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https://www.readbyqxmd.com/read/29929115/matched-pair-86-y-90-y-labeled-bivalent-rgd-bombesin-antagonist-rgd-glu-do3a-6-ahx-rm2-as-a-potential-theranostic-agent-for-prostate-cancer
#1
Nilantha Bandara, Tamila J Stott Reynolds, Rebecca Schehr, Rajendra P Bandari, Philipp J Diebolder, Stephanie Krieger, Jingli Xu, Yubin Miao, Buck E Rogers, Charles J Smith
INTRODUCTION: In this study, we describe development of a true matched-pair theranostic agent that is able to target the αV β3 integrin and the gastrin releasing peptide receptor (GRPR). We herein describe methods to metallate and characterize the new conjugate and to validate its biological efficacy by in vitro and in vivo methods. METHODS: We have previously described the development of [RGD-Glu-6Ahx-RM2] (where RGD: Arg-Gly-Asp; Glu: glutamic acid; 6-Ahx: 6-amino hexanoic acid; RM2: (D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2)) that has been conjugated to a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) bifunctional chelating agent (BFCA) to afford [RGD-Glu-[DO3A]-6-Ahx-RM2] peptide...
June 8, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29928964/spinal-interleukin-10-produces-antinociception-in-neuropathy-through-microglial-%C3%AE-endorphin-expression-separated-from-antineuroinflammation
#2
Hai-Yun Wu, Xiao-Fang Mao, Xue-Qi Tang, Usman Ali, Evhy Apryani, Hao Liu, Xin-Yan Li, Yong-Xiang Wang
Interleukin 10 (IL-10) is antinociceptive in various animal models of pain without induction of tolerance, and its mechanism of action was generally believed to be mediated by inhibition of neuroinflammation. Here we reported that intrathecal IL-10 injection dose dependently attenuated mechanical allodynia and thermal hyperalgesiain male and female neuropathic rats, with ED50 values of 40.8 ng and 24 ng, and Emax values of 61.5% MPE and 100% MPE in male rats. Treatment with IL-10 specifically increased expression of the β-endorphin (but not prodynorphin) gene and protein in primary cultures of spinal microglia but not in astrocytes or neurons...
June 18, 2018: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/29928931/oxytocin-alters-the-morphology-of-hypothalamic-neurons-via-the-transcription-factor-myocyte-enhancer-factor-2a-mef-2a
#3
Magdalena Meyer, Ilona Berger, Julia Winter, Benjamin Jurek
Oxytocin (OT) has gained attention not only as anxiolytic drug and as potential treatment option for autistic children; it also acts as a growth and differentiation factor in neuronal cells. While behavioral effects of OT have been studied in detail, knowledge about the cellular effects of OT is relatively sparse. In this study, we present evidence for three hypotheses: 1) OT leads to neurite retraction in hypothalamic neurons via the OT receptor (OTR) 2) The transcription factor MEF-2A is a central regulator of OT-induced neurite retraction, and 3) The MAPK pathway is critical for OT-induced MEF-2A activation...
June 18, 2018: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/29928875/trpv4-promotes-the-migration-and-invasion-of-glioma-cells-via-akt-rac1-signaling
#4
Qing Ou-Yang, Bing Li, Minhui Xu, Hong Liang
Experimental evidence indicates a critical role of TRPV4 (Transient Receptor Potential Vanilloid 4) in controlling the cell migratory activity of multiple tumors. However, the oncogenic role of TRPV4 in glioma still remains elusive. In this study, we tried to investigate the oncogenic role of TRPV4 in glioma. We found that the expression levels of TRPV4 were upregulated in glioma and the high levels of TRPV4 indicated a worse prognosis in patients with glioma. TRPV4 was critical for glioma migration and invasion: activating TRPV4 by agonist GSK1016790 A enhanced glioma migration and invasion, while, the specific TRPV4 antagonist HC-067047 suppressed glioma migration and invasion...
June 19, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29928508/a-parthenogenetic-quasi-program-causes-teratoma-like-tumors-during-aging-in-wild-type-c-elegans
#5
Hongyuan Wang, Yuan Zhao, Marina Ezcurra, Alexandre Benedetto, Ann F Gilliat, Josephine Hellberg, Ziyu Ren, Evgeniy R Galimov, Trin Athigapanich, Johannes Girstmair, Maximilian J Telford, Colin T Dolphin, Zhizhou Zhang, David Gems
A long-standing belief is that aging (senescence) is the result of stochastic damage accumulation. Alternatively, senescent pathology may also result from late-life, wild-type gene action (i.e., antagonistic pleiotropy, as argued by Williams) leading to non-adaptive run-on of developmental programs (or quasi-programs ) (as suggested more recently by Blagosklonny). In this study, we use existing and new data to show how uterine tumors, a prominent form of senescent pathology in the nematode Caenorhabditis elegans , likely result from quasi-programs...
2018: NPJ Aging and Mechanisms of Disease
https://www.readbyqxmd.com/read/29928441/the-upregulated-expression-of-vascular-endothelial-growth-factor-in-surgically-treated-patients-with-recurrent-radioresistant-cervical-cancer-of-the-uterus
#6
Kosuke Yoshida, Shiro Suzuki, Jun Sakata, Fumi Utsumi, Kaoru Niimi, Nobuhisa Yoshikawa, Kimihiro Nishino, Kiyosumi Shibata, Fumitaka Kikkawa, Hiroaki Kajiyama
Vascular endothelial growth factor (VEGF) inhibitors have been utilized for the treatment against advanced or recurrent cervical carcinoma as a novel therapeutic modality. However, the expression level of VEGF in post-radiotherapy relapsed/persistent cervical cancer remains to be elucidated. The aim of the present study was to investigate the expression of VEGF and associated molecules using tumor samples from patients with post-radiotherapy relapsed/persistent cervical cancer. From a database of 826 patients who were treated at our institution between 2003 and 2015, eight patients with post-radiotherapy relapsed/persistent cervical cancer were identified, and 20 patients who underwent initial surgery alone were used as a control...
July 2018: Oncology Letters
https://www.readbyqxmd.com/read/29928342/quercetin-induced-apoptosis-of-human-oral-cancer-sas-cells-through-mitochondria-and-endoplasmic-reticulum-mediated-signaling-pathways
#7
Yi-Shih Ma, Chien-Ning Yao, Hsin-Chung Liu, Fu-Shun Yu, Jen-Jyh Lin, Kung-Wen Lu, Ching-Lung Liao, Fu-Shin Chueh, Jing-Gung Chung
Oral cancer is a cause of cancer-associated mortality worldwide and the treatment of oral cancer includes radiation, surgery and chemotherapy. Quercetin is a component from natural plant products and it has been demonstrated that quercetin is able to induce cytotoxic effects through induction of cell apoptosis in a number of human cancer cell lines. However, there is no available information to demonstrate that quercetin is able to induce apoptosis in human oral cancer cells. In the present study, the effect of quercetin on the cell death via the induction of apoptosis in human oral cancer SAS cells was investigated using flow cytometry, Annexin V/propidium iodide (PI) double staining, western blotting and confocal laser microscopy examination, to test for cytotoxic effects at 6-48 h after treatment with quercetin...
June 2018: Oncology Letters
https://www.readbyqxmd.com/read/29928315/non-vitamin-k-antagonist-oral-anticoagulant-after-acute-coronary-syndrome-is-there-a-role
#8
REVIEW
Paul Guedeney, Birgit Vogel, Roxana Mehran
Despite dual antiplatelet therapy (DAPT) including potent P2Y12 inhibitors, recurrent ischaemic events occur in a significant number of patients after acute coronary syndrome (ACS), warranting new antithrombotic strategies. Combinations of non-vitamin K antagonist oral anticoagulant (NOAC) with antiplatelet therapy have been tested in several large phases II and III randomised trials. Overall, current evidence suggests that the use of NOACs on top of DAPT after ACS reduces the rate of recurrent ischaemic events, albeit at the price of increased risk for major bleeding...
May 2018: Interventional Cardiology
https://www.readbyqxmd.com/read/29928125/graft-outcomes-following-immunosuppressive-therapy-with-different-combinations-in-kidney-transplant-recipients-a-nationwide-cohort-study
#9
Yung-Fong Tsai, Fu-Chao Liu, Chang-Fu Kuo, Ting-Ting Chung, Huang-Ping Yu
Background: Immunosuppression plays an essential role to overcome immune-related allograft rejection, but it also causes some nephrotoxicity. This study aimed to investigate how the immunosuppressant combinations affect graft outcomes in kidney transplant recipients. Methods: A nationwide population-based cohort study using the Taiwan National Health Insurance Database was conducted. A total of 3,441 kidney transplant recipients who underwent kidney transplantation during the targeted period were included...
2018: Therapeutics and Clinical Risk Management
https://www.readbyqxmd.com/read/29928118/inhaled-glycopyrrolate-for-the-treatment-of-chronic-obstructive-pulmonary-disease
#10
REVIEW
Donald P Tashkin, Nicholas J Gross
Long-acting muscarinic antagonists (LAMAs), along with long-acting β2 -agonists (LABAs), are the mainstay for treatment of patients with COPD. Glycopyrrolate, or glycopyrronium bromide, like other LAMAs, inhibits parasympathetic nerve impulses by selectively blocking the binding of acetylcholine to muscarinic receptors. Glycopyrrolate is unusual in that it preferentially binds to M3 over M2 muscarinic receptors, thereby specifically targeting the primary muscarinic receptor responsible for bronchoconstriction occurring in COPD...
2018: International Journal of Chronic Obstructive Pulmonary Disease
https://www.readbyqxmd.com/read/29928041/high-level-expression-of-a2ars-is-required-for-the-enhancing-function-but-not-for-the-inhibiting-function-of-%C3%AE-%C3%AE-t-cells-in-the-autoimmune-responses-of-eau
#11
Dongchun Liang, Hui Shao, Willi K Born, Rebecca L O'Brien, Henry J Kaplan, Deming Sun
We previously reported that activated γδ T cells greatly enhance autoimmune responses, particularly the Th17 response. To determine the mechanisms involved, we made a series of comparisons between activated and non-activated γδ T cells. Our results showed that activated γδ T cells expressed greatly increased levels of A2A adenosine receptor (A2AR) and decreased amounts of CD73, as well as increased amounts of T cell activation markers such as CD69, CD44 and CD25. We show that A2AR is a major functional molecule in the enhancing activity of γδ T cells...
2018: PloS One
https://www.readbyqxmd.com/read/29928003/elevated-galanin-receptor-type-2-primarily-contributes-to-mechanical-hypersensitivity-after-median-nerve-injury
#12
Seu-Hwa Chen, June-Horng Lue, Yung-Jung Hsiao, Shu-Mei Lai, Hsin-Ying Wang, Chi-Te Lin, Ya-Chin Chen, Yi-Ju Tsai
In this study, we investigated temporal changes in galanin receptor type 2 (GalR2) expression in NF200-, galanin-, neuropeptide Y (NPY)-, and neuronal nitric oxide synthase (nNOS)-like immunoreactive (LI) dorsal root ganglion (DRG) neurons after median nerve chronic constriction injury (CCI), and the effects of GalR2 on c-Fos expression in the cuneate nucleus (CN). Double immunofluorescence labeling methods were used to appraise changes in GalR2 expression in NF200-LI, galanin-LI, NPY-LI, and nNOS-LI DRG neurons after CCI...
2018: PloS One
https://www.readbyqxmd.com/read/29927992/bcl-2-mediated-control-of-trail-induced-apoptotic-response-in-the-non-small-lung-cancer-cell-line-nci-h460-is-effective-at-late-caspase-processing-steps
#13
Lubna Danish, Dirke Imig, Frank Allgöwer, Peter Scheurich, Nadine Pollak
Dysregulation of the mitochondrial signaling pathway of apoptosis induction represents a major hurdle in tumor therapy. The objective of the presented work was to investigate the role of the intrinsic (mitochondrial) apoptotic pathway in the non-small lung cancer cell line NCI-H460 upon induction of apoptosis using the highly bioactive TRAIL derivative Db-scTRAIL. NCI-H460 cells were TRAIL sensitive but an only about 3 fold overexpression of Bcl-2 was sufficient to induce a highly TRAIL resistant phenotype, confirming that the mitochondrial pathway is crucial for TRAIL-induced apoptosis induction...
2018: PloS One
https://www.readbyqxmd.com/read/29927939/opposing-roles-of-microrna-argonautes-during-caenorhabditis-elegans-aging
#14
Antti P Aalto, Ian A Nicastro, James P Broughton, Laura B Chipman, William P Schreiner, Jerry S Chen, Amy E Pasquinelli
Argonaute (AGO) proteins partner with microRNAs (miRNAs) to target specific genes for post-transcriptional regulation. During larval development in Caenorhabditis elegans, Argonaute-Like Gene 1 (ALG-1) is the primary mediator of the miRNA pathway, while the related ALG-2 protein is largely dispensable. Here we show that in adult C. elegans these AGOs are differentially expressed and, surprisingly, work in opposition to each other; alg-1 promotes longevity, whereas alg-2 restricts lifespan. Transcriptional profiling of adult animals revealed that distinct miRNAs and largely non-overlapping sets of protein-coding genes are misregulated in alg-1 and alg-2 mutants...
June 2018: PLoS Genetics
https://www.readbyqxmd.com/read/29927808/accumbal-ghrelin-and-glucagon-like-peptide-1-signaling-in-alcohol-reward-in-female-rats
#15
Shayan Abtahi, Erin Howell, Paul J Currie
The present study investigated the relationship between accumbal ghrelin and glucagon-like peptide 1 (GLP-1) signaling in alcohol reward in female rats. Animals with guide cannulae targeting the nucleus accumbens core (NAcC) and shell (NAcS) were habituated to alcohol for 12 weeks through a two-bottle intermittent access paradigm. JMV2959, a ghrelin antagonist, and exendin-4 (Ex-4), a GLP-1 agonist, were microinjected at the onset of the nocturnal cycle. Alcohol, food, water, and total fluid intake were measured 2, 6, and 24 h postinjection...
June 20, 2018: Neuroreport
https://www.readbyqxmd.com/read/29927790/microglial-p2x4r-evoked-pain-hypersensitivity-is-sexually-dimorphic-in-rats
#16
Josiane C S Mapplebeck, Rebecca Dalgarno, YuShan Tu, Orla Moriarty, Simon Beggs, Charlie H T Kwok, Katherine Halievski, Sofia Assi, Jeffrey S Mogil, Tuan Trang, Michael W Salter
Microglia-neuron signalling in the spinal cord is a key mediator of mechanical allodynia caused by peripheral nerve injury. We recently reported sex differences in microglia in pain signalling in mice: spinal mechanisms underlying nerve injury-induced allodynia are microglial dependent in male but not female mice. Whether this sex difference in pain hypersensitivity mechanisms is conserved in other species is unknown. Here, we show that in rats, the spinal mechanisms of nerve injury-induced hypersensitivity in males differ from those in females, with microglial P2X4 receptors (P2X4Rs) being a key point of divergence...
April 30, 2018: Pain
https://www.readbyqxmd.com/read/29927768/an-update-on-the-basic-and-clinical-science-of-ketamine-analgesia
#17
Lisa V Doan, Jing Wang
OBJECTIVE: In the context of the current opioid epidemic, there has been a renewed interest in the use of ketamine as an analgesic agent. METHODS: We have reviewed ketamine analgesia. RESULTS: Ketamine is well-known as an antagonist for N-methyl-D-aspartate receptors. In addition, it can regulate the function of opioid receptors and sodium channels. Ketamine also increases signaling through α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors...
June 20, 2018: Clinical Journal of Pain
https://www.readbyqxmd.com/read/29927500/7-8-dihydroxyflavone-enhances-cholinergic-contraction-of-rat-gastric-smooth-muscle-via-augmenting-muscarinic-m3-receptor-expression
#18
Baoguo He, Zhiqiang Qu, Zibin Tian, Kun Zhao, Liangzhou Wei, Li Ma
Although 7,8-dihydroxyflavone (7,8-DHF), a synthetic agonist specific for TrkB, has been reported to promote intestinal dynamics, the molecular mechanisms behind its effects are not well known. In this study, we explored how 7,8-DHF affected the carbachol (CCh)-induced contraction of rat gastric muscle by way of measuring the contractile tension of muscular strips. We found that although 7,8-DHF did not directly cause contraction of gastric muscle, it enhanced the CCh-induced contractions, but not substance P- or high K+ -induced contractions...
June 21, 2018: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/29927385/computational-design-of-thermostabilizing-point-mutations-for-g-protein-coupled-receptors
#19
Petr Popov, Yao Peng, Ling Shen, Raymond C Stevens, Vadim Cherezov, Zhi-Jie Liu, Vsevolod Katritch
Engineering of GPCR constructs with improved thermostability is a key for successful structural and biochemical studies of this transmembrane protein family, targeted by 40% of all therapeutic drugs. Here we introduce a comprehensive computational approach to effective prediction of stabilizing mutations in GPCRs, named CompoMug, which employs sequence-based analysis, structural information, and a derived machine learning predictor. Tested experimentally on the serotonin 5-HT2C receptor target, CompoMug predictions resulted in 10 new stabilizing mutations, with an apparent thermostability gain ~8...
June 21, 2018: ELife
https://www.readbyqxmd.com/read/29927356/volatile-organic-compounds-of-endophytic-bacillus-spp-have-biocontrol-activity-against-sclerotinia-sclerotiorum
#20
Venance Colman Massawe, Alvina Hanif Rao, Ayaz Farzand, David Kibe Mburu, Sylvans Ochieng Ochola, Liming Wu, Hafiz Abdul Samad Tahir, Huijun Wu, Qin Gu, Xuewen Gao
To develop an effective biological agent to control S. sclerotiorum, three endophytic Bacillus spp. strains with high antagonistic activity were isolated from maize seeds and characterized. In vitro assays revealed that the Bacillus endophytes could produce volatile organic compounds (VOCs) that reduced sclerotial production, and inhibited mycelial growth of S. sclerotiorum. Gas chromatography-Mass spectrometry (GC-MS) revealed that the selected strains produced sixteen detectable VOCs. Eight of the produced VOCs exhibited negative effects on S...
June 21, 2018: Phytopathology
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