Target Information
| Target General Information | Top | |||||
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| Target ID |
T86734
(Former ID: TTDI02002)
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| Target Name |
Glutaminase (GLS)
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| Synonyms |
L-glutamine amidohydrolase; Glutaminase, mitochondrial; GLS
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| Gene Name |
GLS; GLS2
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 4 Target-related Diseases | + | ||||
| 1 | Breast cancer [ICD-11: 2C60-2C6Y] | |||||
| 2 | Renal cell carcinoma [ICD-11: 2C90] | |||||
| 3 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| 4 | Leukaemia [ICD-11: 2A60-2B33] | |||||
| Function |
Plays a role in maintaining acid-base homeostasis. Regulates the levels of the neurotransmitter glutamate in the brain. Isoform 2 lacks catalytic activity. Catalyzes the first reaction in the primary pathway for the renal catabolism of glutamine.
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| BioChemical Class |
Carbon-nitrogen hydrolase
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| UniProt ID | ||||||
| Sequence |
MMRLRGSGMLRDLLLRSPAGVSATLRRAQPLVTLCRRPRGGGRPAAGPAAAARLHPWWGG
GGWPAEPLARGLSSSPSEILQELGKGSTHPQPGVSPPAAPAAPGPKDGPGETDAFGNSEG KELVASGENKIKQGLLPSLEDLLFYTIAEGQEKIPVHKFITALKSTGLRTSDPRLKECMD MLRLTLQTTSDGVMLDKDLFKKCVQSNIVLLTQAFRRKFVIPDFMSFTSHIDELYESAKK QSGGKVADYIPQLAKFSPDLWGVSVCTVDGQRHSTGDTKVPFCLQSCVKPLKYAIAVNDL GTEYVHRYVGKEPSGLRFNKLFLNEDDKPHNPMVNAGAIVVTSLIKQGVNNAEKFDYVMQ FLNKMAGNEYVGFSNATFQSERESGDRNFAIGYYLKEKKCFPEGTDMVGILDFYFQLCSI EVTCESASVMAATLANGGFCPITGERVLSPEAVRNTLSLMHSCGMYDFSGQFAFHVGLPA KSGVAGGILLVVPNVMGMMCWSPPLDKMGNSVKGIHFCHDLVSLCNFHNYDNLRHFAKKL DPRREGGDQRVKSVINLLFAAYTGDVSALRRFALSAMDMEQRDYDSRTALHVAAAEGHVE VVKFLLEACKVNPFPKDRWNNTPMDEALHFGHHDVFKILQEYQVQYTPQGDSDNGKENQT VHKNLDGLL Click to Show/Hide
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| HIT2.0 ID | T81OKW | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | CB-839 | Drug Info | Phase 2 | Breast cancer | [2] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | CB-839 | Drug Info | [1] | |||
| Inhibitor | [+] 11 Inhibitor drugs | + | ||||
| 1 | PMID30273516-Compound-1 | Drug Info | [3] | |||
| 2 | PMID30273516-Compound-12 | Drug Info | [3] | |||
| 3 | PMID30273516-Compound-13 | Drug Info | [3] | |||
| 4 | PMID30273516-Compound-15 | Drug Info | [3] | |||
| 5 | PMID30273516-Compound-22a | Drug Info | [3] | |||
| 6 | PMID30273516-Compound-22b | Drug Info | [3] | |||
| 7 | PMID30273516-Compound-37 | Drug Info | [3] | |||
| 8 | PMID30273516-Compound-38 | Drug Info | [3] | |||
| 9 | PMID30273516-Compound-39 | Drug Info | [3] | |||
| 10 | PMID30273516-Compound-40 | Drug Info | [3] | |||
| 11 | PMID30273516-Compound-41 | Drug Info | [3] | |||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 9 KEGG Pathways | + | ||||
| 1 | Arginine biosynthesis | |||||
| 2 | Alanine, aspartate and glutamate metabolism | |||||
| 3 | D-Glutamine and D-glutamate metabolism | |||||
| 4 | Metabolic pathways | |||||
| 5 | Glutamatergic synapse | |||||
| 6 | GABAergic synapse | |||||
| 7 | Proximal tubule bicarbonate reclamation | |||||
| 8 | MicroRNAs in cancer | |||||
| 9 | Central carbon metabolism in cancer | |||||
| References | Top | |||||
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| REF 1 | Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol Cancer Ther. 2014 Apr;13(4):890-901. | |||||
| REF 2 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 3 | Glutaminase inhibitors: a patent review.Expert Opin Ther Pat. 2018 Nov;28(11):823-835. | |||||
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