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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Publicat a:ACS Med Chem Lett
Autors principals: 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
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2018
Accés en línia: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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