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Total 1197 results found since Jan 2013.

Molecules, Vol. 27, Pages 8457: CD70-Targeted Micelles Enhance HIF2 & alpha; siRNA Delivery and Inhibit Oncogenic Functions in Patient-Derived Clear Cell Renal Carcinoma Cells
Molecules, Vol. 27, Pages 8457: CD70-Targeted Micelles Enhance HIF2α siRNA Delivery and Inhibit Oncogenic Functions in Patient-Derived Clear Cell Renal Carcinoma Cells Molecules doi: 10.3390/molecules27238457 Authors: Noah Trac Hyun Seok Oh Leila Izzy Jones Randy Caliliw Shinji Ohtake Brian Shuch Eun Ji Chung The majority of clear cell renal cell carcinomas (ccRCCs) are characterized by mutations in the Von Hippel–Lindau (VHL) tumor suppressor gene, which leads to the stabilization and accumulation of the HIF2α transcription factor that upregulates key oncogenic pat...
Source: Molecules - December 2, 2022 Category: Chemistry Authors: Noah Trac Hyun Seok Oh Leila Izzy Jones Randy Caliliw Shinji Ohtake Brian Shuch Eun Ji Chung Tags: Article Source Type: research

A triazolium-anchored self-immolative linker enables self-assembly-driven siRNA binding and esterase-induced release
Chemistry. 2022 Nov 8. doi: 10.1002/chem.202203311. Online ahead of print.ABSTRACTThe increased importance of RNA-based therapeutics comes with a need to develop next-generation stimuli-responsive systems capable of binding, transporting and releasing RNA oligomers. In this work, we describe triazolium-based amphiphiles capable of siRNA binding and enzyme-responsive release of the nucleic acid payload. In aqueous medium, the amphiphile selfassembles into nanocarriers that can disintegrate upon the addition of esterase. Key to the molecular design is a self-immolative linker that is anchored to the triazolium moiety and act...
Source: Chemistry - November 8, 2022 Category: Chemistry Authors: Selina Hollstein Lamiaa M A Ali Maeva Coste Julian Vogel Nadir Bettache S ébastien Ulrich Max von Delius Source Type: research

Structure-Activity Relationships in Nucleic-Acid-Templated Vectors Based on Peptidic Dynamic Covalent Polymers
We describe the combinations that lead to nucleic acid complexation, in saline buffer, using different templates, from short siRNA to long DNA. Finally, we identify a successful peptidic DCP featuring six-arginine repeating unit that promote the safe and effective delivery of siRNA in live cancer cells.PMID:36342312 | DOI:10.1002/chem.202202921
Source: Chemistry - November 7, 2022 Category: Chemistry Authors: Dan-Dan Su Lamiaa M A Ali Ma ëva Coste Nabila Laroui Yannick Bessin Mihail Barboiu Nadir Bettache Sebastien Ulrich Source Type: research

CC1007, a small molecular compound, suppresses multiple myeloma via upregulation of Nur77
CONCLUSIONS: Since CC1007 demonstrates remarkable anti-MM effect on MM cells, it may be a promising drug for the treatment of MM.PMID:36283176 | DOI:10.1016/j.bioorg.2022.106217
Source: Bioorganic Chemistry - October 25, 2022 Category: Chemistry Authors: Shicong Zhu Cheng Xing Guangsen Zhang Hongling Peng Zhihua Wang Source Type: research

Natural carbazole alkaloid murrayafoline A displays potent anti-neuroinflammatory effect by directly targeting transcription factor Sp1 in LPS-induced microglial cells
Bioorg Chem. 2022 Sep 28;129:106178. doi: 10.1016/j.bioorg.2022.106178. Online ahead of print.ABSTRACTNeuroinflammation is a leading cause for neurological disorders. Carbazole alkaloids, isolated from the medicinal plants of Murraya species (Rutaceae), have exhibited wide pharmacological activities particularly for neuroinflammation. However, its underlying cellular targets and molecular mechanisms still remain unclear. In current study, we found that murrayafoline A (MA), a carbazole alkaloid obtained from Murraya tetramera, potently inhibited the production of neuroinflammation mediators, such as nitric oxide (NO), TNF-...
Source: Bioorganic Chemistry - October 11, 2022 Category: Chemistry Authors: Chao-Hua Li Ying Zhou Peng-Fei Tu Ke-Wu Zeng Yong Jiang Source Type: research

IGT mediated Nanog siRNA delivery in prostate cancer cells improves chemosensitization of Epirubicin in vitro
In this report, we have successfully delivered siRNA against Nanog with the help of pentafluorobenzyl modified Internal Oligo-guanidinium transporter (IGT) that has previously shown promising results in peptide and antisense morpholino delivery. Nanog downregulation in prostate cancer cell line DU145 in serum containing media led to suppression of associated proteins such as KLF4, FAK and cMyc and also enhanced the chemosensitivity of Epirubicin, an anthracycline based drug, in DU145 cells by associated MDR-1 downregulation in vitro. These results show that IGT is a promising candidate for siRNA delivery and its conjugatio...
Source: Bioorganic and Medicinal Chemistry Letters - October 9, 2022 Category: Chemistry Authors: Shalini Gupta Ujjal Das Surajit Sinha Source Type: research

Anti-proliferative tirucallane triterpenoids from gum resin of Boswellia sacra
Bioorg Chem. 2022 Sep 26;129:106155. doi: 10.1016/j.bioorg.2022.106155. Online ahead of print.ABSTRACTEight new tirucallane triterpenoids (1-2, 5-10) along with two known compounds (3-4) were isolated from the gum resin of Boswellia sacra. Their structures were elucidated by extensive physicochemical and spectroscopic analysis, as well as computational calculations, and single crystal X-ray diffraction. Spirosacraoic acid A (1) and B (2), possess an unusual 6/5/6/5 rearranged spirocyclic carbon skeleton. All the isolates were evaluated for their anti-proliferative activity against two tumor cell lines (HepG2 and HCT-116 ce...
Source: Bioorganic Chemistry - October 9, 2022 Category: Chemistry Authors: Bingyang Zhang Di Liu Shijie Cao Tie Yao Guanke Liu Liyi Chen Feng Qiu Source Type: research

IGT mediated Nanog siRNA delivery in prostate cancer cells improves chemosensitization of Epirubicin in vitro
In this report, we have successfully delivered siRNA against Nanog with the help of pentafluorobenzyl modified Internal Oligo-guanidinium transporter (IGT) that has previously shown promising results in peptide and antisense morpholino delivery. Nanog downregulation in prostate cancer cell line DU145 in serum containing media led to suppression of associated proteins such as KLF4, FAK and cMyc and also enhanced the chemosensitivity of Epirubicin, an anthracycline based drug, in DU145 cells by associated MDR-1 downregulation in vitro. These results show that IGT is a promising candidate for siRNA delivery and its conjugatio...
Source: Bioorganic and Medicinal Chemistry Letters - October 9, 2022 Category: Chemistry Authors: Shalini Gupta Ujjal Das Surajit Sinha Source Type: research

Molecules, Vol. 27, Pages 6717: Noncoding RNAs Emerging as Drugs or Drug Targets: Their Chemical Modification, Bio-Conjugation and Intracellular Regulation
n Zhang With the increasing understanding of various disease-related noncoding RNAs, ncRNAs are emerging as novel drugs and drug targets. Nucleic acid drugs based on different types of noncoding RNAs have been designed and tested. Chemical modification has been applied to noncoding RNAs such as siRNA or miRNA to increase the resistance to degradation with minimum influence on their biological function. Chemical biological methods have also been developed to regulate relevant noncoding RNAs in the occurrence of various diseases. New strategies such as designing ribonuclease targeting chimeras to degrade endogenous nonco...
Source: Molecules - October 9, 2022 Category: Chemistry Authors: Jin Wang Tian Tian Xin Li Yan Zhang Tags: Review Source Type: research

Achievements and bottlenecks of PEGylation in nano-delivery systems
This article mainly describes the development background, advantages and applications of PEGylation in the field of drug delivery, its defects or development bottlenecks, and possible alternatives.PMID:36177626 | DOI:10.2174/0929867329666220929152644
Source: Current Medicinal Chemistry - September 30, 2022 Category: Chemistry Authors: Ruoyu Shen Hong Yuan Source Type: research