Protein–protein interaction modulator drug discovery: past efforts and future opportunities using a rich source of low- and high-throughput screening assays

Drugging the p53 pathway: understanding the route to clinical efficacy

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

Hepatitis C NS5A protein: two drug targets within the same protein with different mechanisms of resistance

(2014) Precious J Lim et al.   Current Opinion in Virology

A Time-Resolved Fluorescence Resonance Energy Transfer Assay for High-Throughput Screening of 14-3-3 Protein–Protein Interaction Inhibitors

(2013) Yuhong Du et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Identification of small-molecule inhibitors of the human S100B–p53 interaction and evaluation of their activity in human melanoma cells

(2013) Chihoko Yoshimura et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Phenotypic vs. Target-Based Drug Discovery for First-in-Class Medicines

(2013) D C Swinney   CLINICAL PHARMACOLOGY & THERAPEUTICS

Fragment-based drug discovery using NMR spectroscopy

(2013) Mary J. Harner et al.   JOURNAL OF BIOMOLECULAR NMR

Small molecule inhibition of the KRAS–PDEδ interaction impairs oncogenic KRAS signalling

(2013) Gunther Zimmermann et al.   NATURE

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

(2012) Susanne A. I. Seidel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Bimolecular fluorescence complementation (BiFC): A 5-year update and future perspectives

(2012) Yutaka Kodama et al.   BIOTECHNIQUES

Rational Design of Small Molecule Inhibitors Targeting RhoA Subfamily Rho GTPases

(2012) Xun Shang et al.   CHEMISTRY & BIOLOGY

Rational Design of Small Molecule Inhibitors Targeting the Rac GTPase-p67phox Signaling Axis in Inflammation

(2012) Emily E. Bosco et al.   CHEMISTRY & BIOLOGY

Features of protein–protein interactions that translate into potent inhibitors: topology, surface area and affinity

(2012) Matthew C. Smith et al.   EXPERT REVIEWS IN MOLECULAR MEDICINE

Microscale thermophoresis quantifies biomolecular interactions under previously challenging conditions

(2012) Susanne A.I. Seidel et al.   METHODS

Discovery of small molecule cancer drugs: Successes, challenges and opportunities

(2012) Swen Hoelder et al.   Molecular Oncology

Improving FRET dynamic range with bright green and red fluorescent proteins

(2012) Amy J Lam et al.   NATURE METHODS

Structural biology and drug discovery for protein–protein interactions

(2012) Harry Jubb et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye

(2012) Min Zhong et al.   ACS Medicinal Chemistry Letters

An intrinsically labile α-helix abutting the BCL9-binding site of β-catenin is required for its inhibition by carnosic acid

(2012) Marc de la Roche et al.   Nature Communications

Dr. PIAS 2.0: an update of a database of predicted druggable protein–protein interactions

(2012) Nobuyoshi Sugaya et al.   Database-The Journal of Biological Databases and Curation

Molecular Interaction Studies Using Microscale Thermophoresis

(2011) Moran Jerabek-Willemsen et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Dr. PIAS: an integrative system for assessing the druggability of protein-protein interactions

(2011) Nobuyoshi Sugaya et al.   BMC BIOINFORMATICS

Role of the Clathrin Terminal Domain in Regulating Coated Pit Dynamics Revealed by Small Molecule Inhibition

(2011) Lisa von Kleist et al.   CELL

Thermodynamics-based drug design: strategies for inhibiting protein–protein interactions

(2011) Arne Schön et al.   Future Medicinal Chemistry

NF-κB Essential Modulator (NEMO) Interaction with Linear and Lys-63 Ubiquitin Chains Contributes to NF-κB Activation

(2011) Kamyar Hadian et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

An orthosteric inhibitor of the Ras-Sos interaction

(2011) Anupam Patgiri et al.   Nature Chemical Biology

How were new medicines discovered?

(2011) David C. Swinney et al.   NATURE REVIEWS DRUG DISCOVERY

Impact of high-throughput screening in biomedical research

(2011) Ricardo Macarron et al.   NATURE REVIEWS DRUG DISCOVERY

Using BRET to study chemical compound-induced disruptions of the p53-HDM2 interactions in live cells

(2010) Anne Mazars et al.   Biotechnology Journal

Research Article: Effective and Specific Inhibition of the CD40-CD154 Costimulatory Interaction by a Naphthalenesulphonic Acid Derivative

(2010) Emilio Margolles-Clark et al.   Chemical Biology & Drug Design

Fluorescence polarization assays in small molecule screening

(2010) Wendy A Lea et al.   Expert Opinion on Drug Discovery

Proximity ligation assays: a recent addition to the proteomics toolbox

(2010) Irene Weibrecht et al.   Expert Review of Proteomics

Targeting protein–protein interactions for therapeutic intervention: a challenge for the future

(2010) Giovanna Zinzalla et al.   Future Medicinal Chemistry

Small-molecule protein-protein interaction inhibitors: Therapeutic potential in light of molecular size, chemical space, and ligand binding efficiency considerations

(2010) Peter Buchwald   IUBMB LIFE

Drug- and Lead-likeness, Target Class, and Molecular Diversity Analysis of 7.9 Million Commercially Available Organic Compounds Provided by 29 Suppliers

(2010) Alexander Chuprina et al.   Journal of Chemical Information and Modeling

New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

(2010) Jonathan B. Baell et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Novel Tryptamine Derivative JNJ-26854165 Induces Wild-Type p53- and E2F1-Mediated Apoptosis in Acute Myeloid and Lymphoid Leukemias

(2010) K. Kojima et al.   MOLECULAR CANCER THERAPEUTICS

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma

(2010) Gideon Bollag et al.   NATURE

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication

(2010) Frauke Christ et al.   Nature Chemical Biology

A Flow Cytometry-Based FRET Assay to Identify and Analyse Protein-Protein Interactions in Living Cells

(2010) Carina Banning et al.   PLoS One

Protein-binding assays in biological liquids using microscale thermophoresis

(2010) Christoph J. Wienken et al.   Nature Communications

Assessing the druggability of protein-protein interactions by a supervised machine-learning method

(2009) Nobuyoshi Sugaya et al.   BMC BIOINFORMATICS

SPR Imaging for High Throughput, Label-Free Interaction Analysis

(2009) Christopher Lausted et al.   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

Identifying druggable disease-modifying gene products

(2009) Scott J Dixon et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Disrupting the Rb-Raf-1 interaction: A potential therapeutic target for cancer

(2009) R.K. Davis et al.   DRUG NEWS & PERSPECTIVES

Small-molecule costimulatory blockade: organic dye inhibitors of the CD40–CD154 interaction

(2009) Emilio Margolles-Clark et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Bimolecular Fluorescence Complementation (BiFC) Analysis as a Probe of Protein Interactions in Living Cells

(2008) Tom K. Kerppola   Annual Review of Biophysics

The BRET technology and its application to screening assays

(2008) Johan Bacart et al.   Biotechnology Journal

Characterizing proteins and their interactions in cells and tissues using the in situ proximity ligation assay

(2008) Ola Söderberg et al.   METHODS

A Fluorescent Two-hybrid Assay for Direct Visualization of Protein Interactions in Living Cells

(2008) Kourosh Zolghadr et al.   MOLECULAR & CELLULAR PROTEOMICS