Compound class:
Nucleic acid
Comment: Apta-1 is a 90-mer RNA aptamer that is designed to bind to a conserved region of the Plasmodium falciparum erythrocyte membrane protein 1 (PfEMP1) as a mechanism to disrupt infectivity [1]. It contains 2'-OH RNA purine nucleotides and 2'-fluoro pyrimidine nucleotides (marked as 'f' in the sequence provided here). Apta-1 is also reported to bind to the heparin-binding exosite II of thrombin, which drives significant inhibition of protease-activated receptor (PAR) signalling in platelets and antithrombotic sequelae.
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Guide to Malaria Pharmacology Comments |
In P. falciparum infection models Apta-1 disrupts rosette formation on non-infected host erythrocytes. |