of DNA‐Binding Specificity of MyoD

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Computational and Experimental Studies on β-Sheet Breakers Targeting Aβ1–40 Fibrils

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Context-Based Identification of Protein-Protein Interfaces and “Hot-Spot” Residues

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Design, Synthesis and Characterization of a New Anionic Cell‐Penetrating Peptide: SAP(E)

Martín, I., Teixidò, M., & Giralt, E. (2011) · ChemBioChem · doi:10.1002/cbic.201000679 · Cited by 79

Discovery of Light-Responsive Ligands through Screening of a Light-Responsive Genetically Encoded Library

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Synthetic mimetics of protein secondary structure domains

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Modular α-Helical Mimetics with Antiviral Activity against Respiratory Syncitial Virus

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Bio-inspired design and potential biomedical applications of a novel class of high-affinity peptides.

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Solid-phase synthesis of short α-helices stabilized by the hydrogen bond surrogate approach

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