TCH-165 attenuates cardiac ischaemia/reperfusion injury by balancing mitochondrial dynamics via increasing proteasome activity

J Gao, HX Su, PB Li, KN Shi, HH Li - European Journal of Pharmacology, 2023 - Elsevier
The proteasome is the main complex responsible for maintaining intracellular protein
homeostasis, impairment of which is associated with cardiac ischaemia/reperfusion (I/R) …

Proteasome activation: A novel strategy for targeting undruggable intrinsically disordered proteins

Q Yu, Z Wang, Y Tu, Y Cao, H Zhu, J Shao… - Bioorganic …, 2024 - Elsevier
Intrinsically disordered proteins (IDPs) are characterized by their inability to adopt well-
defined tertiary structures under physiological conditions. Nonetheless, they often play …

Enhanced Degradation of Mutant C9ORF72-Derived Toxic Dipeptide Repeat Proteins by 20S Proteasome Activation Results in Restoration of Proteostasis and …

AS Vanecek, J Mojsilovic-Petrovic… - ACS Chemical …, 2023 - ACS Publications
A hexanucleotide repeat expansion (HRE) in an intron of gene C9ORF72 is the most
common cause of familial amyotrophic lateral sclerosis and frontotemporal dementia. The …

Proteasome Activators and Ageing: Restoring Proteostasis Using Small Molecules

A Upadhyay, V Joshi - Biochemistry and Cell Biology of Ageing: Part V …, 2024 - Springer
Ageing is an inevitable phenomenon that remains under control of a plethora of signalling
pathways and regulatory mechanisms. Slowing of cellular homeostasis and repair …

Development of a cell-based alphaLISA assay for high-throughput screening for small molecule proteasome modulators

SD Staerz, EM Lisabeth, E Njomen, TS Dexheimer… - ACS …, 2023 - ACS Publications
The balance between protein degradation and protein synthesis is a highly choreographed
process generally called proteostasis. Most intracellular protein degradation occurs through …

Depleting the 19S proteasome regulatory PSMD1 subunit as a cancer therapy strategy

J Adler, R Oren, Y Shaul - Cancer Medicine, 2023 - Wiley Online Library
Background Proteasome inhibitors are in use in treating certain types of cancers. These
drugs inhibit the catalytic activity of the 20S proteasome, shared by all the different …

Discovery and Design of Novel 20S Proteasome Activators for Targeted Protein Degradation and Their Evaluation in Neurodegeneration Models

SD Staerz - 2024 - search.proquest.com
In cells, proteostasis is a constant and highly choreographed process that maintains a
balance between the synthesis and degradation of proteins. The ubiquitin-proteasome …

Exploring the Potential of 20S Proteasome Modulation as a Novel Therapeutic Strategy for the Treatment of Neurodegenerative Diseases and Cancers

AS Vanecek - 2024 - search.proquest.com
The accumulation of intrinsically disordered proteins (IDPs) and the associated disruption of
cellular proteostasis is implicated in the progression of a number of neurodegenerative …