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Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 4 | 150 | 5q35.3 | LTC4S | leukotriene C4 synthase | 2,6 |
Mouse | 4 | 150 | 11 B1.3 | Ltc4s | leukotriene C4 synthase | |
Rat | 4 | 150 | 10q22 | Ltc4s | leukotriene C4 synthase |
Previous and Unofficial Names |
LTC4 synthase |
Database Links | |
Alphafold | Q16873 (Hs), Q60860 (Mm), Q925U2 (Rn) |
BRENDA | 4.4.1.20 |
CATH/Gene3D | 1.20.120.550 |
ChEMBL Target | CHEMBL1743183 (Hs), CHEMBL2172 (Rn) |
Ensembl Gene | ENSG00000213316 (Hs), ENSMUSG00000020377 (Mm), ENSRNOG00000003244 (Rn) |
Entrez Gene | 4056 (Hs), 17001 (Mm), 114097 (Rn) |
Human Protein Atlas | ENSG00000213316 (Hs) |
KEGG Enzyme | 4.4.1.20 |
KEGG Gene | hsa:4056 (Hs), mmu:17001 (Mm), rno:114097 (Rn) |
OMIM | 246530 (Hs) |
Pharos | Q16873 (Hs) |
RefSeq Nucleotide | NM_145867 (Hs) |
RefSeq Protein | NP_665874 (Hs) |
UniProtKB | Q16873 (Hs), Q60860 (Mm), Q925U2 (Rn) |
Wikipedia | LTC4S (Hs) |
Enzyme Reaction | ||||
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Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Immunopharmacology Comments |
The role of leukotriene C4 synthase (LTC4S) in the production of cysteinyl leukotrienes (cys-LTs) which are potent proinflammatory mediators and bronchoconstrictors implicated in airway inflammation in conditions such as asthma [1,4], makes LTC4S a prominent target for pharmaceutical intervention in relevant diseases [3,7]. |
1. Bigby TD. (2000) The leukotriene C(4) synthase gene and asthma. Am J Respir Cell Mol Biol, 23 (3): 273-6. [PMID:10970815]
2. Bigby TD, Hodulik CR, Arden KC, Fu L. (1996) Molecular cloning of the human leukotriene C4 synthase gene and assignment to chromosome 5q35. Mol Med, 2 (5): 637-46. [PMID:8898379]
3. Kleinschmidt TK, Haraldsson M, Basavarajappa D, Lundeberg E, Thulasingam M, Ekoff M, Fauland A, Lehmann C, Kahnt AS, Lindbom L et al.. (2015) Tandem Benzophenone Amino Pyridines, Potent and Selective Inhibitors of Human Leukotriene C4 Synthase. J Pharmacol Exp Ther, 355 (1): 108-16. [PMID:26283693]
4. MacDonald CA, Bushnell EA, Gauld JW, Boyd RJ. (2014) The catalytic formation of leukotriene C4: a critical step in inflammatory processes. Phys Chem Chem Phys, 16 (30): 16284-9. [PMID:24974917]
5. Munck Af Rosenschöld M, Johannesson P, Nikitidis A, Tyrchan C, Chang HF, Rönn R, Chapman D, Ullah V, Nikitidis G, Glader P et al.. (2019) Discovery of the Oral Leukotriene C4 Synthase Inhibitor (1S,2S)-2-({5-[(5-Chloro-2,4-difluorophenyl)(2-fluoro-2-methylpropyl)amino]-3-methoxypyrazin-2-yl}carbonyl)cyclopropanecarboxylic Acid (AZD9898) as a New Treatment for Asthma. J Med Chem, 62 (17): 7769-7787. [PMID:31415176]
6. Penrose JF, Spector J, Baldasaro M, Xu K, Boyce J, Arm JP, Austen KF, Lam BK. (1996) Molecular cloning of the gene for human leukotriene C4 synthase. Organization, nucleotide sequence, and chromosomal localization to 5q35. J Biol Chem, 271 (19): 11356-61. [PMID:8626689]
7. Ronn R, Lindh CJ, Ringberg E, Andersson EHB, Nilsson P, Schall WR, Munk af RM, Nikitidis A, Nikitidis G, Johannesson PJ et al.. (2016) Cyclopropane carboxylic acid derivatives and pharmaceutical uses thereof. Patent number: WO2016177845. Assignee: Astrazeneca Ab. Priority date: 06/05/2015. Publication date: 10/11/2016.
8. Shiro T, Kakiguchi K, Takahashi H, Nagata H, Tobe M. (2013) 7-Phenyl-imidazoquinolin-4(5H)-one derivatives as selective and orally available mPGES-1 inhibitors. Bioorg Med Chem, 21 (11): 2868-78. [PMID:23623673]