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Alone and together: current approaches to targeting glutaminase enzymes as part of anti-cancer therapies

Metabolic reprogramming is a major hallmark of malignant transformation in cancer, and part of the so-called Warburg effect, in which the upregulation of glutamine catabolism plays a major role. The glutaminase enzymes convert glutamine to glutamate, which initiates this pathway. Inhibition of diffe...

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Autores principales: Nguyen, Thuy-Tien T, Katt, William P, Cerione, Richard A
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Newlands Press Ltd 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10051075/
https://www.ncbi.nlm.nih.gov/pubmed/37009252
http://dx.doi.org/10.4155/fdd-2022-0011
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author Nguyen, Thuy-Tien T
Katt, William P
Cerione, Richard A
author_facet Nguyen, Thuy-Tien T
Katt, William P
Cerione, Richard A
author_sort Nguyen, Thuy-Tien T
collection PubMed
description Metabolic reprogramming is a major hallmark of malignant transformation in cancer, and part of the so-called Warburg effect, in which the upregulation of glutamine catabolism plays a major role. The glutaminase enzymes convert glutamine to glutamate, which initiates this pathway. Inhibition of different forms of glutaminase (KGA, GAC, or LGA) demonstrated potential as an emerging anti-cancer therapeutic strategy. The regulation of these enzymes, and the molecular basis for their inhibition, have been the focus of much recent research. This review will explore the recent progress in understanding the molecular basis for activation and inhibition of different forms of glutaminase, as well as the recent focus on combination therapies of glutaminase inhibitors with other anti-cancer drugs.
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spelling pubmed-100510752023-03-30 Alone and together: current approaches to targeting glutaminase enzymes as part of anti-cancer therapies Nguyen, Thuy-Tien T Katt, William P Cerione, Richard A Future Drug Discov Review Metabolic reprogramming is a major hallmark of malignant transformation in cancer, and part of the so-called Warburg effect, in which the upregulation of glutamine catabolism plays a major role. The glutaminase enzymes convert glutamine to glutamate, which initiates this pathway. Inhibition of different forms of glutaminase (KGA, GAC, or LGA) demonstrated potential as an emerging anti-cancer therapeutic strategy. The regulation of these enzymes, and the molecular basis for their inhibition, have been the focus of much recent research. This review will explore the recent progress in understanding the molecular basis for activation and inhibition of different forms of glutaminase, as well as the recent focus on combination therapies of glutaminase inhibitors with other anti-cancer drugs. Newlands Press Ltd 2023-03-27 2023-03 /pmc/articles/PMC10051075/ /pubmed/37009252 http://dx.doi.org/10.4155/fdd-2022-0011 Text en © 2023 Newlands Press https://creativecommons.org/licenses/by-nc-nd/4.0/This work is licensed under the Attribution-NonCommercial-NoDerivatives 4.0 Unported License (https://creativecommons.org/licenses/by-nc-nd/4.0/)
spellingShingle Review
Nguyen, Thuy-Tien T
Katt, William P
Cerione, Richard A
Alone and together: current approaches to targeting glutaminase enzymes as part of anti-cancer therapies
title Alone and together: current approaches to targeting glutaminase enzymes as part of anti-cancer therapies
title_full Alone and together: current approaches to targeting glutaminase enzymes as part of anti-cancer therapies
title_fullStr Alone and together: current approaches to targeting glutaminase enzymes as part of anti-cancer therapies
title_full_unstemmed Alone and together: current approaches to targeting glutaminase enzymes as part of anti-cancer therapies
title_short Alone and together: current approaches to targeting glutaminase enzymes as part of anti-cancer therapies
title_sort alone and together: current approaches to targeting glutaminase enzymes as part of anti-cancer therapies
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10051075/
https://www.ncbi.nlm.nih.gov/pubmed/37009252
http://dx.doi.org/10.4155/fdd-2022-0011
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