Proteins > Glutaminase kidney isoform, mitochondrial
Page last updated: 2024-08-07 23:07:45
Glutaminase kidney isoform, mitochondrial
A glutaminase kidney isoform, mitochondrial that is encoded in the genome of human. [PRO:DNx, UniProtKB:O94925]
Synonyms
GLS;
EC 3.5.1.2;
K-glutaminase;
L-glutamine amidohydrolase
Research
Bioassay Publications (13)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 8 (61.54) | 24.3611 |
2020's | 5 (38.46) | 2.80 |
Compounds (1)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
cb-839 | Homo sapiens (human) | IC50 | 0.2025 | 15 | 15 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
cb-839 | Homo sapiens (human) | Kd | 0.0987 | 3 | 4 |
Metabolomics-assisted discovery of a new anticancer GLS-1 inhibitor chemotype from a nortopsentin-inspired library: From phenotype screening to target identification.European journal of medicinal chemistry, , Apr-15, Volume: 234, 2022
Discovery of novel glutaminase 1 allosteric inhibitor with 4-piperidinamine linker and aromatic heterocycles.European journal of medicinal chemistry, , Jun-05, Volume: 236, 2022
Structure-Enabled Discovery of Novel Macrocyclic Inhibitors Targeting Glutaminase 1 Allosteric Binding Site.Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Allosteric kidney-type glutaminase (GLS) inhibitors with a mercaptoethyl linker.Bioorganic & medicinal chemistry, , 10-15, Volume: 28, Issue:20, 2020
Novel 1,3,4-Selenadiazole-Containing Kidney-Type Glutaminase Inhibitors Showed Improved Cellular Uptake and Antitumor Activity.Journal of medicinal chemistry, , 01-24, Volume: 62, Issue:2, 2019
Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.Journal of medicinal chemistry, , 07-25, Volume: 62, Issue:14, 2019
Development and Characterization of a Fluorescent Probe for GLS1 and the Application for High-Throughput Screening of Allosteric Inhibitors.Journal of medicinal chemistry, , 11-14, Volume: 62, Issue:21, 2019
Discovery and development of small molecule modulators targeting glutamine metabolism.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Recent Progress in the Discovery of Allosteric Inhibitors of Kidney-Type Glutaminase.Journal of medicinal chemistry, , 01-10, Volume: 62, Issue:1, 2019
Physapubescin, a natural withanolide as a kidney-type glutaminase (KGA) inhibitor.Bioorganic & medicinal chemistry letters, , 03-01, Volume: 27, Issue:5, 2017
Allosteric Glutaminase Inhibitors Based on a 1,4-Di(5-amino-1,3,4-thiadiazol-2-yl)butane Scaffold.ACS medicinal chemistry letters, , May-12, Volume: 7, Issue:5, 2016
Design and evaluation of novel glutaminase inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Enables
This protein enables 2 target(s):
Target | Category | Definition |
glutaminase activity | molecular function | Catalysis of the reaction: L-glutamine + H2O = L-glutamate + NH3. [EC:3.5.1.2] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
Located In
This protein is located in 4 target(s):
Target | Category | Definition |
mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
mitochondrial matrix | cellular component | The gel-like material, with considerable fine structure, that lies in the matrix space, or lumen, of a mitochondrion. It contains the enzymes of the tricarboxylic acid cycle and, in some organisms, the enzymes concerned with fatty acid oxidation. [GOC:as, ISBN:0198506732] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
Involved In
This protein is involved in 7 target(s):
Target | Category | Definition |
suckling behavior | biological process | Specific behavior of a newborn or infant mammal that results in the derivation of nourishment from the breast. [GOC:dph, GOC:pr] |
regulation of respiratory gaseous exchange by nervous system process | biological process | A process carried out by the nervous system that is required for the proper control of respiratory gaseous exchange. This process occurs in the respiratory center of the brain in vertebrates. [GOC:dph, GOC:tb, PMID:12458206] |
glutamate biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of glutamate, the anion of 2-aminopentanedioic acid. [GOC:go_curators] |
glutamine catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of glutamine, 2-amino-4-carbamoylbutanoic acid. [GOC:ai] |
chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |
protein homotetramerization | biological process | The formation of a protein homotetramer, a macromolecular structure consisting of four noncovalently associated identical subunits. [GOC:go_curators] |
intracellular glutamate homeostasis | biological process | A homeostatic process involved in the maintenance of a steady state level of glutamate within a cell. [GOC:tb] |