Joseph F Cortese
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Explore the profile of Joseph F Cortese including associated specialties, affiliations and a list of published articles.
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1192
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Recent Articles
1.
Herman J, Pepper L, Cortese J, Estiu G, Galinsky K, Zuzarte-Luis V, et al.
Sci Transl Med
. 2015 May;
7(288):288ra77.
PMID: 25995223
The emergence of drug resistance is a major limitation of current antimalarials. The discovery of new druggable targets and pathways including those that are critical for multiple life cycle stages...
2.
Skerlj R, Bastos C, Booker M, Kramer M, Barker Jr R, Celatka C, et al.
ACS Med Chem Lett
. 2014 Jun;
2(9):708-13.
PMID: 24900364
Inhibition of dihydroorotate dehydrogenase (DHODH) for P. falciparum potentially represents a new treatment option for malaria, since DHODH catalyzes the rate-limiting step in the pyrimidine biosynthetic pathway and P. falciparum...
3.
Keller T, Zocco D, Sundrud M, Hendrick M, Edenius M, Yum J, et al.
Nat Chem Biol
. 2012 Feb;
8(3):311-7.
PMID: 22327401
Febrifugine, the bioactive constituent of one of the 50 fundamental herbs of traditional Chinese medicine, has been characterized for its therapeutic activity, though its molecular target has remained unknown. Febrifugine...
4.
Dong C, Urgaonkar S, Cortese J, Gamo F, Garcia-Bustos J, LaFuente M, et al.
Chem Biol
. 2011 Dec;
18(12):1602-10.
PMID: 22195562
Here we report the discovery of tetracyclic benzothiazepines (BTZs) as highly potent and selective antimalarials along with the identification of the Plasmodium falciparum cytochrome bc(1) complex as the primary functional...
5.
Van Tyne D, Park D, Schaffner S, Neafsey D, Angelino E, Cortese J, et al.
PLoS Genet
. 2011 May;
7(4):e1001383.
PMID: 21533027
The Plasmodium falciparum parasite's ability to adapt to environmental pressures, such as the human immune system and antimalarial drugs, makes malaria an enduring burden to public health. Understanding the genetic...
6.
Barker Jr R, Urgaonkar S, Mazitschek R, Celatka C, Skerlj R, Cortese J, et al.
Antimicrob Agents Chemother
. 2011 Mar;
55(6):2612-22.
PMID: 21422215
This study characterizes aminoindole molecules that are analogs of Genz-644442. Genz-644442 was identified as a hit in a screen of ~70,000 compounds in the Broad Institute's small-molecule library and the...
7.
Urgaonkar S, Cortese J, Barker R, Cromwell M, Serrano A, Wirth D, et al.
Org Lett
. 2010 Aug;
12(18):3998-4001.
PMID: 20718474
The development of a concise strategy to access 2-amino-3-hydroxy-indoles, which are disclosed as novel antimalarials with potent in vivo activity, is reported. Starting from isatins the target compounds are synthesized...
8.
Booker M, Bastos C, Kramer M, Barker Jr R, Skerlj R, Sidhu A, et al.
J Biol Chem
. 2010 Aug;
285(43):33054-33064.
PMID: 20702404
Plasmodium falciparum, the causative agent of the most deadly form of human malaria, is unable to salvage pyrimidines and must rely on de novo biosynthesis for survival. Dihydroorotate dehydrogenase (DHODH)...
9.
Martyn D, Cortese J, Tyndall E, Dick J, Mazitschek R, Munoz B, et al.
Bioorg Med Chem Lett
. 2009 Nov;
20(1):218-21.
PMID: 19914069
A high-throughput screening program identified two piperazine sulfonamides with activity against Plasmodium falciparum. Both screening positives had three structural features with potential liabilities: furanyl, thiourea and nitrophenyl groups. The furan...
10.
Martyn D, Nijjar A, Celatka C, Mazitschek R, Cortese J, Tyndall E, et al.
Bioorg Med Chem Lett
. 2009 Nov;
20(1):228-31.
PMID: 19914064
Two sets of diaminopyrimidines, totalling 45 compounds, were synthesized and assayed against Plasmodium falciparum. The SAR was relatively shallow, with only the presence of a 2-(pyrrolidin-1-yl)ethyl group at R(2) significantly...