BibTex format
@article{Wilson:2015:10.1186/s12915-015-0162-0,
author = {Wilson, DW and Goodman, CD and Sleebs, BE and Weiss, GE and de, Jong NWM and Angrisano, F and Langer, C and Baum, J and Crabb, BS and Gilson, PR and McFadden, GI and Beeson, JG},
doi = {10.1186/s12915-015-0162-0},
journal = {BMC Biology},
title = {Macrolides rapidly inhibit red blood cell invasion by the human malaria parasite, Plasmodium falciparum},
url = {http://dx.doi.org/10.1186/s12915-015-0162-0},
volume = {13},
year = {2015}
}
RIS format (EndNote, RefMan)
TY - JOUR
AB - Background: Malaria invasion of red blood cells involves multiple parasite-specific targets that are easily accessibleto inhibitory compounds, making it an attractive target for antimalarial development. However, no current antimalarialagents act against host cell invasion.Results: Here, we demonstrate that the clinically used macrolide antibiotic azithromycin, which is known to kill humanmalaria asexual blood-stage parasites by blocking protein synthesis in their apicoplast, is also a rapid inhibitor of redblood cell invasion in human (Plasmodium falciparum) and rodent (P. berghei) malarias. Multiple lines of evidencedemonstrate that the action of azithromycin in inhibiting parasite invasion of red blood cells is independent ofits inhibition of protein synthesis in the parasite apicoplast, opening up a new strategy to develop a single drugwith multiple parasite targets. We identified derivatives of azithromycin and erythromycin that are better invasioninhibitors than parent compounds, offering promise for development of this novel antimalarial strategy.Conclusions: Safe and effective macrolide antibiotics with dual modalities could be developed to combat malariaand reduce the parasite’s options for resistance.
AU - Wilson,DW
AU - Goodman,CD
AU - Sleebs,BE
AU - Weiss,GE
AU - de,Jong NWM
AU - Angrisano,F
AU - Langer,C
AU - Baum,J
AU - Crabb,BS
AU - Gilson,PR
AU - McFadden,GI
AU - Beeson,JG
DO - 10.1186/s12915-015-0162-0
PY - 2015///
SN - 1741-7007
TI - Macrolides rapidly inhibit red blood cell invasion by the human malaria parasite, Plasmodium falciparum
T2 - BMC Biology
UR - http://dx.doi.org/10.1186/s12915-015-0162-0
UR - http://hdl.handle.net/10044/1/25642
VL - 13
ER -
