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

TTT Nguyen, WP Katt, RA Cerione - Future Drug Discovery, 2022 - Taylor & Francis
Plain Language Summary Metabolic reprogramming is a major hallmark of malignant
transformation in cancer, and part of the so-called Warburg effect, in which the upregulation …

Glutaminase inhibition as potential cancer therapeutics: current status and future applications

R Cyriac, K Lee - Journal of Enzyme Inhibition and Medicinal …, 2024 - Taylor & Francis
Alterations in normal metabolic processes are defining features of cancer. Glutamine, an
abundant amino acid in the human blood, plays a critical role in regulating several …

Glutaminase regulation in cancer cells: a druggable chain of events

WP Katt, RA Cerione - Drug discovery today, 2014 - Elsevier
Highlights•Inhibition of glutamine metabolism is an important mechanism in cancer
control.•Novel drugs offer a mechanism by which the key metabolic enzyme glutaminase …

Metabolic reprogramming of cancer by chemicals that target glutaminase isoenzymes

JM Matés, JA Campos-Sandoval… - Current medicinal …, 2020 - ingentaconnect.com
Background: Metabolic reprogramming of tumours is a hallmark of cancer. Among the
changes in the metabolic network of cancer cells, glutaminolysis is a key reaction altered in …

Targeting glutaminolysis: new perspectives to understand cancer development and novel strategies for potential target therapies

Z Wang, F Liu, N Fan, C Zhou, D Li, T Macvicar… - Frontiers in …, 2020 - frontiersin.org
Metabolism rewiring is an important hallmark of cancers. Being one of the most abundant
free amino acids in the human blood, glutamine supports bioenergetics and biosynthesis …

[HTML][HTML] Glutaminolysis as a target for cancer therapy

L Jin, GN Alesi, S Kang - Oncogene, 2016 - nature.com
Cancer cells display an altered metabolic circuitry that is directly regulated by oncogenic
mutations and loss of tumor suppressors. Mounting evidence indicates that altered …

[HTML][HTML] Inhibition of glutaminolysis in combination with other therapies to improve cancer treatment

YA Shen, CL Chen, YH Huang, EE Evans… - Current opinion in …, 2021 - Elsevier
Targeting glutamine catabolism has been attracting more research attention on the
development of successful cancer therapy. Catalytic enzymes such as glutaminase (GLS) in …

A tale of two glutaminases: homologous enzymes with distinct roles in tumorigenesis

WP Katt, MJ Lukey, RA Cerione - Future medicinal chemistry, 2017 - Taylor & Francis
Many cancer cells exhibit an altered metabolic phenotype, in which glutamine consumption
is upregulated relative to healthy cells. This metabolic reprogramming often depends upon …

High-throughput screening reveals new glutaminase inhibitor molecules

RK E. Costa, CT Rodrigues… - ACS Pharmacology & …, 2021 - ACS Publications
The glutaminase (GLS) enzyme hydrolyzes glutamine into glutamate, an important
anaplerotic source for the tricarboxylic acid cycle in rapidly growing cancer cells under the …

[HTML][HTML] Therapeutic targeting of glutaminolysis as an essential strategy to combat cancer

JM Matés, FJ Di Paola, JA Campos-Sandoval… - Seminars in cell & …, 2020 - Elsevier
Metabolic reprogramming in cancer targets glutamine metabolism as a key mechanism to
provide energy, biosynthetic precursors and redox requirements to allow the massive …