Abstract
The protozoans Cryptosporidium parvum and Toxoplasma gondii are parasites of major health concern to humans. Both parasites contain a group of calcium-dependent protein kinases (CDPKs) which are found in plants and ciliates but not in humans or fungi. Here, we describe a series of potent inhibitors that target CDPK1 in C. parvum (CpCDPK1) and T. gondii (TgCDPK1). These inhibitors are highly selective for CpCDPK1 and TgCDPK1 over the mammalian kinases SRC and ABL. Furthermore, they are able to block an early stage of C. parvum invasion of HCT-8 host cells, which is similar to their effects on T. gondii invasion of human fibroblasts.
Original language | English (US) |
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Pages (from-to) | 331-335 |
Number of pages | 5 |
Journal | ACS Medicinal Chemistry Letters |
Volume | 1 |
Issue number | 7 |
DOIs | |
State | Published - Oct 14 2010 |
Keywords
- Cryptosporidium parvum
- Phosphorylation
- Toxoplasma gondii
- apicomplexan
- calcium-dependent protein kinases
- protozoans
ASJC Scopus subject areas
- Biochemistry
- Drug Discovery
- Organic Chemistry