About: Direct High‐Throughput Screening Assay for mRNA Cap Guanine‐N7 Methyltransferase Activity

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An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Direct High‐Throughput Screening Assay for mRNA Cap Guanine‐N7 Methyltransferase Activity
Creator	Cowling, V Kowalska, Cowling, Victoria Fido, M Fido, Mateusz Jemielity, J Jemielity, Jacek Kasprzyk, Renata Kasprzyk, ] Kopcial, M Kopcial, Michal Kowalska, Joanna Mamot, Adam Mamot, P Smietanski, M Smietanski, Miroslaw Wanat, J Wanat, Przemyslaw
Source	Medline; PMC
abstract	In eukaryotes, mature mRNA is formed through modifications of precursor mRNA, one of which is 5′ cap biosynthesis, involving RNA cap guanine‐N7 methyltransferase (N7‐MTase). N7‐MTases are also encoded by some eukaryotic viruses and facilitate their replication. N7‐MTase inhibitors have therapeutic potential, but their discovery is difficult because long RNA substrates are usually required for activity. Herein, we report a universal N7‐MTase activity assay based on small‐molecule fluorescent probes. We synthesized 12 fluorescent substrate analogs (GpppA and GpppG derivatives) varying in the dye type, dye attachment site, and linker length. GpppA labeled with pyrene at the 3′‐O position of adenosine acted as an artificial substrate with properties of a turn‐off probe for all three tested N7‐MTases (human, parasite, and viral). Using this compound, a high‐throughput N7‐MTase inhibitor assay was developed and used for screening of synthetic substrate analogs and a commercial library. Several inhibitors with nanomolar activities were identified.
has issue date	2020-04-07(xsd:dateTime)
bibo:doi	10.1002/chem.202001036
bibo:pmid	32259329
has license	no-cc
sha1sum (hex)	7f23a480b87f2ac99933ab7cc2328f4b54b0b065
schema:url	https://doi.org/10.1002/chem.202001036
resource representing a document's title	Direct High‐Throughput Screening Assay for mRNA Cap Guanine‐N7 Methyltransferase Activity
has PubMed Central identifier	PMC7262028
has PubMed identifier	32259329
schema:publication	Chemistry
resource representing a document's body	covid:7f23a480b87f2ac99933ab7cc2328f4b54b0b065#body_text
is schema:about of	named entity 'pyrene' named entity 'attachment' named entity 'substrate' named entity 'cap' named entity 'dye' named entity 'Assay' named entity 'Title' named entity 'USED' named entity 'ANALOGS' named entity 'ENCODED' named entity 'ACTIVITY' named entity 'PRECURSOR MRNA' named entity 'VARYING' named entity 'SMALL' named entity 'INHIBITORS' named entity 'fluorescent probes' named entity 'synthesized' named entity 'acted' named entity 'length' named entity 'artificial' named entity 'viral' named entity 'identified' named entity 'inhibitor' named entity 'RNA' named entity 'Cap' named entity 'parasite' named entity 'assay' named entity 'substrate' named entity 'substrates' named entity 'pyrene' named entity 'high-throughput screening' named entity 'RNA' named entity 'High-Throughput Screening' named entity 'mRNA' named entity 'Guanine' named entity 'IC50' named entity 'Suramin' named entity 'SAM' named entity 'post-transcriptionally' named entity 'GMP' named entity 'Encephalitozoon cuniculi' named entity 'GTP' named entity 'Ecm1' named entity 'fluorescence' named entity 'Hill equation' named entity 'RNA' named entity 'radioactivity' named entity 'NS14' named entity 'viral infections' named entity 'suramin' named entity 'kinetics' named entity 'SAM' named entity '10 nM' named entity 'histone' named entity 'RNMT' named entity 'GMP' named entity '5' cap' named entity 'fluorescent labeling' named entity 'biosynthesis' named entity 'myricetin' named entity 'enzyme' named entity 'substrate' named entity 'fluorescent dyes' named entity 'methyl'

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