Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II

Koushi Hidaka; Tooru Kimura; Yumi Tsuchiya; Mami Kamiya; Adam J. Ruben; Ernesto Freire; Yoshio Hayashi; Yoshiaki Kiso

doi:10.1016/j.bmcl.2007.03.052

Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II

Koushi Hidaka, Tooru Kimura, Yumi Tsuchiya, Mami Kamiya, Adam J. Ruben, Ernesto Freire, Yoshio Hayashi, Yoshiaki Kiso

School of Arts and Sciences

Research output: Contribution to journal › Article › peer-review

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 K_i values of less than 0.1 nM suggesting successful hydrophobic interactions.

Original language	English (US)
Pages (from-to)	3048-3052
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2007.03.052
State	Published - Jun 1 2007

Keywords

Allophenylnorstatine
Aspartic protease
Malaria
Peptidomimetic
Plasmepsin inhibitor

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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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.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 17, No. 11, 01.06.2007, p. 3048-3052.

Research output: Contribution to journal › Article › peer-review

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AU - Kamiya, Mami

AU - Ruben, Adam J.

AU - Freire, Ernesto

AU - Hayashi, Yoshio

AU - Kiso, Yoshiaki

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