Suramin
A polyanionic antiparasitic drug.
General information
Suramin is a broad-spectrum antiviral. It has also been used for African sleeping sickness and river blindness treatment. It has multiple mechanisms of action. Suramin was observed to bind SARS-CoV-2 RNA-dependent RNA polymerase on two sites and to inhibit the enzyme 20-fold more potently than remdesivir. The compound blocks RNA template strand binding and it also interacts with RNA primer stand adjacent to the active site. Suramin also inhibited viral replication in cell culture. Negative charge possibly limits its cell entry, however (Yin et al., 2021).
Suramin on DrugBank
Suramin on PubChem
Suramin on Wikipedia
Marketed as
309 FOURNEAU; ANTRYPOL; BAYER 205; BELGANYL; GERMANIN; MORANYL; NAGANIN; NAGANINE; NAGANOL; NAPHURIDE
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Supporting references
| Link | Tested on | Impact factor | Notes | Publication date |
|---|---|---|---|---|
|
Suramin Inhibits SARS-CoV-2 Infection in Cell Culture by Interfering with Early Steps of the Replication Cycle
|
Calu-3 human airway epithelial cells | 4.90 | Jul/22/2020 | |
|
Structural basis for inhibition of the SARS-CoV-2 RNA polymerase by suramin
RdRpol Cryo-EM Small molecule Enzyme assay In vitro Mechanism |
in vitro binding assay; in vitro enzyme assay; cryo-EM; Vero E6 cells; SARS-CoV-2 strain nCoV-2019BetaCoV/Wuhan/WIV04/2019 | 11.98 | Observed to bind SARS-CoV-2 RNA-dependent RNA polymerase on two sites and to inhibit the enzyme with an IC50 of ca. 0.26 μM, which means it is 20-fold more potent than remdesivir. The compound blocks RNA template strand binding and it also interacts with RNA primer stand adjacent to the active site. Suramin inhibited viral replication in Vero E6 cells with an EC50 of ca. 2.93 μM and an SI of >341. Some of the compound’s derivatives displayed even lower IC50 values in enzyme inhibition assays but these parameters did not translate into improved efficacy in cell culture, possibly due to poor cellular uptake of the compounds. |
Mar/05/2021 |
