Targeting intrinsically disordered proteins in rational drug discovery

Folding of the Tau Protein on Microtubules

(2015) Harindranath Kadavath et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Quantitative Biophysical Characterization of Intrinsically Disordered Proteins

(2015) Eric B. Gibbs et al.   BIOCHEMISTRY

How Common Is Disorder? Occurrence of Disordered Residues in Four Domains of Life

(2015) Mikhail Lobanov et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

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

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

Single-molecule spectroscopy of protein conformational dynamics in live eukaryotic cells

(2015) Iwo König et al.   NATURE METHODS

Intrinsically disordered proteins in cellular signalling and regulation

(2015) Peter E. Wright et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Small molecule Mcl-1 inhibitors for the treatment of cancer

(2015) Johannes Belmar et al.   PHARMACOLOGY & THERAPEUTICS

Tau stabilizes microtubules by binding at the interface between tubulin heterodimers

(2015) Harindranath Kadavath et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Probing protein disorder and complexity at single-molecule resolution

(2015) Taehyung Lee et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

Structural Impact of Tau Phosphorylation at Threonine 231

(2015) Martin Schwalbe et al.   STRUCTURE

Targeting disordered proteins with small molecules using entropy

(2015) Gabriella T. Heller et al.   TRENDS IN BIOCHEMICAL SCIENCES

New dimension in therapeutic targeting of BCL-2 family proteins

(2015) Samaher Besbes et al.   Oncotarget

Role of the Tau N-terminal region in microtubule stabilization revealed by new endogenous truncated forms

(2015) Maxime Derisbourg et al.   Scientific Reports

HYCUD: a computational tool for prediction of effective rotational correlation time in flexible proteins

(2014) Nasrollah Rezaei-Ghaleh et al.   BIOINFORMATICS

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

Pathological Unfoldomics of Uncontrolled Chaos: Intrinsically Disordered Proteins and Human Diseases

(2014) Vladimir N. Uversky et al.   CHEMICAL REVIEWS

Exploring Free-Energy Landscapes of Intrinsically Disordered Proteins at Atomic Resolution Using NMR Spectroscopy

(2014) Malene Ringkjøbing Jensen et al.   CHEMICAL REVIEWS

Single-Molecule Studies of Intrinsically Disordered Proteins

(2014) Marco Brucale et al.   CHEMICAL REVIEWS

Physicochemical Properties of Cells and Their Effects on Intrinsically Disordered Proteins (IDPs)

(2014) Francois-Xavier Theillet et al.   CHEMICAL REVIEWS

Assessing the accuracy of physical models used in protein-folding simulations: quantitative evidence from long molecular dynamics simulations

(2014) Stefano Piana et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

What Macromolecular Crowding Can Do to a Protein

(2014) Irina Kuznetsova et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Molecular Basis for Preventing α-Synuclein Aggregation by a Molecular Tweezer

(2014) Srabasti Acharya et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Oligomer Formation of Tau Protein Hyperphosphorylated in Cells

(2014) Katharina Tepper et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A six-dimensional alpha proton detection-based APSY experiment for backbone assignment of intrinsically disordered proteins

(2014) Xuejun Yao et al.   JOURNAL OF BIOMOLECULAR NMR

NMR contributions to structural dynamics studies of intrinsically disordered proteins

(2014) Robert Konrat   JOURNAL OF MAGNETIC RESONANCE

Folding of an intrinsically disordered protein by phosphorylation as a regulatory switch

(2014) Alaji Bah et al.   NATURE

Targeting the disordered C terminus of PTP1B with an allosteric inhibitor

(2014) Navasona Krishnan et al.   Nature Chemical Biology

Drugging the p53 pathway: understanding the route to clinical efficacy

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

Conformational propensities and dynamics of a βγ-crystallin, an intrinsically disordered protein

(2014) Sunita Patel et al.   PHYSICAL CHEMISTRY CHEMICAL PHYSICS

Targeting the Intrinsically Disordered Structural Ensemble of α-Synuclein by Small Molecules as a Potential Therapeutic Strategy for Parkinson’s Disease

(2014) Gergely Tóth et al.   PLoS One

Temperature-dependent solvation modulates the dimensions of disordered proteins

(2014) R. Wuttke et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Single-molecule spectroscopy reveals polymer effects of disordered proteins in crowded environments

(2014) Andrea Soranno et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Small molecule-mediated stabilization of vesicle-associated helical α-synuclein inhibits pathogenic misfolding and aggregation

(2014) Luis Fonseca-Ornelas et al.   Nature Communications

Predicting the Rotational Tumbling of Dynamic Multidomain Proteins and Supramolecular Complexes

(2013) Nasrollah Rezaei-Ghaleh et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Mechanistic Basis of Phenothiazine-Driven Inhibition of Tau Aggregation

(2013) Elias Akoury et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Single-Molecule Spectroscopy of Cold Denaturation and the Temperature-Induced Collapse of Unfolded Proteins

(2013) Mikayel Aznauryan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Inhibition of Tau Filament Formation by Conformational Modulation

(2013) Elias Akoury et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Structural Characterization of Intrinsically Disordered Proteins by NMR Spectroscopy

(2013) Simone Kosol et al.   MOLECULES

Modulation of allostery by protein intrinsic disorder

(2013) Allan Chris M. Ferreon et al.   NATURE

Parkinson's disease dementia: convergence of α-synuclein, tau and amyloid-β pathologies

(2013) David J. Irwin et al.   NATURE REVIEWS NEUROSCIENCE

SUMO and Alzheimer’s Disease

(2013) Linda Lee et al.   NEUROMOLECULAR MEDICINE

pE-DB: a database of structural ensembles of intrinsically disordered and of unfolded proteins

(2013) Mihaly Varadi et al.   NUCLEIC ACIDS RESEARCH

Phosphorylation Drives a Dynamic Switch in Serine/Arginine-Rich Proteins

(2013) ShengQi Xiang et al.   STRUCTURE

Predictive Atomic Resolution Descriptions of Intrinsically Disordered hTau40 and α-Synuclein in Solution from NMR and Small Angle Scattering

(2013) Martin Schwalbe et al.   STRUCTURE

Ligand Clouds around Protein Clouds: A Scenario of Ligand Binding with Intrinsically Disordered Proteins

(2013) Fan Jin et al.   PLoS Computational Biology

Intrinsically disordered proteins undergo and assist folding transitions in the proteome

(2012) D. Kovacs et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Describing sequence–ensemble relationships for intrinsically disordered proteins

(2012) Albert H. Mao et al.   BIOCHEMICAL JOURNAL

Mechanisms of small-molecule binding to intrinsically disordered proteins: Figure 1

(2012) Rémi Cuchillo et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

Intrinsically Disordered Proteins: From Sequence and Conformational Properties toward Drug Discovery

(2012) Nasrollah Rezaei-Ghaleh et al.   CHEMBIOCHEM

Beyond the genome and proteome: targeting protein modifications in cancer

(2012) Anatoliy Markiv et al.   CURRENT OPINION IN PHARMACOLOGY

Probing the diverse landscape of protein flexibility and binding

(2012) Joseph A Marsh et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Recent progress in NMR spectroscopy: Toward the study of intrinsically disordered proteins of increasing size and complexity

(2012) Isabella C. Felli et al.   IUBMB LIFE

Structure and Dynamics of an Unfolded Protein Examined by Molecular Dynamics Simulation

(2012) Kresten Lindorff-Larsen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

More than just tails: intrinsic disorder in histone proteins

(2012) Zhenling Peng et al.   Molecular BioSystems

100 years of Lewy pathology

(2012) Michel Goedert et al.   Nature Reviews Neurology

A Novel “Molecular Tweezer” Inhibitor of α-Synuclein Neurotoxicity in Vitro and in Vivo

(2012) Shubhangi Prabhudesai et al.   Neurotherapeutics

Structural Disorder in Eukaryotes

(2012) Rita Pancsa et al.   PLoS One

The Impact of Small Molecule Binding on the Energy Landscape of the Intrinsically Disordered Protein C-Myc

(2012) Julien Michel et al.   PLoS One

Counteracting chemical chaperone effects on the single-molecule  -synuclein structural landscape

(2012) A. C. M. Ferreon et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Conserved features of intermediates in amyloid assembly determine their benign or toxic states

(2012) R. Krishnan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Linear motifs: lost in (pre)translation

(2012) Robert J. Weatheritt et al.   TRENDS IN BIOCHEMICAL SCIENCES

Tau Oligomers as Potential Targets for Immunotherapy for Alzheimers Disease and Tauopathies

(2011) C. A. Lasagna-Reeves et al.   Current Alzheimer Research

Constructing ensembles for intrinsically disordered proteins

(2011) Charles K Fisher et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Intrinsically disordered proteins: regulation and disease

(2011) M Madan Babu et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Antibody-based therapy in Alzheimer's disease

(2011) Refik Pul et al.   EXPERT OPINION ON BIOLOGICAL THERAPY

Conserved, Disordered C Terminus of DnaK Enhances Cellular Survival upon Stress and DnaKin VitroChaperone Activity

(2011) Robert G. Smock et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Nature of the Amyloid-β Monomer and the Monomer-Oligomer Equilibrium

(2011) Suman Nag et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural analysis of intrinsically disordered proteins by small-angle X-ray scattering

(2011) Pau Bernadó et al.   Molecular BioSystems

Molecular chaperones in protein folding and proteostasis

(2011) F. Ulrich Hartl et al.   NATURE

“Lest we forget you — methylene blue …”

(2011) R. Heiner Schirmer et al.   NEUROBIOLOGY OF AGING

The acetylation of tau inhibits its function and promotes pathological tau aggregation

(2011) Todd J. Cohen et al.   Nature Communications

Alteration of the α-Synuclein Folding Landscape by a Mutation Related to Parkinson’s Disease

(2010) Allan Chris M. Ferreon et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

α-Synuclein: Membrane Interactions and Toxicity in Parkinson's Disease

(2010) Pavan K. Auluck et al.   Annual Review of Cell and Developmental Biology

PONDR-FIT: A meta-predictor of intrinsically disordered amino acids

(2010) Bin Xue et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Understanding protein non-folding

(2010) Vladimir N. Uversky et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

p53-family proteins and their regulators: hubs and spokes in tumor suppression

(2010) L Collavin et al.   CELL DEATH AND DIFFERENTIATION

Enzymatic activity in disordered states of proteins

(2010) Michele Vendruscolo   CURRENT OPINION IN CHEMICAL BIOLOGY

Intrinsically disordered proteins are potential drug targets

(2010) Steven J Metallo   CURRENT OPINION IN CHEMICAL BIOLOGY

Targeting intrinsically disordered proteins in neurodegenerative and protein dysfunction diseases: another illustration of the D2concept

(2010) Vladimir N Uversky   Expert Review of Proteomics

Automatic Assignment of the Intrinsically Disordered Protein Tau with 441-Residues

(2010) Rhagavendran L. Narayanan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

NMR Characterization of Long-Range Order in Intrinsically Disordered Proteins

(2010) Loïc Salmon et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Alzheimer's disease: clinical trials and drug development

(2010) Francesca Mangialasche et al.   LANCET NEUROLOGY

Catalytic and chaperone-like functions in an intrinsically disordered protein associated with desiccation tolerance

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

Biology of Amyloid: Structure, Function, and Regulation

(2010) Jason Greenwald et al.   STRUCTURE

Protein disorder in the human diseasome: unfoldomics of human genetic diseases

(2009) Uros Midic et al.   BMC GENOMICS

Unfoldomics of human diseases: linking protein intrinsic disorder with diseases

(2009) Vladimir N Uversky et al.   BMC GENOMICS

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

Determination of the Free Energy Landscape of α-Synuclein Using Spin Label Nuclear Magnetic Resonance Measurements

(2009) Jane R. Allison et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Interplay of  -synuclein binding and conformational switching probed by single-molecule fluorescence

(2009) A. C. M. Ferreon et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Quantitative Determination of the Conformational Properties of Partially Folded and Intrinsically Disordered Proteins Using NMR Dipolar Couplings

(2009) Malene Ringkjøbing Jensen et al.   STRUCTURE

Structural Polymorphism of 441-Residue Tau at Single Residue Resolution

(2009) Marco D Mukrasch et al.   PLOS BIOLOGY

Intrinsic Structural Disorder Confers Cellular Viability on Oncogenic Fusion Proteins

(2009) Hedi Hegyi et al.   PLoS Computational Biology

Probing Invisible, Low-Populated States of Protein Molecules by Relaxation Dispersion NMR Spectroscopy: An Application to Protein Folding

(2008) Dmitry M. Korzhnev et al.   ACCOUNTS OF CHEMICAL RESEARCH

Intrinsically Disordered Proteins in Human Diseases: Introducing the D2 Concept

(2008) Vladimir N. Uversky et al.   Annual Review of Biophysics

Structural Rationale for the Coupled Binding and Unfolding of the c-Myc Oncoprotein by Small Molecules

(2008) Ariele Viacava Follis et al.   CHEMISTRY & BIOLOGY

Biochemistry of Tau in Alzheimer’s disease and related neurological disorders

(2008) Nicolas Sergeant et al.   Expert Review of Proteomics

Role of Intrinsic Flexibility in Signal Transduction Mediated by the Cell Cycle Regulator, p27Kip1

(2008) Charles A. Galea et al.   JOURNAL OF MOLECULAR BIOLOGY