Discovery of the first small-molecule CsrA-RNA interaction inhibitors using biophysical screening technologies.

2.50
Hdl Handle:
http://hdl.handle.net/10033/618599
Title:
Discovery of the first small-molecule CsrA-RNA interaction inhibitors using biophysical screening technologies.
Authors:
Maurer, Christine K; Fruth, Martina; Empting, Martin ( 0000-0002-0503-5830 ) ; Avrutina, Olga; Hoßmann, Jörn; Nadmid, Suvd; Gorges, Jan; Herrmann, Jennifer; Kazmaier, Uli; Dersch, Petra ( 0000-0001-8177-3280 ) ; Müller, Rolf; Hartmann, Rolf W
Abstract:
CsrA is a global post-transcriptional regulator protein affecting mRNA translation and/or stability. Widespread among bacteria, it is essential for their full virulence and thus represents a promising anti-infective drug target. Therefore, we aimed at the discovery of CsrA-RNA interaction inhibitors. Results & methodology: We followed two strategies: a screening of small molecules (A) and an RNA ligand-based approach (B). Using surface plasmon resonance-based binding and fluorescence polarization-based competition assays, (A) yielded seven small-molecule inhibitors, among them MM14 (IC50 of 4 µM). (B) resulted in RNA-based inhibitor GGARNA (IC50 of 113 µM).
Affiliation:
German Centre for Infection Research (DZIF), PartnerSite Hannover-Braunschweig, 30625 Hannover, Germany.
Citation:
Discovery of the first small-molecule CsrA-RNA interaction inhibitors using biophysical screening technologies. 2016, 8 (9):931-47 Future Med Chem
Journal:
Future medicinal chemistry
Issue Date:
Jun-2016
URI:
http://hdl.handle.net/10033/618599
DOI:
10.4155/fmc-2016-0033
PubMed ID:
27253623
Type:
Article
Language:
en
ISSN:
1756-8927
Appears in Collections:
publications of the department drug design and optimization (HIPS]DDOP)

Full metadata record

DC FieldValue Language
dc.contributor.authorMaurer, Christine Ken
dc.contributor.authorFruth, Martinaen
dc.contributor.authorEmpting, Martinen
dc.contributor.authorAvrutina, Olgaen
dc.contributor.authorHoßmann, Jörnen
dc.contributor.authorNadmid, Suvden
dc.contributor.authorGorges, Janen
dc.contributor.authorHerrmann, Jenniferen
dc.contributor.authorKazmaier, Ulien
dc.contributor.authorDersch, Petraen
dc.contributor.authorMüller, Rolfen
dc.contributor.authorHartmann, Rolf Wen
dc.date.accessioned2016-08-19T12:59:04Z-
dc.date.available2016-08-19T12:59:04Z-
dc.date.issued2016-06-
dc.identifier.citationDiscovery of the first small-molecule CsrA-RNA interaction inhibitors using biophysical screening technologies. 2016, 8 (9):931-47 Future Med Chemen
dc.identifier.issn1756-8927-
dc.identifier.pmid27253623-
dc.identifier.doi10.4155/fmc-2016-0033-
dc.identifier.urihttp://hdl.handle.net/10033/618599-
dc.description.abstractCsrA is a global post-transcriptional regulator protein affecting mRNA translation and/or stability. Widespread among bacteria, it is essential for their full virulence and thus represents a promising anti-infective drug target. Therefore, we aimed at the discovery of CsrA-RNA interaction inhibitors. Results & methodology: We followed two strategies: a screening of small molecules (A) and an RNA ligand-based approach (B). Using surface plasmon resonance-based binding and fluorescence polarization-based competition assays, (A) yielded seven small-molecule inhibitors, among them MM14 (IC50 of 4 µM). (B) resulted in RNA-based inhibitor GGARNA (IC50 of 113 µM).en
dc.language.isoenen
dc.rights.urihttp://creativecommons.org/licenses/by-nc-sa/4.0/*
dc.titleDiscovery of the first small-molecule CsrA-RNA interaction inhibitors using biophysical screening technologies.en
dc.typeArticleen
dc.contributor.departmentGerman Centre for Infection Research (DZIF), PartnerSite Hannover-Braunschweig, 30625 Hannover, Germany.en
dc.identifier.journalFuture medicinal chemistryen

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