PMID- 15501070 OWN - NLM STAT- MEDLINE DCOM- 20050322 LR - 20091119 IS - 0960-894X (Print) IS - 0960-894X (Linking) VI - 14 IP - 23 DP - 2004 Dec 6 TI - Identification of peptidomimetic HTLV-I protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic. PG - 5925-9 AB - 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. FAU - Maegawa, Hikoichiro AU - Maegawa H AD - Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan. FAU - Kimura, Tooru AU - Kimura T FAU - Arii, Yasuhiro AU - Arii Y FAU - Matsui, Yasuko AU - Matsui Y FAU - Kasai, Soko AU - Kasai S FAU - Hayashi, Yoshio AU - Hayashi Y FAU - Kiso, Yoshiaki AU - Kiso Y LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - England TA - Bioorg Med Chem Lett JT - Bioorganic & medicinal chemistry letters JID - 9107377 RN - 0 (Protease Inhibitors) RN - EC 3.4.23.- (Aspartic Acid Endopeptidases) RN - EC 3.4.23.- (HTLV-1 protease) SB - IM MH - Amino Acid Sequence MH - Aspartic Acid Endopeptidases/*antagonists & inhibitors/genetics/metabolism MH - Humans MH - Molecular Sequence Data MH - Protease Inhibitors/*chemistry/pharmacology EDAT- 2004/10/27 09:00 MHDA- 2005/03/23 09:00 CRDT- 2004/10/27 09:00 PHST- 2004/08/03 00:00 [received] PHST- 2004/09/03 00:00 [accepted] PHST- 2004/10/27 09:00 [pubmed] PHST- 2005/03/23 09:00 [medline] PHST- 2004/10/27 09:00 [entrez] AID - S0960-894X(04)01146-1 [pii] AID - 10.1016/j.bmcl.2004.09.034 [doi] PST - ppublish SO - Bioorg Med Chem Lett. 2004 Dec 6;14(23):5925-9. doi: 10.1016/j.bmcl.2004.09.034.