Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes

[Image: see text] The imidazolyl-tetrahydro-β-carboline class of sstr3 antagonists have demonstrated efficacy in a murine model of glucose excursion and may have potential as a treatment for type 2 diabetes. The first candidate in this class caused unacceptable QTc interval prolongation in oral, tel...

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Gepubliceerd in:ACS Med Chem Lett
Hoofdauteurs: Shah, Shrenik K., He, Shuwen, Guo, Liangqin, Truong, Quang, Qi, Hongbo, Du, Wu, Lai, Zhong, Liu, Jian, Jian, Tianying, Hong, Qingmei, Dobbelaar, Peter, Ye, Zhixiong, Sherer, Edward, Feng, Zhe, Yu, Yang, Wong, Frederick, Samuel, Koppara, Madiera, Maria, Karanam, Bindhu V., Reddy, Vijay B., Mitelman, Stan, Tong, Sharon X., Chicchi, Gary G., Tsao, Kwei-Lan, Trusca, Dorina, Feng, Yue, Wu, Margaret, Shao, Qing, Trujillo, Maria E., Eiermann, George J., Li, Cai, Pachanski, Michele, Fernandez, Guillermo, Nelson, Donald, Bunting, Patricia, Morissette, Pierre, Volksdorf, Sylvia, Kerr, Janet, Zhang, Bei B., Howard, Andrew D., Zhou, Yun-Ping, Pasternak, Alexander, Nargund, Ravi P., Hagmann, William K.
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: American Chemical Society 2015
Online toegang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4434471/
https://ncbi.nlm.nih.gov/pubmed/26005524
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml500514w
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