Discovery of Small-Molecule Degraders for Alpha-Synuclein Aggregates

Current Progress in the Development of Probes for Targeting α-Synuclein Aggregates

(2022) Qi Zeng et al.   ACS Chemical Neuroscience

Safety, tolerability and pharmacokinetics of the oligomer modulator anle138b with exposure levels sufficient for therapeutic efficacy in a murine Parkinson model: A randomised, double-blind, placebo-controlled phase 1a trial

(2022) Johannes Levin et al.   EBioMedicine

Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras

(2022) Xufen Yu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effective degradation of EGFRL858R+T790M mutant proteins by CRBN-based PROTACs through both proteosome and autophagy/lysosome degradation systems

(2021) Xiaojuan Qu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeting autophagy using small-molecule compounds to improve potential therapy of Parkinson’s disease

(2021) Kai Zhang et al.   Acta Pharmaceutica Sinica B

Unraveling the Role of Linker Design in Proteolysis Targeting Chimeras

(2021) Troy A. Bemis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synucleinopathies: Where we are and where we need to go

(2020) Inês Caldeira Brás et al.   JOURNAL OF NEUROCHEMISTRY

Expression and purification of amyloid β-protein, tau, and α-synuclein in Escherichia coli: a review

(2020) Longgang Jia et al.   CRITICAL REVIEWS IN BIOTECHNOLOGY

PROTAC Compounds Targeting α-Synuclein Protein for Treating Neurogenerative Disorders: Alzheimer’s and Parkinson’s Diseases

(2020) Robert B. Kargbo   ACS Medicinal Chemistry Letters

In vitro models of synucleinopathies: informing on molecular mechanisms and protective strategies

(2019) Amir Tayaranian Marvian et al.   JOURNAL OF NEUROCHEMISTRY

α‐synuclein oligomers and fibrils: a spectrum of species, a spectrum of toxicities

(2019) Parvez Alam et al.   JOURNAL OF NEUROCHEMISTRY

Advances in the development of imaging probes and aggregation inhibitors for alpha-synuclein

(2019) Ming-ming Xu et al.   ACTA PHARMACOLOGICA SINICA

Cellular quality control by the ubiquitin-proteasome system and autophagy

(2019) Christian Pohl et al.   SCIENCE

Targeting Alpha-Synuclein as a Therapy for Parkinson’s Disease

(2019) Carroll Rutherford Fields et al.   Frontiers in Molecular Neuroscience

Alpha Synuclein Fibrils Contain Multiple Binding Sites for Small Molecules

(2018) Chia-Ju Hsieh et al.   ACS Chemical Neuroscience

Small molecule inhibits α-synuclein aggregation, disrupts amyloid fibrils, and prevents degeneration of dopaminergic neurons

(2018) Jordi Pujols et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

In VivoKnockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs)

(2017) Nobumichi Ohoka et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Therapeutic potential of autophagy-enhancing agents in Parkinson’s disease

(2017) Tim E. Moors et al.   Molecular Neurodegeneration

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

Solid-state NMR structure of a pathogenic fibril of full-length human α-synuclein

(2016) Marcus D Tuttle et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Solid-state NMR structure of a pathogenic fibril of full-length human α-synuclein

(2016) Marcus D Tuttle et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Structure, function and toxicity of alpha-synuclein: the Bermuda triangle in synucleinopathies

(2015) Anna Villar-Piqué et al.   JOURNAL OF NEUROCHEMISTRY

Lewy body dementias

(2015) Zuzana Walker et al.   LANCET

Parkinson's disease

(2015) Lorraine V Kalia et al.   LANCET

Targeting α-synuclein for treatment of Parkinson's disease: mechanistic and therapeutic considerations

(2015) Benjamin Dehay et al.   LANCET NEUROLOGY

Multiple-System Atrophy

(2015) Alessandra Fanciulli et al.   NEW ENGLAND JOURNAL OF MEDICINE

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

(2014) Carles Galdeano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Addition of exogenous α-synuclein preformed fibrils to primary neuronal cultures to seed recruitment of endogenous α-synuclein to Lewy body and Lewy neurite–like aggregates

(2014) Laura A Volpicelli-Daley et al.   Nature Protocols

Anle138b: a novel oligomer modulator for disease-modifying therapy of neurodegenerative diseases such as prion and Parkinson’s disease

(2013) Jens Wagner et al.   ACTA NEUROPATHOLOGICA

Guidelines for the use and interpretation of assays for monitoring autophagy

(2012) Daniel J. Klionsky et al.   Autophagy

Basic Caenorhabditis elegans Methods: Synchronization and Observation

(2012) Montserrat Porta-de-la-Riva et al.   Jove-Journal of Visualized Experiments

Seeded Aggregation and Toxicity of α-Synuclein and Tau

(2010) Takashi Nonaka et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Exogenous  -synuclein fibrils seed the formation of Lewy body-like intracellular inclusions in cultured cells

(2009) K. C. Luk et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Characterization of α-Synuclein Interactions with Selected Aggregation-Inhibiting Small Molecules†

(2008) Jampani Nageswara Rao et al.   BIOCHEMISTRY

Small Molecules Destabilize cIAP1 by Activating Auto-ubiquitylation

(2008) Keiko Sekine et al.   JOURNAL OF BIOLOGICAL CHEMISTRY