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https://www.readbyqxmd.com/read/28805972/in-vitro-pharmacological-characterization-of-a-novel-unbiased-nop-receptor-selective-nonpeptide-agonist-at-403
#1
Federica Ferrari, Davide Malfacini, Blair V Journigan, Mark F Bird, Claudio Trapella, Remo Guerrini, David G Lambert, Girolamo Calo', Nurulain T Zaveri
Nociceptin/orphanin FQ (N/OFQ) regulates several biological functions via selective activation of the N/OFQ receptor (NOP), a member of the opioid receptor family. We recently identified a new high affinity and highly selective NOP agonist AT-403. In this study, we characterized the functional profile of AT-403 and compared it to other known nonpeptide NOP agonists Ro 65-6570, Ro 2q, SCH-221510, MCOPPB, AT-202 and SCH-486757, using the following assays: GTPγ[(35) S] stimulated binding, calcium mobilization assay in cells-expressing human NOP or classical opioid receptors and chimeric G proteins, bioluminescence resonance energy transfer (BRET) based assay for studying NOP receptor interaction with G protein and arrestin, and the electrically stimulated mouse vas deferens bioassay...
August 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28795803/identification-and-characterization-of-the-first-selective-y4-receptor-positive-allosteric-modulator
#2
Mario Schubert, Jan Stichel, Yu Du, Iain R Tough, Gregory Sliwoski, Jens Meiler, Helen M Cox, C David Weaver, Annette G Beck-Sickinger
The human Y4 receptor (Y4R) and its cognate ligand, pancreatic polypeptide (PP), are involved in the regulation of energy exposure, satiety and food intake. This system represents a potential target for the treatment of metabolic diseases and has been extensively investigated and validated in vivo. Here, we present the compound tBPC (tertbutyl-phenoxy-cyclohexanol), a novel and selective Y4R positive allosteric modulator that potentiates Y4R activation in G-protein signaling and arrestin 3 recruitment experiments...
August 10, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28782483/arrdc3-inhibits-the-progression-of-human-prostate-cancer-through-arrdc3-itg%C3%AE-4-pathway
#3
Y Zheng, Z-Y Lin, J-J Xie, F-N Jiang, C-J Chen, J-X Li, X Zhou, W-D Zhong
Arrestin domain-containing protein 3 (ARRDC3) is a member of the mammalian α-arrestins family, which has been identified as a tumor suppressor gene in human breast cancer, but its functions are still not clear in human prostate cancer (PCa). The purpose of the present study was to investigate clinical significance, biological functions and underlying mechanisms of ARRDC3 deregulation in PCa. Microarray analysis found that ARRDC3 low expression was significantly associated with high Gleason score in TMA, and the expression level of ARRDC3 was negatively correlated with Gleason score, metastasis and biochemical recurrence in online Taylor Dataset...
August 7, 2017: Current Molecular Medicine
https://www.readbyqxmd.com/read/28768954/mir-29a-and-mir-652-attenuate-liver-fibrosis-by-inhibiting-the-differentiation-of-cd4-t-cells
#4
Ji Xuan, Shu-Lin Guo, Ang Huang, Hua-Bing Xu, Mei Shao, Ya Yang, Wei Wen
BACKGROUND: Liver fibrosis is the response of liver diseases that puzzles patients. MiRNAs were involved in the regulating processes of liver fibrosis. This study aims to investigate the effects of ARRB1 mediated by miR-29a and miR-652 on liver fibrosis and its possible mechanism. METHODS: Liver fibrosis of mice was induced by intraperitoneal injection of CCl4. Liver function was observed by the levels of alanine transaminase (ALT) and aspartate transaminase (AST)...
2017: Cell Structure and Function
https://www.readbyqxmd.com/read/28753425/identification-of-phosphorylation-codes-for-arrestin-recruitment-by-g-protein-coupled-receptors
#5
X Edward Zhou, Yuanzheng He, Parker W de Waal, Xiang Gao, Yanyong Kang, Ned Van Eps, Yanting Yin, Kuntal Pal, Devrishi Goswami, Thomas A White, Anton Barty, Naomi R Latorraca, Henry N Chapman, Wayne L Hubbell, Ron O Dror, Raymond C Stevens, Vadim Cherezov, Vsevolod V Gurevich, Patrick R Griffin, Oliver P Ernst, Karsten Melcher, H Eric Xu
G protein-coupled receptors (GPCRs) mediate diverse signaling in part through interaction with arrestins, whose binding promotes receptor internalization and signaling through G protein-independent pathways. High-affinity arrestin binding requires receptor phosphorylation, often at the receptor's C-terminal tail. Here, we report an X-ray free electron laser (XFEL) crystal structure of the rhodopsin-arrestin complex, in which the phosphorylated C terminus of rhodopsin forms an extended intermolecular β sheet with the N-terminal β strands of arrestin...
July 27, 2017: Cell
https://www.readbyqxmd.com/read/28750809/assessing-allosteric-modulation-of-cb1-at-the-receptor-and-cellular-levels
#6
Caitlin E Scott, Debra A Kendall
The cannabinoid CB1 receptor is abundant in the central nervous system and regulates neuronal transmission and other key physiological processes including those leading to pain, inflammation, memory, and feeding behavior. CB1 is activated by the endogenous ligands, arachidonoyl ethanolamine and 2-arachidonoyl glycerol, by various synthetic ligands (e.g., CP55940), and by Δ(9)-tetrahydrocannabinol, the psychoactive component of Cannabis sativa. These CB1 ligands are orthosteric and transduce downstream signals by binding CB1 and primarily inducing Gi coupling, but Gs and β-arrestin coupling are also possible...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28750807/approaches-to-assess-biased-signaling-at-the-cb1r-receptor
#7
Robert B Laprairie, Edward L Stahl, Laura M Bohn
G protein-coupled receptors, such as the cannabinoid type 1 receptor (CB1R), have been shown to interact with multiple binding partners to transmit signals. In both transfected cell systems and in endogenously expressing cell lines, CB1R signaling has been described as multifaceted. The question remains as to how this highly widely expressed receptor signals in a given cell at a given time in vivo. The concept of functional selectivity, or biased agonism, describes the ability of an agonist to engage the receptor in a manner that preferentially engages certain signaling interactions (e...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28747926/agonist-induced-activation-of-human-ffa1-receptor-signals-to-extracellular-signal-regulated-kinase-1-and-2-through-gq-and-gi-coupled-signaling-cascades
#8
Jing Qian, Yuyang Gu, Chun Wu, Feng Yu, Yuqi Chen, Jingmei Zhu, Xingyi Yao, Chen Bei, Qingqing Zhu
BACKGROUND: FFA1 is abundantly expressed in the liver, skeletal muscle, monocytes and nervous system, but is particularly abundant in pancreatic β cells. It is widely believed that FFA1 exerts its regulatory roles in a variety of physiological and pathological functions. In response to oleic acid, FFA1 has been shown to induce the activation of extracellular signal-regulated kinase 1 and 2 (ERK1/2) through a mechanism involving EGFR transactivation in a breast cancer cell line. However, the underlying molecular mechanism for ERK1/2 activation mediated by n-6 free fatty acid (LA) in HEK293 cells remains to be further elucidated...
2017: Cellular & Molecular Biology Letters
https://www.readbyqxmd.com/read/28746336/discovery-of-novel-brain-permeable-and-g-protein-biased-beta-1-adrenergic-receptor-partial-agonists-for-the-treatment-of-neurocognitive-disorders
#9
Bitna Yi, Alam Jahangir, Andrew K Evans, Denise Briggs, Kristine Ravina, Jacqueline Ernest, Amir B Farimani, Wenchao Sun, Jayakumar Rajadas, Michael Green, Evan N Feinberg, Vijay S Pande, Mehrdad Shamloo
The beta-1 adrenergic receptor (ADRB1) is a promising therapeutic target intrinsically involved in the cognitive deficits and pathological features associated with Alzheimer's disease (AD). Evidence indicates that ADRB1 plays an important role in regulating neuroinflammatory processes, and activation of ADRB1 may produce neuroprotective effects in neuroinflammatory diseases. Novel small molecule modulators of ADRB1, engineered to be highly brain permeable and functionally selective for the G protein with partial agonistic activity, could have tremendous value both as pharmacological tools and potential lead molecules for further preclinical development...
2017: PloS One
https://www.readbyqxmd.com/read/28743719/the-atypical-receptor-ccrl2-is-required-for-cxcr2-dependent-neutrophil-recruitment-and-tissue-damage
#10
Annalisa Del Prete, Laura Martínez-Muñoz, Cristina Mazzon, Lara Toffali, Francesca Sozio, Lorena Za, Daniela Bosisio, Luisa Gazzurelli, Valentina Salvi, Laura Tiberio, Chiara Liberati, Eugenio Scanziani, Annunciata Vecchi, Carlo Laudanna, Mario Mellado, Alberto Mantovani, Silvano Sozzani
CCRL2 is a seven transmembrane domain receptor that shares structural and functional similarities with the family of the Atypical Chemokine Receptors (ACKRs). CCRL2 is upregulated by inflammatory signals and, unlike from other ACKRs, is not a chemoattractant scavenging receptor, does not activate β-arrestins and is widely expressed by many leukocyte subsets. Therefore, the biological role of CCRL2 in immunity is still unclear. Here we report that CCRL2-deficient mice have a defect in neutrophil recruitment and are protected in two models of inflammatory arthritis...
July 25, 2017: Blood
https://www.readbyqxmd.com/read/28743488/mu-opioid-receptor-biased-ligands-a-safer-and-painless-discovery-of-analgesics
#11
REVIEW
Abraham Madariaga-Mazón, Andrés F Marmolejo-Valencia, Yangmei Li, Lawrence Toll, Richard A Houghten, Karina Martinez-Mayorga
Biased activation of G-protein-coupled receptors (GPCRs) is shifting drug discovery efforts and appears promising for the development of safer drugs. The most effective analgesics to treat acute pain are agonists of the μ opioid receptor (μ-OR), a member of the GPCR superfamily. However, the analgesic use of opioid drugs, such as morphine, is hindered by adverse effects. Only a few μ-OR agonists have been reported to selectively activate the Gi over β-arrestin signaling pathway, resulting in lower gastrointestinal dysfunction and respiratory suppression...
July 22, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28733085/functional-consequences-of-chemically-induced-%C3%AE-arrestin-binding-to-chemokine-receptors-cxcr4-and-ccr5-in-the-absence-of-ligand-stimulation
#12
Marcel Liebick, Sarah Henze, Viola Vogt, Martin Oppermann
Chemokine receptor signaling is a tightly regulated process which was for a long time exclusively attributed to heterotrimeric G proteins. β-Arrestins constitute a separable signaling arm from classical heterotrimeric G proteins, in addition to their well-established roles in receptor desensitization and endocytosis. In order to clearly dissect β-arrestin- from G protein-dependent effects we forced the recruitment of β-arrestin to CXCR4 and CCR5 independently of agonist-promoted receptor activation through chemically-induced dimerization...
July 18, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28733084/reciprocal-regulation-of-%C3%AE-2-adrenoceptor-activated-camp-response-element-binding-protein-signalling-by-arrestin2-and-arrestin3
#13
Alexander Pearce, Lucy Sanders, Paul J Brighton, Shashi Rana, Justin C Konje, Jonathon M Willets
Activation of Gs coupled receptors (e.g. β2-adrenoreceptor (β2AR)) expressed within the uterine muscle layer (myometrium), promotes intracellular cAMP generation, inducing muscle relaxation through short-term inhibition of contractile proteins, and longer-term modulation of cellular phenotype to promote quiescence. In the myometrium cAMP-driven modulation of cell phenotype is facilitated by CREB activity, however despite the importance of CREB signalling in the promotion of myometrial quiescence during pregnancy, little is currently known regarding the molecular mechanisms involved...
July 18, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28732166/mel-n16-a-series-of-novel-endomorphin-analogs-with-good-analgesic-activity-and-a-favorable-side-effect-profile
#14
Xin Liu, Long Zhao, Yuan Wang, Jingjing Zhou, Dan Wang, Yixin Zhang, Xianghui Zhang, Zhaojuan Wang, Dongxu Yang, Lingyun Mou, Rui Wang
Opioid peptides are neuromodulators that bind to opioid receptors and reduce pain sensitivity. Endomorphins are one of the most active endogenous opioid peptides, and they have good affinity and selectivity toward the μ opioid receptor. However, their clinical usage is hindered by their inability to cross the blood-brain barrier, and their poor in vivo activity after peripheral injection. In order to overcome these defects, we have designed and synthesized a series of novel endomorphin analogs with multiple site modifications...
July 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28719611/rna-sequencing-to-determine-the-contribution-of-kinase-receptor-transactivation-to-g-protein-coupled-receptor-signalling-in-vascular-smooth-muscle-cells
#15
Danielle Kamato, Venkata Vijayanand Bhaskarala, Nitin Mantri, Tae Gyu Oh, Dora Ling, Reearna Janke, Wenhua Zheng, Peter J Little, Narin Osman
G protein coupled receptor (GPCR) signalling covers three major mechanisms. GPCR agonist engagement allows for the G proteins to bind to the receptor leading to a classical downstream signalling cascade. The second mechanism is via the utilization of the β-arrestin signalling molecule and thirdly via transactivation dependent signalling. GPCRs can transactivate protein tyrosine kinase receptors (PTKR) to activate respective downstream signalling intermediates. In the past decade GPCR transactivation dependent signalling was expanded to show transactivation of serine/threonine kinase receptors (S/TKR)...
2017: PloS One
https://www.readbyqxmd.com/read/28718821/tick-haller-s-organ-a-new-paradigm-for-arthropod-olfaction-how-ticks-differ-from-insects
#16
Ann L Carr, Robert D Mitchell Iii, Anirudh Dhammi, Brooke W Bissinger, Daniel E Sonenshine, R Michael Roe
Ticks are the vector of many human and animal diseases; and host detection is critical to this process. Ticks have a unique sensory structure located exclusively on the 1st pairs of legs; the fore-tarsal Haller's organ, not found in any other animals, presumed to function like the insect antennae in chemosensation but morphologically very different. The mechanism of tick chemoreception is unknown. Utilizing next-generation sequencing and comparative transcriptomics between the 1st and 4th legs (the latter without the Haller's organ), we characterized 1st leg specific and putative Haller's organ specific transcripts from adult American dog ticks, Dermacentor variabilis...
July 18, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28700749/correction-adipocyte-arrestin-domain-containing-3-protein-arrdc3-regulates-uncoupling-protein-1-ucp1-expression-in-white-adipose-independently-of-canonical-changes-in-%C3%AE-adrenergic-receptor-signaling
#17
Shannon H Carroll, Ellen Zhang, Bing F Wang, Katherine B LeClair, Arifeen Rahman, David E Cohen, Jorge Plutzky, Parth Patwari, Richard T Lee
[This corrects the article DOI: 10.1371/journal.pone.0173823.].
2017: PloS One
https://www.readbyqxmd.com/read/28687596/expression-and-light-dependent-translocation-of-%C3%AE-arrestin-in-the-visual-system-of-the-terrestrial-slug-limax-valentianus
#18
Ryota Matsuo, Yuka Takatori, Shun Hamada, Mitsumasa Koyanagi, Yuko Matsuo
Vertebrates, cephalopods, and arthropods are equipped with eyes having the highest spatiotemporal resolution among the animal phyla. In parallel, it is only the animals in these three phyla that have visual arrestin specialized for the termination of visual signaling triggered by opsin, in addition to ubiquitously expressed β-arrestin that serves in terminating general G protein-coupled receptor signaling. Indeed, visual arrestin in Drosophila and rodents translocates to the opsin-rich subcellular region in response to light to reduce the overall sensitivity of photoreceptors in an illuminated environment (i...
July 7, 2017: Journal of Experimental Biology
https://www.readbyqxmd.com/read/28683816/uncovering-missing-pieces-duplication-and-deletion-history-of-arrestins-in-deuterostomes
#19
Henrike Indrischek, Sonja J Prohaska, Vsevolod V Gurevich, Eugenia V Gurevich, Peter F Stadler
BACKGROUND: The cytosolic arrestin proteins mediate desensitization of activated G protein-coupled receptors (GPCRs) via competition with G proteins for the active phosphorylated receptors. Arrestins in active, including receptor-bound, conformation are also transducers of signaling. Therefore, this protein family is an attractive therapeutic target. The signaling outcome is believed to be a result of structural and sequence-dependent interactions of arrestins with GPCRs and other protein partners...
July 6, 2017: BMC Evolutionary Biology
https://www.readbyqxmd.com/read/28679059/role-and-potential-targeting-of-hepatic-apurinic-apyrimidinic-endonuclease-1-and-cyclin-dependent-kinase-4-in-hepatocellular-carcinoma
#20
Kadry Sadek, Tarek Abouzed, Sherif Nasr, Moustafa Shukry
Apurinic/apyrimidinic endonuclease/redox element 1 (APE1/Ref-1) is a pervasive multifunctional protein required in the DNA base extraction repair (BER) pathway and a noteworthy reducing-oxidizing (redox) factor that upgrades the authoritative of various transcription components to DNA. Cyclin-dependent kinases (CDKs) assume a key part in directing the movement of the cell-cycle. The present study evaluates the synergistic efficacy of using licochalcone B (LCB) and fullerene C60 (FnC60) nanoparticles against diethylnitrosamine (DEN)-induced hepatocarcinoma (HCC) in rats...
July 5, 2017: Canadian Journal of Physiology and Pharmacology
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