化学
药理学
氮杂环丁烷
特发性肺纤维化
肺
肺移植
酪氨酸激酶
癌症研究
受体
纤维化
细胞外基质
药物发现
受体酪氨酸激酶
任天堂
闭塞性细支气管炎
药品
移植
药物开发
吸入
作者
Laura Carzaniga,Fabio Rancati,Andrea Rizzi,Roberta Mazzucato,Nicolò Iotti,Eleonora Ghidini,Serena Bertolini,Fabio Bignami,Alessandro Fioni,Valentina Mileo,Fabio Vaccaro,Annalisa Murgo,Allisson Freire Bento,Anna Maria Capelli,Benjamin Paul Whittaker,Stefano Levanto,Robert S. L. Chapman,Zuzana Hamasova,C.J. Hardy,David Edward Clark
标识
DOI:10.1021/acs.jmedchem.5c02830
摘要
was identified as the most promising one for its nanomolar potency, improved kinase selectivity, reduced cardiotoxicity risk, and excellent inhaled PK profile. It demonstrated activity in a collagen-induced pharmacodynamic mouse model, supporting its potential as an inhaled DDR inhibitor for IPF and validating the azetidine scaffold as a promising starting point for further optimization.
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