Repository logo
 
Publication

Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entity

2010Journal article Restricted access
Simple item page
dc.contributor.authorGibbons, Peter D.
dc.contributor.authorVerissimo, Edite
dc.contributor.authorAraujo, Nuna C. P.
dc.contributor.authorBarton, Victoria
dc.contributor.authorNixon, Gemma L.
dc.contributor.authorAmewu, Richard K.
dc.contributor.authorChadwick, J.
dc.contributor.authorStocks, Paul A.
dc.contributor.authorBiagini, Giancarlo A.
dc.contributor.authorSrivastava, Abhishek
dc.contributor.authorRosenthal, Philip J.
dc.contributor.authorGut, Jiri
dc.contributor.authorGuedes, Rita C.
dc.contributor.authorMoreira, Rui
dc.contributor.authorSharma, Raman
dc.contributor.authorBerry, Neil
dc.contributor.authorCristiano, Maria Lurdes Santos
dc.contributor.authorShone, Alison E.
dc.contributor.authorWard, Stephen A.
dc.contributor.authorO'Neill, Paul M.
dc.date.accessioned2014-06-06T14:07:11Z
dc.date.available2014-06-06T14:07:11Z
dc.date.issued2010
dc.date.updated2014-06-05T11:25:48Z
dc.description.abstractWe extend our approach of combination chemotherapy through a single prodrug entity (O’Neill et al. Angew. Chem., Int. Ed. 2004, 43, 4193) by using a 1,2,4-trioxolane as a protease inhibitor carbonylmasking group. These molecules are designed to target the malaria parasite through two independent mechanisms of action: iron(II) decomposition releases the carbonyl protease inhibitor and potentially cytotoxic C-radical species in tandem. Using a proposed target “heme”, we also demonstrate heme alkylation/carbonyl inhibitor release and quantitatively measure endoperoxide turnover in parasitized red blood cells.por
dc.identifier.citationGibbons, Peter; Verissimo, Edite; Araujo, Nuna C.; Barton, Victoria; Nixon, Gemma L.; Amewu, Richard K.; Chadwick, James; Stocks, Paul A.; Biagini, Giancarlo A.; Srivastava, Abhishek; Rosenthal, Philip J.; Gut, Jiri; Guedes, Rita C.; Moreira, Rui; Sharma, Raman; Berry, Neil; Cristiano, M. Lurdes S.; Shone, Alison E.; Ward, Stephen A.; O’Neill, Paul M. Endoperoxide Carbonyl Falcipain 2/3 Inhibitor Hybrids: Toward Combination Chemotherapy of Malaria through a Single Chemical Entity, Journal of Medicinal Chemistry, 53, 22, 8202-8206, 2010.por
dc.identifier.doihttp://dx.doi.org/10.1021/jm1009567
dc.identifier.issn0022-2623
dc.identifier.otherAUT: MCR00716;
dc.identifier.urihttp://hdl.handle.net/10400.1/4219
dc.language.isoengpor
dc.peerreviewedyespor
dc.publisherAmerican Chemical Societypor
dc.relation.publisherversionhttp://pubs.acs.org/jmcpor
dc.titleEndoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entitypor
dc.typejournal article
dspace.entity.typePublication
oaire.citation.endPage8206por
oaire.citation.issue22por
oaire.citation.startPage8202por
oaire.citation.titleJournal of Medicinal Chemistrypor
oaire.citation.volume53por
person.familyNameVerissimo
person.familyNameAraujo
person.familyNameCristiano
person.givenNameEdite
person.givenNameNuna
person.givenNameMaria de Lurdes
person.identifier.ciencia-idE411-6006-5A01
person.identifier.orcid0000-0003-0352-5446
person.identifier.orcid0000-0002-7602-0150
person.identifier.orcid0000-0002-9447-2855
person.identifier.ridN-8531-2013
person.identifier.ridG-2345-2012
person.identifier.scopus-author-id9238724800
rcaap.rightsrestrictedAccesspor
rcaap.typearticlepor
relation.isAuthorOfPublication2f678005-d8fb-4cf4-8cd0-0d15f464b9c1
relation.isAuthorOfPublication3423e71b-934d-4da7-9c81-4e56c7930252
relation.isAuthorOfPublicationb16751a6-748e-44b0-9c59-058cbd5b2cc3
relation.isAuthorOfPublication.latestForDiscoveryb16751a6-748e-44b0-9c59-058cbd5b2cc3

Files

Original bundle
Now showing 1 - 1 of 1
No Thumbnail Available
Name:
Endoperoxide Carbonyl Falcipain.pdf
Size:
2.91 MB
Format:
Adobe Portable Document Format
Download
License bundle
Now showing 1 - 1 of 1
No Thumbnail Available
Name:
license.txt
Size:
1.61 KB
Format:
Item-specific license agreed upon to submission
Description:
Download

Collections

CCM2-Artigos (em revistas ou actas indexadas)