Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTCW0KX)

• DTT Name: Glutaminase (GLS)
• Synonyms: L-glutamine amidohydrolase; Glutaminase, mitochondrial; GLS
• Gene Name: GLS
• DTT Type: Clinical trial target; [1]
• BioChemical Class: Carbon-nitrogen hydrolase
• UniProt ID: GLSK_HUMAN ; GLSL_HUMAN
• TTD ID: T86734
• Sequence:
  MMRLRGSGMLRDLLLRSPAGVSATLRRAQPLVTLCRRPRGGGRPAAGPAAAARLHPWWGG
  GGWPAEPLARGLSSSPSEILQELGKGSTHPQPGVSPPAAPAAPGPKDGPGETDAFGNSEG
  KELVASGENKIKQGLLPSLEDLLFYTIAEGQEKIPVHKFITALKSTGLRTSDPRLKECMD
  MLRLTLQTTSDGVMLDKDLFKKCVQSNIVLLTQAFRRKFVIPDFMSFTSHIDELYESAKK
  QSGGKVADYIPQLAKFSPDLWGVSVCTVDGQRHSTGDTKVPFCLQSCVKPLKYAIAVNDL
  GTEYVHRYVGKEPSGLRFNKLFLNEDDKPHNPMVNAGAIVVTSLIKQGVNNAEKFDYVMQ
  FLNKMAGNEYVGFSNATFQSERESGDRNFAIGYYLKEKKCFPEGTDMVGILDFYFQLCSI
  EVTCESASVMAATLANGGFCPITGERVLSPEAVRNTLSLMHSCGMYDFSGQFAFHVGLPA
  KSGVAGGILLVVPNVMGMMCWSPPLDKMGNSVKGIHFCHDLVSLCNFHNYDNLRHFAKKL
  DPRREGGDQRVKSVINLLFAAYTGDVSALRRFALSAMDMEQRDYDSRTALHVAAAEGHVE
  VVKFLLEACKVNPFPKDRWNNTPMDEALHFGHHDVFKILQEYQVQYTPQGDSDNGKENQT
  VHKNLDGLL
• 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.
• KEGG Pathway:
  Arginine biosynthesis (hsa00220)
  Alanine, aspartate and glutamate metabolism (hsa00250)
  D-Glutamine and D-glutamate metabolism (hsa00471)
  Metabolic pathways (hsa01100)
  Glutamatergic synapse (hsa04724)
  GABAergic synapse (hsa04727)
  Proximal tubule bicarbonate reclamation (hsa04964)
  MicroRNAs in cancer (hsa05206)
  Central carbon metabolism in cancer (hsa05230)
• Reactome Pathway:
  TP53 Regulates Metabolic Genes (R-HSA-5628897)
  Glutamate and glutamine metabolism (R-HSA-8964539)
  Glutamate Neurotransmitter Release Cycle (R-HSA-210500)

Molecular Interaction Atlas (MIA) of This DTT

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CB-839	DM094UH	Breast cancer	2C60-2C65	Phase 2	[1]

12 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID30273516-Compound-1	DM52MKV	N. A.	N. A.	Patented	[2]
PMID30273516-Compound-12	DMIWEZH	N. A.	N. A.	Patented	[2]
PMID30273516-Compound-13	DMK9TJP	N. A.	N. A.	Patented	[2]
PMID30273516-Compound-14	DMURZHA	N. A.	N. A.	Patented	[2]
PMID30273516-Compound-15	DMSD647	N. A.	N. A.	Patented	[2]
PMID30273516-Compound-22a	DMVZA0U	N. A.	N. A.	Patented	[2]
PMID30273516-Compound-22b	DMZ5O3K	N. A.	N. A.	Patented	[2]
PMID30273516-Compound-37	DM8NBJV	N. A.	N. A.	Patented	[2]
PMID30273516-Compound-38	DMRPJBF	N. A.	N. A.	Patented	[2]
PMID30273516-Compound-39	DMBF3ZE	N. A.	N. A.	Patented	[2]
PMID30273516-Compound-40	DM5N8YJ	N. A.	N. A.	Patented	[2]
PMID30273516-Compound-41	DM5UBMJ	N. A.	N. A.	Patented	[2]

References

• [1] Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol Cancer Ther. 2014 Apr;13(4):890-901.
• [2] Glutaminase inhibitors: a patent review.Expert Opin Ther Pat. 2018 Nov;28(11):823-835.