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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References |
1. Barfod A, Persson T, Lindh J. (2009)
In vitro selection of RNA aptamers against a conserved region of the Plasmodium falciparum erythrocyte membrane protein 1. Parasitol Res, 105 (6): 1557-66. [PMID:19693540] |
2. Jedlina L, Olin O, Bylock A, Casslén V, Eriksson M, Brewinska-Olchowik M, Piwocka K, Lindstam M. (2020)
A novel protein-binding RNA aptamer, Apta-1—A new therapeutic tool to combat sepsis. Crit Care, 24: 506. |
3. Jedlina L, Olin O, Bylock A, Lindstam M. (2020)
Promising Therapeutic Effects of a Novel RNA Aptamer, Apta-1, in a Severe Systemic Inflammation Model on Non-human Primates. Res Pract Thromb Haemost, 4. |
4. Wang Y, Lindstam M, Hwang D, Jedlina L, Liu M. (2024)
Therapeutic Effects of a Novel Aptamer on Coronaviral Infection-Induced Lung Injury and Systemic Inflammatory Responses. Cells, 13 (5). [PMID:38474386] |