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Extensive pharmacological and structural analysis shows GCGR
2021-09-11
Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in 3CAI mg 14, 17, 20. Functionally identical to REMD-477, REMD2.59 is
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br Conclusion br Ethics statements file br Conflict
2021-09-11
Conclusion Ethics statements file Conflict of interest Acknowledgements This study was supported by the National Research Foundation of Korea (NRF) Grant funded by the Korean Government (MSIP) (Nos. 2011-0030074 and 2018R1D1A3B07050361) and Sookmyung Women’s University Specialization Pro
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While ghrelin s role in addictive behaviors has
2021-09-11
While ghrelin's role in addictive behaviors has been most extensively explored with alcohol, ghrelin has also been implicated in biobehavioral substrates of other drugs of abuse. For example, preclinical experiments suggest that GHS-R1a blockade may improve nicotine [155,156], opioids [[157], [158],
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br Histamine H R The cloning of
2021-09-10
Histamine H4R The cloning of the H3R (Lovenberg et al., 1999) provided a template for the search of other tetracycline hcl sale receptors, and resulted in the most recent discovery of histamine H4R. This concluded with six independent groups that have reported the cloning of the H4R (Leurs et al.
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The H autoreceptors distributed mainly in the CNS act as
2021-09-10
The H3 autoreceptors distributed mainly in the CNS act as a negative feedback on histamine synthesis and release from histaminergic neurons. Histamine is involved in many physiological functions such as sleep-wake regulation, circadian and feeding rhythm, thermal regulation, locomotion, learning, co
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The selection of mutations in vivo
2021-09-10
The selection of mutations in vivo with antivirals is a complex process involving, among other things, the frequency of a given mutation prior to treatment, the effect of that mutation on viral protein function, and the interplay of a given mutation pattern with host immune mechanisms. Investigation
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br STAR Methods br Acknowledgments We thank Prof Y
2021-09-10
STAR★Methods Acknowledgments We thank Prof. Y. Tomari at the University of Tokyo for experimental advice and K. Hanada for technical assistance. This research was supported by Grants-in-Aid for Scientific Research on Innovative Areas “Nascent Chain Biology” (JP15H01548 and JP17H05677 to T.I. a
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HCC is one of the most
2021-09-10
HCC is one of the most prevalent malignant tumors and a leading cause of cancer-related death, globally [[11], [12], [13]]. Hepatitis B virus (HBV) infection is closely related to the development of liver diseases [[14], [15], [16], [17]]. More than 350 million people are chronically infected with H
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br Membrane Fusion Requires Rab GTPases Tethers and SNAREs b
2021-09-10
Membrane Fusion Requires Rab-GTPases, Tethers, and SNAREs Regulation and Function of Rab5 Following endocytosis in metazoan cells, the Rab5-specific GEF Rabex5 binds to ubiquitinated cargo proteins, such as cell surface receptors or metabolite transporters, and subsequently activates Rab5 on e
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We have previously established the pharmacokinetic profile a
2021-09-10
We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in Amikacin receptor and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The c
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siRNA construction and transfection For small interfering RN
2021-09-10
siRNA construction and transfection. For small interfering RNA (siRNA) experiments, we used Stealth™ select RNAi oligonucleotides targeted against GPR120 (Gibco/Invitrogen). The target sequence of siGPR120 used were; sense 5′-AAGUGGGUGCGAUUGACUUGGUCCA-3′ and antisense 5′-UGGACCAAGUCAAUCGCACCCACUU-3′
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br Evolution of multiple GnRH forms and GnRH receptors
2021-09-10
Evolution of multiple GnRH forms and GnRH receptors across vertebrates GnRH is an evolutionary ancient peptide that first appears prior to the protostome-deuterostome split, and is a member of the GnRH-adipokinetic hormone-corazonin superfamily of peptides (Roch et al., 2011, Roch et al., 2014).
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br Ghrelin interactions with the opioid
2021-09-09
Ghrelin interactions with the opioid system The endogenous opioid system is an important regulator of appetite and metabolism (Bodnar, 2017, Nogueiras et al., 2012). In fact, several pharmacological studies have demonstrated that agonists of the three opioid receptors (mu, kappa, and delta) incre
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Most of the tumors showed relatively higher GalR mRNA
2021-09-09
Most of the tumors showed relatively higher GalR1 mRNA levels than the controls (Fig. 1a, Table 3). However one patient with the lower GalR1 mRNA levels (#12) had, in fact, relatively lower levels of transcript for galanin and the other galanin receptors. Patient #10 and 4 who were also expressing l
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Most of the above mechanisms are implicated in
2021-09-09
Most of the above mechanisms are implicated in attenuation of myocardial I/R injury. However, the role of GalR2 receptor activation in cardioprotection remains unclear because of the lack of receptor subtype selectivity of peptides G2 and G3. It has been shown that Ala5-galanin (2–11) (G4) has a hig
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