Leukotriene C4 synthase | Leukotriene and lipoxin metabolism | IUPHAR/BPS Guide to PHARMACOLOGY

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Leukotriene C4 synthase

target has curated data in GtoImmuPdb

Target id: 1391

Nomenclature: Leukotriene C4 synthase

Family: Leukotriene and lipoxin metabolism

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 4 150 5q35.3 LTC4S leukotriene C4 synthase 2,5
Mouse - - Ltc4s leukotriene C4 synthase
Rat - - Ltc4s leukotriene C4 synthase
Previous and Unofficial Names
LTC4 synthase
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction
EC Number: LTC4 = glutathione + LTA4

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
TK05 Hs Inhibition 8.2 pKi 3
pKi 8.2 (Ki 6x10-9 M) [3]
Description: Using isolated human enzyme.
AZD9898 Hs Inhibition 9.5 pIC50 6
pIC50 9.5 (IC50 2.89x10-10 M) [6]
Description: IC50 vs human recombinant purified LTC4 synthase determined by determination of inhibition of LTC4 methyl ester product formation in vitro
example 36 [WO2016177845] Hs Inhibition 8.1 pIC50 6
pIC50 8.1 (IC50 9x10-9 M) [6]
compound 39 [PMID: 23623673] Hs Inhibition <5.5 pIC50 7
pIC50 <5.5 (IC50 >3x10-6 M) [7]
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 [3,6].


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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. 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]

6. 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.

7. 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]


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