Hyperphosphorylated tau (p-tau) and drug discovery in the context of Alzheimer's disease and related tauopathies

KBE Moore, TJ Hung, JS Fortin - Drug discovery today, 2023 - Elsevier
Highlights•Dementia involves the chronic and progressive deterioration of cognitive
functions.•Alzheimer's disease is the most common form of dementia.•Abnormally …

Peptide-based approaches to directly target alpha-synuclein in Parkinson's disease

SG Allen, RM Meade, LL White Stenner… - Molecular …, 2023 - Springer
Peptides and their mimetics are increasingly recognised as drug-like molecules, particularly
for intracellular protein-protein interactions too large for inhibition by small molecules, and …

Lysine-specific molecular tweezers are broad-spectrum inhibitors of assembly and toxicity of amyloid proteins

S Sinha, DHJ Lopes, Z Du, ES Pang… - Journal of the …, 2011 - ACS Publications
Amyloidoses are diseases characterized by abnormal protein folding and self-assembly, for
which no cure is available. Inhibition or modulation of abnormal protein self-assembly …

Intracerebroventricular injection of amyloid-β peptides in normal mice to acutely induce Alzheimer-like cognitive deficits

HY Kim, DK Lee, BR Chung, HV Kim… - Journal of visualized …, 2016 - pmc.ncbi.nlm.nih.gov
Amyloid-β (Aβ) is a major pathological mediator of both familial and sporadic Alzheimer's
disease (AD). In the brains of AD patients, progressive accumulation of Aβ oligomers and …

Molecular tweezers for lysine and arginine–powerful inhibitors of pathologic protein aggregation

T Schrader, G Bitan, FG Klärner - Chemical communications, 2016 - pubs.rsc.org
Molecular tweezers represent the first class of artificial receptor molecules that have made
the way from a supramolecular host to a drug candidate with promising results in animal …

Amylin and beta amyloid proteins interact to form amorphous heterocomplexes with enhanced toxicity in neuronal cells

P Bharadwaj, T Solomon, BR Sahoo, K Ignasiak… - Scientific Reports, 2020 - nature.com
Human pancreatic islet amyloid polypeptide (hIAPP) and beta amyloid (Aβ) can accumulate
in Type 2 diabetes (T2D) and Alzheimer's disease (AD) brains and evidence suggests that …

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

S Prabhudesai, S Sinha, A Attar, A Kotagiri… - …, 2012 - Springer
Aggregation of α-synuclein (α-syn) is implicated as being causative in the pathogenesis of
Parkinson's disease, multiple system atrophy, and dementia with Lewy bodies. Despite …

Coffee components inhibit amyloid formation of human islet amyloid polypeptide in vitro: possible link between coffee consumption and diabetes mellitus

B Cheng, X Liu, H Gong, L Huang, H Chen… - Journal of agricultural …, 2011 - ACS Publications
Global epidemic studies have suggested that coffee consumption is reversely correlated
with the incidence of type 2 diabetes mellitus (T2DM), a metabolic disease. The misfolding of …

Comparison of Three Amyloid Assembly Inhibitors: The Sugar scyllo-Inositol, the Polyphenol Epigallocatechin Gallate, and the Molecular Tweezer CLR01

S Sinha, Z Du, P Maiti, FG Klärner… - ACS chemical …, 2012 - ACS Publications
Many compounds have been tested as inhibitors or modulators of amyloid β-protein (Aβ)
assembly in hope that they would lead to effective, disease-modifying therapy for …

A key role for lysine residues in amyloid β-protein folding, assembly, and toxicity

S Sinha, DHJ Lopes, G Bitan - ACS Chemical Neuroscience, 2012 - ACS Publications
A combination of hydrophobic and electrostatic interactions is important in initiating the
aberrant self-assembly process that leads to formation of toxic oligomers and aggregates by …