| Literature DB >> 20688188 |
Kosuke Nakamura1, Sunao Fujioka, Shinya Fukumoto, Noboru Inoue, Kimitoshi Sakamoto, Haruyuki Hirata, Yasutoshi Kido, Yoshisada Yabu, Takashi Suzuki, Yoh-ichi Watanabe, Hiroyuki Saimoto, Hiroshi Akiyama, Kiyoshi Kita.
Abstract
Trypanosoma brucei rhodesiense and T. b. gambiense are known causes of human African trypanosomiasis (HAT), or "sleeping sickness," which is deadly if untreated. We previously reported that a specific inhibitor of trypanosome alternative oxidase (TAO), ascofuranone, quickly kills African trypanosomes in vitro and cures mice infected with another subspecies, non-human infective T. b. brucei, in in vivo trials. As an essential factor for trypanosome survival, TAO is a promising drug target due to the absence of alternative oxidases in the mammalian host. This study found TAO expression in HAT-causing trypanosomes; its amino acid sequence was identical to that in non-human infective T. b. brucei. The biochemical understanding of the TAO including its 3 dimensional structure and inhibitory compounds against TAO could therefore be applied to all three T. brucei subspecies in search of a cure for HAT. Our in vitro study using T. b. rhodesiense confirmed the effectiveness of ascofuranone (IC(50) value: 1 nM) to eliminate trypanosomes in human infective strain cultures.Entities:
Mesh:
Substances:
Year: 2010 PMID: 20688188 DOI: 10.1016/j.parint.2010.07.006
Source DB: PubMed Journal: Parasitol Int ISSN: 1383-5769 Impact factor: 2.230