scholarly journals Three‐Color Imaging Enables Simultaneous Screening of Multiple RNA Targets on Small Molecule Microarrays

2020 ◽  
Vol 12 (4) ◽  
Author(s):  
Deondre Jordan ◽  
Mo Yang ◽  
John S. Schneekloth
Keyword(s):  
Small Molecule ◽  
Color Imaging ◽  
Rna Targets

scholarly journals SCAN ™—A High-Throughput Assay for Detecting Small Molecule Binding to RNA Targets

2009 ◽  
Vol 14 (3) ◽  
pp. 219-229 ◽  
Author(s):  
Chris Baugh ◽  
Shaohui Wang ◽  
Bin Li ◽  
James R. Appleman ◽  
Peggy A. Thompson
Keyword(s):  
Small Molecule ◽  
High Throughput ◽  
High Throughput Screening ◽  
Screening Assay ◽  
Laboratory Equipment ◽  
Rna Targets ◽  
High Throughput Screening Assay ◽  
Small Molecule Ligands ◽  
Hcv Ires ◽  
High Throughput Assay

A novel optical-based high-throughput screening technology has been developed for increasing the rate of discovering chemical leads against RNA targets. SCAN™ ( Screen for Compounds with Affinity for Nucleic Acids) is an affinity-based assay that identifies small molecules that bind and recognize structured RNA elements. This technology provides the opportunity to conduct high-throughput screening of a new class of targets—RNA. SCAN™ offers many attractive features including a simple homogeneous format, low screening costs, and the ability to use common laboratory equipment. A SCAN™ assay was developed for the HCV IRES Loop IIId RNA domain. A high-throughput screen of our entire compound library resulted in the identification of small molecule ligands that bind to Loop IIId. The Z′ values were greater than 0.8, showing this to be a robust high-throughput screening assay. A correlation between SCAN™ EC50 and KD values is reported suggesting the ability to use the assay for compound optimization. ( Journal of Biomolecular Screening 2009:219-229)

scholarly journals A Chemical Probe Based on the PreQ1 Metabolite Enables Transcriptome-wide Mapping of Binding Sites

2021 ◽  
Author(s):  
Sumirtha Balaratnam ◽  
Curran Rhodes ◽  
Desta Bume ◽  
Colleen Connelly ◽  
Christopher Lai ◽  
...  
Keyword(s):  
Small Molecule ◽  
Binding Sites ◽  
X Ray ◽  
X Ray Crystallography ◽  
Rna Targets ◽  
Active Probe ◽  
Selective Interaction ◽  
Molecule Interactions ◽  
Competition Assays

Abstract The role of metabolite-responsive riboswitches in regulating gene expression in bacteria is well known and makes them useful systems for the study of RNA-small molecule interactions. Here, we study the PreQ1 riboswitch system, assessing sixteen diverse PreQ1-derived probes for their ability to selectively modify the riboswitch aptamer covalently. For the most active probe, a diazirine-based photocrosslinker, X-ray crystallography and gel-based competition assays demonstrated the mode of binding of the ligand to the aptamer, and functional assays demonstrated that the probe retains activity against the full riboswitch. Transcriptome-wide mapping using Chem-CLIP revealed a highly selective interaction between the bacterial aptamer and the small molecule. In addition, a small number of RNA targets in endogenous human transcripts were found to bind specifically to PreQ1, providing evidence for candidate PreQ1 aptamers in human RNA. This work demonstrates a stark influence of linker chemistry and structure on the ability of molecules to crosslink RNA, reveals that the PreQ1 aptamer/ligand pair are broadly useful for chemical biology applications, and provides insights into how PreQ1 interacts with human RNAs.

scholarly journals Unveiling the druggable RNA targets and small molecule therapeutics

2019 ◽  
Vol 27 (10) ◽  
pp. 2149-2165 ◽  
Author(s):  
Joanna Sztuba-Solinska ◽  
Gabriela Chavez-Calvillo ◽  
Sabrina Elizabeth Cline
Keyword(s):  
Small Molecule ◽  
Rna Targets ◽  
Small Molecule Therapeutics

Small-molecule fluorescent probes for specific RNA targets

2011 ◽  
Vol 47 (16) ◽  
pp. 4712 ◽  
Author(s):  
Asako Murata ◽  
Shin-ichi Sato ◽  
Yoshinori Kawazoe ◽  
Motonari Uesugi
Keyword(s):  
Small Molecule ◽  
Fluorescent Probes ◽  
Rna Targets

scholarly journals Fluorescent peptide displacement as a general assay for screening small molecule libraries against RNA

2019 ◽  
Vol 17 (7) ◽  
pp. 1778-1786 ◽  
Author(s):  
Neeraj N. Patwardhan ◽  
Zhengguo Cai ◽  
Colby N. Newson ◽  
Amanda E. Hargrove
Keyword(s):  
Statistical Analysis ◽  
Small Molecules ◽  
Small Molecule ◽  
Rna Targets ◽  
Fluorescent Peptide ◽  
Small Molecule Libraries ◽  
Displacement Assay

A fluorescent peptide displacement assay combined with statistical analysis is used for screening small molecules against different RNA targets and profiling their affinity/selectivity patterns.

A privileged ternary blend enabling non-fullerene organic photovoltaics with over 14% efficiency

2020 ◽  
Vol 8 (43) ◽  
pp. 15135-15141
Author(s):  
Jing Yan ◽  
Yuan-Qiu-Qiang Yi ◽  
Jianqi Zhang ◽  
Huanran Feng ◽  
Yanfeng Ma ◽  
...  
Keyword(s):  
Small Molecule ◽  
Organic Photovoltaics ◽  
Power Conversion ◽  
Ternary Blend ◽  
Conversion Efficiencies

Two non-fullerene small molecule acceptors, NT-4F and NT-4Cl, were designed and synthesized. Power conversion efficiencies of 11.44% and 14.55% were achieved for NT-4Cl-based binary and ternary devices, respectively.

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