Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS

• Published in: ACS medicinal chemistry letters Vol. 9; no. 7; pp. 623 - 628
• Main Authors: Schenck Eidam, Hilary, Russell, John, Raha, Kaushik, DeMartino, Michael, Qin, Donghui, Guan, Huiping Amy, Zhang, Zhiliu, Zhen, Gong, Yu, Haiyu, Wu, Chengde, Pan, Yan, Joberty, Gerard, Zinn, Nico, Laquerre, Sylvie, Robinson, Sharon, White, Angela, Giddings, Amanda, Mohammadi, Ehsan, Greenwood-Van Meerveld, Beverly, Oliff, Allen, Kumar, Sanjay, Cheung, Mui
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 12.07.2018; Amer Chemical Soc
• Subjects: Chemistry, Medicinal; Letter; Life Sciences & Biomedicine; Pharmacology & Pharmacy; Science & Technology; genotoxicity; RET kinase; IBS; AMES; gut restricted; DISORDERS; MECHANISMS; HIRSCHSPRUNGS-DISEASE; FAMILY; GDNF; GROWTH; NEURONS; EXPRESSION; IRRITABLE-BOWEL-SYNDROME; HYPERSENSITIVITY

Abdominal pain and abnormal bowel habits represent major symptoms for irritable bowel syndrome (IBS) patients that are not adequately managed. Although the etiology of IBS is not completely understood, many of the functions of the gastrointestinal (GI) tract are regulated by the enteric nervous syst...