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

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The proteasome as a druggable target with multiple therapeutic potentialities : Cutting and non-cutting edges. / Tundo, G. R.; Sbardella, D.; Santoro, A. M.; Coletta, A.; Oddone, F.; Grasso, G.; Milardi, D.; Lacal, P. M.; Marini, S.; Purrello, R.; Graziani, G.; Coletta, M.

I: Pharmacology and Therapeutics, Bind 213, 107579, 09.2020.

Publikation: Bidrag til tidsskrift/Konferencebidrag i tidsskrift /Bidrag til avisReviewForskningpeer review

Harvard

Tundo, GR, Sbardella, D, Santoro, AM, Coletta, A, Oddone, F, Grasso, G, Milardi, D, Lacal, PM, Marini, S, Purrello, R, Graziani, G & Coletta, M 2020, 'The proteasome as a druggable target with multiple therapeutic potentialities: Cutting and non-cutting edges', Pharmacology and Therapeutics, bind 213, 107579. https://doi.org/10.1016/j.pharmthera.2020.107579

APA

Tundo, G. R., Sbardella, D., Santoro, A. M., Coletta, A., Oddone, F., Grasso, G., Milardi, D., Lacal, P. M., Marini, S., Purrello, R., Graziani, G., & Coletta, M. (2020). The proteasome as a druggable target with multiple therapeutic potentialities: Cutting and non-cutting edges. Pharmacology and Therapeutics, 213, [107579]. https://doi.org/10.1016/j.pharmthera.2020.107579

CBE

Tundo GR, Sbardella D, Santoro AM, Coletta A, Oddone F, Grasso G, Milardi D, Lacal PM, Marini S, Purrello R, Graziani G, Coletta M. 2020. The proteasome as a druggable target with multiple therapeutic potentialities: Cutting and non-cutting edges. Pharmacology and Therapeutics. 213:Article 107579. https://doi.org/10.1016/j.pharmthera.2020.107579

MLA

Vancouver

Tundo GR, Sbardella D, Santoro AM, Coletta A, Oddone F, Grasso G o.a. The proteasome as a druggable target with multiple therapeutic potentialities: Cutting and non-cutting edges. Pharmacology and Therapeutics. 2020 sep;213. 107579. https://doi.org/10.1016/j.pharmthera.2020.107579

Author

Tundo, G. R. ; Sbardella, D. ; Santoro, A. M. ; Coletta, A. ; Oddone, F. ; Grasso, G. ; Milardi, D. ; Lacal, P. M. ; Marini, S. ; Purrello, R. ; Graziani, G. ; Coletta, M. / The proteasome as a druggable target with multiple therapeutic potentialities : Cutting and non-cutting edges. I: Pharmacology and Therapeutics. 2020 ; Bind 213.

Bibtex

@article{af23b7dda7354b8ea8268a54d6e9d31a,
title = "The proteasome as a druggable target with multiple therapeutic potentialities: Cutting and non-cutting edges",
abstract = "Ubiquitin Proteasome System (UPS) is an adaptable and finely tuned system that sustains proteostasis network under a large variety of physiopathological conditions. Its dysregulation is often associated with the onset and progression of human diseases; hence, UPS modulation has emerged as a promising new avenue for the development of treatments of several relevant pathologies, such as cancer and neurodegeneration. The clinical interest in proteasome inhibition has considerably increased after the FDA approval in 2003 of bortezomib for relapsed/refractory multiple myeloma, which is now used in the front-line setting. Thereafter, two other proteasome inhibitors (carfilzomib and ixazomib), designed to overcome resistance to bortezomib, have been approved for treatment-experienced patients, and a variety of novel inhibitors are currently under preclinical and clinical investigation not only for haematological malignancies but also for solid tumours. However, since UPS collapse leads to toxic misfolded proteins accumulation, proteasome is attracting even more interest as a target for the care of neurodegenerative diseases, which are sustained by UPS impairment. Thus, conceptually, proteasome activation represents an innovative and largely unexplored target for drug development. According to a multidisciplinary approach, spanning from chemistry, biochemistry, molecular biology to pharmacology, this review will summarize the most recent available literature regarding different aspects of proteasome biology, focusing on structure, function and regulation of proteasome in physiological and pathological processes, mostly cancer and neurodegenerative diseases, connecting biochemical features and clinical studies of proteasome targeting drugs.",
keywords = "Cancer, Neurodegeneration, Proteasome, Proteasome inhibitors, SARS-Cov-2",
author = "Tundo, {G. R.} and D. Sbardella and Santoro, {A. M.} and A. Coletta and F. Oddone and G. Grasso and D. Milardi and Lacal, {P. M.} and S. Marini and R. Purrello and G. Graziani and M. Coletta",
year = "2020",
month = sep,
doi = "10.1016/j.pharmthera.2020.107579",
language = "English",
volume = "213",
journal = "Pharmacology & Therapeutics",
issn = "0163-7258",
publisher = "Elsevier Inc.",

}

RIS

TY - JOUR

T1 - The proteasome as a druggable target with multiple therapeutic potentialities

T2 - Cutting and non-cutting edges

AU - Tundo, G. R.

AU - Sbardella, D.

AU - Santoro, A. M.

AU - Coletta, A.

AU - Oddone, F.

AU - Grasso, G.

AU - Milardi, D.

AU - Lacal, P. M.

AU - Marini, S.

AU - Purrello, R.

AU - Graziani, G.

AU - Coletta, M.

PY - 2020/9

Y1 - 2020/9

N2 - Ubiquitin Proteasome System (UPS) is an adaptable and finely tuned system that sustains proteostasis network under a large variety of physiopathological conditions. Its dysregulation is often associated with the onset and progression of human diseases; hence, UPS modulation has emerged as a promising new avenue for the development of treatments of several relevant pathologies, such as cancer and neurodegeneration. The clinical interest in proteasome inhibition has considerably increased after the FDA approval in 2003 of bortezomib for relapsed/refractory multiple myeloma, which is now used in the front-line setting. Thereafter, two other proteasome inhibitors (carfilzomib and ixazomib), designed to overcome resistance to bortezomib, have been approved for treatment-experienced patients, and a variety of novel inhibitors are currently under preclinical and clinical investigation not only for haematological malignancies but also for solid tumours. However, since UPS collapse leads to toxic misfolded proteins accumulation, proteasome is attracting even more interest as a target for the care of neurodegenerative diseases, which are sustained by UPS impairment. Thus, conceptually, proteasome activation represents an innovative and largely unexplored target for drug development. According to a multidisciplinary approach, spanning from chemistry, biochemistry, molecular biology to pharmacology, this review will summarize the most recent available literature regarding different aspects of proteasome biology, focusing on structure, function and regulation of proteasome in physiological and pathological processes, mostly cancer and neurodegenerative diseases, connecting biochemical features and clinical studies of proteasome targeting drugs.

AB - Ubiquitin Proteasome System (UPS) is an adaptable and finely tuned system that sustains proteostasis network under a large variety of physiopathological conditions. Its dysregulation is often associated with the onset and progression of human diseases; hence, UPS modulation has emerged as a promising new avenue for the development of treatments of several relevant pathologies, such as cancer and neurodegeneration. The clinical interest in proteasome inhibition has considerably increased after the FDA approval in 2003 of bortezomib for relapsed/refractory multiple myeloma, which is now used in the front-line setting. Thereafter, two other proteasome inhibitors (carfilzomib and ixazomib), designed to overcome resistance to bortezomib, have been approved for treatment-experienced patients, and a variety of novel inhibitors are currently under preclinical and clinical investigation not only for haematological malignancies but also for solid tumours. However, since UPS collapse leads to toxic misfolded proteins accumulation, proteasome is attracting even more interest as a target for the care of neurodegenerative diseases, which are sustained by UPS impairment. Thus, conceptually, proteasome activation represents an innovative and largely unexplored target for drug development. According to a multidisciplinary approach, spanning from chemistry, biochemistry, molecular biology to pharmacology, this review will summarize the most recent available literature regarding different aspects of proteasome biology, focusing on structure, function and regulation of proteasome in physiological and pathological processes, mostly cancer and neurodegenerative diseases, connecting biochemical features and clinical studies of proteasome targeting drugs.

KW - Cancer

KW - Neurodegeneration

KW - Proteasome

KW - Proteasome inhibitors

KW - SARS-Cov-2

UR - http://www.scopus.com/inward/record.url?scp=85088019708&partnerID=8YFLogxK

U2 - 10.1016/j.pharmthera.2020.107579

DO - 10.1016/j.pharmthera.2020.107579

M3 - Review

C2 - 32442437

AN - SCOPUS:85088019708

VL - 213

JO - Pharmacology & Therapeutics

JF - Pharmacology & Therapeutics

SN - 0163-7258

M1 - 107579

ER -