Journal of Receptors and Signal Transduction最新文献_第2页

Low pH modulates lipopolysaccharide-induced tumor necrosis factor-alpha expression and macropinocytotic activity in RAW264.7 cells. 低pH值可调节脂多糖诱导的RAW264.7细胞中肿瘤坏死因子-α的表达和巨细胞吞噬活性。

IF 2.6 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2024-04-01 Epub Date: 2024-08-22 DOI: 10.1080/10799893.2024.2395310

Miku Otsugu, Ayumi Mine, Izumi Uchida, Yuta Miyake, Ryo Tachihara, Kurumi Fujiwara, Ayako Ichimura, Koichi Sato, Hideaki Tomura

{"title":"Low pH modulates lipopolysaccharide-induced tumor necrosis factor-alpha expression and macropinocytotic activity in RAW264.7 cells.","authors":"Miku Otsugu, Ayumi Mine, Izumi Uchida, Yuta Miyake, Ryo Tachihara, Kurumi Fujiwara, Ayako Ichimura, Koichi Sato, Hideaki Tomura","doi":"10.1080/10799893.2024.2395310","DOIUrl":"10.1080/10799893.2024.2395310","url":null,"abstract":"Inflammation triggers various types of diseases that need to be addressed. Macrophages play important roles in the inflammatory responses. As atherosclerosis progresses, macrophages transform into foam cells. Extracellular acidification is observed at and around bacterial infection and atherosclerotic sites. However, the effects of acidification on the inflammatory response of macrophages and the progression of atherosclerosis have not been fully understood. This study investigates the impact of extracellular acidification on lipopolysaccharide-induced tumor necrosis factor-alpha (TNF-α) expression and macropinocytotic activity in RAW264.7 cells. TNF-α expression is measured by real-time polymerase chain reaction (relative value to glyceraldehyde-3-phosphate dehydrogenase expression). Macropinocytotic activity is measured by neutral red uptake (absorbance at 540 nm). Results show that TNF-α expression increased with decreasing extracellular pH in both un-foamed and foamed cells. Macropinocytotic activity was upregulated at pH 6.8 in un-foamed cells, but downregulated in foamed cells stimulated at low pH. Proton-sensing G protein-coupled receptors (GPCRs) were involved in the expression of TNF-α and in the macropinocytotic activity of foamed cells. In conclusion, this study reveals that extracellular acidification differently affect various inflammatory responses such as LPS-induced TNF-α expression and macropinocytotic activity of RAW264.7 cells and different proton-sensing GPCRs are involved in the different inflammatory responses.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":" ","pages":"63-71"},"PeriodicalIF":2.6,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142036062","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Heat shock protein (Hsp27)-ceramide synthase (Cers1) protein-protein interactions provide a new avenue for unexplored anti-cancer mechanism and therapy. 热休克蛋白（Hsp27）-甘油酰胺合成酶（Cers1）蛋白之间的相互作用为尚未探索的抗癌机制和疗法提供了一条新途径。

IF 2.6 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2024-04-01 Epub Date: 2024-08-27 DOI: 10.1080/10799893.2024.2392711

Musab Ali, Zhichao Zhang, Mahmoud A A Ibrahim, Mahmoud E S Soliman

{"title":"Heat shock protein (Hsp27)-ceramide synthase (Cers1) protein-protein interactions provide a new avenue for unexplored anti-cancer mechanism and therapy.","authors":"Musab Ali, Zhichao Zhang, Mahmoud A A Ibrahim, Mahmoud E S Soliman","doi":"10.1080/10799893.2024.2392711","DOIUrl":"10.1080/10799893.2024.2392711","url":null,"abstract":"Hsp27 is a member of the small heat-shock proteins (sHSPs) - the known cellular line of defence against abnormal protein folding behaviors. Nevertheless, its upregulation is linked to a variety of pathological disorders, including several types of cancers. The ceramide synthases (CerS) mediate the synthesis of ceramide, a critical structural and signaling lipid. Functionally, downstream ceramide metabolites are implicated in the apoptosis process and their abnormal functionality has been linked to anticancer resistance. Studies showed that CerS1 are possibly inhibited by Hsp27 leading to biochemical anticancer effects in vitro. Nevertheless, the nature of such protein-protein interaction (PPI) has not been considerably investigated in molecular terms, hence, we present the first description of the dynamics CerS1-Hsp27 interaction landscapes using molecular dynamics simulations. Time-scale molecular dynamics simulation analysis indicated a system-wide conformational events of decreased stability, increased flexibility, reduced compactness, and decreased folding of CerS1. Analysis of binding energy showed a favorable interaction entailing 56 residues at the interface and a total stabilizing energy of -158 KJ/mol. The CerS1 catalytic domain experienced an opposite trend compared to the protein backbone. Yet, these residues adopted a highly compact conformation as per DCCM and DSSP analysis. Furthermore, conserved residues (SER 212, ASP 213, ALA 240, GLY 243, ASP 319) comprising the substrate shuttling machinery showed notable rigidity implying a restrained ceramide precursor access and assembly; hence, a possible inhibitory mechanism. Findings from this report would streamline a better molecular understanding of CerS1-Hsp27 interactions and decipher its potential avenue toward unexplored anti-cancer mechanisms and therapy.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":" ","pages":"41-53"},"PeriodicalIF":2.6,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142073132","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

The vasodilator effect of Eugenol on uterine artery - potential therapeutic applications in pregnancy-associated hypertension. 丁香酚对子宫动脉的血管扩张作用--在妊娠相关性高血压中的潜在治疗应用。

IF 2.6 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2024-04-01 Epub Date: 2024-08-26 DOI: 10.1080/10799893.2024.2395301

Harithalakshmi Jandhyam, Bimal Prasanna Mohanty, Subas Chandra Parija

{"title":"The vasodilator effect of Eugenol on uterine artery - potential therapeutic applications in pregnancy-associated hypertension.","authors":"Harithalakshmi Jandhyam, Bimal Prasanna Mohanty, Subas Chandra Parija","doi":"10.1080/10799893.2024.2395301","DOIUrl":"10.1080/10799893.2024.2395301","url":null,"abstract":"Preeclampsia, a gestational associated hypertension, has been reported in 6-8% of pregnant women worldwide leading to premature delivery and low birth weight of newborn due to reduced blood flow to placenta. Although several vasodilators (Methyl dopa, hydralazine, β-blockers and diuretics) are currently in use to treat preeclampsia, still there is a search for safer drugs with better efficacy. Lately, antihypertensive vasodilators from natural sources are gaining importance in treating preeclampsia. Eugenol (Eug), a natural essential oil, has been traditionally used in health and food products without any risk. In the present study, ex vivo experiments were designed to examine the vasorelaxation effect of Eug and its signaling pathways in a middle uterine artery (MUA) of pregnant Capra hircus (Ch). In presence of different blockers (L-NAME, indomethacin, ODQ, Ouabain, glibenclamide, 4-AP, Ba2, Carbenoxolone and 18β Glycyrrhetinic acid), Eug-induced concentration-dependent vasorelaxation response was elicited. The results showed that Eug caused a greater vasorelaxation effect in the MU of pregnant animals, which is mediated by potential activation of eNOS, KATP channels, and Kir channels with moderate activation of Na+- K+- ATPase and sGC and MEGJ. These findings provide a strong basis for developing Eug as a therapeutic candidate in the treatment of pregnancy-associated hypertension.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":" ","pages":"54-62"},"PeriodicalIF":2.6,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142055849","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

The roles of angiotensin-converting enzyme 2 inhibitor, melatonin and its agonist on angiotensin II reactivity in intact and denuded rat aortic rings. 血管紧张素转换酶 2 抑制剂、褪黑激素及其激动剂对完整和变性大鼠主动脉环中血管紧张素 II 反应性的作用

IF 2.6 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2024-02-01 Epub Date: 2024-04-26 DOI: 10.1080/10799893.2024.2345907

Nazar M Shareef Mahmood, Almas Mr Mahmud, Ismail M Maulood

{"title":"The roles of angiotensin-converting enzyme 2 inhibitor, melatonin and its agonist on angiotensin II reactivity in intact and denuded rat aortic rings.","authors":"Nazar M Shareef Mahmood, Almas Mr Mahmud, Ismail M Maulood","doi":"10.1080/10799893.2024.2345907","DOIUrl":"10.1080/10799893.2024.2345907","url":null,"abstract":"Background: The pineal product melatonin (MEL) modulates blood vessels through G protein-coupled receptors (GPCRs) called melatonin type 1 receptor (MT1R) and melatonin type 2 receptor (MT2R), in that order. The renin-angiotensin system (RAS), which breaks down angiotensin II (Ang II) to create Ang 1-7, is thought to be mostly controlled by angiotensin-converting enzyme-2 (ACE2).Aim: The current work examines the involvement of ACE2 inhibitor, MEL, and ramelteon (RAM) in the vascular response to Ang II activities in the endothelial denuded (E-) and intact (E+) rat isolated thoracic aortic rings.Method: The isometric tension was measured to evaluate the vascular Ang II contractility using dose response curve (DRC).Results: MEL and RAM caused a rightward shift of Ang II in endothelium E + and endothelium E- aorta.Conclusion: According to the current study, the distribution of MEL receptors and the endothelium's condition are related to the vasomodulatory effect of MEL and ACE2 on Ang II attenuation. These physiological interactions can control vascular tone and increase Ang II reactivity denude endothelial layaer.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":" ","pages":"35-40"},"PeriodicalIF":2.6,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140870521","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

cGAS-STING and PD1/PDL-1 pathway in breast cancer: a window to new therapies. 乳腺癌中的 cGAS-STING 和 PD1/PDL-1 通路：通向新疗法的窗口。

IF 2.6 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2024-02-01 Epub Date: 2024-03-12 DOI: 10.1080/10799893.2024.2325353

Milad Khorasani, Maryam Alaei

引用次数: 0

Mechanistic insights into sodium ion-mediated ligand binding affinity and modulation of 5-HT2B GPCR activity: implications for drug discovery and development. 钠离子介导的配体结合亲和力和 5-HT2B GPCR 活性调节的机理研究：对药物发现和开发的启示。

IF 2.6 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2024-02-01 Epub Date: 2024-03-26 DOI: 10.1080/10799893.2024.2332886

Arushi Chauhan, Jitender Singh, Namrata Sangwan, Pramod K Avti

{"title":"Mechanistic insights into sodium ion-mediated ligand binding affinity and modulation of 5-HT2B GPCR activity: implications for drug discovery and development.","authors":"Arushi Chauhan, Jitender Singh, Namrata Sangwan, Pramod K Avti","doi":"10.1080/10799893.2024.2332886","DOIUrl":"10.1080/10799893.2024.2332886","url":null,"abstract":"Purpose: The G-protein coupled receptor (GPCR) family, implicated in neurological disorders and drug targets, includes the sensitive serotonin receptor subtype, 5-HT2B. The influence of sodium ions on ligand binding at the receptor's allosteric region is being increasingly studied for its impact on receptor structure.Methods: High-throughput virtual screening of three libraries, specifically the Asinex-GPCR library, which contains 8,532 compounds and FDA-approved (2466 compounds) and investigational compounds (2731)) against the modeled receptor [4IB4-5HT2BRM] using the standard agonist/antagonist (Ergotamine/Methysergide), as previously selected from our studies based on ADMET profiling, and further on basis of binding free energy a single compound - dihydroergotamine is chosen.Results: This compound displayed strong interactions with the conserved active site. Ions influence ligand binding, with stronger interactions (3-H-bonds and 1-π-bond around 3.35 Å) observed when an agonist and ions are present. Ions entry is guided by conserved motifs in helices III, IV, and VII, which regulate the receptor. Dihydroergotamine, the selected drug, showed binding variance based on ions presence/absence, affecting amino acid residues in these motifs. DCCM and PCA confirmed the stabilization of ligands, with a greater correlation (∼46.6%-PC1) observed with ions. Dihydroergotamine-modified interaction sites within the receptor necessary for activation, serving as a potential 5HT2BRM agonist. RDF analysis showed the sodium ions density around the active site during dihydroergotamine binding.Conclusion: Our study provides insights into sodium ion mobility's role in controlling ligand binding affinity in 5HT2BR, offering therapeutic development insights.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":" ","pages":"8-18"},"PeriodicalIF":2.6,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140288408","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

The route of autophagy regulation by osteopontin: a review on the linking mechanisms 补骨脂素调控自噬的途径：关联机制综述

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2023-12-11 DOI: 10.1080/10799893.2023.2291563

Zohreh Abdolvahabi, Samira Ezzati-Mobaser, Zahra Hesari

引用次数: 0

Cerebrolysin provides effective protection on high glucose-induced neuropathy in cultured rat dorsal root ganglion neurons 脑蛋白酶能有效保护培养的大鼠背根神经节神经元免受高血糖诱导的神经病变影响

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2023-12-11 DOI: 10.1080/10799893.2023.2291566

Ugur Yazar, Ali Rıza Guvercin, Mahindokht Rouhikia, Mehmet Aktoklu, Mehmet Ali Demirci, Ibrahim Erbay, Ahmet Ayar

引用次数: 0

Verapamil modulates NFAT2 to inhibit tumor growth and potentiates PD1ab immune checkpoint inhibitor therapy in cervical cancer treatment 维拉帕米调节 NFAT2 以抑制肿瘤生长，并增强 PD1ab 免疫检查点抑制剂治疗宫颈癌的效果

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2023-12-09 DOI: 10.1080/10799893.2023.2291562

Yao-Qing Liao, Bin-Bo Fang, Qing-Xia Wu, Wei-Ying Dong, Guan-Ming Deng

引用次数: 0

Synthesis, in silico and in vitro anti-cancer studies of phosphorylated derivatives of didanosine targeting MDA-MB-231 breast cancer cell lines. 针对 MDA-MB-231 乳腺癌细胞系的地达诺辛磷酸化衍生物的合成、硅学和体外抗癌研究。

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2023-12-01 Epub Date: 2024-02-13 DOI: 10.1080/10799893.2024.2303013

S K Thaslim Basha, S Mahaboob Basha, D Subba Rao, S Rasheed, M Varalakshmi, C Naga Raju

引用次数: 0