Discovery of Selective RNA-Binding Small Molecules by Affinity-Selection Mass Spectrometry.

No abstract is available for this paper.

• Publication year

  2018

• Venue

  ACS Chemical Biology

• Publication date

  2018-02-07

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1021/acschembio.7b01013PMID 29412640
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Antibacterial small molecules targeting the conserved TOPRIM domain of DNA gyrase

  2017cited by this paper
• RNA as a small molecule druggable target.

  2017cited by this paper
• Detection of Ligand-Induced Conformational Changes in Oligonucleotides by Second-Harmonic Generation at a Supported Lipid Bilayer Interface.

  2016cited by this paper
• Atomic resolution mechanistic studies of ribocil: A highly selective unnatural ligand mimic of the E. coli FMN riboswitch

  2016cited by this paper
• Non-coding RNAs as drug targets

  2016cited by this paper
• Development of Small Molecules with a Noncanonical Binding Mode to HIV-1 Trans Activation Response (TAR) RNA.

  2016cited by this paper
• Selective small-molecule inhibition of an RNA structural element

  2015cited by this paper
• Tuning riboswitch-mediated gene regulation by rational control of aptamer ligand binding properties.

  2015cited by this paper
• Protein Conformational Changes Are Detected and Resolved Site Specifically by Second-Harmonic Generation

  2015cited by this paper
• The ribB FMN riboswitch from Escherichia coli operates at the transcriptional and translational level and regulates riboflavin biosynthesis

  2015cited by this paper
• Small Molecules Detected by Second-Harmonic Generation Modulate the Conformation of Monomeric α-Synuclein and Reduce Its Aggregation in Cells*

  2015cited by this paper
• SMN2 splice modulators enhance U1-pre-mRNA association and rescue SMA mice.

  2015cited by this paper
• Validating fragment-based drug discovery for biological RNAs: lead fragments bind and remodel the TPP riboswitch specifically.

  2014cited by this paper
• Two-dimensional combinatorial screening enables the bottom-up design of a microRNA-10b inhibitor.

  2014cited by this paper
• Flavoproteins Are Potential Targets for the Antibiotic Roseoflavin in Escherichia coli

  2013cited by this paper
• Metal Complexes of Quinolone Antibiotics and Their Applications: An Update

  2013cited by this paper
• Urea-induced denaturation of preQ1-riboswitch.

  2013cited by this paper
• Two high-throughput screening assays for aberrant RNA–protein interactions in myotonic dystrophy type 1

  2012cited by this paper
• Recent advances in developing small molecules targeting RNA.

  2012cited by this paper
• Discovery of selective bioactive small molecules by targeting an RNA dynamic ensemble.

  2011cited by this paper
• Molecular sensing by the aptamer domain of the FMN riboswitch: a general model for ligand binding by conformational selection

  2011cited by this paper
• Prospects for riboswitch discovery and analysis.

  2011cited by this paper
• Novel Ligands for a Purine Riboswitch Discovered by RNA-Ligand Docking

  2011cited by this paper
• The roles of metal ions in regulation by riboswitches.

  2011cited by this paper
• The Riboflavin analog Roseoflavin targets an FMN-riboswitch and blocks Listeria monocytogenes growth, but also stimulates virulence gene-expression and infection

  2011cited by this paper
• The molecular interactions that stabilize RNA tertiary structure: RNA motifs, patterns, and networks.

  2011cited by this paper
• Structure-activity relationships through sequencing (StARTS) defines optimal and suboptimal RNA motif targets for small molecules.

  2010cited by this paper
• A Modular Approach to Synthetic RNA Binders of the Hepatitis C Virus Internal Ribosome Entry Site

  2010cited by this paper
• Roseoflavin is a natural antibacterial compound that binds to FMN riboswitches and regulates gene expression

  2009cited by this paper
• Conformational inhibition of the hepatitis C virus internal ribosome entry site RNA.

  2009cited by this paper
• Coenzyme recognition and gene regulation by a flavin mononucleotide riboswitch

  2009cited by this paper
• Targeting RNA with small molecules.

  2008cited by this paper
• Riboswitches that sense S-adenosylhomocysteine and activate genes involved in coenzyme recycling.

  2008cited by this paper
• Two-dimensional combinatorial screening identifies specific aminoglycoside-RNA internal loop partners.

  2008cited by this paper
• Affinity selection-mass spectrometry screening techniques for small molecule drug discovery.

  2007cited by this paper
• Method for quantitative protein-ligand affinity measurements in compound mixtures.

  2007cited by this paper
• The Anticancer Drug Ellipticine Is a Potent Inducer of Rat Cytochromes P450 1A1 and 1A2, Thereby Modulating Its Own Metabolism

  2007cited by this paper
• Using Selection to Identify and Chemical Microarray to Study the RNA Internal Loops Recognized by 6′‐N‐Acylated Kanamycin A

  2007cited by this paper
• Structure of the Eukaryotic Thiamine Pyrophosphate Riboswitch with Its Regulatory Ligand

  2006cited by this paper
• SAR by MS: discovery of a new class of RNA-binding small molecules for the hepatitis C virus: internal ribosome entry site IIA subdomain.

  2005cited by this paper
• Gene regulation by riboswitches

  2004cited by this paper
• A general technique to rank protein-ligand binding affinities and determine allosteric versus direct binding site competition in compound mixtures.

  2004cited by this paper
• Coenzyme B12 riboswitches are widespread genetic control elements in prokaryotes.

  2004cited by this paper
• An mRNA structure that controls gene expression by binding S-adenosylmethionine

  2003cited by this paper
• An mRNA structure that controls gene expression by binding FMN

  2002cited by this paper
• Structure-based computational database screening, in vitro assay, and NMR assessment of compounds that target TAR RNA.

  2002cited by this paper
• Applicability of urea in the thermodynamic analysis of secondary and tertiary RNA folding.

  1999cited by this paper
• Topoisomerase IV is a target of quinolones in Escherichia coli.

  1995cited by this paper
• Inhibition of p53 Protein Phosphorylation by 9‐Hydroxyellipticine: A Possible Anticancer Mechanism

  1995cited by this paper
• Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.

  1994cited by this paper
• Antitumor activity, pharmacology, and toxicity of ellipticines, ellipticinium, and 9-hydroxy derivatives: preliminary clinical trials of 2-methyl-9-hydroxy ellipticinium (NSC 264-137).

  1980cited by this paper

• Affinity selection mass spectrometry (AS-MS) as a tool to accelerate drug discovery efforts

  2026cites this paper
• Chemical biology of precise RNA targeting and intervention: advances and perspectives

  2026cites this paper
• A virtual system-coupled molecular dynamics simulation free from experimental knowledge on binding sites: Application to RNA-ligand binding free-energy landscape

  2025cites this paper
• Development and Application of a Customized Online Affinity Selection Mass Spectrometry Screening Platform.

  2025cites this paper
• Breaking the boundaries of affinity selection-mass spectrometry: From ligand screening to target-ligand interaction insights.

  2025cites this paper
• Riboswitch Dynamics and Their Expanding Biotechnological Applications

  2025cites this paper
• Designing small molecules targeting a cryptic RNA binding site through base displacement.

  2025cites this paper
• Small molecule screening of RNA aptamers using native mass spectrometry.

  2025cites this paper
• The evolution and application of RNA-focused small molecule libraries

  2025cites this paper
• The Druggable Transcriptome Project: From Chemical Probes to Precision Medicines.

  2025cites this paper
• Designing small molecules that target a cryptic RNA binding site via base displacement

  2025cites this paper
• Fluorescent Ligand Equilibrium Displacement: A High-Throughput Method for Identification of FMN Riboswitch-Binding Small Molecules

  2024cites this paper
• Mass Spectrometry Analysis of Nucleic Acid Modifications: From Beginning to Future.

  2024cites this paper
• RNA-Binding Small Molecules in Drug Discovery and Delivery: An Overview from Fundamentals.

  2024cites this paper
• Development of a DNA-encoded library screening method “DEL Zipper” to empower the study of RNA-targeted chemical matter

  2024cites this paper
• Targeting RNA with small molecules, from RNA structures to precision medicines: IUPHAR review: 40

  2024cites this paper
• RNATACs: Multispecific small molecules targeting RNA by induced proximity.

  2024cites this paper
• Investigating the Intramolecular Competition of Different RNA Binding Motifs for Neomycin B by Native Top-Down Mass Spectrometry.

  2024cites this paper
• A sensitive and scalable fluorescence anisotropy single stranded RNA targeting approach for monitoring riboswitch conformational states

  2024cites this paper
• Small molecule approaches to targeting RNA

  2024cites this paper
• Identifying small-molecules binding sites in RNA conformational ensembles with SHAMAN

  2024cites this paper
• A perspective on the changing landscape of HTS.

  2023cites this paper
• Biophysical screening and characterisation in medicinal chemistry.

  2023cites this paper
• Advances in Ultrahigh Throughput Hit Discovery with Tandem Mass Spectrometry Encoded Libraries

  2023cites this paper
• Binding free-energy landscapes of small molecule binder and non-binder to FMN riboswitch: All-atom molecular dynamics

  2023cites this paper
• Riboswitches as therapeutic targets: promise of a new era of antibiotics

  2023cites this paper
• Fluorescent indicator displacement assay for the discovery of UGGAA repeat-targeted small molecules.

  2023cites this paper
• Development of the Inverse Sonogashira Reaction for DEL Synthesis.

  2023cites this paper
• Contemporary Progress and Opportunities in RNA-Targeted Drug Discovery.

  2023cites this paper
• Rock, scissors, paper: How RNA structure informs function

  2023cites this paper
• Targeting RNA with small molecules: lessons learned from Xist RNA

  2023cites this paper
• Targeting RNA with small molecules—A safety perspective

  2023cites this paper
• Developing New Tools to Fight Human Pathogens: A Journey through the Advances in RNA Technologies

  2022cites this paper
• Brief considerations on targeting RNA with small molecules

  2022cites this paper
• Method for Identifying Sequence Motifs in Pre-miRNAs for Small-Molecule Binding

  2022cites this paper
• A Riboswitch-Driven Era of New Antibacterials

  2022cites this paper
• Targeting RNA structures with small molecules

  2022cites this paper
• Discovery of RNA-targeted small molecules through the merging of experimental and computational technologies

  2022cites this paper
• Strategies for targeting RNA with small molecule drugs

  2022cites this paper
• SILCS-RNA: Toward a Structure-Based Drug Design Approach for Targeting RNAs with Small Molecules.

  2022cites this paper
• Targeting Xist with compounds that disrupt RNA structure and X inactivation

  2022cites this paper
• Designing strategies of small-molecule compounds for modulating non-coding RNAs in cancer therapy

  2022cites this paper
• The kinase inhibitor Palbociclib is a potent and specific RNA-binding molecule

  2022cites this paper
• Drug discovery from natural products using affinity selection-mass spectrometry.

  2021cites this paper
• Riboswitches as Drug Targets for Antibiotics

  2021cites this paper
• High-Throughput Mass Spectrometry for Hit Identification: Current Landscape and Future Perspectives

  2021cites this paper
• Speeding drug discovery targeting RNAs: An iterative "RNA selection-compounds screening cycle" for exploring RNA-small molecule pairs.

  2021cites this paper
• [High-throughput Screening Technology for Selective Inhibitors of Transporters and Its Application in Drug Discovery].

  2021cites this paper
• Small molecule targeting of biologically relevant RNA tertiary and quaternary structures.

  2021cites this paper
• Lessons in Organic Fluorescent Probe Discovery

  2021cites this paper
• High-Throughput Affinity Selection Mass Spectrometry Using SAMDI-MS to Identify Small-Molecule Binders of the Human Rhinovirus 3C Protease

  2021cites this paper
• Screening strategies for identifying RNA- and ribonucleoprotein-targeted compounds.

  2021cites this paper
• Synthesis and evaluation of antimycobacterial activity of riboflavin derivatives.

  2021cites this paper
• Quantum Mechanics Helps Uncover Atypical Recognition Features in the Flavin Mononucleotide Riboswitch.

  2021cites this paper
• Mass Spectrometry of Nucleic Acid Noncovalent Complexes.

  2021cites this paper
• Exploring new targets and chemical space with affinity selection-mass spectrometry

  2020cites this paper
• High-Throughput Amenable MALDI-MS Detection of RNA and DNA with On-Surface Analyte Enrichment Using Fluorous Partitioning

  2020cites this paper
• Affinity selection-mass spectrometry for the discovery of pharmacologically active compounds from combinatorial libraries and natural products.

  2020cites this paper
• A two-step resin based approach to reveal survivin-selective fluorescent probes

  2020cites this paper
• RNA Drugs and RNA Targets for Small Molecules: Principles, Progress, and Challenges

  2020cites this paper
• Recent advances in screening active components from natural products based on bioaffinity techniques

  2020cites this paper
• Structural Ensembles of Ribonucleic Acids From Solvent Accessibility Data: Application to the S-Adenosylmethionine (SAM)-Responsive Riboswitch

  2020cites this paper
• Target-Directed Approaches for Screening Small Molecules against RNA Targets

  2020cites this paper
• Ligand Binding Mechanism and Its Relationship with Conformational Changes in Adenine Riboswitch

  2020cites this paper
• A drug discovery toolbox for Nuclear Magnetic Resonance (NMR) characterization of ligands and their targets.

  2020cites this paper
• Three‐Color Imaging Enables Simultaneous Screening of Multiple RNA Targets on Small Molecule Microarrays

  2020influential citation
• Modulating RNA secondary and tertiary structures by mismatch binding ligands.

  2019cites this paper
• RNA-ALIS: Methodology for screening soluble RNAs as small molecule targets using ALIS affinity-selection mass spectrometry.

  2019cites this paper
• Unveiling the druggable RNA targets and small molecule therapeutics

  2019cites this paper
• One-Pot Production of RNA Nanoparticles via Automated Processing and Self-Assembly.

  2019cites this paper
• Synthetic ligands for PreQ1 riboswitches provide structural and mechanistic insights into targeting RNA tertiary structure

  2019cites this paper
• Visualizing RNA Conformational Changes via Pattern Recognition of RNA by Small Molecules.

  2019cites this paper
• Fluorescent peptide displacement as a general assay for screening small molecule libraries against RNA.

  2019cites this paper
• Predicting RNA-RNA Interactions in Three-Dimensional Structures

  2019cites this paper
• LABEL-FREE BIO-AFFINITY MASS SPECTROMETRY FOR SCREENING AND LOCATING BIOACTIVE MOLECULES.

  2019cites this paper
• Targeting RNA with Small Molecules: Identification of Selective, RNA-Binding Small Molecules Occupying Drug-Like Chemical Space

  2019cites this paper
• Methods to identify and optimize small molecules interacting with RNA (SMIRNAS).

  2019cites this paper
• Emerging modes-of-action in drug discovery.

  2019cites this paper
• NMR characterization of RNA small molecule interactions.

  2019cites this paper
• Second-harmonic generation-based methods to detect and characterize ligand-induced RNA conformational changes.

  2019cites this paper
• Synthetic small-molecule RNA ligands: future prospects as therapeutic agents.

  2019cites this paper
• Challenges of Connecting Chemistry to Pharmacology: Perspectives from Curating the IUPHAR/BPS Guide to PHARMACOLOGY

  2018cites this paper
• Identification of G-Quadruplex-Binding Inhibitors of Myc Expression through Affinity Selection–Mass Spectrometry

  2018cites this paper
• Structure-activity relationship of flavin analogs that target the FMN riboswitch

  2018cites this paper
• RNA Structural Differentiation: Opportunities with Pattern Recognition.

  2018cites this paper
• Identification of thienopyridine carboxamides as selective binders of HIV-1 trans Activation Response (TAR) and Rev Response Element (RRE) RNAs.

  2018cites this paper
• Second-Harmonic Generation (SHG) for Conformational Measurements: Assay Development, Optimization, and Screening.

  2018cites this paper
• Small molecules get the message

  2018cites this paper
• Structure-Activity Relationship of Flavin Analogues That Target the Flavin Mononucleotide Riboswitch.

  2018cites this paper
• New Modalities, Technologies, and Partnerships in Probe and Lead Generation: Enabling a Mode-of-Action Centric Paradigm.

  2018cites this paper