Leukotriene C4 synthase

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

   GtoImmuPdb view: OFF :     Leukotriene C4 synthase has curated GtoImmuPdb data

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
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 4.4.1.20 LTC4 = glutathione + LTA4

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

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
TK05 Hs Inhibition 8.2 pKi 3
pKi 8.2 (Ki 6x10-9 M) [3]
Description: Using isolated human enzyme.
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].

References

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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 Phys16 (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]

How to cite this page

Leukotriene and lipoxin metabolism: Leukotriene C4 synthase. Last modified on 26/04/2017. Accessed on 11/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1391.