Identification of peptidomimetic HTLV-I protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic

Hikoichiro Maegawa; Tooru Kimura; Yasuhiro Arii; Yasuko Matsui; Soko Kasai; Yoshio Hayashi; Yoshiaki Kiso

doi:10.1016/j.bmcl.2004.09.034

Identification of peptidomimetic HTLV-I protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic

Bioorg Med Chem Lett. 2004 Dec 6;14(23):5925-9. doi: 10.1016/j.bmcl.2004.09.034.

Authors

Hikoichiro Maegawa¹, Tooru Kimura, Yasuhiro Arii, Yasuko Matsui, Soko Kasai, Yoshio Hayashi, Yoshiaki Kiso

Affiliation

¹ Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan.

PMID: 15501070
DOI: 10.1016/j.bmcl.2004.09.034

Abstract

Towards the development of chemotherapy for the infection by human T-cell leukemia virus type I (HTLV-I), we have established evaluation systems for HTLV-I protease (PR) inhibitors using both recombinant and chemically synthesized HTLV-I PRs. Newly synthesized substrate-based inhibitors containing hydroxymethylcarbonyl (HMC) isostere showed potent anti-HTLV-I PR activity.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Amino Acid Sequence
Aspartic Acid Endopeptidases / antagonists & inhibitors*
Aspartic Acid Endopeptidases / genetics
Aspartic Acid Endopeptidases / metabolism
Humans
Molecular Sequence Data
Protease Inhibitors / chemistry*
Protease Inhibitors / pharmacology

Substances

Protease Inhibitors
Aspartic Acid Endopeptidases
HTLV-1 protease