Screening chemical libraries for nucleic-acid-binding drugs by in vitro selection: A test case with lividomycin

1996 ◽  
Vol 2 (1-2) ◽  
pp. 103-110 ◽  
Author(s):  
Susan M. Lato ◽  
Andrew D. Ellington
Keyword(s):  
Nucleic Acid ◽  
In Vitro Selection ◽  
Test Case ◽  
Nucleic Acid Binding ◽  
Chemical Libraries

scholarly journals In Vitro RNase and Nucleic Acid Binding Activities Implicate Coilin in U snRNA Processing

PLoS ONE ◽  
2012 ◽  
Vol 7 (4) ◽  
pp. e36300 ◽  
Author(s):  
Hanna J. Broome ◽  
Michael D. Hebert
Keyword(s):  
Nucleic Acid ◽  
Nucleic Acid Binding

In vitro selection of high-affinity nucleic acid ligands to parasite target molecules

2003 ◽  
Vol 33 (12) ◽  
pp. 1309-1317 ◽  
Author(s):  
H.Ulrich Göringer ◽  
Matthias Homann ◽  
Mihaela Lorger
Keyword(s):  
Nucleic Acid ◽  
In Vitro Selection ◽  
High Affinity ◽  
Target Molecules ◽  
Selection Of

Inside Cover: Light-Controlled Cellular Internalization and Cytotoxicity of Nucleic Acid-Binding Agents: Studies in Vitro and in Zebrafish Embryos (ChemBioChem 1/2016)

ChemBioChem ◽  
2016 ◽  
Vol 17 (1) ◽  
pp. 2-2
Author(s):  
Cristina Penas ◽  
Mateo I. Sánchez ◽  
Jorge Guerra-Varela ◽  
Laura Sanchez ◽  
M. Eugenio Vázquez ◽  
...  
Keyword(s):  
Nucleic Acid ◽  
Zebrafish Embryos ◽  
Cellular Internalization ◽  
Nucleic Acid Binding ◽  
Binding Agents

Benzo(a)pyrene diol epoxides as intermediates in nucleic acid binding in vitro and in vivo

Science ◽  
1976 ◽  
Vol 193 (4253) ◽  
pp. 592-595 ◽  
Author(s):  
I. Weinstein ◽  
A. Jeffrey ◽  
K. Jennette ◽  
S. Blobstein ◽  
R. Harvey ◽  
...  
Keyword(s):  
Nucleic Acid ◽  
Nucleic Acid Binding ◽  
Diol Epoxides

scholarly journals Novel Nucleic Acid Binding Small Molecules Discovered Using DNA-Encoded Chemistry

Molecules ◽  
2019 ◽  
Vol 24 (10) ◽  
pp. 2026 ◽  
Author(s):  
Alexander Litovchick ◽  
Xia Tian ◽  
Michael I. Monteiro ◽  
Kaitlyn M. Kennedy ◽  
Marie-Aude Guié ◽  
...  
Keyword(s):  
Nucleic Acid ◽  
Small Molecules ◽  
Dna Sequences ◽  
High Specificity ◽  
Nucleic Acid Binding ◽  
Promoter Regions ◽  
Structural Motifs ◽  
Chemical Libraries ◽  
Cellular Context ◽  
The Many

Inspired by the many reported successful applications of DNA-encoded chemical libraries in drug discovery projects with protein targets, we decided to apply this platform to nucleic acid targets. We used a 120-billion-compound set of 33 distinct DNA-encoded chemical libraries and affinity-mediated selection to discover binders to a panel of DNA targets. Here, we report the successful discovery of small molecules that specifically interacted with DNA G-quartets, which are stable structural motifs found in G-rich regions of genomic DNA, including in the promoter regions of oncogenes. For this study, we chose the G-quartet sequence found in the c-myc promoter as a primary target. Compounds enriched using affinity-mediated selection against this target demonstrated high-affinity binding and high specificity over DNA sequences not containing G-quartet motifs. These compounds demonstrated a moderate ability to discriminate between different G-quartet motifs and also demonstrated activity in a cell-based assay, suggesting direct target engagement in the cell. DNA-encoded chemical libraries and affinity-mediated selection are uniquely suited to discover binders to targets that have no inherent activity outside of a cellular context, and they may also be of utility in other nucleic acid structural motifs.

scholarly journals The Gly/Arg-rich (GAR) domain of Xenopus nucleolin facilitates in vitro nucleic acid binding and in vivo nucleolar localization.

1993 ◽  
Vol 4 (11) ◽  
pp. 1189-1204 ◽  
Author(s):  
M A Heine ◽  
M L Rankin ◽  
P J DiMario
Keyword(s):  
Nucleic Acid ◽  
Binding Activity ◽  
Full Length ◽  
Nucleic Acid Binding ◽  
Binding Assays ◽  
Nucleic Acid Probes ◽  
E Coli ◽  
Indirect Immunofluorescence Staining

Epitope-tagged Xenopus nucleolin was expressed in Escherichia coli cells and in Xenopus oocytes either as a full-length wild-type protein or as a truncation that lacked the distinctive carboxy glycine/arginine-rich (GAR) domain. Both full-length and truncated versions of nucleolin were tagged at their amino termini with five tandem human c-myc epitopes. Whether produced in E. coli or in Xenopus, epitope-tagged full-length nucleolin bound nucleic acid probes in in vitro filter binding assays. Conversely, the E. coli-expressed GAR truncation failed to bind the nucleic acid probes, whereas the Xenopus-expressed truncation maintained slight binding activity. Indirect immunofluorescence staining showed that myc-tagged full-length nucleolin properly localized to the dense fibrillar regions within the multiple nucleoli of Xenopus oocyte nuclei. The epitope-tagged GAR truncation also translocated to the oocyte nuclei, but it failed to efficiently localize to the nucleoli. Our results show that the carboxy GAR domain must be present for nucleolin to efficiently bind nucleic acids in vitro and to associate with nucleoli in vivo.

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