Unknown

Dataset Information

0

Identification of potent and selective non-covalent inhibitors of the Plasmodium falciparum proteasome.

ABSTRACT: We have identified short N,C-capped peptides that selectively inhibit the proteasome of the malaria-causing pathogen Plasmodium falciparum. These compounds are highly potent in culture with no toxicity in host cells. One cyclic biphenyl ether compound inhibited intraerythrocytic growth of P. falciparum with an IC50 of 35 nM, and we show that even a pulse treatment with this cyclic peptide induced parasite death due to proteasome inhibition. These compounds represent promising new antimalarial agents that target the essential proteasomal machinery of the parasite without toxicity toward the host.

SUBMITTER: Li H 

PROVIDER: S-EPMC4183598 | biostudies-literature | 2014 Oct

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

Identification of potent and selective non-covalent inhibitors of the Plasmodium falciparum proteasome.

Li Hao H   Tsu Christopher C   Blackburn Christopher C   Li Gang G   Hales Paul P   Dick Lawrence L   Bogyo Matthew M  

Journal of the American Chemical Society 20140919 39

We have identified short N,C-capped peptides that selectively inhibit the proteasome of the malaria-causing pathogen Plasmodium falciparum. These compounds are highly potent in culture with no toxicity in host cells. One cyclic biphenyl ether compound inhibited intraerythrocytic growth of P. falciparum with an IC50 of 35 nM, and we show that even a pulse treatment with this cyclic peptide induced parasite death due to proteasome inhibition. These compounds represent promising new antimalarial ag  ...[more]

Similar Datasets

Genomics Development of potent and selective KDM5 covalent inhibitors
2018-12-10 | GSE118589 | GEO
Unknown Covalent Plasmodium falciparum-selective proteasome inhibitors exhibit a low propensity for generating resistance in vitro and synergize with multiple antimalarial agents.
| S-EPMC6553790 | biostudies-literature
Unknown Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome.
| S-EPMC6257627 | biostudies-literature
Unknown Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG).
| S-EPMC6193536 | biostudies-literature
Unknown Substituted imidazopyridazines are potent and selective inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1).
| S-EPMC3898741 | biostudies-other
Unknown Discovery of potent and selective covalent inhibitors of JNK.
| S-EPMC3270411 | biostudies-literature
Unknown Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum.
| S-EPMC2624570 | biostudies-literature
Genomics Development of potent and selective KDM5 covalent inhibitors
| PRJNA486160 | ENA
Unknown Identification of a potent and selective covalent Pin1 inhibitor.
| S-EPMC7442691 | biostudies-literature
Unknown Structure- and function-based design of Plasmodium-selective proteasome inhibitors.
| S-EPMC4755332 | biostudies-literature