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CoV 2'-O-methyltransferase

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Target not currently curated in GtoImmuPdb

Target id: 3277

Nomenclature: CoV 2'-O-methyltransferase

Family: Coronavirus (CoV) proteins

Contents:

Quaternary Structure: Subunits
CoV Non-structural protein 10
CoV Non-structural protein 16
Quaternary Structure Comments
The coronavirus nsp10 and nsp16 proteins form an enzymatically active heterodimer with 2'-O-methyltransferase activity.
Previous and Unofficial Names Click here for help
RNA 2′-O-MTase
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  High-resolution structures of the SARS-CoV-2 2'- O -methyltransferase reveal strategies for structure-based inhibitor design.
PDB Id:  6W4H
Resolution:  1.8Å
Species:  SARS-CoV-2
References:  4

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
sinefungin Small molecule or natural product Ligand has a PDB structure SARS-CoV-2 Inhibition 5.5 pIC50 3
⤷ pIC50 5.5 (IC50 3.4x10-6 M) [3]
nsp16 inhibitor 5a Small molecule or natural product Ligand has a PDB structure SARS-CoV-2 Inhibition 5.1 pIC50 2
⤷ pIC50 5.1 (IC50 9x10-6 M) [2]
RS-1 Small molecule or natural product SARS-CoV-2 Inhibition 4.9 pIC50 1
⤷ pIC50 4.9 (IC50 1.33x10-5 M) [1]
Description: Inhibition potency for purified SARS-CoV-2 2′-O-MTase
RS-2 Small molecule or natural product SARS-CoV-2 Inhibition 4.9 pIC50 1
⤷ pIC50 4.9 (IC50 1.36x10-5 M) [1]
Description: Inhibition potency for purified SARS-CoV-2 2′-O-MTase

References

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1. Hanna GS, Benjamin MM, Choo YM, De R, Schinazi RF, Nielson SE, Hevel JM, Hamann MT. (2024) Informatics and Computational Approaches for the Discovery and Optimization of Natural Product-Inspired Inhibitors of the SARS-CoV-2 2'-O-Methyltransferase. J Nat Prod, 87 (2): 217-227. [PMID:38242544]

2. Inniss NL, Kozic J, Li F, Rosas-Lemus M, Minasov G, Rybáček J, Zhu Y, Pohl R, Shuvalova L, Rulíšek L et al.. (2023) Discovery of a Druggable, Cryptic Pocket in SARS-CoV-2 nsp16 Using Allosteric Inhibitors. ACS Infect Dis, 9 (10): 1918-1931. [PMID:37728236]

3. Khalili Yazdi A, Li F, Devkota K, Perveen S, Ghiabi P, Hajian T, Bolotokova A, Vedadi M. (2021) A High-Throughput Radioactivity-Based Assay for Screening SARS-CoV-2 nsp10-nsp16 Complex. SLAS Discov, 26 (6): 757-765. [PMID:33874769]

4. Rosas-Lemus M, Minasov G, Shuvalova L, Inniss NL, Kiryukhina O, Brunzelle J, Satchell KJF. (2020) High-resolution structures of the SARS-CoV-2 2'-O-methyltransferase reveal strategies for structure-based inhibitor design. Sci Signal, 13 (651). [PMID:32994211]

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