Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma

[Image: see text] A novel series of tricyclic tetrahydroquinolines were identified as potent and selective CRTh2 receptor antagonists. The agonism and antagonism switch was achieved through structure-based drug design (SBDD) using a CRTh2 receptor homologue model. The challenge of very low exposures...

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Vydáno v:ACS Med Chem Lett
Hlavní autoři: Huang, Xianhai, Brubaker, Jason, Zhou, Wei, Biju, Purakkattle J., Xiao, Li, Shao, Ning, Huang, Ying, Dong, Li, Liu, Zhidan, Bitar, Rema, Buevich, Alexei, Jung, Joon, Peterson, Scott L., Butcher, John W., Close, Joshua, Martinez, Michelle, MacCoss, Rachel N., Zhang, Hongjun, Crawford, Scott, McCormick, Kevin D., Aslanian, Robert, Nargund, Ravi, Correll, Craig, Gervais, Francois, Qiu, Hongchen, Yang, Xiaoxin, Garlisi, Charles, Rindgen, Diane, Maloney, Kevin M., Siliphaivanh, Phieng, Palani, Anandan
Médium: Artigo
Jazyk:Inglês
Vydáno: American Chemical Society 2018
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC6047040/
https://ncbi.nlm.nih.gov/pubmed/30034600
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.8b00145
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