NASH Target Development Service for Leukotriene Receptor Antagonists

Nonalcoholic fatty liver disease/nonalcoholic steatohepatitis (NAFLD/NASH) is thought to become the leading liver disease worldwide currently. Leukotriene receptor is regarded as a potential target since it is involved in the NASH occurrence. Creative Biolabs is a pioneer company in providing target identification for drug discovery services. Our professional scientists are committed to the identification of potential drug targets research, and now we can provide high-quality leukotriene receptor antagonists for the treatment of NASH. Our experienced scientists will take part in every step of your program to accelerate your project development. With the help of our professional scientists, we are confident in providing NASH-associated services to meet every customer's requirements.

Introduction of Leukotriene Receptor

The leukotriene (LT) receptors are a class of G protein-coupled receptors that recognize and are activated by the leukotrienes. In general, leukotrienes (LTs) include two distinct classes, hydroxy acids (such as LTB4), and cysteinyl leukotrienes (such as LTC4, LTD4, and LTE4). Correspondingly, leukotriene receptors have also been classified into BLT and CysLT types. BLT has two subtypes termed BLT1 and BLT2, and the two subtypes of CysLT termed CysLT1 and CysLT2. The human BLT1 receptor was first identified in 1999 and was shown to be a G protein-coupled receptor. It was later found that the promoter for the BLT1 receptor is located in the ORF of the gene for the BLT2 receptor. The CysLT1 and the CysLT2 receptors are members of the G protein-coupled receptor superfamily, both found in 2000. LT receptors may couple via Gi to inhibit adenylate cyclase, and Gq/11 to modulate inositol phospholipid hydrolysis and calcium mobilization. CysLT receptors can regulate a wide range of other pro-inflammatory effects, such as constriction of airways and vascular smooth muscle, enhancement of endothelial membrane permeability and mucus secretion, induction of plasma exudation and edema.

Fig.1 Leukotriene (LT) signal pathway as one of the targets of current asthma medication. (Singh, 2007)

Leukotriene Receptor Antagonists for NASH Treatment

Patients with NASH have the potential to develop fibrosis and cirrhosis which result in portal hypertension, liver decompensation, and hepatocellular carcinoma. There is evidence that the fibrosis process in NASH is associated with the leukotriene receptor. Therefore, the leukotriene receptor can be a target for the NASH treatment. To date, several leukotriene receptor antagonists have been developed. The potent, long-acting, orally active CysLT receptor antagonists, such as zafirlukast, montelukast, and pranlukast, have been used in NASH and asthma therapy, these compounds are now being increasingly regarded as useful additions to the therapeutic NASH and armory in the treatment of this disease. Furthermore, other types of antagonists target BLT receptors and CysLT1 receptors have been presented, such as the non-selective CysLT antagonist, BAYu9773, which has presented a significant therapeutic effect during the targeted leukotriene receptor-associated disease.

Fig.2 Leukotriene receptor antagonist mechanism of action. (Matthes, 2015)

Features

• Fast: Screening can be accomplished in a short time.
• High-Throughput: Our target screening is high-throughput compatible.
• Professional: Highly experienced Ph.D. scientists in charge of every project with a specialized team for quality control in every step of the process; expert R&D team dedicated to the optimization of protocols to deliver data with enhanced quality.
• Integrity: Custom services including but not limited to target screening, as well as the drug production to fulfill your needs.

Along with years of rich experience in the field of disease target development, Creative Biolabs has successfully finished lots of projects for our customers all over the world. We are now confident in offering customized proposals and products to meet your specific needs. If you are interested in our NSAH treatment services, please do not hesitate to contact us for more details.

References

1. Singh, A.M., et al. Bronchiolitis to asthma. American Journal of Respiratory & Critical Care Medicine. 2007.
2. Matthes, S.A., et al. Comparative Biology of the Normal Lung (Second Edition). 2015.