819083-90-4Relevant academic research and scientific papers
Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II
Hidaka, Koushi,Kimura, Tooru,Tsuchiya, Yumi,Kamiya, Mami,Ruben, Adam J.,Freire, Ernesto,Hayashi, Yoshio,Kiso, Yoshiaki
, p. 3048 - 3052 (2007)
Based on a highly potent allophenylnorstatine-containing inhibitor, KNI-10006, against the plasmepsins of Plasmodium falciparum, we synthesized a series of tripeptide-type compounds with various N-terminal moieties and evaluated their inhibitory activitie
How much binding affinity can be gained by filling a cavity?
Kawasaki, Yuko,Chufan, Eduardo E.,Lafont, Virginie,Hidaka, Koushi,Kiso, Yoshiaki,Mario Amzel,Freire, Ernesto
experimental part, p. 143 - 151 (2011/02/25)
Binding affinity optimization is critical during drug development. Here, we evaluate the thermodynamic consequences of filling a binding cavity with functionalities of increasing van der Waals radii (-H, -F, -Cl, and CH 3) that improve the geom
