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Clemastine Fumarate in Plasmodium

ABSTRACT: The binding target for clemastine fumarate in Plasmodium Falciparum 3D7 strain is identified by two techniques: SPROX and TPP.

INSTRUMENT(S): Orbitrap Fusion Lumos

ORGANISM(S): Homo Sapiens (human) Plasmodium Falciparum (isolate 3d7)

TISSUE(S): Liver

SUBMITTER: Baiyi Quan

LAB HEAD: Michael C. Fitzgerald

PROVIDER: PXD014308 | Pride | 2020-02-21

REPOSITORIES: Pride

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Plasmodium chaperonin TRiC/CCT identified as a target of the antihistamine clemastine using parallel chemoproteomic strategy.

Lu Kuan-Yi KY Quan Baiyi B Sylvester Kayla K Srivastava Tamanna T Fitzgerald Michael C MC Derbyshire Emily R ER

Proceedings of the National Academy of Sciences of the United States of America 20200303 11

The antihistamine clemastine inhibits multiple stages of the Plasmodium parasite that causes malaria, but the molecular targets responsible for its parasite inhibition were unknown. Here, we applied parallel chemoproteomic platforms to discover the mechanism of action of clemastine and identify that clemastine binds to the Plasmodium falciparum TCP-1 ring complex or chaperonin containing TCP-1 (TRiC/CCT), an essential heterooligomeric complex required for de novo cytoskeletal prote ...[more]

PMID: 32127489

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