A5109515870- RNA Interference and Gene Delivery
- Advanced biosensing and bioanalysis techniques
- Cancer therapeutics and mechanisms
- Catalytic Cross-Coupling Reactions
- Organoboron and organosilicon chemistry
- Catalytic C–H Functionalization Methods
- RNA and protein synthesis mechanisms
- DNA and Nucleic Acid Chemistry
- CRISPR and Genetic Engineering
- Viral Infections and Immunology Research
- Synthesis and Characterization of Heterocyclic Compounds
- RNA modifications and cancer
- RNA Research and Splicing
- Synthesis and Biological Evaluation
- Melanoma and MAPK Pathways
- Synthesis and Catalytic Reactions
- Waste Management and Recycling
- Photochromic and Fluorescence Chemistry
- Protein Kinase Regulation and GTPase Signaling
- Synthesis and Reactivity of Heterocycles
- Protein Degradation and Inhibitors
- Click Chemistry and Applications
- Composting and Vermicomposting Techniques
- Synthesis and biological activity
Scripps Research Institute
2024
Scripps (United States)
2024
Sun Yat-sen University
2017-2023
Peking University
2020-2021
The specificity of nucleic acids' binders is crucial for developing this kind drug, especially novel G-quadruplexes' binders. Quindoline derivatives have been developed as G-quadruplex stabilizers with good interactive activities. In order to improve the selectivity and binding affinity quindoline c-myc ligands, triazole containing benzofuroquinoline (T-BFQs) were designed synthesized by using 1,3-dipolar cycloaddition a series alkyne azide building blocks. toward DNA these T-BFQs was...
There is an urgent need to develop antiviral drugs and alleviate the current COVID-19 pandemic. Herein we report design construction of chimeric oligonucleotides comprising a 2'-OMe-modified antisense oligonucleotide 5'-phosphorylated 2'-5' poly(A)4 (4A2-5 ) degrade envelope spike RNAs SARS-CoV-2. The was used for searching recognizing target viral RNA sequence, conjugated 4A2-5 guided RNase L activation sequence-specifically RNAs. Since can potently cleave single-stranded during innate...
Abstract Target validation and identification of binding sites are keys to the development bioactive small molecules that target RNA. Herein, we describe optimized protocols profile molecule–RNA interactions define in RNAs using covalent chemistry. Various reactive modules appended an RNA-binding molecule were studied for cross-linking RNA target. Electrophilic modules, whether N-chloroethyl aniline or diazirine, have profiles consistent with induced proximity; however, probes more specific...
The human proto-oncogene neuroblastoma RAS ( NRAS) contains a guanine-rich sequence in the 5'-untranslated regions (5'-UTR) of mRNA that could form an RNA G-quadruplex structure. This structure acts as repressor for NRAS translation and be potential target anticancer drugs. Our previous studies found effective scaffold, quindoline binding stabilizing DNA structures. Here, on basis reported RNA-specific probes, series novel p-(methylthio)styryl substituted (MSQ) derivatives were designed,...
Abstract The flexible synthesis of tetra- and triarylethenes bearing different aryl groups has been a long-standing challenge in organic synthesis. Here we report palladium-catalysed syn -diarylation arylethynyl N -methyliminodiacetyl (MIDA) boronates. products, triarylalkenyl boronates, allow step-economic modular or via subsequent stereospecific Suzuki-Miyaura coupling reaction base-promoted protodeborylation, respectively. Use the sp 3 -B(MIDA) masked alkyne is key factor for success by...
α-Boryl ketones are traditionally challenging targets in organic synthesis. Reported herein is a mild and metal-free synthesis of α-boryl via the hydration or oxidation N-methyliminodiacetyl boronate (B(MIDA))-decorated alkynes. A new system comprised AcCl H2O HFIP allows arylethynyl B(MIDA)s at room temperature with decent functional group tolerance. An oxidative carbon deletion process propargylic also developed for aliphatic ketones. intriguing β-boron effect was observed to account...
Abstract Currently CRISPR/Cas9 is a widely used efficient tool for gene editing. Precise control over the system with high temporal and spatial resolution essential studying regulation Here, we synthesized novel light‐controlled crRNA by coupling vitamin E photolabile linker at 5′ terminus to inactivate system. The modification did not affect ribonucleoprotein (RNP) formation of Cas9/crRNA/tracrRNA complexes but inhibit association RNP target DNA. Upon light irradiation, E‐caged was...
Various approaches have been developed to target RNA and modulate its function with modes of action including binding cleavage. Herein, we explored how small molecule is correlated cleavage induced by heterobifunctional ribonuclease targeting chimeras (RiboTACs), where RNase L recruited cleave the bound target, in a transcriptome-wide, unbiased fashion. Only fraction targets was cleaved L, RiboTAC binding. Global analysis suggested that (i) generally form region stable structure encompasses...
Small molecules targeting RNA can be valuable chemical probes and potential therapeutics. The interactions between small molecules, particularly fragments, RNA, however, difficult to detect due their modest affinities short residence times. Here, we present a protocol for mapping the molecular fingerprints of in vitro throughout human transcriptome live cells. We describe steps compound treatment, cross-linking, extraction, fragmentation, pull-down. then detail procedures sequencing data...
Small molecules targeting RNA can be valuable chemical probes and potential therapeutics. The interactions between small molecules, particularly fragments, RNA, however, difficult to detect due their modest affinities short residence times. Here, we describe the procedures for mapping molecular fingerprints of in vitro throughout human transcriptome live cells, identifying both targets bound by molecule sites binding therein. For complete details on use execution this protocol, please refer 1.
Abstract There is an urgent need to develop antiviral drugs and alleviate the current COVID‐19 pandemic. Herein we report design construction of chimeric oligonucleotides comprising a 2′‐OMe‐modified antisense oligonucleotide 5′‐phosphorylated 2′‐5′ poly(A) 4 (4A 2‐5 ) degrade envelope spike RNAs SARS‐CoV‐2. The was used for searching recognizing target viral RNA sequence, conjugated 4A guided RNase L activation sequence‐specifically RNAs. Since can potently cleave single‐stranded during...
The previously published version of this Article contained errors in Fig. 1, where the B(MIDA) fragment was incorrectly labelled. These have been corrected both PDF and HTML versions Article.
Abstract There is an urgent need for effective antiviral drugs to alleviate the current COVID-19 pandemic. Here, we rationally designed and developed chimeric antisense oligonucleotides degrade envelope spike RNAs of SARS-CoV-2. Each oligonucleotide comprises a 3’ sequence target recognition 5’-phosphorylated 2’-5’ poly(A)4 guided ribonuclease L (RNase L) activation. Since RNase can potently cleave single strand RNA during innate response, improved degradation efficiency was twice as much...
SARS-Cov-2 In der Zuschrift aus S. 21830 berichten Xinjing Tang et al. über die effiziente Hemmung von SARS-CoV-2 mit chimären Antisense-Oligonukleotiden durch Aktivierung RNase L.