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Carrier-Free Immunotherapeutic Nano-Booster with Dual Synergistic Effects Based on Glutaminase Inhibition Combined with Photodynamic Therapy.

ACS Nano, 2023
The immunotherapeutic effect elicited by photodynamic therapy (PDT) is attenuated by tumor defense mechanisms associated with glutamine metabolism, including the metabolic regulation of redox homeostasis and the limitation of the immunosuppressive tumor ...
Ziyi Mai   +11 more
semanticscholar   +1 more source

Upregulation of the Glutaminase II Pathway Contributes to Glutamate Production upon Glutaminase 1 Inhibition in Pancreatic Cancer

open access: yesProteomics, 2019
The targeting of glutamine metabolism specifically via pharmacological inhibition of glutaminase 1 (GLS1) has been translated into clinical trials as a novel therapy for several cancers. The results, though encouraging, show room for improvement in terms
Giang Hoang, Tu Nguyen, Khoa Pham
exaly   +2 more sources

Structure-Enabled Discovery of Novel Macrocyclic Inhibitors Targeting Glutaminase 1 Allosteric Binding Site.

Journal of Medicinal Chemistry, 2021
The inhibition of glutaminase 1 (GLS1) represents a potential treatment of malignant tumors. Structural analysis led to the design of a novel series of macrocyclic GLS1 allosteric inhibitors.
Xi Xu   +16 more
semanticscholar   +1 more source

Glutaminases

2016
Mammalian glutaminases catalyze the stoichiometric conversion of L-glutamine to L-glutamate and ammonium ions. In brain, glutaminase is considered the prevailing pathway for synthesis of the neurotransmitter pool of glutamate. Besides neurotransmission, the products of glutaminase reaction also fulfill crucial roles in energy and metabolic homeostasis ...
Javier, Márquez   +2 more
openaire   +2 more sources

Tumor Glutaminase Purification

Protein Expression and Purification, 1995
Two alternative purification schemes to obtain the glutaminase from Ehrlich tumor cells in a highly purified form have been developed. One experimental approach is based on conventional and high-performance liquid chromatography fractionation techniques, yielding a 37-fold higher purification than has been previously reported.
J A, Segura   +4 more
openaire   +2 more sources

Dysregulation of glutaminase and glutamine synthetase in cancer.

Cancer Letters, 2019
Besides fast glucose catabolism, many types of cancers are characterized by elevated glutamine consumption. Medical oncology pursuits to block specific pathways, mainly glycolysis and glutaminolysis, in tumor cells to arrest cancer development.
J. Matés   +3 more
semanticscholar   +1 more source

Glutaminase in human platelets

Clinica Chimica Acta, 1983
Summary The activity of phosphate activated glutaminase, which is the major enzyme yielding glutamate from glutamine has been measured in human blood platelets. The enzyme shows good reproducibility in split duplicate assays and is stable over time. Platelets retain more enzyme activity when stored at 4°C in a buffered medium than when stored frozen.
openaire   +2 more sources

MODULATORS OF GLUTAMINASE ACTIVITY

Journal of Neurochemistry, 1972
Abstract— The activating effect of GTP on particulate preparations of glutaminase from rat brain or rat kidney was competitively inhibited by cyclic guanosine 3′,5′‐monophosphate (c‐GMP). Similarly, the effect of ATP was inhibited by cyclic adenosine 3′,5′‐monophosphate (c‐AMP). In the absence of an added activator, the glutaminase activity of brain or
openaire   +2 more sources

Mammalian glutaminase isozymes in brain

Metabolic Brain Disease, 2012
Glutamine/glutamate homeostasis must be exquisitely regulated in mammalian brain and glutaminase (GA, E.C. 3.5.1.2) is one of the main enzymes involved. The products of GA reaction, glutamate and ammonia, are essential metabolites for energy and biosynthetic purposes but they are also hazardous compounds at concentrations beyond their normal ...
Javier, Márquez   +6 more
openaire   +2 more sources

Hormonal control of hepatic glutaminase

Advances in Enzyme Regulation, 1995
(1) Glucagon activates hepatic glutaminase in vivo. Mitochondria from glucagon-injected rats retain an enhanced capacity to catabolize glutamine and this is more sensitive to activation by inorganic phosphate. The glucagon-elicited stimulation of glutaminase is not evident in broken mitochondria.
J T, Brosnan, H S, Ewart, S A, Squires
openaire   +2 more sources

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