AIM: To screen antifungal drug candidates using in vitro and in vivo assays based on type I methionine aminopep- tidase from Saccharomyces cerevisiae (ScMetAP1). METHODS: A colorimetric assay suitable for high throughput screening (HTS) using recombinant ScMetAP1 protein expressed in Escherichia coli was established for antifungal lead discovery. A series of pyridine-2-carboxylic acid derivatives were characterized and a chemical library of 12 800 pure organic compounds was screened with the in vitro Sc...
【基金】
Project supported by the National Natural Science Foundation of China; No 30271528 and 39725032 and by the NIH COBRE award 1 P20 RR15563 and matching support from the State of Kansas.
【更新日期】
2005-08-19
【分类号】
R965.1
【正文快照】
INTRODUCTION Methionine aminopeptidase (MetAP), existing inboth prokaryotic and eukaryotic cells, plays an impor-tant role in removing the first methionine from nascentpolypeptides[1,2]. Up to now, two major isoforms ofMetAP (type I and type II MetA
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