Search results for: Receptor
#34118788 2021/06/06 To Up
Design, synthesis, and biological evaluation of novel bifunctional thyrointegrin antagonists for neuroblastoma.Receptor-mediated cancer therapy has received much attention in the last few decades. Neuroblastoma and other cancers of the sympathetic nervous system highly express norepinephrine transporter (NET) and cell plasma membrane integrin Î±vÎ²3. Dual targeting of the NET and integrin Î±vÎ²3 receptors using a Drug-Drug Conjugate (DDC) might provide effective treatment strategy in the fight against neuroblastoma and other neuroendocrine tumors. In this work, we synthesized three dual-targeting BG-P-TAT derivatives, dI-BG-P-TAT, dM-BG-P-TAT, and BG-P-PAT containing di-iodobenzene, di-methoxybenzene, and piperazine groups, respectively. These derivatives utilize to norepinephrine transporter (NET) and the integrin Î±vÎ²3 receptor to simultaneously modulate both targets based on evaluation in a neuroblastoma animal model using the neuroblastoma SK-N-F1 cell line. Among the three synthesized agents, the piperazine substituted BG-P-PAT exhibited potent integrin Î±vÎ²3 antagonism and reduced neuroblastoma tumor growth and cancer cell viability by >90%. In conclusion, BG-P-PAT and derivatives represent a potential therapeutic approach in the management of neuroblastoma.
Ozlem Ozen Karakus, Kavitha Godugu, Kazutoshi Fujioka, Shaker A Mousa
1696 related Products with: Design, synthesis, and biological evaluation of novel bifunctional thyrointegrin antagonists for neuroblastoma.100ul10 mg10 ug 1000 ml 1 mg 1 G25 Rxns Kit100 ml100ul
#34118770 2021/06/09 To Up
Clinical benefits of precision medicine in treating solid cancers: European Society of Medical Oncology-Magnitude of Clinical Benefit Scale score-based analysis.Precision and matched cancer medicine has the potential to complement the existing biomarker approaches in cancer treatment. However, despite their promising potential, certain negative results have highlighted their limitations in molecular biology-driven treatment strategies. This study aimed to evaluate the clinical benefits of precision therapies.
Y Hibino, M Ito, T Satake, S Kondo
1423 related Products with: Clinical benefits of precision medicine in treating solid cancers: European Society of Medical Oncology-Magnitude of Clinical Benefit Scale score-based analysis.
#34118723 2021/05/24 To Up
Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARÎ³ with potential anti-diabetic efficacy.Peroxisome proliferator-activated receptor gamma (PPARÎ³) is a valuable drug target for diabetic treatment and ligands of PPARÎ³ have shown potent anti-diabetic efficacy. However, to overcome the severe side effects of current PPARÎ³-targeted drugs, novel PPARÎ³ ligands need to be developed. Sulindac, an identified ligand of PPARÎ³, is widely used in clinic as a non-steroidal anti-inflammatory drug. To explore its potential application for diabetes, we designed and synthesized a series of sulindac derivatives to investigate their structure-activity relationship as PPARÎ³ ligand and potential anti-diabetic effect. We found that meta-substitution in sulindac's benzylidene moiety was beneficial to PPARÎ³ binding and transactivation. Z rather than E configuration of the benzylidene double bond endowed derivatives with the selectivity of PPARÎ³ activation. The indene fluorine is essential for binding and regulating PPARÎ³. Compared with rosiglitazone, compound 6b with benzyloxyl meta-substitution and Z benzylidene double bond weakly induced adipogenesis and PPARÎ³-targeted gene expression. However, 6b potently improved glucose tolerance in a diabetic mice model. Unlike rosiglitazone, 6b was devoid of apparent toxicity to osteoblastic formation. Thus, we provided some useful guidelines for PPARÎ³-based optimization of sulindac and an anti-diabetic lead compound with less side effects.
Fengyu Huang, Zhiping Zeng, Weidong Zhang, Zhiqiang Yan, Jiayun Chen, Liangfa Yu, Qian Yang, Yihuan Li, Hongyu Yu, Junjie Chen, Caisheng Wu, Xiao-Kun Zhang, Ying Su, Hu Zhou
2825 related Products with: Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARÎ³ with potential anti-diabetic efficacy.100μl100ug100ug Lyophilized100ug Lyophilized100ul100ug Lyophilized100ug100 ul
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#34118720 2021/05/20 To Up
Benzofuranyl-2-imidazoles as imidazoline I receptor ligands for Alzheimer's disease.Recent findings unveil the pharmacological modulation of imidazoline I receptors (I-IR) as a novel strategy to face unmet medical neurodegenerative diseases. In this work, we report the chemical characterization, three-dimensional quantitative structure-activity relationship (3D-QSAR) and ADMET in silico of a family of benzofuranyl-2-imidazoles that exhibit affinity against human brain I-IR and most of them have been predicted to be brain permeable. Acute treatment in mice with 2-(2-benzofuranyl)-2-imidazole, known as LSL60101 (garsevil), showed non-warning properties in the ADMET studies and an optimal pharmacokinetic profile. Moreover, LSL60101 induced hypothermia in mice while decreased pro-apoptotic FADD protein in the hippocampus. InÂ vivo studies in the familial Alzheimer's disease 5xFAD murine model with the representative compound, revealed significant decreases in the protein expression levels of antioxidant enzymes superoxide dismutase and glutathione peroxidase in hippocampus. Overall, LSL60101 plays a neuroprotective role by reducing apoptosis and modulating oxidative stress.
Sergio Rodriguez-ArÃ©valo, Andrea BagÃ¡n, Christian GriÃ±Ã¡n-FerrÃ©, Foteini Vasilopoulou, MercÃ¨ PallÃ s, Iria Brocos-Mosquera, Luis F Callado, M Isabel Loza, AntÃ³n L MartÃnez, JosÃ© Brea, BelÃ©n PÃ©rez, Elies Molins, Steven De Jonghe, Dirk Daelemans, Milica Radan, Teodora Djikic, Katarina Nikolic, Elena HernÃ¡ndez-HernÃ¡ndez, M Julia GarcÃa-Fuster, JesÃºs A GarcÃa-Sevilla, Carmen Escolano
2887 related Products with: Benzofuranyl-2-imidazoles as imidazoline I receptor ligands for Alzheimer's disease.96 tests96 tests96 tests96 tests100 assays200 assays
#34118667 2021/05/29 To Up
A sensing network involving citizens for high spatio-temporal resolution monitoring of fugitive emissions from a petroleum pre-treatment plant.In this study an innovative sensing network consisting of eight photoionization detectors, meteorological sensors, a video camera and a telephonic system able to systematize the population complaints was developed for the monitoring of odor emissions. The development of monitoring approaches with high temporal and spatial resolution and actively involving citizens, is strategic in areas where relevant and also short-term emissive events frequently occur and the conventional approaches fail due to the high variability of fugitive emissions. Moreover, even if unpleasant odors are not necessarily direct triggers of health effects, they could be associated with the release of other harmful compounds. Monitoring approaches also involving citizens are thus strategic tools because odors annoyance perceived by population may be a potential health risk warning. Therefore, the developed sensing network was set up in Val d'Agri (Basilicata, Italy) where a petroleum pre-treatment plant (COVA) rises in a rural and inhabited area. The data collected during the monitoring campaign from the 16th February to the 30th July 2017, showed Total Volatile Organic Compounds (TVOCs) concentrations decreasing moving away from the plant and up to five times higher than levels registered in the closest municipality (Viggiano). Moreover, recurrent short-term critical events characterized by concentration values far above the average of the period and with maximum values ranging from 0.92 to 1.89 ppm, were registered in correspondence with high levels of benzene (up to 23.9 Î¼g/m) and anemometric conditions able to transport pollutants from COVA to each receptor site. The spatial and temporal distribution of TVOC concentrations proved to be affected by the distance from COVA, wind direction and industrial activities verified using video reportage and citizen claims. Therefore, the developed approach has proven to be a useful tool to credit people's perception of odors and also to quantify citizen exposure to VOCs during short-term events.
Alessia Di Gilio, Jolanda Palmisani, Stefania Petraccone, Gianluigi de Gennaro
2902 related Products with: A sensing network involving citizens for high spatio-temporal resolution monitoring of fugitive emissions from a petroleum pre-treatment plant.2 Pieces/Box4 Membranes/Box250 mg2 Pieces/Box1ml100ug Lyophilized
#34118640 2021/05/23 To Up
OXTR moderates adverse childhood experiences on depressive symptoms among incarcerated males.This study examined the moderation of an oxytocin receptor (OXTR) gene in the link between childhood adversity and depressive symptoms among incarcerated males.
Jieting Zhang, Cuimei Yang, Junhui Leng, Jinting Liu, Pingyuan Gong, Gianluca Esposito
1455 related Products with: OXTR moderates adverse childhood experiences on depressive symptoms among incarcerated males.100 μg 2 ml Ready-to-use 2 25 ml Ready-to-use 25 MG 6 ml 1 mg 2 ml Ready-to-use 0.2 mg 6 ml Ready-to-use 100.00 ug 25 ml Ready-to-use
#34118637 2021/06/02 To Up
Differential lncRNA expression profiling of cognitive function in middle and old aged monozygotic twins using generalized association analysis.Cognitive impairment is the most prominent symptom in neurodegenerative disorders affecting quality of life and mortality. However, despite years of research, the molecular mechanism underlying the regulation of cognitive function and its impairment is poorly understood. This study aims to elucidate the role of long non-coding RNAs (lncRNAs) expression and lncRNA-mRNA interaction networks, by analyzing lncRNA expression in whole blood samples of 400 middle and old aged monozygotic twins in association with cognitive function using both linear models and a generalized correlation coefficient (GCC) to capture the diverse patterns of correlation. We detected 13 probes (pÂ <Â 1e-03) displaying nonlinear and 7 probes (pÂ <Â 1e-03) showing linear correlations. After combining the results, we identified 20 lncRNA probes with pÂ <Â 1e-03. The top lncRNA probes were annotated to genes, along with the non-coding MALAT1, that play roles in neurodegenerative diseases. The top lncRNAs were linked to functional clusters including peptidyl-glycine modification, vascular smooth muscle cells, mitotic spindle organization and protein tyrosine phosphatase. In addition, mapping of the top significant lncRNAs to the lncRNA-mRNA interaction network detected significantly enriched biological pathways involving neuroactive ligand-receptor interaction, proteasome and chemokines. We show that GCC served as a complementary approach in detecting lncRNAs missed by the conventional linear models. A combination of GCC and linear models identified lncRNAs of diverse patterns of association enriched for GO biological and molecular functions meaningful in cognitive performance and cognitive decline. The novel lncRNA regulatory network further contributed to detect significant pathways implicated in cognition.
Afsaneh Mohammadnejad, Jan Baumbach, Weilong Li, Jesper Lund, Martin J Larsen, Shuxia Li, Jonas Mengel-From, Tanja Maria Michel, Lene Christiansen, Kaare Christensen, Jacob Hjelmborg, Qihua Tan
1271 related Products with: Differential lncRNA expression profiling of cognitive function in middle and old aged monozygotic twins using generalized association analysis.300 units12100 μg1 Set
#34118596 2021/05/31 To Up
Apolipoprotein A-I mimetic peptide inhibits atherosclerosis by increasing tetrahydrobiopterin via regulation of GTP-cyclohydrolase 1 and reducing uncoupled endothelial nitric oxide synthase activity.The apolipoprotein A-I mimetic peptide D-4F, among its anti-atherosclerotic effects, improves vasodilation through mechanisms not fully elucidated yet.
Da-Sheng Ning, Jian Ma, Yue-Ming Peng, Yan Li, Ya-Ting Chen, Shang-Xuan Li, Zui Liu, Yu-Quan Li, Yi-Xin Zhang, Yu-Peng Jian, Zhi-Jun Ou, Jing-Song Ou
1714 related Products with: Apolipoprotein A-I mimetic peptide inhibits atherosclerosis by increasing tetrahydrobiopterin via regulation of GTP-cyclohydrolase 1 and reducing uncoupled endothelial nitric oxide synthase activity.100 96tests100 100 100ug Lyophilized100ug Lyophilized100ug Lyophilized 1 mg 100ug Lyophilized100ug Lyophilized50 ug
#34118565 2021/06/05 To Up
Metabolic maturation of differentiating cardiosphere-derived cells.Cardiosphere-derived cells (CDCs) can be expanded in vitro and induced to differentiate along the cardiac lineage. To recapitulate the phenotype of an adult cardiomyocyte, differentiating progenitors need to upregulate mitochondrial glucose and fatty acid oxidation. Here we cultured and differentiated CDCs using protocols aimed to maintain stemness or to promote differentiation, including triggering fatty acid oxidation using an agonist of peroxisome proliferator-activated receptor alpha (PPARÎ±). Metabolic changes were characterised in undifferentiated CDCs and during differentiation towards a cardiac phenotype. CDCs from rat atria were expanded on fibronectin or collagen IV via cardiosphere formation. Differentiation was assessed using flow cytometry and qPCR and substrate metabolism was quantified using radiolabelled substrates. Collagen IV promoted proliferation of CDCs whereas fibronectin primed cells for differentiation towards a cardiac phenotype. In both populations, treatment with 5-Azacytidine induced a switch towards oxidative metabolism, as shown by changes in gene expression, decreased glycolytic flux and increased oxidation of glucose and palmitate. Addition of a PPARÎ± agonist during differentiation increased both glucose and fatty acid oxidation and expression of cardiac genes. We conclude that oxidative metabolism and cell differentiation act in partnership with increases in one driving an increase in the other.
Khadijeh Kathy Pakzad, Jun Jie Tan, Stephanie Anderson, Mary Board, Kieran Clarke, Carolyn A Carr4 x 96-well plate1.00 flask1.00 flask100 µg2ug25ml96T1.5x10(6) cells100 U215ml
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