Stabilization of protein-protein interactions in drug discovery

Stabilization of protein–protein interaction complexes through small molecules

(2016) Barbara Zarzycka et al.   DRUG DISCOVERY TODAY

A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

(2016) Mary E. Matyskiela et al.   NATURE

Activation of NMDA receptors and the mechanism of inhibition by ifenprodil

(2016) Nami Tajima et al.   NATURE

Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase

(2016) Georg Petzold et al.   NATURE

Potent and selective bivalent inhibitors of BET bromodomains

(2016) Michael J Waring et al.   Nature Chemical Biology

Repositioning tolcapone as a potent inhibitor of transthyretin amyloidogenesis and associated cellular toxicity

(2016) Ricardo Sant'Anna et al.   Nature Communications

Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1)

(2016) Krzysztof M. Zak et al.   Oncotarget

Stabilizer-Guided Inhibition of Protein-Protein Interactions

(2015) Lech-Gustav Milroy et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Inhibition by stabilization: targeting the Plasmodium falciparum aldolase–TRAP complex

(2015) Sondra Maureen Nemetski et al.   MALARIA JOURNAL

Stabilization of Protein–Protein Interactions in chemical biology and drug discovery

(2015) David Bier et al.   PROGRESS IN BIOPHYSICS & MOLECULAR BIOLOGY

Structure and inhibition of EV-D68, a virus that causes respiratory illness in children

(2015) Y. Liu et al.   SCIENCE

Modulators of Protein–Protein Interactions

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

Stabilization of protein–protein interactions by small molecules

(2014) Fabrizio Giordanetto et al.   DRUG DISCOVERY TODAY

Anthracycline-induced cardiotoxicity: Overview of studies examining the roles of oxidative stress and free cellular iron

(2014) Tomáš Šimůnek et al.   Pharmacological Reports

Actin Dynamics, Architecture, and Mechanics in Cell Motility

(2014) Laurent Blanchoin et al.   PHYSIOLOGICAL REVIEWS

Rational Design of Small-Molecule Stabilizers of Spermine Synthase Dimer by Virtual Screening and Free Energy-Based Approach

(2014) Zhe Zhang et al.   PLoS One

Crystal structure of a heterotetrameric NMDA receptor ion channel

(2014) E. Karakas et al.   SCIENCE

A Novel Class of Anticancer Compounds Targets the Actin Cytoskeleton in Tumor Cells

(2013) J. R. Stehn et al.   CANCER RESEARCH

Transcriptional Regulation and Its Misregulation in Disease

(2013) Tong Ihn Lee et al.   CELL

A Semisynthetic Fusicoccane Stabilizes a Protein-Protein Interaction and Enhances the Expression of K+ Channels at the Cell Surface

(2013) Carolin Anders et al.   CHEMISTRY & BIOLOGY

Chromatin proteins and modifications as drug targets

(2013) Kristian Helin et al.   NATURE

E2 enzyme inhibition by stabilization of a low-affinity interface with ubiquitin

(2013) Hao Huang et al.   Nature Chemical Biology

Catalytic Inhibitors of Topoisomerase II Differently Modulate the Toxicity of Anthracyclines in Cardiac and Cancer Cells

(2013) Anna Vavrova et al.   PLoS One

Unstructured to structured transition of an intrinsically disordered protein peptide in coupling Ca2+-sensing and SK channel activation

(2013) M. Zhang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Interaction of 14-3-3 proteins with the Estrogen Receptor Alpha F domain provides a drug target interface

(2013) I. J. De Vries-van Leeuwen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Ligand binding and aggregation of pathogenic SOD1

(2013) Gareth S.A. Wright et al.   Nature Communications

Synthesis of a Phosphoserine Mimetic Prodrug with Potent 14-3-3 Protein Inhibitory Activity

(2012) Allison Arrendale et al.   CHEMISTRY & BIOLOGY

An Optimised Small-Molecule Stabiliser of the 14-3-3-PMA2 Protein-Protein Interaction

(2012) Anja Richter et al.   CHEMISTRY-A EUROPEAN JOURNAL

X-ray Structures of Progesterone Receptor Ligand Binding Domain in Its Agonist State Reveal Differing Mechanisms for Mixed Profiles of 11β-Substituted Steroids

(2012) Scott J. Lusher et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Selective Chemical Imaging of Static Actin in Live Cells

(2012) Lech-Gustav Milroy et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Activation of the p53 pathway by small-molecule-induced MDM2 and MDMX dimerization

(2012) B. Graves et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Tafamidis, a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade

(2012) C. E. Bulawa et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of the functional binding pocket for compounds targeting small-conductance Ca2+-activated potassium channels

(2012) Miao Zhang et al.   Nature Communications

Actin Structure and Function

(2011) Roberto Dominguez et al.   Annual Review of Biophysics

An Allosteric Inhibitor of the Human Cdc34 Ubiquitin-Conjugating Enzyme

(2011) Derek F. Ceccarelli et al.   CELL

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Plasmodium sporozoite motility: an update

(2011) Georgina et al.   Frontiers in Bioscience-Landmark

Cancer immunotherapy comes of age

(2011) Ira Mellman et al.   NATURE

Subunit arrangement and phenylethanolamine binding in GluN1/GluN2B NMDA receptors

(2011) Erkan Karakas et al.   NATURE

Rapamycin passes the torch: a new generation of mTOR inhibitors

(2011) Don Benjamin et al.   NATURE REVIEWS DRUG DISCOVERY

Inhibition of influenza virus replication via small molecules that induce the formation of higher-order nucleoprotein oligomers

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

Identification and Structure of Small-Molecule Stabilizers of 14-3-3 Protein-Protein Interactions

(2010) Rolf Rose et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Two Molecules of Lobophorolide Cooperate to Stabilize an Actin Dimer Using Both Their “Ring” and “Tail” Region

(2010) J. Craig Blain et al.   CHEMISTRY & BIOLOGY

Structure-based design of kinetic stabilizers that ameliorate the transthyretin amyloidoses

(2010) Stephen Connelly et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Improving Binding Specificity of Pharmacological Chaperones That Target Mutant Superoxide Dismutase-1 Linked to Familial Amyotrophic Lateral Sclerosis Using Computational Methods

(2010) Richard J. Nowak et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Substructure Combination Strategy To Create Potent and Selective Transthyretin Kinetic Stabilizers That Prevent Amyloidogenesis and Cytotoxicity

(2010) Sungwook Choi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A unique secondary-structure switch controls constitutive gene repression by retinoic acid receptor

(2010) Albane le Maire et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Moonlighting enzymes in parasitic protozoa

(2010) PETER W. COLLINGRIDGE et al.   PARASITOLOGY

Phenothiazines inhibit S100A4 function by inducing protein oligomerization

(2010) V. N. Malashkevich et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Trapping of palindromic ligands within native transthyretin prevents amyloid formation

(2010) S. E. Kolstoe et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Differential Action on Coregulator Interaction Defines Inverse Retinoid Agonists and Neutral Antagonists

(2009) Pierre Germain et al.   CHEMISTRY & BIOLOGY

Characterization of two classes of small molecule inhibitors of Arp2/3 complex

(2009) B. J. Nolen et al.   NATURE

Chondramide C: Synthesis, Configurational Assignment, and Structure-Activity Relationship Studies

(2008) Ulrike Eggert et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Total Synthesis of Chondramide C and Its Binding Mode to F-Actin

(2008) Herbert Waldmann et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The Absolute Configuration of Rhizopodin and Its Inhibition of Actin Polymerization by Dimerization

(2008) Gregor Hagelueken et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Quantification of the Thermodynamically Linked Quaternary and Tertiary Structural Stabilities of Transthyretin and Its Disease-Associated Variants: The Relationship between Stability and Amyloidosis†

(2008) Amy R. Hurshman Babbes et al.   BIOCHEMISTRY

Metastasis-Inducing S100A4 Protein: Implication in Non-Malignant Human Pathologies

(2008) Mariam Grigorian et al.   CURRENT MOLECULAR MEDICINE

KCa3.1: target and marker for cancer, autoimmune disorder and vascular inflammation?

(2008) Chuan-Chu Chou et al.   EXPERT REVIEW OF MOLECULAR DIAGNOSTICS

Anthracycline Cardiotoxicity: From Bench to Bedside

(2008) Luca Gianni et al.   JOURNAL OF CLINICAL ONCOLOGY

Toward Optimization of the Linker Substructure Common to Transthyretin Amyloidogenesis Inhibitors Using Biochemical and Structural Studies†

(2008) Steven M. Johnson et al.   JOURNAL OF MEDICINAL CHEMISTRY

S100A4: a common mediator of epithelial–mesenchymal transition, fibrosis and regeneration in diseases?

(2008) Mikael Schneider et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Studies of an Influenza A Virus Temperature-Sensitive Mutant Identify a Late Role for NP in the Formation of Infectious Virions

(2008) S. L. Noton et al.   JOURNAL OF VIROLOGY

Targeted rescue of a destabilized mutant of p53 by an in silico screened drug

(2008) F. M. Boeckler et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A Biosensor of S100A4 Metastasis Factor Activation:  Inhibitor Screening and Cellular Activation Dynamics†

(2007) Sarah C. Garrett et al.   BIOCHEMISTRY

Biochemical and Structural Evaluation of Highly Selective 2-Arylbenzoxazole-Based Transthyretin Amyloidogenesis Inhibitors

(2007) Steven M. Johnson et al.   JOURNAL OF MEDICINAL CHEMISTRY