Journal of Receptors and Signal Transduction最新文献_第3页

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

Exploring the composition of protein-ligand binding sites for cancerous inhibitor of PP2A (CIP2A) by inhibitor guided binding analysis: paving a new way for the Discovery of drug candidates against triple negative breast cancer (TNBC). 通过抑制剂引导结合分析探索 PP2A 癌症抑制剂 (CIP2A) 蛋白质-配体结合位点的组成：为发现治疗三阴性乳腺癌 (TNBC) 的候选药物开辟新途径。

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: 10.1080/10799893.2023.2298903

Oluwayimika Ibitoye, Mahmoud A A Ibrahim, Mahmoud E S Soliman

{"title":"Exploring the composition of protein-ligand binding sites for cancerous inhibitor of PP2A (CIP2A) by inhibitor guided binding analysis: paving a new way for the Discovery of drug candidates against triple negative breast cancer (TNBC).","authors":"Oluwayimika Ibitoye, Mahmoud A A Ibrahim, Mahmoud E S Soliman","doi":"10.1080/10799893.2023.2298903","DOIUrl":"10.1080/10799893.2023.2298903","url":null,"abstract":"Triple-negative breast cancer (TNBC) is associated with high-grade invasive carcinoma leading to a 10% to 15% death rate in younger premenopausal women. Targeting cancerous inhibitors of protein phosphatase (CIP2A) has been a highly effective approach for exploring therapeutic drug candidates. Lapatinib, a dual tyrosine kinase inhibitor, has shown promising inhibition properties by inducing apoptosis in TNBC carcinogenesis in vivo. Despite knowledge of the 3D structure of CIP2A, no reports provide insight into CIP2A ligand binding sites. To this effect, we conducted in silico site identification guided by lapatinib binding. Four of the five sites identified were cross-validated, and the stem domain revealed more excellent ligand binding affinity. The binding affinity of lapatinib in these sites was further computed using the Molecular Mechanics/Poisson-Boltzmann Surface Area (MM/PBSA) approach. According to MM/PBSA//200 ns MD simulations, lapatinib exhibited a higher binding affinity against CIP2A in site 2 with ΔG critical values of -37.1 kcal/mol. The steadiness and tightness of lapatinib with CIP2A inside the stem domain disclosed glutamic acid-318 as the culprit amino acid with the highest electrostatic energy. These results provide clear information on the CIP2A domain capable of ligand binding and validate lapatinib as a promising CIP2A inhibitor in TNBC carcinogenesis.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":" ","pages":"133-143"},"PeriodicalIF":2.8,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139087325","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

New synthetic derivatives of isoindoline-dione: synthesis, neuroprotection assay and impact on the expression level of oxidative stress-related genes in neuronal-like cell line. 异吲哚啉二酮的新合成衍生物：合成、神经保护试验以及对神经元样细胞系中氧化应激相关基因表达水平的影响。

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: 10.1080/10799893.2023.2291559

Abdolrahim Pourparizi, Mina Vazirinia, Fatemeh Pourrajab, Hamid Nadri, Asghar Davood

{"title":"New synthetic derivatives of isoindoline-dione: synthesis, neuroprotection assay and impact on the expression level of oxidative stress-related genes in neuronal-like cell line.","authors":"Abdolrahim Pourparizi, Mina Vazirinia, Fatemeh Pourrajab, Hamid Nadri, Asghar Davood","doi":"10.1080/10799893.2023.2291559","DOIUrl":"10.1080/10799893.2023.2291559","url":null,"abstract":"Purpose: Oxidative stress can damage cells and cause age-related illnesses such as Alzheimer's, Parkinson's, and Huntington's. This study looked at newly synthesized isoindole derivatives and their effects on SH-SY5Y as a neuroblastoma cell under oxidative stress through the NRF2 signaling pathway. NRF2 transcription factor plays a vital role in the oxidative stress response and cellular homeostasis.Method: Three isoindoline-dione derivatives were synthesized by reacting phthalic anhydrides with 4-(2-aminoethyl)-1-benzyl piperidine. Their structures were confirmed through FT-IR, NMR, and Mass spectroscopy. The derivatives were then tested on human SH-SY5Y cells under an oxidative stress model induced by hydrogen peroxide (H2O2). The cell viability, ROS levels, protein carbonyl content, and gene expression of NRF2 and phase II antioxidative enzymes were measured after 24 h.Results: Three isoindoline derivatives (3a-3c) were observed to increase the viability of SH-SY5Y cells by protective against oxidative stress, reducing intracellular reactive oxygen species and carbonylated proteins, and increasing gene expression levels of NRF2 and associated genes such as NQO-1, and GSTK1.Conclusion: Isoindoline derivatives demonstrated a neuroprotective effect on SH-SY5Y cells through various neuroprotective mechanisms, although more studies are needed.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":" ","pages":"123-132"},"PeriodicalIF":2.8,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139545446","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