<> "The repository administrator has not yet configured an RDF license."^^ . <> . . . "Post-translational import of protein into the endoplasmic reticulum of a trypanosome: An in vitro system for discovery of anti-trypanosomal chemical entities"^^ . "HAT (human African trypanosomiasis), caused by the protozoan parasite Trypanosoma brucei, is an emerging disease for which new drugs are needed. Expression of plasma membrane proteins [e.g. VSG (variant surface glycoprotein)] is crucial for the establishment and maintenance of an infection by T. brucei. Transport of a majority of proteins to the plasma membrane involves their translocation into the ER (endoplasmic reticulum). Thus inhibition of protein import into the ER of T. brucei would be a logical target for discovery of lead compounds against trypanosomes. We have developed a TbRM (T. brucei microsome) system that imports VSG_117 post-translationally. Using this system, MAL3-101, equisetin and CJ-21,058 were discovered to be small molecule inhibitors of VSG_117 translocation into the ER. These agents also killed bloodstream T. brucei in vitro; the concentrations at which 50% of parasites were killed (IC50) were 1.5 μM (MAL3-101), 3.3 μM (equisetin) and 7 μM (CJ-21,058). Thus VSG_117 import into TbRMs is a rapid and novel assay to identify 'new chemical entities' (e.g. MAL3-101, equisetin and CJ-21,058) for anti-trypanosome drug development. © The Authors Journal compilation."^^ . "2009-04-15" . . "419" . "2" . . "Biochemical Journal"^^ . . . "02646021" . . . . . . . . . . . . . . . . . . . . . . . . . . . . "RC"^^ . "Davis"^^ . "RC Davis"^^ . . "J"^^ . "Duffy"^^ . "J Duffy"^^ . . "B"^^ . "Patham"^^ . "B Patham"^^ . . "JL"^^ . "Brodsky"^^ . "JL Brodsky"^^ . . "SW"^^ . "Fewell"^^ . "SW Fewell"^^ . . "P"^^ . "Wipf"^^ . "P Wipf"^^ . . "A"^^ . "Lane"^^ . "A Lane"^^ . . "K"^^ . "Mensa-Wilmot"^^ . "K Mensa-Wilmot"^^ . . . . . . "Post-translational import of protein into the endoplasmic reticulum of a trypanosome: An in vitro system for discovery of anti-trypanosomal chemical entities (Plain Text)"^^ . . . "licence.txt"^^ . . . "Post-translational import of protein into the endoplasmic reticulum of a trypanosome: An in vitro system for discovery of anti-trypanosomal chemical entities (Other)"^^ . . . . . . "indexcodes.txt"^^ . . "HTML Summary of #18942 \n\nPost-translational import of protein into the endoplasmic reticulum of a trypanosome: An in vitro system for discovery of anti-trypanosomal chemical entities\n\n" . "text/html" . .