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Inhibitory receptors

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https://www.readbyqxmd.com/read/28449029/a-genome-wide-association-study-identifies-nucleotide-variants-at-siglec5-and-defa1a3-as-risk-loci-for-periodontitis
#1
Matthias Munz, Christina Willenborg, Gesa M Richter, Yvonne Jockel-Schneider, Christian Graetz, Ingmar Staufenbiel, Jürgen Wellmann, Klaus Berger, Bastian Krone, Per Hoffmann, Nathalie van der Velde, André G Uitterlinden, Lisette C P G M de Groot, Amr Sawalha, Haner Direskeneli, Güher Saruhan-Direskeneli, Esra Guzeldemir-Akcakanat, Gencay Keceli, Matthias Laudes, Barbara Noack, Alexander Teumer, Birte Holtfreter, Thomas Kocher, Peter Eickholz, Jörg Meyle, Christof Doerfer, Corinna Bruckmann, Wolfgang Lieb, Andre Franke, Stefan Schreiber, Rahime M Nohutcu, Jeanette Erdmann, Bruno G Loos, Soeren Jepsen, Henrik Dommisch, Arne S Schaefer
Periodontitis is one of the most common inflammatory diseases, with a prevalence of 11% worldwide for the severe forms and an estimated heritability of 50%. The disease is characterized by destruction of the alveolar bone due to an aberrant host inflammatory response to a dysbiotic oral microbiome. Previous genome-wide association studies (GWAS) have reported several suggestive susceptibility loci. Here, we conducted a GWAS using a German and Dutch case-control sample of aggressive periodontitis (AgP, 896 cases, 7,104 controls), a rare but highly severe and early-onset form of periodontitis, validated the associations in a German sample of severe forms of the more moderate phenotype chronic periodontitis (CP) (993 cases, 1,419 controls)...
April 25, 2017: Human Molecular Genetics
https://www.readbyqxmd.com/read/28447469/two-pairs-of-rare-naturally-occurring-4-hydroxy-4-methyl-2-5-heptanedione-derivatives-from-the-red-alga-chondria-crassicaulis
#2
Lin Tong, Yi Zhang, Ai-Hong Liu, Li-Gong Yao, Yue-Wei Guo, Shui-Chun Mao, Bin Wang
Two pairs of rare naturally occurring racemic lipids, (±)-4,7-dihydroxy-4-methyl-2,5-heptanedione (1), and (±)-7-butoxy-4-hydroxy-4-methyl-2,5-heptanedione (2) were isolated from the red alga Chondria crassicaulis Harv. The structures of the racemic mixtures of 1 and 2 were elucidated by detailed spectroscopic techniques, including 1D and 2D NMR ((1)H and (13)C NMR, (1)H-(1)H COSY, HSQC, and HMBC) as well as mass spectrometry and optical rotation experiments, and by comparison with data for related known analogs...
April 27, 2017: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/28446875/cannabinoid-modulation-of-memory-consolidation-in-rats-beyond-the-role-of-cannabinoid-receptor-subtype-1
#3
Patrizia Ratano, Maura Palmery, Viviana Trezza, Patrizia Campolongo
The effects induced by exogenous manipulation of endocannabinoid neurotransmission on emotion and memory are often contradictory. Among the different factors involved, of particular interest is the binding affinity of endocannabinoids, and their analogs, for other receptor families beyond cannabinoid receptors, such as the peroxisome proliferator-activated receptors (PPARs), and the transient receptor potential cation channel subfamily V member 1 (TRPV1). The aim of this study was to investigate which receptor subtype mediates cannabinoid effects on memory consolidation for emotionally arousing experiences...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28446615/proliferation-of-pd-1-cd8-t-cells-in-peripheral-blood-after-pd-1-targeted-therapy-in-lung-cancer-patients
#4
Alice O Kamphorst, Rathi N Pillai, Shu Yang, Tahseen H Nasti, Rama S Akondy, Andreas Wieland, Gabriel L Sica, Ke Yu, Lydia Koenig, Nikita T Patel, Madhusmita Behera, Hong Wu, Megan McCausland, Zhengjia Chen, Chao Zhang, Fadlo R Khuri, Taofeek K Owonikoko, Rafi Ahmed, Suresh S Ramalingam
Exhausted T cells in chronic infections and cancer have sustained expression of the inhibitory receptor programmed cell death 1 (PD-1). Therapies that block the PD-1 pathway have shown promising clinical results in a significant number of advanced-stage cancer patients. Nonetheless, a better understanding of the immunological responses induced by PD-1 blockade in cancer patients is lacking. Identification of predictive biomarkers is a priority in the field, but whether peripheral blood analysis can provide biomarkers to monitor or predict patients' responses to treatment remains to be resolved...
April 26, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28446587/temporal-integration-and-1-f-power-scaling-in-a-circuit-model-of-cerebellar-interneurons
#5
Reinoud Maex, Boris Samuel Gutkin
Inhibitory interneurons interconnected via electrical and chemical (GABAA receptor) synapses form extensive circuits in several brain regions. They are thought to be involved in timing and synchronization through fast feed-forward control of principal neurons. Theoretical studies have shown, however, that whereas self-inhibition does indeed reduce response duration, lateral inhibition, in contrast, may generate slow response components through a process of gradual disinhibition. Here we simulated a circuit of interneurons (stellate and basket cells) of the molecular layer of the cerebellar cortex, and observed circuit time-constants that could rise, depending on the parameter values, to more than one second...
April 26, 2017: Journal of Neurophysiology
https://www.readbyqxmd.com/read/28446460/inhibition-of-cholinergic-neurotransmission-by-%C3%AE-3-adrenoceptors-depends-on-adenosine-release-and-a1-receptors-activation-in-human-and-rat-urinary-bladders
#6
Isabel Silva, Ana Filipa Costa, Sílvia Moreira, Fátima Ferreirinha, Maria Teresa Magalhães-Cardoso, Isabel Calejo, Miguel Silva-Ramos, Paulo Correia-de-Sá
The direct detrusor relaxant effect of β3-adrenoceptor agonists as a primary mechanism to improve overactive bladder symptoms has been questioned. Among other targets, activation of β3-adrenoceptors down-modulate nerve-evoked acetylcholine (ACh) release, but there is insufficient evidence for the presence of these receptors on bladder cholinergic nerve terminals. Our hypothesis is that adenosine formed from the catabolism of cyclic AMP in the detrusor may act as a retrograde messenger via prejunctional A1 receptors to explain inhibition of cholinergic activity by β3-adrenoceptors...
April 26, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28446239/dasatinib%C3%A2-%C3%A2-gefitinib-a-non-platinum-based-combination-with-enhanced-growth-inhibitory-anti-migratory-and-anti-invasive-potency-against-human-ovarian-cancer-cells
#7
Benoît Thibault, Bertrand Jean-Claude
BACKGROUND: Ovarian cancer is the leading cause of death for gynecological cancers and the 6th cause of women cancer death in developed countries. The late stage detection, the peritoneal dissemination and the acquisition of resistance against carboplatin are the main reasons to explain this poor prognosis and strengthen the need of alternative treatments to improve the management of ovarian cancer and/or to sensitize tumors to platinum salts. Epidermal growth factor receptor (EGFR), hepatocyte growth factor receptor (Met) and cellular Src kinase (c-Src) are crucial kinases implied in ovarian tumor growth, survival, invasion and resistance to carboplatin...
April 26, 2017: Journal of Ovarian Research
https://www.readbyqxmd.com/read/28445782/the-immunohistochemical-distribution-of-the-gabaa-receptor-%C3%AE-1-%C3%AE-2-%C3%AE-3-%C3%AE-2-3-and-%C3%AE-2-subunits-in-the-human-thalamus
#8
H J Waldvogel, M Munkle, W van Roon-Mom, H Mohler, R L M Faull
The GABAA receptor is the most abundant inhibitory receptor in the human brain and is assembled from a variety of different subunit subtypes which determines their pharmacology and physiology. To determine which GABAA receptor subunit proteins are found in the human thalamus we investigated the distribution of five major GABAA receptor subunits α1, α2, α3, β2,3 and γ2 using immunohistochemical techniques. The α1-, β2,3- and γ2- subunits which combine to form a benzodiazepine sensitive GABAA receptor showed the most intense levels of staining and were the most common subunits found throughout the human thalamus especially in the ventral and posterior nuclear groups...
April 23, 2017: Journal of Chemical Neuroanatomy
https://www.readbyqxmd.com/read/28444988/inhibitory-action-of-oxytocin-on-spontaneous-contraction-of-rat-distal-colon-by-nitrergic-mechanism-involvement-of-cyclic-gmp-and-apamin-sensitive-k-channels
#9
R Wang, M T Han, X L Lv, Y A Yu, S Q Chai, C M Qu, C Y Liu
AIM: The mechanisms underlying the inhibitory effects of oxytocin (OT) on colon tone are not totally understood. We explore the mechanisms of OT on spontaneous contractility in rat distal colon, and identify the mediators involved in this action. METHODS: In rat distal colon strips, mechanical activity was analyzed and the production of nitric oxide (NO) in tissue loaded with the fluorochrome DAF-FM was visualized by confocal microscopy. OT receptor (OTR) expression was determined by western blotting and immunofluorescence...
April 26, 2017: Acta Physiologica
https://www.readbyqxmd.com/read/28444246/lateral-orbitofrontal-cortical-modulation-on-medial-prefrontal-cortex-amygdala-pathway-differential-regulation-of-intra-amygdala-gabaa-and-gabab-receptors
#10
Chun-Hui Chang
Background: The basolateral complex of the amygdala receives inputs from neocortical areas, including the medial prefrontal cortex (mPFC) and lateral orbitofrontal cortex (lOFC). Earlier studies have shown that lOFC activation exerts an inhibitory gating on mPFC-amygdala information flow. Here we examined the individual role of GABAA and GABAB receptors in this process. Methods: In vivo extracellular single-unit recordings were done in anesthetized rats. We searched amygdala neurons that fire in response to mPFC activation, tested lOFC gating at different delays (lOFC-mPFC delays: 25, 50, 100, 250, 500, and 1000 ms), and examined differential contribution of GABAA and GABAB receptors with iontophoresis...
April 22, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28442805/proton-pump-inhibitors-are-associated-with-a-reduced-likelihood-for-sexually-transmitted-diseases-in-women-in-the-emergency-department
#11
Johnathan Michael Sheele, Nathan Morris, Donald Byars, Frank Counselman
BACKGROUND: Proton pump inhibitors (PPIs) have been shown in cell culture to kill Trichomonas vaginalis (TV) at lower half maximal inhibitory concentration values than metronidazole (Flagyl), the most common medication used to treat the infection. However, there have been no previous clinical investigations to determine if PPIs are associated with reduced risk for TV. MATERIALS AND METHODS: We examined the records of female patients who received testing in the emergency department for TV, Neisseria gonorrhoea (GC), and Chlamydia trachomatis (CT) between 2010 and 2014 at two academic medical centers to determine if PPI and histamine type 2 receptor antagonist (H2RA) drugs were associated with TV and GC/CT infections...
January 2017: Indian Journal of Sexually Transmitted Diseases
https://www.readbyqxmd.com/read/28442196/mechanism-of-neuronal-activity-and-synaptic-transmission-in-rostral-ventrolateral-medulla
#12
Liangchen Zhao, Tianji Liu, Rutao Xu, Liu He, Man Duan, Dejun Xu
Rostral ventrolateral medulla (RVLM) plays an essential role in blood pressure homeostasis. This study was aimed to investigate the mechanism of neuronal activity and synaptic transmission in the RVLM. Medulla oblongata slices were carefully obtained from brainstem of rats. With continues perfusion of artificial cerebrospinal fluid (ACSF), the spontaneous firing of slices and amplitudes were assayed by conventional whole cell patch-clamp recording after addition of gamma-aminobutyric acid (GABA), α-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) and N-methyl d-aspartate (NMDA)...
April 22, 2017: Journal of Clinical Neuroscience: Official Journal of the Neurosurgical Society of Australasia
https://www.readbyqxmd.com/read/28441851/-quantities-and-function-of-nk-cells-in-patients-with-immune-thrombocytopenia
#13
Y J Zhang, W Qu, H Liu, Y H Wang, C Y Liu, L J Li, H Q Wang, R Fu, L M Xing, Z H Shao
Objective: To investigate natural killer (NK) cell quantities and function in patients with immune thrombocytopenia (ITP) . Methods: A total of 66 ITP patients (34 newly diagnosed and 32 in complete remission) were collected from September 2015 to May 2016 in Tianjin Medical University General Hospital, and 30 healthy volunteers were recruited as controls. The percentages of NK cells and their subsets in peripheral blood, the expression of activating receptor (NKp44), inhibitory receptor (NKG2A) and CD16, perforin and granzyme β were detected by flow cytometry...
April 25, 2017: Zhonghua Yi Xue za Zhi [Chinese medical journal]
https://www.readbyqxmd.com/read/28441784/tim-3-up-regulation-in-patients-with-gastric-cancer-and-peptic-ulcer-disease
#14
Mahdieh aghavi-Alhosseini, Mohsen Tehrani, Abolghasem Ajami, Alireza Rafiei, Tarang Taghvaei, Laleh Vahedi-Larijani, Hadi Hossein-Nataj, Hossein Asgarian-Omran
Background: T-cell immunoglobulin and mucin domain protein-3 (Tim-3), an inhibitory immunoregulatory receptor, has been recently implicated in tumor biology and tumor-associated immune suppression. In the present study, expression of Tim-3 was evaluated in gastric cancer (GC) and peptic ulcer disease (PUD) at both mRNA and protein levels. Methods: A total of 133 gastric tissue biopsies, comprising 43 from GC cases, 48 from PUD and 42 from non-ulcer dyspepsia (NUD) serving as controls were collected. Additionally, non-neoplastic adjacent tissue biopsies were also obtained from 6 patients with GC...
March 1, 2017: Asian Pacific Journal of Cancer Prevention: APJCP
https://www.readbyqxmd.com/read/28441750/adenosine-a1-and-a2a-receptors-in-the-brain-current-research-and-their-role-in-neurodegeneration
#15
REVIEW
Jocelyn Stockwell, Elisabet Jakova, Francisco S Cayabyab
The inhibitory adenosine A1 receptor (A1R) and excitatory A2A receptor (A2AR) are predominantly expressed in the brain. Whereas the A2AR has been implicated in normal aging and enhancing neurotoxicity in multiple neurodegenerative diseases, the inhibitory A1R has traditionally been ascribed to have a neuroprotective function in various brain insults. This review provides a summary of the emerging role of prolonged A1R signaling and its potential cross-talk with A2AR in the cellular basis for increased neurotoxicity in neurodegenerative disorders...
April 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28441692/physiological-role-of-endothelin-1-in-flow-mediated-vasodilatation-in-humans-and-impact-of-cardiovascular-risk-factors
#16
Jérémy Bellien, Michèle Iacob, Christelle Monteil, Isabelle Rémy-Jouet, Clothilde Roche, Thomas Duflot, Cathy Vendeville, Laurence Gutierrez, Christian Thuillez, Vincent Richard, Robinson Joannidès
OBJECTIVES: The current study addressed the hypothesis that the local decrease in endothelin-1 (ET-1) bioavailability during sustained flow increases contributes to endothelium-dependent, flow-mediated dilatation (FMD) of conduit arteries and is altered in presence of cardiovascular risk factors. METHODS AND RESULTS: In nine young healthy individuals, the decrease in local ET-1 plasma levels and radial artery FMD in response to hand skin heating (from 34 to 44 °C) was not affected by endothelin type A (ETA) receptor blockade, achieved using the brachial infusion of BQ-123 (100 nmol/min per l of forearm), as compared with physiological saline (0...
June 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28440726/expression-of-c-type-lectin-receptor-mrna-in-chronic-otitis-media-with-cholesteatoma
#17
Sang Hoon Kim, Seung-Ho Han, Jae Yong Byun, Moon Suh Park, Young Il Kim, Seung Geun Yeo
CONCLUSIONS: The levels of expression of various C-type lectin receptors (CLRs) messenger ribo nucleic acids (mRNAs) were significantly higher in cholesteatomas than in normal skin, suggesting that these CLRs may be involved in the pathogenesis of cholesteatoma. OBJECTIVES: Altered expression of pattern recognition receptors may be associated with immune responses in patients with cholesteatoma. This study assessed the levels of expression of CLR mRNAs in normal skin and in cholesteatoma...
June 2017: Acta Oto-laryngologica
https://www.readbyqxmd.com/read/28440465/5-furan-2-yl-4-3-4-5-trimethoxyphenyl-3h-1-2-dithiol-3-one-oxime-6f-a-new-synthetic-compound-causes-human-%C3%AF-brosarcoma-ht-1080-cell-apoptosis-by-disrupting-tubulin-polymerisation-and-inducing-g2-m-arrest
#18
Daiying Zuo, Lili Pang, Jiwei Shen, Qi Guan, Zhaoshi Bai, Huijuan Zhang, Yao Li, Guodong Lu, Weige Zhang, Yingliang Wu
In the current study, we synthesized a series of new compounds targeting tubulin and tested their anti-proliferative activities. Among these new synthetic com-pounds, 5-(furan-2-yl)-4-(3,4,5-trimethoxyphenyl)-3H-1,2-dithiol-3-one oxime (6f) exhibited significant anti-proliferative activity against different human cancer cell lines including human gastric adenocarcinoma SGC-7901, human non-small cell lung cancer A549, and human fibrosarcoma HT-1080. As a result, 6f was selected to further test the sensitivity to different cancer cell lines including human cervical cancer cell line HeLa, human breast cancer cell line MCF-7, non-small cell lung cancer cell line A549, human liver carcinoma cell line HepG-2, human oral squamous cell carcinoma cell lines KB, SGC-7901 and HT-1080...
April 18, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28440456/tetrahydropalmatine-inhibits-lipid-accumulation-through-ampk-signaling-pathway-in-3t3%C3%A2-l1-adipocytes
#19
Guang-Chun Piao, Guan-Cheng Liu, Xue-Jun Jin, Dan Jin, Hai-Dan Yuan
Tetrahydropalmatine (THP), one of the active components of Rhizoma corydalis, has been reported to exert several pharmacological effects, including anti‑inflammatory, anti‑tumor and analgesic activities. However, its effect on obesity and the underlying molecular mechanisms that may be involved have not yet been elucidated. In the present study, the inhibitory effects of THP on the adipogenesis in 3T3‑L1 adipocytes was examined using hstology, western blotting and RT‑qPCR. THP was identified to significantly suppress lipid accumulation in 3T3‑L1 cells and it inhibited pre‑adipocyte differentiation in a concentration‑dependent manner, as evidenced by the reduced formation of lipid droplets and decreased triglyceride levels and glycerol‑3‑phosphate dehydrogenase activity...
April 12, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28440452/bambi-overexpression-together-with-%C3%AE-sitosterol-ameliorates-nsclc-via-inhibiting-autophagy-and-inactivating-tgf-%C3%AE-smad2-3-pathway
#20
Xingchun Wang, Minjie Li, Mengyao Hu, Ping Wei, Wei Zhu
Non-small cell lung cancer (NSCLC) has the highest mortality rate among all solid tumors with a poor prognosis. The BMP and activin receptor membrane bound inhibitor (BAMBI) has been identified as a hallmark of NSCLC and β-sitosterol possesses antitumor potentiality. This study explores the effect of BAMBI overexpression and β-sitosterol in the context of NSCLC. The results revealed that the transfection of pcDNA‑BAMBI and β-sitosterol treatment significantly reduced the levels of autophagy markers light chain 3 (LC3) II and Beclin 1, whereas the levels of LC3 I and p62 were promoted...
May 2017: Oncology Reports
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