About: 19F‐NMR‐based fragment screening for 14 different biologically active RNAs and 10 DNA and protein counter‐screens

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About: 19F‐NMR‐based fragment screening for 14 different biologically active RNAs and 10 DNA and protein counter‐screens Goto Sponge NotDistinct Permalink

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

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type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	19F‐NMR‐based fragment screening for 14 different biologically active RNAs and 10 DNA and protein counter‐screens
Creator	Schwalbe, Harald Alexandra, Maria Alexandra, Wirtz Azzaoui, Kamal Azzaoui, Marcel Bains, Jasleen Bains, Kaur Berg, Hannes Biedenbänder, Thomas Binas, Oliver Blommers, Christian Blommers, José De Jesus, Vanessa Fürtig, Boris Gande, Anna Gande, Lakshmi Hymon, Daniel Jasleen, ] Jules, José Jules, Marcel Landgraf, Tom Mar-Tins, Jason Martin, Elke Martin, Wirtz Martins, Jason Niesteruk, Andreas Niesteruk, Anna Nusrat, Shahin Nusrat, ] Oxenfarth, Oxenfarth, Andreas Oxenfarth, Shahin Qureshi, Shahin Qureshi, Tatja-Na Qureshi, Tatjana Rich-Ter,, Christian Richter, Sridhar Santosh, Lakshmi Santosh, ] Schamber, Robbin Schamber, Tatjana Schnieders, Alix Schnieders, Robbin Schwalbe, Sreeramulu, Harald Sreeramulu, Sridhar Stirnal, Christian Stirnal, Elke Stirnal, Kamal Tröster, Alix Tröster, Anna Völklein, Albrecht Wacker, Anna Wacker, Julia Wirm-Er-Bartoschek, Julia Wirmer-Bartoschek, Maria
topic	covid:4d26482e51098c1d00d367d485a71338eb78573a#this
Source	Medline; PMC
abstract	We report here on the nuclear magnetic resonance (NMR) 19 F screening of 14 RNA targets with different secondary and tertiary structure to systematically assess druggability of RNAs. Our RNA targets include representative bacterial riboswitches that naturally bind with nanomolar affinity and high specificity to cellular metabolites of low molecular weight. Based on counter‐screens against five DNAs and five proteins, we can show that RNA can be specifically targeted. To demonstrate the quality of the initial fragment library that has been designed for easy follow‐up chemistry, we further show how to increase binding affinity from an initial fragment hit by chemistry that links the identified fragment to the intercalator acridine. Thus, we achieve low micromolar binding affinity without losing binding specificity between two different terminator structures.
has issue date	2020-08-14(xsd:dateTime)
bibo:doi	10.1002/cbic.202000476
bibo:pmid	32794266
has license	no-cc
sha1sum (hex)	4d26482e51098c1d00d367d485a71338eb78573a
schema:url	https://doi.org/10.1002/cbic.202000476
resource representing a document's title	19F‐NMR‐based fragment screening for 14 different biologically active RNAs and 10 DNA and protein counter‐screens
has PubMed Central identifier	PMC7436455
has PubMed identifier	32794266
schema:publication	Chembiochem
resource representing a document's body	covid:4d26482e51098c1d00d367d485a71338eb78573a#body_text
is http://vocab.deri.ie/void#inDataset of	proxy:http/ns.inria.fr/covid19/4d26482e51098c1d00d367d485a71338eb78573a
is schema:about of	named entity 'demonstrate' named entity 'naturally' named entity 'nanomolar' named entity 'Combining' named entity 'fragment' named entity 'representative' named entity 'metabolites' named entity 'binding' named entity 'systematically' named entity 'cellular' named entity 'nuclear magnetic resonance (NMR)' named entity 'RNA' named entity 'protein' named entity 'Biology' named entity 'micromolar' named entity 'RNAs' named entity 'follow-up' named entity 'Chemistry' named entity 'biologically active' named entity 'protein' named entity 'G-Quadruplex' named entity 'guanidine' named entity 'undruggable' named entity 'plasmid'

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