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Total 1197 results found since Jan 2013.

Molecules, Vol. 25, Pages 5192: Antiglioma Potential of Coumarins Combined with Sorafenib
ubowicz-Gil Coumarins, which occur naturally in the plant kingdom, are diverse class of secondary metabolites. With their antiproliferative, chemopreventive and antiangiogenetic properties, they can be used in the treatment of cancer. Their therapeutic potential depends on the type and location of the attachment of substituents to the ring. Therefore, the aim of our study was to investigate the effect of simple coumarins (osthole, umbelliferone, esculin, and 4-hydroxycoumarin) combined with sorafenib (specific inhibitor of Raf (Rapidly Accelerated Fibrosarcoma) kinase) in programmed death induction in human glioblastom...
Source: Molecules - November 8, 2020 Category: Chemistry Authors: Joanna Sumorek-Wiadro Adrian Zaj ąc Ewa Langner Krystyna Skalicka-Wo źniak Aleksandra Maciejczyk Wojciech Rzeski Joanna Jakubowicz-Gil Tags: Article Source Type: research

In silico and in vitro screening for potential anticancer candidates targeting GPR120.
In this study, a homology model of GPR120S (short isoform) was generated to identify potential anti-cancer compounds targeting the GPR120 receptor using a combined in silico docking-based virtual screening (DBVS), structure-activity relationships (SAR) and in vitro screening approach. SPECS database of synthetic chemical compounds (∼350,000) was screened using the developed GPR120S model to identify molecules binding to the orthosteric binding pocket followed by an AutoDock SMINA rigid-flexible docking protocol. The best 13 hit molecules were then tested in vitro to evaluate their cytotoxic activity against SW480 - human...
Source: Bioorganic and Medicinal Chemistry Letters - November 5, 2020 Category: Chemistry Authors: Pal A, Curtin JF, Kinsella GK Tags: Bioorg Med Chem Lett Source Type: research

Angiotensin AT1 receptor antagonism by losartan stimulates adipocyte browning via induction of apelin Cell Biology
Adipocyte browning appears to be a potential therapeutic strategy to combat obesity and related metabolic disorders. Recent studies have shown that apelin, an adipokine, stimulates adipocyte browning and has negative cross-talk with angiotensin II receptor type 1 (AT1 receptor) signaling. Here, we report that losartan, a selective AT1 receptor antagonist, induces browning, as evidenced by an increase in browning marker expression, mitochondrial biogenesis, and oxygen consumption in murine adipocytes. In parallel, losartan up-regulated apelin expression, concomitant with increased phosphorylation of protein kinase B and AMP...
Source: Journal of Biological Chemistry - October 30, 2020 Category: Chemistry Authors: Dong Young Kim, Mi Jin Choi, Tae Kyung Ko, Na Hyun Lee, Ok-Hee Kim, Hyae Gyeong Cheon Tags: Cell Biology Source Type: research

Regulation of the thrombin/protease-activated receptor 1 axis by chemokine (CXC motif) receptor 4 Cell Biology
The chemokine receptor CXCR4, a G protein–coupled receptor (GPCR) capable of heteromerizing with other GPCRs, is involved in many processes, including immune responses, hematopoiesis, and organogenesis. Evidence suggests that CXCR4 activation reduces thrombin/protease-activated receptor 1 (PAR1)-induced impairment of endothelial barrier function. However, the mechanisms underlying cross-talk between CXCR4 and PAR1 are not well-understood. Using intermolecular bioluminescence resonance energy transfer and proximity ligation assays, we found that CXCR4 heteromerizes with PAR1 in the HEK293T expression system and in human p...
Source: Journal of Biological Chemistry - October 30, 2020 Category: Chemistry Authors: Xianlong Gao, You-Hong Cheng, Garrett A. Enten, Anthony J. DeSantis, Vadim Gaponenko, Matthias Majetschak Tags: Signal Transduction Source Type: research

ASAP Property-Driven Design and Development of Lipids for Efficient Delivery of siRNA
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.0c01407
Source: Journal of Medicinal Chemistry - October 29, 2020 Category: Chemistry Authors: Kumar Rajappan, Steven P. Tanis, Rajesh Mukthavaram, Scott Roberts, Michelle Nguyen, Kiyoshi Tachikawa, Amit Sagi, Marciano Sablad, Pattraranee Limphong, Angel Leu, Hailong Yu, Padmanabh Chivukula, Joseph E. Payne, and Priya Karmali Source Type: research

ASAP Progress in Natural Compounds/siRNA Co-delivery Employing Nanovehicles for Cancer Therapy
ACS Combinatorial ScienceDOI: 10.1021/acscombsci.0c00099
Source: ACS Combinatorial Science - October 23, 2020 Category: Chemistry Authors: Milad Ashrafizadeh, Ali Zarrabi, Kiavash Hushmandi, Farid Hashemi, Ebrahim Rahmani Moghadam, Mehdi Raei, Mahshad Kalantari, Shima Tavakol □, Reza Mohammadinejad■, Masoud Najafi, Franklin R. Tay△, and Pooyan Makvandi▽ Source Type: research

A tubular DNA nanodevice as a siRNA/chemo-drug co-delivery vehicle for combined  cancer therapy.
A tubular DNA nanodevice as a siRNA/chemo-drug co-delivery vehicle for combined cancer therapy. Angew Chem Int Ed Engl. 2020 Oct 21;: Authors: Wang Z, Song L, Liu Q, Tian R, Shang Y, Liu F, Liu S, Zhao S, Han Z, Sun J, Jiang Q, Ding B Abstract Using the DNA origami technique, we constructed a DNA nanodevice functionalized with small interference RNA (siRNA) within its inner cavity and the chemotherapeutic drug doxorubicin (DOX), intercalated in the DNA duplexes. The incorporation of disulfide bonds allows the triggered mechanical opening and release of siRNA in response to intracellular glutathione (...
Source: Angewandte Chemie - October 21, 2020 Category: Chemistry Authors: Wang Z, Song L, Liu Q, Tian R, Shang Y, Liu F, Liu S, Zhao S, Han Z, Sun J, Jiang Q, Ding B Tags: Angew Chem Int Ed Engl Source Type: research

ASAP Characterizing an siRNA-Containing Lipid-Nanoparticle Prepared by a Microfluidic Reactor: Small-Angle X-ray Scattering and Cryotransmission Electron Microscopic Studies
LangmuirDOI: 10.1021/acs.langmuir.0c01079
Source: Langmuir - October 19, 2020 Category: Chemistry Authors: Kenichi Aburai, Kentaro Hatanaka, Shin Takano, Shota Fujii, and Kazuo Sakurai Source Type: research

Branched Antisense and siRNA Co-assembled Nanoplatform for Combined Gene Silencing and Tumor Therapy.
Abstract Chemically modified DNA has been widely developed to fabricate various nucleic acid nanostructures for biomedical applications. Herein, we report a facile strategy for construction of branched antisense DNA and small interfering RNA (siRNA) co-assembled nanoplatform for combined gene silencing in vitro and in vivo. In our design, the branched antisense can efficiently capture siRNA with 3' overhangs through DNA-RNA hybridization. After being equipped with an active targeting group and an endosomal escape peptide by host-guest interaction, the tailored nucleic acid nanostructure functions efficiently as bo...
Source: Angewandte Chemie - October 15, 2020 Category: Chemistry Authors: Liu J, Lu X, Wu T, Wu X, Han L, Ding B Tags: Angew Chem Int Ed Engl Source Type: research

Non-invasive intranasal administration route directly to the brain using dendrimer nanoplatforms: An opportunity to develop new CNS drugs.
Abstract There are several routes of administration to the brain, including intraparenchymal, intraventricular, and subarachnoid injections. The blood-brain barrier (BBB) impedes the permeation and access of most drugs to the central nervous system (CNS), and consequently, many neurological diseases remain undertreated. For past decades, to circumvent this effect, several nanocarriers have been developed to deliver drugs to the brain. Importantly, intranasal (IN) administration can allow direct delivery of drugs into the brain through the anatomical connection between the nasal cavity and brain without crossing th...
Source: European Journal of Medicinal Chemistry - October 11, 2020 Category: Chemistry Authors: Mignani S, Shi X, Karpus A, Majoral JP Tags: Eur J Med Chem Source Type: research

Molecules, Vol. 25, Pages 4591: Magnolol Enhances the Therapeutic Effects of TRAIL through DR5 Upregulation and Downregulation of c-FLIP and Mcl-1 Proteins in Cancer Cells
Kwon Magnolol is a biologically active compound, isolated from the Chinese herb Magnolia, that regulates antiproliferative, anticancer, antiangiogenic and antimetastatic activities. We found that magnolol sensitizes TRAIL-induced apoptotic cell death via upregulation of DR5 and downregulation of cellular FLICE-inhibitory protein (c-FLIP) and Mcl-1 in cancer cells, but not in normal cells. Mechanistically, magnolol increased ATF4-dependent DR5 expression at the transcription level, and knockdown of ATF4 markedly inhibited magnolol-induced DR5 upregulation. Silencing DR5 with siRNA prevented combined treatment with magn...
Source: Molecules - October 8, 2020 Category: Chemistry Authors: Seon Min Woo Kyoung-jin Min Taeg Kyu Kwon Tags: Article Source Type: research

Molecules, Vol. 25, Pages 4136: The Potential Role of Cathepsin K in Non-Small Cell Lung Cancer
Conclusion: Cathepsin K may potentially represent a viable drug target for NSCLC treatment.
Source: Molecules - September 9, 2020 Category: Chemistry Authors: Hui Yang Jasmine Heyer Hui Zhao Shengxian Liang Rui Guo Li Zhong Tags: Article Source Type: research

Phosphorus dendrimers as powerful nanoplatforms for drug delivery, as fluorescent probes and for liposome interaction studies: A concise overview.
Abstract Gene therapy is a new and promising tool to treat many severe diseases and the silencing of proteins is the safest and the most efficient tool to treat diseases because it does not induce changes in human genome and avoids a huge problem encompassing insertional mutagenesis. Using small RNAs to switch on/off target proteins is limited due to existence of some barriers for them in the human body (blood RNAses, serum albumins, cell walls, etc). For therapeutic applications they need the efficient and non-toxic carrier which will deliver them into cell cytoplasm. Within the huge range of carriers available, ...
Source: European Journal of Medicinal Chemistry - August 30, 2020 Category: Chemistry Authors: Shcharbin D, Bryszewska M, Mignani S, Shi X, Majoral JP Tags: Eur J Med Chem Source Type: research

Combined p53- and PTEN-deficiency activates expression of mesenchyme homeobox 1 (MEOX1) required for growth of triple-negative breast cancer Molecular Bases of Disease
In this study, we discovered that combined p53- and PTEN-deficiency in TNBC activates expression of the transcription factor mesenchyme homeobox 1 (MEOX1). We found that MEOX1 is expressed only in TNBC cells with frequent deficiencies in p53 and PTEN, and that its expression is undetectable in luminal A, luminal B, and HER2+ subtypes, as well as in normal breast cells with wild-type (WT) p53 and PTEN. Notably, siRNA knockdown of both p53 and PTEN activated MEOX1 expression in breast cancer cells, whereas individual knockdowns of either p53 or PTEN had only minimal effects on MEOX1 expression. MEOX1 knockdown abolished cell...
Source: Journal of Biological Chemistry - August 20, 2020 Category: Chemistry Authors: Mari Gasparyan, Miao-Chia Lo, Hui Jiang, Chang-Ching Lin, Duxin Sun Tags: Molecular Bases of Disease Source Type: research

The WD40-repeat protein WDR-48 promotes the stability of the deubiquitinating enzyme USP-46 by inhibiting its ubiquitination and degradation Cell Biology
Ubiquitination is a reversible post-translational modification that has emerged as a critical regulator of synapse development and function. However, the mechanisms that regulate the deubiquitinating enzymes (DUBs) responsible for the removal of ubiquitin from target proteins are poorly understood. We have previously shown that the DUB ubiquitin-specific protease 46 (USP-46) removes ubiquitin from the glutamate receptor GLR-1 and regulates its trafficking and degradation in Caenorhabditis elegans. We found that the WD40-repeat proteins WDR-20 and WDR-48 bind and stimulate the catalytic activity of USP-46. Here, we identifi...
Source: Journal of Biological Chemistry - August 13, 2020 Category: Chemistry Authors: Molly Hodul, Rakesh Ganji, Caroline L. Dahlberg, Malavika Raman, Peter Juo Tags: Protein Synthesis and Degradation Source Type: research