A practical review of proteasome pharmacology

TA Thibaudeau, DM Smith, Q Ma - Pharmacological reviews, 2019 - Elsevier
The ubiquitin proteasome system (UPS) degrades individual proteins in a highly regulated
fashion and is responsible for the degradation of misfolded, damaged, or unneeded cellular …

Proteasomes and several aspects of their heterogeneity relevant to cancer

AV Morozov, VL Karpov - Frontiers in Oncology, 2019 - frontiersin.org
The life of every organism is dependent on the fine-tuned mechanisms of protein synthesis
and breakdown. The degradation of most intracellular proteins is performed by the ubiquitin …

The proteasome as a druggable target with multiple therapeutic potentialities: Cutting and non-cutting edges

GR Tundo, D Sbardella, AM Santoro, A Coletta… - Pharmacology & …, 2020 - Elsevier
Abstract Ubiquitin Proteasome System (UPS) is an adaptable and finely tuned system that
sustains proteostasis network under a large variety of physiopathological conditions. Its …

Comparative structural analysis of 20S proteasome ortholog protein complexes by native mass spectrometry

S Vimer, G Ben-Nissan, D Morgenstern… - ACS Central …, 2020 - ACS Publications
Ortholog protein complexes are responsible for equivalent functions in different organisms.
However, during evolution, each organism adapts to meet its physiological needs and the …

Aim for the core: suitability of the ubiquitin-independent 20S proteasome as a drug target in neurodegeneration

KA Opoku-Nsiah, JE Gestwicki - Translational Research, 2018 - Elsevier
Neurodegenerative diseases are a class of age-associated proteopathies characterized by
the accumulation of misfolded and/or aggregation-prone proteins. This imbalance has been …

[HTML][HTML] Beyond cells: The extracellular circulating 20S proteasomes

V Dwivedi, K Yaniv, M Sharon - … et Biophysica Acta (BBA)-Molecular Basis …, 2021 - Elsevier
Accumulating evidence arising from numerous clinical studies indicate that assembled and
functional 20S proteasome complexes circulate freely in plasma. Elevated levels of this core …

Exploring the proteasome system: A novel concept of proteasome inhibition and regulation

X Wang, T Meul, S Meiners - Pharmacology & Therapeutics, 2020 - Elsevier
The proteasome is a well-identified therapeutic target for cancer treatment. It acts as the
main protein degradation system in the cell and degrades key mediators of cell growth …

Proline-and arginine-rich peptides as flexible allosteric modulators of human proteasome activity

M Giżyńska, J Witkowska, P Karpowicz… - Journal of Medicinal …, 2018 - ACS Publications
Proline-and arginine-rich peptide PR11 is an allosteric inhibitor of 20S proteasome. We
modified its sequence inter alia by introducing HbYX, RYX, or RHbX C-terminal extensions …

The interplay between lipid and Aβ amyloid homeostasis in Alzheimer's Disease: risk factors and therapeutic opportunities

S García-Viñuales, MFM Sciacca, V Lanza… - Chemistry and Physics …, 2021 - Elsevier
Alzheimer's Diseases (AD) is characterized by the accumulation of amyloid deposits of Aβ
peptide in the brain. Besides genetic background, the presence of other diseases and an …

Discovery and Development of Cyclic Peptide Proteasome Stimulators

S Nelson, TJ Harris, CS Muli, ME Maresh… - …, 2024 - Wiley Online Library
The proteasome degrades proteins, which is essential for cellular homeostasis. Ubiquitin
independent proteolysis degrades highly disordered and misfolded proteins. A decline of …