Linked Life Data

17145800

Source:http://linkedlifedata.com/resource/pubmed/id/17145800

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2007-1-22
pubmed:abstractText
RBX11160 (OZ277) is a fully synthetic peroxidic antimalarial in clinical development. To study the possible mechanisms of action of RBX11160, we have examined its ability to inhibit PfATP6, a sarcoplasmic reticulum calcium ATPase and proposed target for semisynthetic peroxidic artemisinin derivatives. RBX11160 inhibits PfATP6 (apparent half-maximal inhibitory constant=7,700 nM) less potently than artemisinin (79 nM). Inhibition of PfATP6 is abrogated by desferrioxamine, an iron-chelating agent. Consistent with this finding, the killing of Plasmodium falciparum organisms by RBX11160 in vitro is antagonized by desferrioxamine. Artesunate and RBX11160 also act antagonistically against P. falciparum in vitro. A fluorescent derivative of RBX11160 localizes to the parasite cytosol in some parasites and to the food vacuole in other parasites. These data demonstrate that there are both similarities and differences between the antimalarial properties of RBX11160 and those of semisynthetic antimalarials such as artesunate and artemisinin.
pubmed:commentsCorrections
http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-10066789, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-11145964, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-12931192, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-15262108, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-15318224, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-15555542, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-15701735, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-16569877, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-16612385, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-16616639, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-16699808, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-16719805, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-16735432, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-6380017, http://linkedlifedata.com/resource/pubmed/commentcorrection/17145800-8467901
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0066-4804
pubmed:author
pubmed:issnType
Print
pubmed:volume
51
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
667-72
pubmed:dateRevised
2011-11-17
pubmed:meshHeading
pubmed:year
2007
pubmed:articleTitle
Mechanism of antimalarial action of the synthetic trioxolane RBX11160 (OZ277).
pubmed:affiliation
Division of Cellular and Molecular Medicine, Centre for Infection, St. George's University of London, and Dept. of Infectious Diseases, St. George's Hospital Medical School, Cranmer Terrace, London SW17 ORE, United Kingdom.
pubmed:publicationType
Journal Article, Comparative Study