Article
"Network leaning" as a mechanism of insurmountable antagonism of the angiotensin II type 1 receptor by non-peptide antagonists.
The Journal of biological chemistry - 9 Apr 2004
Takezako Takanobu, Gogonea Camelia, Saad Yasser, Noda Keita, Karnik Sadashiva S
Abstract excerpt
A mechanistic understanding of the insurmountable antagonism of the angiotensin II type 1 (AT(1)) receptor could be fundamental in the quest for discovery and improvement of drugs. Candesartan and EXP3174 are competitive, reversible insurmountable antagonists of the AT(1) receptor. They contain di-acidic substitutions, whereas the surmountable antagonist, losartan, contains only one acidic group. We tested the...
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