@article{72cf2bf1dad74450a498e4cb82e76f11,
title = "Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II",
abstract = "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 activities against plasmepsin II. Certain phenylacetyl derivatives exhibited extremely high affinity with Ki values of less than 0.1 nM suggesting successful hydrophobic interactions.",
keywords = "Allophenylnorstatine, Aspartic protease, Malaria, Peptidomimetic, Plasmepsin inhibitor",
author = "Koushi Hidaka and Tooru Kimura and Yumi Tsuchiya and Mami Kamiya and Ruben, {Adam J.} and Ernesto Freire and Yoshio Hayashi and Yoshiaki Kiso",
note = "Funding Information: This research was supported in part by the Frontier Research Program, the 21st Century COE Program of Ministry of Education, Culture, Sports, Science, and Technology of Japan (MEXT), and grants from MEXT. E.F. and A.J.R. also thank the Johns Hopkins Malaria Institute for a Pilot Research Grant and a Graduate Student Fellowship. We gratefully acknowledge Ms. Y. Iteya for synthetic assistance, and Mr. T. Hamada for the determination of HIV-1 PR inhibitory activity. We are grateful to Dr. J.-T. Nguyen for consult and revision of the manuscript. We thank the Swiss Tropical Institute for performing the erythrocyte inhibition assays.",
year = "2007",
month = jun,
day = "1",
doi = "10.1016/j.bmcl.2007.03.052",
language = "English (US)",
volume = "17",
pages = "3048--3052",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "11",
}