1259314-99-2Relevant academic research and scientific papers
Optimization of purine-nitrile TbcatB inhibitors for use in vivo and evaluation of efficacy in murine models
Mallari, Jeremy P.,Zhu, Fangyi,Lemoff, Andrew,Kaiser, Marcel,Lu, Min,Brun, Reto,Guy, R. Kiplin
experimental part, p. 8302 - 8309 (2011/03/17)
There are currently only four clinical drugs available for treating human African trypanosomiasis (HAT), three of which were developed over 60 years ago. Despite years of effort, there has been relatively little progress towards identifying orally availab
Structure-guided development of selective TbcatB inhibitors
Mallari, Jeremy P.,Shelat, Anang A.,Kosinski, Aaron,Caffrey, Conor R.,Connelly, Michele,Zhu, Fangyi,McKerrow, James H.,Kiplin Guy
supporting information; experimental part, p. 6489 - 6493 (2010/03/31)
The trypanosomal cathepsin TbcatB is essential for parasite survival and is an attractive therapeutic target. Herein we report the structure-guided development of TbcatB inhibitors with specificity relative to rhodesain and human cathepsins B and L. Inhib
