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Total 1197 results found since Jan 2013.

Molecules, Vol. 26, Pages 3238: Size- and Surface- Dual Engineered Small Polyplexes for Efficiently Targeting Delivery of siRNA
This study provides a promising strategy to engineer the size and surface of polyplexes, allowing long blood circulation and targeted delivery of siRNA.
Source: Molecules - May 27, 2021 Category: Chemistry Authors: Shuang Liu Shaohui Deng Xiaoxia Li Du Cheng Tags: Article Source Type: research

Integration of 12aneN3 and Acenaphtho1,2-bquinoxaline as non-viral gene vectors with two-photon property for enhanced DNA/siRNA delivery and bioimaging
Bioorg Chem. 2021 May 11;113:104983. doi: 10.1016/j.bioorg.2021.104983. Online ahead of print.ABSTRACTTwo-photon fluorescent Acenaphtho[1,2-b]quinoxaline (ANQ) and the hydrophilic di-(triazole-[12]aneN3) moieties were combined through an alkyl chain (ANQ-A-M) or a β-hairpin motif with two aromatic γ-amino acid residues (ANQ-H-M) to explore their capabilities for in vitro and in vivo gene delivery and tracing. ANQ-A-M and ANQ-H-M showed the same maximum absorption at 420 nm, and their fluorescent intensities around 650 nm were varied in different solvents and became poor in the protic solvents. Gel electrophoresis assays ...
Source: Bioorganic Chemistry - May 24, 2021 Category: Chemistry Authors: Jin-Yu Liu Xu-Ying Liu Rui Liu Fang Tang Jing-Bo Yang Quan Tang Zhong-Lin Lu Hai-Jun Qiao Lan He Source Type: research

ASAP Syntheses of Morpholine-Based Nucleotide Analogs for Hepatic siRNA Targeting and Stabilization
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.1c00144
Source: Journal of Medicinal Chemistry - May 5, 2021 Category: Chemistry Authors: Armin Hofmeister, Kerstin Jahn-Hofmann, Bodo Brunner, Mike W. Helms, Christiane Metz-Weidmann, Arne Krack, Michael Kurz, Ziyu Li, Merle M. Weitzenberg, Elsa Pflimlin, Oliver Plettenburg, and Sabine Scheidler Source Type: research

HDAC8 promotes daunorubicin resistance of human acute myeloid leukemia cells via regulation of IL-6 and IL-8
Biol Chem. 2020 Dec 17;402(4):461-468. doi: 10.1515/hsz-2020-0196. Print 2021 Mar 26.ABSTRACTThe chemoresistance is one of the major challenges for acute myeloid leukemia (AML) treatment. We found that the expression of histone deacetylase 8 (HDAC8) was increased in daunorubicin (DNR) resistant AML cells, while targeted inhibition of HDAC8 by its specific siRNA or inhibitor can restore sensitivity of DNR treatment . Further, targeted inhibition of HDAC8 can suppress expression of interleukin 6 (IL-6) and IL-8. While recombinant IL-6 (rIL-6) and rIL-8 can reverse si-HDAC8-resored DNR sensitivity of AML cells. Mechanistical ...
Source: Biological Chemistry - May 3, 2021 Category: Chemistry Authors: Jieying Wu Ling Zhang Yashu Feng Bijay Khadka Zhigang Fang Jiajun Liu Source Type: research

Molecules, Vol. 26, Pages 2610: In Vitro Inhibitory Analysis of Rationally Designed siRNAs against MERS-CoV Replication in Huh7 Cells
In this report, we have discussed the prediction, designing, and evaluation of potential siRNA targeting the ORF1ab gene for the inhibition of MERS-CoV replication. The online software, siDirect 2.0 was used to predict and design the siRNAs, their secondary structure and their target accessibility. ORF1ab gene folding was performed by RNAxs and RNAfold software. A total of twenty-one siRNAs were selected from 462 siRNAs according to their scoring and specificity. siRNAs were evaluated in vitro for their cytotoxicity and antiviral efficacy in Huh7 cell line. No significant cytotoxicity was observed for all siRNAs in Huh7 ce...
Source: Molecules - April 29, 2021 Category: Chemistry Authors: Sherif Aly El-Kafrawy Sayed Sartaj Sohrab Zeenat Mirza Ahmed M. Hassan Fatima Alsaqaf Esam Ibraheem Azhar Tags: Article Source Type: research

Beyond ribose and phosphate: Selected nucleic acid modifications for structure – function investigations and therapeutic applications
Abstract Over the past 25 years, the acceleration of achievements in the development of oligonucleotide-based therapeutics has resulted in numerous new drugs making it to the market for the treatment of various diseases. Oligonucleotides with alterations to their scaffold, prepared with modified nucleosides and solid-phase synthesis, have yielded molecules with interesting biophysical properties that bind to their targets and are tolerated by the cellular machinery to elicit a therapeutic outcome. Structural techniques, such as crystallography, have provided insights to rationalize numerous properties including binding aff...
Source: Beilstein Journal of Organic Chemistry - April 28, 2021 Category: Chemistry Authors: Beilstein Journal of Organic Chemistry - Syndicated Feeds Tags: antisense chemically modified oligonucleotides crystallography siRNA structure Review Source Type: research

Molecules, Vol. 26, Pages 2382: Elucidating Role of Reactive Oxygen Species (ROS) in Cisplatin Chemotherapy: A Focus on Molecular Pathways and Possible Therapeutic Strategies
arrabi Kwang Seok Ahn The failure of chemotherapy is a major challenge nowadays, and in order to ensure effective treatment of cancer patients, it is of great importance to reveal the molecular pathways and mechanisms involved in chemoresistance. Cisplatin (CP) is a platinum-containing drug with anti-tumor activity against different cancers in both pre-clinical and clinical studies. However, drug resistance has restricted its potential in the treatment of cancer patients. CP can promote levels of free radicals, particularly reactive oxygen species (ROS) to induce cell death. Due to the double-edged sword role of ROS ...
Source: Molecules - April 19, 2021 Category: Chemistry Authors: Sepideh Mirzaei Kiavash Hushmandi Amirhossein Zabolian Hossein Saleki Seyed Mohammad Reza Torabi Adnan Ranjbar SeyedHesam SeyedSaleh Seyed Omid Sharifzadeh Haroon Khan Milad Ashrafizadeh Ali Zarrabi Kwang Seok Ahn Tags: Review Source Type: research

Multi-targeting siRNA nanoparticles for simultaneous inhibition of PI3K and Rac1 in PTEN-deficient prostate cancer
Publication date: Available online 16 April 2021Source: Journal of Industrial and Engineering ChemistryAuthor(s): Min Ju Kim, Hyosuk Kim, Xueliang Gao, Ju Hee Ryu, Yoosoo Yang, Ick Chan Kwon, Thomas M. Roberts, Sun Hwa Kim
Source: Journal of Industrial and Engineering Chemistry - April 17, 2021 Category: Chemistry Source Type: research

Molecules, Vol. 26, Pages 2119: A Versatile Solid-Phase Approach to the Synthesis of Oligonucleotide Conjugates with Biodegradable Hydrazone Linker
aminova One of the ways to efficiently deliver various drugs, including therapeutic nucleic acids, into the cells is conjugating them with different transport ligands via labile or stable bonds. A convenient solid-phase approach for the synthesis of 5′-conjugates of oligonucleotides with biodegradable pH-sensitive hydrazone covalent bonds is proposed in this article. The approach relies on introducing a hydrazide of the ligand under aqueous/organic media to a fully protected support-bound oligonucleotide containing aldehyde function at the 5′-end. We demonstrated the proof-of-principle of this approach by synthesiz...
Source: Molecules - April 7, 2021 Category: Chemistry Authors: Mariya I. Meschaninova Nina S. Entelis Elena L. Chernolovskaya Alya G. Venyaminova Tags: Article Source Type: research

Molecules, Vol. 26, Pages 2092: Simultaneous Quantitative Analysis of Ginsenosides Isolated from the Fruit of Panax ginseng C.A. Meyer and Regulation of HO-1 Expression through EGFR Signaling Has Anti-Inflammatory and Osteogenic Induction Effects in HPDL Cells
In conclusion, this study evaluated the contents of ginsenosides-Re, -Ra8, and -Rf isolated from P. ginseng fruit extract. Therefore, these results provide important basic data for future P. ginseng fruit component studies and suggest that ginsenosides Re, Ra8, and Rf have potential as future treatment options for periodontitis.
Source: Molecules - April 6, 2021 Category: Chemistry Authors: Eun-Nam Kim Oryon Kaygusuz Hyun-Su Lee Gil-Saeng Jeong Tags: Article Source Type: research

Molecules, Vol. 26, Pages 2018: An Activatable T1-Weighted MR Contrast Agent: A Noninvasive Tool for Tracking the Vicinal Thiol Motif of Thioredoxin in Live Cells
iya Kwan Soo Hong We have synthesized new magnetic resonance imaging (MRI) T1 contrast agents (CA1 and CA2) that permit the activatable recognition of the cellular vicinal thiol motifs of the protein thioredoxin. The contrast agents showed MR relaxivities typical of gadolinium complexes with a single water molecule coordinated to a Gd3+ center (i.e., ~4.54 mM−1s−1) for both CA1 and CA2 at 60 MHz. The contrast agent CA1 showed a ~140% relaxivity enhancement in the presence of thioredoxin, a finding attributed to a reduction in the flexibility of the molecule after binding to thioredoxin. Support for this rationale...
Source: Molecules - April 1, 2021 Category: Chemistry Authors: Jongeun Kang Eunha Hwang Hyunseung Lee Mi Young Cho Sanu Karan Hak Nam Kim Jong Seung Kim Jonathan L. Sessler Sankarprasad Bhuniya Kwan Soo Hong Tags: Article Source Type: research

Nanomedical Applications of Amphiphilic Dendrimeric Micelles
Curr Med Chem. 2021 Mar 29. doi: 10.2174/0929867328666210329125601. Online ahead of print.ABSTRACTIn recent years, polymeric materials with the ability to self-assemble into micelles have been increasingly investigated for application in various fields, but mainly in biomedicine. Micellar morphology is interesting in the field of drug transport and delivery, since micelles can encapsulate hydrophobic molecules in their nucleus, have active molecules in their outer layer, and due to their nanometric size, can take advantage of the enhanced permeability and retention (EPR) effect, prolong the time in circulation and avoid re...
Source: Current Medicinal Chemistry - March 30, 2021 Category: Chemistry Authors: Guillermo Leobardo Rodr íguez-Acosta Carlos Hern ández-Montalbán Mar ía Fernanda Sabrina Vega-Razo Irving Osiel Castillo-Rodr íguez Marcos Mart ínez-García Source Type: research