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Total 1197 results found since Jan 2013.

Mitochondria-Targeted Gene Silencing Facilitated by Mito-CPDs
We report herein a universal mitochondria-targeted gene-delivery approach by using cell-penetrating poly(disulfide)s (CPDs). Novel CPD-based mitochondrial transporters, named Mito-CPDs, were synthesized by using triphenylphosphonium (TPP)-fused propagating monomers containing either disulfide or diselenide backbones. Upon spontaneous complex formation with an oligonucleotide (single- or double-stranded), the resulting nanoscale Mito-CPD@Oligo exhibited excellent properties in common biological media. While the intracellular gene-delivery efficiency of these Mito-CPDs was comparable to that of commercial transfection agents...
Source: Chemistry - February 22, 2023 Category: Chemistry Authors: Wenjie Lang Wei Tan Bizhong Zhou Yuli Zhuang Bei Zhang Linye Jiang Shao Q Yao Jingyan Ge Source Type: research

ASAP Nuclease P1 Digestion for Bottom-Up RNA Sequencing of Modified siRNA Therapeutics
Analytical ChemistryDOI: 10.1021/acs.analchem.2c04902
Source: Analytical Chemistry - February 22, 2023 Category: Chemistry Authors: Joshua D. Jones, Kathleen T. Grassmyer, Robert T. Kennedy, Kristin S. Koutmou, and Todd D. Maloney Source Type: research

Molecules, Vol. 28, Pages 1874: Berberine Ameliorates Metabolic-Associated Fatty Liver Disease Mediated Metabolism Disorder and Redox Homeostasis by Upregulating Clock Genes: Clock and Bmal1 Expressions
Shijian Quan Metabolic-associated fatty liver disease (MAFLD) is one of the most common chronic liver diseases, which in turn triggers mild inflammation, metabolic dysfunction, fibrosis, and even cancer. Accumulating evidence has suggested that Berberine (BBR) could significantly improve MAFLD progression. Clock and Bmal1 as heterodimer proteins highly participated in the development of MAFLD, but whether BBR targets Clock and Bmal1 in MAFLD remains poorly understood. The result suggested that the protein levels of Clock and Bmal1 were decreased in MAFLD mice, which was negatively correlated with elevated reactive o...
Source: Molecules - February 16, 2023 Category: Chemistry Authors: Cunsi Ye Yajing Zhang Shaomin Lin Yi Chen Zimiao Wang Haoyinghua Feng Guangqing Fang Shijian Quan Tags: Article Source Type: research

Molecules, Vol. 28, Pages 1802: Critical Review on the Different Roles of Exosomes in TNBC and Exosomal-Mediated Delivery of microRNA/siRNA/lncRNA and Drug Targeting Signalling Pathways in Triple-Negative Breast Cancer
This article highlights the significant roles of exosomes associated with TNBC, the involvement of exosomes in breast cancer diagnosis, progression, and the treatment of triple-negative breast cancer by the exosomes as a drug delivery system. This review paper also illustrates the role of exosomes in initiating EMT in breast cancer, including novel signalling.
Source: Molecules - February 14, 2023 Category: Chemistry Authors: Manosi Banerjee Vijayarangan Devi Rajeswari Tags: Review Source Type: research

ASAP Metabolically Stable Anomeric Linkages Containing GalNAc –siRNA Conjugates: An Interplay among ASGPR, Glycosidase, and RISC Pathways
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.2c01337
Source: Journal of Medicinal Chemistry - February 9, 2023 Category: Chemistry Authors: Pachamuthu Kandasamy, Shohei Mori, Shigeo Matsuda, Namrata Erande, Dhrubajyoti Datta, Jennifer L. S. Willoughby, Nate Taneja, Jonathan O ’Shea, Anna Bisbe, Rajar M. Manoharan, Kristina Yucius, Tuyen Nguyen, Ramesh Indrakanti, Swati Gupta, Jason A. Gilbe Source Type: research

Molecules, Vol. 28, Pages 1618: A Novel Hybridization LC-MS/MS Methodology for Quantification of siRNA in Plasma, CSF and Tissue Samples
sian Therapeutic oligonucleotides, such as antisense oligonucleotide (ASO) and small interfering RNA (siRNA), are a new class of therapeutics rapidly growing in drug discovery and development. A sensitive and reliable method to quantify oligonucleotides in biological samples is critical to study their pharmacokinetic and pharmacodynamic properties. Hybridization LC-MS/MS was recently established as a highly sensitive and specific methodology for the quantification of single-stranded oligonucleotides, e.g., ASOs, in various biological matrices. However, there is no report of this methodology for the bioanalysis of doubl...
Source: Molecules - February 8, 2023 Category: Chemistry Authors: Long Yuan Jean-Fran çois Dupuis Kevork Mekhssian Tags: Article Source Type: research

Molecules, Vol. 28, Pages 1611: Anemoside A3 Inhibits Macrophage M2-Like Polarization to Prevent Triple-Negative Breast Cancer Metastasis
In conclusion, these results indicate that A3 could attenuate the metastasis of TNBC by inhibiting the M2-type polarization of macrophages, which may be related to the STAT3 pathway.
Source: Molecules - February 7, 2023 Category: Chemistry Authors: Peng Liu Yahui Liu Lanying Chen Zeping Fan Yingying Luo Yaru Cui Tags: Article Source Type: research

Molecules, Vol. 28, Pages 917: Site-Specific Antibody Conjugation with Payloads beyond Cytotoxins
u As antibody–drug conjugates have become a very important modality for cancer therapy, many site-specific conjugation approaches have been developed for generating homogenous molecules. The selective antibody coupling is achieved through antibody engineering by introducing specific amino acid or unnatural amino acid residues, peptides, and glycans. In addition to the use of synthetic cytotoxins, these novel methods have been applied for the conjugation of other payloads, including non-cytotoxic compounds, proteins/peptides, glycans, lipids, and nucleic acids. The non-cytotoxic compounds include polyethyl...
Source: Molecules - January 17, 2023 Category: Chemistry Authors: Qun Zhou Tags: Review Source Type: research

Synthesis of 2'-modified N6-methyladenosine phosphoramidites and their incorporation into siRNA
Bioorg Med Chem Lett. 2023 Jan 9:129126. doi: 10.1016/j.bmcl.2023.129126. Online ahead of print.ABSTRACTA synthesis of 2'-fluoro and 2'-methoxy N6-methyladenosine phosphoramidites and their successful incorporation into oligonucleotides is reported. 2'-fluoro and 2́-methoxy modifications of sugars in siRNAs are known to aid stability and N6-methylation modifies the potency of therapeutic silencing RNAs (siRNA). We demonstrate that a combination of those modifications incorporated into the antisense strand of siRNA leads to efficient knockdown of a target gene in cells. This work broadens the available pool of chemical mod...
Source: Bioorganic and Medicinal Chemistry Letters - January 12, 2023 Category: Chemistry Authors: Anna M Rydzik Doris Riether Dirk Gottschling Source Type: research

Photoaffinity labelling-based chemoproteomic strategy identifies PEBP1 as the target of ethyl gallate against macrophage activation
Chem Commun (Camb). 2023 Jan 4. doi: 10.1039/d2cc05440j. Online ahead of print.ABSTRACTUlcerative colitis (UC) is an inflammatory disease of the colon with an unmet need for therapeutic targets. Ethyl gallate (EG) is a natural small molecule for UC treatment, but its cellular target is unknown. By labelling EG with a diazirine photocrosslinker and a click chemistry handle, we identified phosphatidyl-ethanolamine binding protein1 (PEBP1) as a direct cellular target of EG by forming hydrogen bonds with Asp70 and Tyr120. In particular, hydrogen/deuterium exchange mass spectrometry indicated that EG induced the sequence (resid...
Source: Chemical Communications - January 4, 2023 Category: Chemistry Authors: Wei Yu Min Liao Yang Chen Rui Xue Xiao-Meng Shi Dan Liu Fang-Fang Zhuo Hui Tang Zhi-Yuan Lu Peng-Fei Tu Bo Han Xin Jia Ke-Wu Zeng Source Type: research

Improving reactivity of naphthalimide-based GST probe by imparting TPP cation: Development and application for live cell imaging
Bioorg Med Chem Lett. 2022 Dec 19:129109. doi: 10.1016/j.bmcl.2022.129109. Online ahead of print.ABSTRACTGlutathione S-transferases (GSTs) Glutathione S-transferases (GSTs); triphenylphosphonium (TPP); 4-bromo-1,8-naphthalimide (BrNaph); reduced glutathione (GSH); hexahistidine (6×His); internal ribosome entry site (IRES); Hanks' Balanced Salt Solution (HBSS); small interfering RNA (siRNA) are a superfamily of multifunctional enzymes comprising multiple classes and subtypes. This paper describes the synthesis and characterization of TPPBN-1, a naphthalimide derivative conjugated with a triphenylphosphonium (TPP) cation. W...
Source: Bioorganic and Medicinal Chemistry Letters - December 22, 2022 Category: Chemistry Authors: Yuuta Fujikawa Kenta Terakado Sayaka Nezu Kota Noritsugu Yuki Maemoto Akihiro Ito Hideshi Inoue Source Type: research

Molecules, Vol. 28, Pages 97: Alpha Ketoglutarate Downregulates the Neutral Endopeptidase and Enhances the Growth Inhibitory Activity of Thiorphan in Highly Aggressive Osteosarcoma Cells
sińska Since natural substances are widely explored as epigenetic modulators of gene expression and epigenetic abnormalities are important causes of cancerogenesis, factors with pro-tumor activities subjected to epigenetic control, e.g., neutral endopeptidase (NEP, neprilysin), are promising anticancer targets for potential therapies acting via epigenetic regulation of gene expression. Alpha-ketoglutarate (AKG) is a naturally occurring co-substrate for enzymes involved in histone and DNA demethylation with suggested anti-cancer activity. Hence, we investigated a potential effect of AKG on the NEP expression in cells d...
Source: Molecules - December 22, 2022 Category: Chemistry Authors: Magdalena Mizerska-Kowalska Adrianna S ławińska-Brych Emilia Niedziela Viktor Brodovskiy Barbara Zdzisi ńska Tags: Article Source Type: research

A hybrid nanoassembly for ultrasound-inducible cytosolic siRNA delivery and cancer sono-gene therapy
Ultrason Sonochem. 2022 Dec 9;92:106262. doi: 10.1016/j.ultsonch.2022.106262. Online ahead of print.NO ABSTRACTPMID:36512940 | DOI:10.1016/j.ultsonch.2022.106262
Source: Ultrasonics Sonochemistry - December 13, 2022 Category: Chemistry Authors: Gaigai Li Yan Zhang Jinbo Li Source Type: research

Molecules, Vol. 27, Pages 8564: Epigallocatechin Gallate Attenuates Gentamicin-Induced Nephrotoxicity by Suppressing Apoptosis and Ferroptosis
Jin Chao Shi Jia-Gen Wen Gentamicin (GEN) is a kind of aminoglycoside antibiotic with the adverse effect of nephrotoxicity. Currently, no effective measures against the nephrotoxicity have been approved. In the present study, epigallocatechin gallate (EG), a useful ingredient in green tea, was used to attenuate its nephrotoxicity. EG was shown to largely attenuate the renal damage and the increase of malondialdehyde (MDA) and the decrease of glutathione (GSH) in GEN-injected rats. In NRK-52E cells, GEN increased the cellular ROS in the early treatment phase and ROS remained continuously high from 1.5 H to 24 H. Mo...
Source: Molecules - December 5, 2022 Category: Chemistry Authors: Lin Yue Ya-Ru Yang Wen-Xian Ma Hong-Yan Wang Qian-Wen Fan Yue-Yue Wang Chao Li Jing Wang Zi-Mu Hu Xue-Fu Wang Feng-He Li Ming-Ming Liu Juan Jin Chao Shi Jia-Gen Wen Tags: Article Source Type: research