Ontology highlight
ABSTRACT:
SUBMITTER: Cherney EC
PROVIDER: S-EPMC8274105 | biostudies-literature | 2021 Jul
REPOSITORIES: biostudies-literature
Cherney Emily C EC Zhang Liping L Guo Weiwei W Huang Audris A Williams David D Seitz Steven S Shan Weifang W Zhu Xiao X Gullo-Brown Johnni J Maley Derrick D Lin Tai-An TA Hunt John T JT Huang Christine C Yang Zheng Z D'Arienzo Celia J CJ Discenza Lorell N LN Ranasinghe Asoka A Grubb Mary F MF Traeger Sarah C SC Li Xin X Johnston Kathy A KA Kopcho Lisa L Fereshteh Mark M Foster Kimberly A KA Stefanski Kevin K Delpy Diane D Dhar Gopal G Anandam Aravind A Mahankali Sandeep S Padmanabhan Shweta S Rajanna Prabhakar P Murali Venkata V Mariappan T Thanga TT Pattasseri Shabeerali S Nimje Roshan Y RY Hong Zhenqiu Z Kempson James J Rampulla Richard R Mathur Arvind A Gupta Anuradha A Borzilleri Robert R Vite Gregory G Balog Aaron A
ACS medicinal chemistry letters 20210616 7
IDO1 inhibitors have shown promise as immunotherapies for the treatment of a variety of cancers, including metastatic melanoma and renal cell carcinoma. We recently reported the identification of several novel heme-displacing IDO1 inhibitors, including the clinical molecules linrodostat (BMS-986205) and BMS-986242. Both molecules contain quinolines that, while being present in successful medicines, are known to be potentially susceptible to oxidative metabolism. Efforts to swap this quinoline wi ...[more]