Cargando…
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...
Autores principales: | , , |
---|---|
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 |
_version_ | 1785014786696675328 |
---|---|
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. |
format | Online Article Text |
id | pubmed-10051075 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | Newlands Press Ltd |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT nguyenthuytient aloneandtogethercurrentapproachestotargetingglutaminaseenzymesaspartofanticancertherapies AT kattwilliamp aloneandtogethercurrentapproachestotargetingglutaminaseenzymesaspartofanticancertherapies AT cerionericharda aloneandtogethercurrentapproachestotargetingglutaminaseenzymesaspartofanticancertherapies |