期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 17, 页码 5629-5646出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.02.016
关键词
Phosphoribosyltransferase; Malaria; HGXPRTase; Purine salvage; Protozoa
资金
- NIAID NIH HHS [R01 AI049512] Funding Source: Medline
The pathogenic protozoa responsible for malaria lack enzymes for the de novo synthesis of purines and rely on purine salvage from the host. In Plasmodium falciparum (Pf), hypoxanthine-guanine-xanthine phosphoribosyltransferase (HGXPRT) converts hypoxanthine to inosine monophosphate and is essential for purine salvage making the enzyme an anti-malarial drug target. We have synthesized a number of simple acyclic aza-C-nucleosides and shown that some are potent inhibitors of Pf HGXPRT while showing excellent selectivity for the Pf versus the human enzyme. (C) 2013 Elsevier Ltd. All rights reserved.
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