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Total 109 results found since Jan 2013.

Molecules, Vol. 25, Pages 645: Discovery of Novel Inhibitors Targeting Multi-UDP-hexose Pyrophosphorylases as Anticancer Agents
In this study, we focused on, among the altered metabolic processes in cancerous cells, altered glycosylation due to its documented roles in cancer tumorigenesis, metastasis and drug resistance. We hypothesize that the enzymes required for the biosynthesis of UDP-hexoses, glycosyl donors for glycan synthesis, could serve as therapeutic targets for cancers. Through structure-based virtual screening and kinetic assay, we identified a drug-like chemical fragment, GAL-012, that inhibit a small family of UDP-hexose pyrophosphorylases-galactose pyro-phosphorylase (GALT), UDP-glucose pyrophosphorylase (UGP2) and UDP-N-acetylgluco...
Source: Molecules - February 2, 2020 Category: Chemistry Authors: Yueqin Yang Hariprasad Vankayalapati Manshu Tang Yingbo Zheng Yingri Li Cong Ma Kent Lai Tags: Article Source Type: research

Molecules, Vol. 24, Pages 4208: Deficiency of Urokinase Plasminogen Activator May Impair β Cells Regeneration and Insulin Secretion in Type 2 Diabetes Mellitus
Conclusion: uPA may play a substantial role in insulin secretion, β cell regeneration, and progressive development of T2DM. Supplementation of uPA might be a novel approach for prevention and treatment of T2DM in the future.
Source: Molecules - November 19, 2019 Category: Chemistry Authors: Wu Ou Chang Lin Pei Chen Tags: Article Source Type: research

Molecules, Vol. 24, Pages 3413: Design of Peptidomimetic Functionalized Cholesterol Based Lipid Nanoparticles for Efficient Delivery of Therapeutic Nucleic Acids
a Baigude Lipid nanoparticles (LNP) are the most potent carriers for the delivery of nucleic acid-based therapeutics. The first FDA approved a short interfering RNA (siRNA) drug that uses a cationic LNP system for the delivery of siRNA against human transthyretin (hTTR). However, preparation of such LNP involves tedious multi-step synthesis with relatively low yields. In the present study, we synthesized cationic peptidomimetic functionalized cholesterol (denote Chorn) in straightforward chemical approaches with high yield. When formulated with helper lipids, Chorn LNPs complexed with siRNA to form nanoparticles with a...
Source: Molecules - September 18, 2019 Category: Chemistry Authors: Ehexige Ehexige Tsogzolmaa Ganbold Xiang Yu Shuqin Han Huricha Baigude Tags: Article Source Type: research

Molecules, Vol. 24, Pages 3287: Site Selective Antibody-Oligonucleotide Conjugation via Microbial Transglutaminase
even F. Dowdy Nucleic Acid Therapeutics (NATs), including siRNAs and AntiSense Oligonucleotides (ASOs), have great potential to drug the undruggable genome. Targeting siRNAs and ASOs to specific cell types of interest has driven dramatic improvement in efficacy and reduction in toxicity. Indeed, conjugation of tris-GalNAc to siRNAs and ASOs has shown clinical efficacy in targeting diseases driven by liver hepatocytes. However, targeting non-hepatic diseases with oligonucleotide therapeutics has remained problematic for several reasons, including targeting specific cell types and endosomal escape. Monoclonal antibody (m...
Source: Molecules - September 9, 2019 Category: Chemistry Authors: Ian J. Huggins Carlos A. Medina Aaron D. Springer Arjen van den Berg Satish Jadhav Xianshu Cui Steven F. Dowdy Tags: Article Source Type: research

Molecules, Vol. 24, Pages 2570: Natural Polysaccharides for siRNA Delivery: Nanocarriers Based on Chitosan, Hyaluronic Acid, and Their Derivatives
Fuente Natural polysaccharides are frequently used in the design of drug delivery systems due to their biocompatibility, biodegradability, and low toxicity. Moreover, they are diverse in structure, size, and charge, and their chemical functional groups can be easily modified to match the needs of the final application and mode of administration. This review focuses on polysaccharidic nanocarriers based on chitosan and hyaluronic acid for small interfering RNA (siRNA) delivery, which are highly positively and negatively charged, respectively. The key properties, strengths, and drawbacks of each polysaccharide are discu...
Source: Molecules - July 14, 2019 Category: Chemistry Authors: In és Serrano-Sevilla Álvaro Artiga Scott G. Mitchell Laura De Matteis Jes ús M. de la Fuente Tags: Review Source Type: research

Molecules, Vol. 24, Pages 2211: Current Aspects of siRNA Bioconjugate for In Vitro and In Vivo Delivery
i Studies on siRNA delivery have seen intense growth in the past decades since siRNA has emerged as a new class of gene therapeutics for the treatment of various diseases. siRNA bioconjugate, as one of the major delivery strategies, offers the potential to enhance and broaden pharmacological properties of siRNA, while minimizing the heterogeneity and stability-correlated toxicology. This review summarizes the recent developments of siRNA bioconjugate, including the conjugation with antibody, peptide, aptamer, small chemical, lipidoid, cell-penetrating peptide polymer, and nanoparticle. These siRNA bioconjugate, either ...
Source: Molecules - June 12, 2019 Category: Chemistry Authors: Wanyi Tai Tags: Review Source Type: research

Molecules, Vol. 24, Pages 2079: Novel pH Selective, Highly Lytic Peptides Based on a Chimeric Influenza Hemagglutinin Peptide/Cell Penetrating Peptide Motif
as J. Tucker Delivery of macromolecular cargos such as siRNA to the cytosol after endocytosis remains a critical challenge. Numerous approaches including viruses, lipid nanoparticles, polymeric constructs, and various peptide-based approaches have yet to yield a general solution to this delivery issue. In this manuscript, we describe our efforts to design novel endosomolytic peptides that could be used to facilitate the release of cargos from a late endosomal compartment. These amphiphilic peptides, based on a chimeric influenza hemagglutinin peptide/cell-penetrating peptide (CPP) template, utilize a pH-triggering mech...
Source: Molecules - May 30, 2019 Category: Chemistry Authors: Bethany Algayer Ann O ’Brien Aaron Momose Dennis J. Murphy William Procopio David M. Tellers Thomas J. Tucker Tags: Article Source Type: research

Molecules, Vol. 24, Pages 1829: RA-XII Suppresses the Development and Growth of Liver Cancer by Inhibition of Lipogenesis via SCAP-dependent SREBP Supression
Mao Tan Lipogenesis plays a critical role in the growth and metastasis of tumors, which is becoming an attractive target for anti-tumor drugs. RA-XII, one of the cyclopeptide glycosides isolated from Rubia yunnanensis, exerts anti-tumor effects on liver cancer. However, the underlying mechanisms are not clear. In the present study, the effects of RA-XII on lipogenesis were evaluated and the underlying mechanisms were investigated. The results indicated that RA-XII strongly inhibited tumor growth and lipogenesis (triglycerides and lipid droplets) in HepG2 cells, and the expression of key factors involved in lipog...
Source: Molecules - May 11, 2019 Category: Chemistry Authors: Guo Wang Wang Song Wang Mao Tan Tags: Article Source Type: research

Molecules, Vol. 24, Pages 1377: Regulation of the Nrf2 Pathway by Glycogen Synthase Kinase-3 β in MPP+-Induced Cell Damage
Molecules, Vol. 24, Pages 1377: Regulation of the Nrf2 Pathway by Glycogen Synthase Kinase-3β in MPP+-Induced Cell Damage Molecules doi: 10.3390/molecules24071377 Authors: Armagan Sevgili Gürkan Köse Bilgiç Dagcı Saso Recently, nuclear translocation and stability of nuclear factor erythroid 2 (NF-E2)-related factor 2 (Nrf2) have gained increasing attention in the prevention of oxidative stress. The present study was aimed to evaluate the regulatory role of glycogen synthase kinase-3β (GSK-3β) inhibition by tideglusib through the Nrf2 pathway in a cellular damage mod...
Source: Molecules - April 7, 2019 Category: Chemistry Authors: Armagan Sevgili G ürkan K öse Bilgi ç Dagc ı Saso Tags: Article Source Type: research

Molecules, Vol. 24, Pages 225: S-Acyl-2-Thioethyl: A Convenient Base-Labile Protecting Group for the Synthesis of siRNAs Containing 5 ′-Vinylphosphonate
Molecules, Vol. 24, Pages 225: S-Acyl-2-Thioethyl: A Convenient Base-Labile Protecting Group for the Synthesis of siRNAs Containing 5′-Vinylphosphonate Molecules doi: 10.3390/molecules24020225 Authors: Mehran Nikan Wenyu Li Garth A. Kinberger Punit P. Seth Eric E. Swayze Thazha P. Prakash We recently reported that (E)-5′-vinylphosphonate (5′-VP) is a metabolically-stable phosphate mimic for siRNA and demonstrated that 5′-VP improves the potency of the fully modified siRNAs in vivo. Here, we report an alternative synthesis of 5′-VP modified guide st...
Source: Molecules - January 9, 2019 Category: Chemistry Authors: Mehran Nikan Wenyu Li Garth A. Kinberger Punit P. Seth Eric E. Swayze Thazha P. Prakash Tags: Article Source Type: research

Molecules, Vol. 23, Pages 3306: 23-Hydroxyursolic Acid Isolated from the Stem Bark of Cussonia bancoensis Induces Apoptosis through Fas/Caspase-8-Dependent Pathway in HL-60 Human Promyelocytic Leukemia Cells
san Kyung-Tae Lee The natural product 23-hydroxyursolic acid (23-HUA) is a derivative of ursolic acid, which is known to induce cancer cell apoptosis. However, apoptotic effects and mechanisms of 23-HUA have not been well characterized yet. Herein, we investigated the molecular mechanisms of 23-HUA-induced apoptosis in HL-60 human promyelocytic leukemia cells. 23-HUA-treated HL-60 cells showed apoptotic features including internucleosomal DNA condensation and fragmentation as well as externalization of phosphatidylserine residues. 23-HUA induced a series of mitochondrial events including disruption of mitochondrial m...
Source: Molecules - December 13, 2018 Category: Chemistry Authors: Jong-Heon Won Kyung-Sook Chung Eun-Young Park Jeong-Hun Lee Jung-Hye Choi Leon Azefack Tapondjou Hee-Juhn Park Masaaki Nomura Ahmed H.E. Hassan Kyung-Tae Lee Tags: Article Source Type: research

Molecules, Vol. 23, Pages 3209: Aquaporin 11-Dependent Inhibition of Proliferation by Deuterium Oxide in Activated Hepatic Stellate Cells
Pyo Kim Deuterium oxide (D2O) has been reported to be active toward various in vitro cell lines in combination with phytochemicals. Our objective was to describe, for the first time, the effect of D2O on the proliferation of hepatic stellate cells (HSCs). After D2O treatment, the p53-cyclin-dependent kinase (CDK) pathway was stimulated, leading to inhibition of the proliferation of HSCs and an increase in the [ATP]/[ADP] ratio. We also evaluated the role of aquaporin (AQP) 11 in activated HSCs. We found that D2O treatment decreased AQP11 expression levels. Of note, AQP11 levels elevated by a genetic approach counteract...
Source: Molecules - December 5, 2018 Category: Chemistry Authors: Phil Jun Lee Hye-Jin Park Namki Cho Hong Pyo Kim Tags: Article Source Type: research

Molecules, Vol. 23, Pages 2884: Identification and Characterization of NTB451 as a Potential Inhibitor of Necroptosis
Tae-Bong Kang Necroptosis, or caspase-independent programmed cell death, is known to be involved in various pathological conditions, such as ischemia/reperfusion injury, myocardial infarction, atherosclerosis, and inflammatory bowel diseases. Although several inhibitors of necroptosis have been identified, none of them are currently in clinical use. In the present study, we identified a new compound, 4-({[5-(4-aminophenyl)-4-ethyl-4H-1,2,4-triazol-3-yl]sulfanyl}methyl)-N-(1,3-thiazol-2-yl) benzamide (NTB451), with significant inhibitory activity on the necroptosis induced by various triggers, such as tumor necrosis fac...
Source: Molecules - November 5, 2018 Category: Chemistry Authors: Eun-Jung In Yuno Lee Sushruta Koppula Tae-Yeon Kim Jun-Hyuk Han Kwang-Ho Lee Tae-Bong Kang Tags: Article Source Type: research

Molecules, Vol. 23, Pages 2833: 3,5-Diethoxy-3 ′-Hydroxyresveratrol (DEHR) Ameliorates Liver Fibrosis via Caveolin-1 Activation in Hepatic Stellate Cells and in a Mouse Model of Bile Duct Ligation Injury
Molecules, Vol. 23, Pages 2833: 3,5-Diethoxy-3′-Hydroxyresveratrol (DEHR) Ameliorates Liver Fibrosis via Caveolin-1 Activation in Hepatic Stellate Cells and in a Mouse Model of Bile Duct Ligation Injury Molecules doi: 10.3390/molecules23112833 Authors: Phil Jun Lee Hye-Jin Park Namki Cho Hong Pyo Kim Hepatic stellate cells (HSCs) are involved in the pathogenesis of liver fibrosis. Resveratrol, 3,5,4′-trihydroxystilbene, is a dietary polyphenol found in natural food products. Here, we evaluated the anti-proliferative effects of a synthetic resveratrol derivative, 3,5-diethoxy-3′-h...
Source: Molecules - October 31, 2018 Category: Chemistry Authors: Phil Jun Lee Hye-Jin Park Namki Cho Hong Pyo Kim Tags: Article Source Type: research

Molecules, Vol. 23, Pages 2828: 8e Protects against Acute Cerebral Ischemia by Inhibition of PI3K γ-Mediated Superoxide Generation in Microglia
Molecules, Vol. 23, Pages 2828: 8e Protects against Acute Cerebral Ischemia by Inhibition of PI3Kγ-Mediated Superoxide Generation in Microglia Molecules doi: 10.3390/molecules23112828 Authors: Linna Wang Xiaoli Wang Tingting Li Yihua Zhang Hui Ji The inflammatory response mediated by microglia plays a critical role in the progression of ischemic stroke. Phosphoinositide 3-kinase gamma (PI3Kγ) has been implicated in multiple inflammatory and autoimmune diseases, making it a promising target for therapeutic intervention. The aim of this study was to evaluate the efficacy of 8e, a hydrogen sulfi...
Source: Molecules - October 31, 2018 Category: Chemistry Authors: Linna Wang Xiaoli Wang Tingting Li Yihua Zhang Hui Ji Tags: Article Source Type: research