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

Selective and Potent Proteomimetic Inhibitors of Intracellular Protein-Protein Interactions

(2015) Anna Barnard et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Biology-Oriented Synthesis of a Withanolide-Inspired Compound Collection Reveals Novel Modulators of Hedgehog Signaling

(2015) Jakub Švenda et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Divergent Cascade Construction of Skeletally Diverse “Privileged” Pyrazole-Derived Molecular Architectures

(2015) Yongqiang Zhang et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Fragment-Based Drug Discovery of 2-Thiazolidinones as BRD4 Inhibitors: 2. Structure-Based Optimization

(2015) Lele Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Perturbation of the c-Myc–Max Protein–Protein Interaction via Synthetic α-Helix Mimetics

(2015) Kwan-Young Jung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selectivity by Small-Molecule Inhibitors of Protein Interactions Can Be Driven by Protein Surface Fluctuations

(2015) David K. Johnson et al.   PLoS Computational Biology

A novel drug discovery strategy: Mechanistic investigation of an enantiomeric antitumor agent targeting dual p53 and NF-κB pathways

(2015) Chunlin Zhuang et al.   Oncotarget

Inhibition of CDC25B Phosphatase Through Disruption of Protein–Protein Interaction

(2014) George Lund et al.   ACS Chemical Biology

Diversity-Oriented Synthesis of Drug-Like Macrocyclic Scaffolds Using an Orthogonal Organo- and Metal Catalysis Strategy

(2014) André Grossmann 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

Modulators of Protein–Protein Interactions

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

NMR-Based Approaches for the Identification and Optimization of Inhibitors of Protein–Protein Interactions

(2014) Elisa Barile et al.   CHEMICAL REVIEWS

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

Updated Research and Applications of Small Molecule Inhibitors of Keap1-Nrf2 Protein-Protein Interaction: a Review

(2014) Chunlin Zhuang et al.   CURRENT MEDICINAL CHEMISTRY

Structure-based design of small-molecule protein–protein interaction modulators: the story so far

(2014) Federico Falchi et al.   Future Medicinal Chemistry

Rapid Identification of Keap1–Nrf2 Small-Molecule Inhibitors through Structure-Based Virtual Screening and Hit-Based Substructure Search

(2014) Chunlin Zhuang et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Double-Edged Swords as Cancer Therapeutics: Novel, Orally Active, Small Molecules Simultaneously Inhibit p53–MDM2 Interaction and the NF-κB Pathway

(2014) Chunlin Zhuang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure Guided Design and Kinetic Analysis of Highly Potent Benzimidazole Inhibitors Targeting the PDEδ Prenyl Binding Site

(2014) Gunther Zimmermann et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Potent Keap1–Nrf2 Protein–Protein Interaction Inhibitor Based on Molecular Binding Determinants Analysis

(2014) Zheng-Yu Jiang et al.   JOURNAL OF MEDICINAL CHEMISTRY

High-Affinity Small-Molecule Inhibitors of the Menin-Mixed Lineage Leukemia (MLL) Interaction Closely Mimic a Natural Protein–Protein Interaction

(2014) Shihan He et al.   JOURNAL OF MEDICINAL CHEMISTRY

Thienoquinolines as Novel Disruptors of the PKCε/RACK2 Protein–Protein Interaction

(2014) Florian Rechfeld et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of an Atg8-Atg3 Protein–Protein Interaction Inhibitor from the Medicines for Malaria Venture Malaria Box Active in Blood and Liver Stage Plasmodium falciparum Parasites

(2014) Adelaide U.P. Hain et al.   JOURNAL OF MEDICINAL CHEMISTRY

Drug Design Targeting Protein–Protein Interactions (PPIs) Using Multiple Ligand Simultaneous Docking (MLSD) and Drug Repositioning: Discovery of Raloxifene and Bazedoxifene as Novel Inhibitors of IL-6/GP130 Interface

(2014) Huameng Li 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

Privileged Structures: Efficient Chemical “Navigators” toward Unexplored Biologically Relevant Chemical Spaces

(2014) Jonghoon Kim et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Drug-Like ProteinProtein Interaction Modulators: Challenges and Opportunities for Drug Discovery and Chemical Biology

(2014) Bruno O. Villoutreix et al.   Molecular Informatics

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

Fragment-Based Library Generation for the Discovery of a Peptidomimetic p53-Mdm4 Inhibitor

(2014) André Boltjes et al.   ACS Combinatorial Science

Targeting the Tcf4 G13ANDE17 Binding Site To Selectively Disrupt β-Catenin/T-Cell Factor Protein–Protein Interactions

(2013) Zheng Huang et al.   ACS Chemical Biology

Inhibitors of Difficult Protein–Protein Interactions Identified by High-Throughput Screening of Multiprotein Complexes

(2013) Laura C. Cesa et al.   ACS Chemical Biology

Catalytic Asymmetric Synthesis of Mixed 3,3′-Bisindoles and Their Evaluation as Wnt Signaling Inhibitors

(2013) Takayoshi Arai et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Targeting Protein-Protein Interaction by Small Molecules

(2013) Lingyan Jin et al.   Annual Review of Pharmacology and Toxicology

Small molecules inhibit the interaction of Nrf2 and the Keap1 Kelch domain through a non-covalent mechanism

(2013) Douglas Marcotte et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of a small-molecule inhibitor and cellular probe of Keap1–Nrf2 protein–protein interaction

(2013) Longqin Hu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

MDM2 Small-Molecule Antagonist RG7112 Activates p53 Signaling and Regresses Human Tumors in Preclinical Cancer Models

(2013) C. Tovar et al.   CANCER RESEARCH

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

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

Protein–protein interactions as druggable targets: recent technological advances

(2013) Alicia P Higueruelo et al.   CURRENT OPINION IN PHARMACOLOGY

Structural Properties of Non-Traditional Drug Targets Present New Challenges for Virtual Screening

(2013) Ragul Gowthaman et al.   Journal of Chemical Information and Modeling

Fragment-Based Drug Discovery of 2-Thiazolidinones as Inhibitors of the Histone Reader BRD4 Bromodomain

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

Fragment-Based Identification of a Locus in the Sec7 Domain of Arno for the Design of Protein–Protein Interaction Inhibitors

(2013) Jad Rouhana et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Novel Small Molecule Inhibitor Targeting the Frataxin/Ubiquitin Interaction via Structure-Based Virtual Screening and Bioassays

(2013) Antonio Lavecchia et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Making of I-BET762, a BET Bromodomain Inhibitor Now in Clinical Development

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

Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening

(2013) Lewis R. Vidler et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Discovery of 8-Hydroxyquinoline Inhibitors of the HIV-1 Integrase–Lens Epithelium-Derived Growth Factor/p75 (IN–LEDGF/p75) Interaction

(2013) Erik Serrao et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2013) Gunther Zimmermann et al.   NATURE

Drug for an 'undruggable' protein

(2013) Nicole M. Baker et al.   NATURE

A strategy for the diversity-oriented synthesis of macrocyclic scaffolds using multidimensional coupling

(2013) Henning S. G. Beckmann et al.   Nature Chemistry

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

(2013) Valeria Azzarito et al.   Nature Chemistry

Targeting protein–protein interactions as an anticancer strategy

(2013) Andrei A. Ivanov et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

(2013) Binh Vu et al.   ACS Medicinal Chemistry Letters

High-Throughput Selectivity Assays for Small-Molecule Inhibitors of β-Catenin/T-Cell Factor Protein–Protein Interactions

(2013) Min Zhang et al.   ACS Medicinal Chemistry Letters

Facile Construction of Structurally Diverse Thiazolidinedione-Derived Compounds via Divergent Stereoselective Cascade Organocatalysis and Their Biological Exploratory Studies

(2013) Yongqiang Zhang et al.   ACS Combinatorial Science

Druggable Protein Interaction Sites Are More Predisposed to Surface Pocket Formation than the Rest of the Protein Surface

(2013) David K. Johnson et al.   PLoS Computational Biology

Structure-Based Virtual Screening for Drug Discovery: a Problem-Centric Review

(2012) Tiejun Cheng et al.   AAPS Journal

Comprehensive Peptidomimetic Libraries Targeting Protein–Protein Interactions

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

Regulating the ARNT/TACC3 Axis: Multiple Approaches to Manipulating Protein/Protein Interactions with Small Molecules

(2012) Yirui Guo et al.   ACS Chemical Biology

Rational Design of Small-Molecule Inhibitors for β-Catenin/T-Cell Factor Protein–Protein Interactions by Bioisostere Replacement

(2012) Binxun Yu et al.   ACS Chemical Biology

Small-Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α

(2012) Dennis L. Buckley et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of Small-Molecule Inhibitors of the TLR1/TLR2 Complex

(2012) Kui Cheng et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Sekikaic Acid and Lobaric Acid Target a Dynamic Interface of the Coactivator CBP/p300

(2012) Chinmay Y. Majmudar et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

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

Pharmacophore identification of c-Myc inhibitor 10074-G5

(2012) Jeremy L. Yap et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

An integrated fragment based screening approach for the discovery of small molecule modulators of the VWF–GPIbα interaction

(2012) Rani A. Jose et al.   CHEMICAL COMMUNICATIONS

Diversity-oriented synthesis: producing chemical tools for dissecting biology

(2012) Cornelius J. O' Connor et al.   CHEMICAL SOCIETY REVIEWS

Dissecting Fragment-Based Lead Discovery at the von Hippel-Lindau Protein:Hypoxia Inducible Factor 1α Protein-Protein Interface

(2012) Inge Van Molle et al.   CHEMISTRY & BIOLOGY

Phase II Study of Single-Agent Navitoclax (ABT-263) and Biomarker Correlates in Patients with Relapsed Small Cell Lung Cancer

(2012) C. M. Rudin et al.   CLINICAL CANCER RESEARCH

A Leap into the Chemical Space of Protein-Protein Interaction Inhibitors

(2012) B. O. Villoutreix et al.   CURRENT PHARMACEUTICAL DESIGN

Using Fragment-Based Technologies to Target Protein-Protein Interactions

(2012) Justin F. Bower et al.   CURRENT PHARMACEUTICAL DESIGN

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

Relationship between Hot Spot Residues and Ligand Binding Hot Spots in Protein–Protein Interfaces

(2012) Brandon S. Zerbe et al.   Journal of Chemical Information and Modeling

Antagonists of Protein–Protein Interactions Made Easy?

(2012) Maurizio Pellecchia   JOURNAL OF MEDICINAL CHEMISTRY

Discovery, Synthesis, and Biological Evaluation of Orally Active Pyrrolidone Derivatives as Novel Inhibitors of p53–MDM2 Protein–Protein Interaction

(2012) Chunlin Zhuang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Potent Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods and Structure-Based Design

(2012) Anders Friberg et al.   JOURNAL OF MEDICINAL CHEMISTRY

Progress in the Development and Application of Small Molecule Inhibitors of Bromodomain–Acetyl-lysine Interactions

(2012) David S. Hewings et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting the von Hippel–Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1α Interaction

(2012) Dennis L. Buckley et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Effect of the MDM2 antagonist RG7112 on the P53 pathway in patients with MDM2-amplified, well-differentiated or dedifferentiated liposarcoma: an exploratory proof-of-mechanism study

(2012) Isabelle Ray-Coquard et al.   LANCET ONCOLOGY

Small Molecule Modulators of Keap1-Nrf2-ARE Pathway as Potential Preventive and Therapeutic Agents

(2012) Sadagopan Magesh et al.   MEDICINAL RESEARCH REVIEWS

Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia

(2012) Jolanta Grembecka et al.   Nature Chemical Biology

Protein–protein interaction inhibitors get into the groove

(2012) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Enabling Large-Scale Design, Synthesis and Validation of Small Molecule Protein-Protein Antagonists

(2012) David Koes et al.   PLoS One

Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity

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

Biophysical and computational fragment-based approaches to targeting protein–protein interactions: applications in structure-guided drug discovery

(2012) Anja Winter et al.   QUARTERLY REVIEWS OF BIOPHYSICS

Structural biology and drug discovery for protein–protein interactions

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

Place your BETs: the therapeutic potential of bromodomains

(2012) R.K. Prinjha et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Targeting Multiple Conformations Leads to Small Molecule Inhibitors of the uPAR·uPA Protein–Protein Interaction That Block Cancer Cell Invasion

(2011) May Khanna et al.   ACS Chemical Biology

Immunosuppressive Small Molecule Discovered by Structure-Based Virtual Screening for Inhibitors of Protein-Protein Interactions

(2011) Tim Geppert et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Biology-Oriented Synthesis

(2011) Stefan Wetzel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Multicomponent Reaction Design in the Quest for Molecular Complexity and Diversity

(2011) Eelco Ruijter et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Small molecule inhibitor of the RPA70 N-terminal protein interaction domain discovered using in silico and in vitro methods

(2011) Jason G. Glanzer et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A Small Molecule Binding to the Coactivator CREB-Binding Protein Blocks Apoptosis in Cardiomyocytes

(2011) Jagat C. Borah et al.   CHEMISTRY & BIOLOGY

Non-Peptidic α-Helical Mimetics as Protein-Protein Interaction Inhibitors

(2011) M. B. Dewal et al.   CURRENT MEDICINAL CHEMISTRY

State-of-the-art in ligand-based virtual screening

(2011) Peter Ripphausen et al.   DRUG DISCOVERY TODAY

Druggability assessment of protein–protein interfaces

(2011) Jutta Wanner et al.   Future Medicinal Chemistry

Hot Spots and Transient Pockets: Predicting the Determinants of Small-Molecule Binding to a Protein–Protein Interface

(2011) Alexander Metz et al.   Journal of Chemical Information and Modeling

Virtual screening for compounds that mimic protein-protein interface epitopes

(2011) Tim Geppert et al.   JOURNAL OF COMPUTATIONAL CHEMISTRY

Fragment-based drug discovery: what really works. An interview with Sandy Farmer of Boehringer Ingelheim

(2011) Wendy A. Warr   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

A Small Nonrule of 3 Compatible Fragment Library Provides High Hit Rate of Endothiapepsin Crystal Structures with Various Fragment Chemotypes

(2011) Helene Köster et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Structure−Activity Relationship Exploration of 1-Substituted 4-Aroyl-3-hydroxy-5-phenyl-1H-pyrrol-2(5H)-one Analogues as Inhibitors of the Annexin A2−S100A10 Protein Interaction

(2011) Tummala R. K. Reddy et al.   JOURNAL OF MEDICINAL CHEMISTRY

Screening Multicomponent Reactions for X-Linked Inhibitor of Apoptosis-Baculoviral Inhibitor of Apoptosis Protein Repeats Domain Binder

(2011) Ilaria Monfardini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Macrocycles Are Great Cycles: Applications, Opportunities, and Challenges of Synthetic Macrocycles in Drug Discovery

(2011) Eric Marsault et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Discovery of Bromodomain Inhibitors Part 1: Inhibitor Binding Modes and Implications for Lead Discovery

(2011) Chun-wa Chung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Discovery of Bromodomain Inhibitors Part 2: Optimization of Phenylisoxazole Sulfonamides

(2011) Paul Bamborough et al.   JOURNAL OF MEDICINAL CHEMISTRY

Assessing Helical Protein Interfaces for Inhibitor Design

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

Natural product–inspired cascade synthesis yields modulators of centrosome integrity

(2011) Heiko Dückert et al.   Nature Chemical Biology

Structural conservation of druggable hot spots in protein-protein interfaces

(2011) D. Kozakov et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Route to three-dimensional fragments using diversity-oriented synthesis

(2011) A. W. Hung et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Minimal ensembles of side chain conformers for modeling protein-protein interactions

(2011) Dmitri Beglov et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

Hydrophobic Binding Hot Spots of Bcl-xL Protein−Protein Interfaces by Cosolvent Molecular Dynamics Simulation

(2011) Chao-Yie Yang et al.   ACS Medicinal Chemistry Letters

Bioactivity-Guided Navigation of Chemical Space

(2010) Robin S. Bon et al.   ACCOUNTS OF CHEMICAL RESEARCH

Robust Generation of Lead Compounds for Protein-Protein Interactions by Computational and MCR Chemistry: p53/Hdm2 Antagonists

(2010) Anna Czarna et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Application of a novel in silico high-throughput screen to identify selective inhibitors for protein–protein interactions

(2010) Catherine Joce et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of the first non-peptidic small molecule inhibitor of the c-Abl/14-3-3 protein–protein interactions able to drive sensitive and Imatinib-resistant leukemia cells to apoptosis

(2010) Valentina Corradi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structure–activity relationship (SAR) of the α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists

(2010) Min Zhong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Fragmenting the S100B-p53 Interaction: Combined Virtual/Biophysical Screening Approaches to Identify Ligands

(2010) Mariangela Agamennone et al.   ChemMedChem

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

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

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

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

Highly enantioselective synthesis and cellular evaluation of spirooxindoles inspired by natural products

(2010) Andrey P. Antonchick et al.   Nature Chemistry

Oligooxopiperazines as Nonpeptidic α-Helix Mimetics

(2010) Petra Tošovská et al.   ORGANIC LETTERS

Diversity-oriented synthesis as a tool for the discovery of novel biologically active small molecules

(2010) Warren R.J.D. Galloway et al.   Nature Communications

Designing Focused Chemical Libraries Enriched in Protein-Protein Interaction Inhibitors using Machine-Learning Methods

(2010) Christelle Reynès et al.   PLoS Computational Biology

Efficient Drug Lead Discovery and Optimization

(2009) William L. Jorgensen   ACCOUNTS OF CHEMICAL RESEARCH

Identification of small-molecule inhibitors of the JIP–JNK interaction

(2009) Tracy Chen et al.   BIOCHEMICAL JOURNAL

Diversity-oriented synthesis of a cytisine-inspired pyridone library leading to the discovery of novel inhibitors of Bcl-2

(2009) Lisa A. Marcaurelle et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

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

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

Long-timescale molecular dynamics simulations of protein structure and function

(2009) John L Klepeis et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Fragment Library Screening and Lead Characterization Using SPR Biosensors

(2009) U. Danielson   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Identifying and Characterizing Binding Sites and Assessing Druggability

(2009) Thomas A. Halgren   Journal of Chemical Information and Modeling

Potent and Orally Active Small-Molecule Inhibitors of the MDM2−p53 Interaction

(2009) Shanghai Yu et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Multiple Independent Binding Sites for Small-Molecule Inhibitors on the Oncoprotein c-Myc

(2009) Dalia I. Hammoudeh et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

An MDM2 antagonist (MI-319) restores p53 functions and increases the life span of orally treated follicular lymphoma bearing animals

(2009) Ramzi M Mohammad et al.   Molecular Cancer

Molecular diversity by design

(2009) Stuart L. Schreiber   NATURE

A small molecule that binds Hedgehog and blocks its signaling in human cells

(2009) Benjamin Z Stanton et al.   Nature Chemical Biology

The rise of fragment-based drug discovery

(2009) Christopher W. Murray et al.   Nature Chemistry

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

(2008) Ozlem Keskin et al.   CHEMICAL REVIEWS

In Silico-In Vitro Screening of Protein-Protein Interactions: Towards the Next Generation of Therapeutics

(2008) Bruno Villoutreix et al.   CURRENT PHARMACEUTICAL BIOTECHNOLOGY

Drug-Like Inhibitors of Protein-Protein Interactions: A Structural Examination of Effective Protein Mimicry

(2008) D. Fry   CURRENT PROTEIN & PEPTIDE SCIENCE

Ligand efficiency and fragment-based drug discovery

(2008) Scott D. Bembenek et al.   DRUG DISCOVERY TODAY

Predicting druggable binding sites at the protein–protein interface

(2008) Jonathan C. Fuller et al.   DRUG DISCOVERY TODAY

Synthesis of an Oxazole–Pyrrole–Piperazine Scaffold as an α-Helix Mimetic

(2008) Lionel Moisan et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

What induces pocket openings on protein surface patches involved in protein–protein interactions?

(2008) Susanne Eyrisch et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Recent Developments in Fragment-Based Drug Discovery

(2008) Miles Congreve et al.   JOURNAL OF MEDICINAL CHEMISTRY

Differences between High- and Low-Affinity Complexes of Enzymes and Nonenzymes

(2008) Heather A. Carlson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of an Orally Bioavailable Small Molecule Inhibitor of Prosurvival B-Cell Lymphoma 2 Proteins

(2008) Cheol-Min Park et al.   JOURNAL OF MEDICINAL CHEMISTRY

Minimal Pharmacophoric Elements and Fragment Hopping, an Approach Directed at Molecular Diversity and Isozyme Selectivity. Design of Selective Neuronal Nitric Oxide Synthase Inhibitors

(2008) Haitao Ji et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

An empirical framework for binary interactome mapping

(2008) Kavitha Venkatesan et al.   NATURE METHODS

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

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

Identification of a new JNK inhibitor targeting the JNK-JIP interaction site

(2008) J. L. Stebbins 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

Towards the Optimal Screening Collection: A Synthesis Strategy

(2007) Thomas E. Nielsen et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION