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Accordingly a bioassay guided approach
2022-03-21

Accordingly, a bioassay-guided approach was been used to study the bioactive compounds in VAS contribute to the α-glucosidase inhibitory and antioxidant activity. The 95% ethanol extraction of VAS was successively partitioned with petroleum ether, ethyl acetate and n-butanol. Ethyl acetate fraction
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Next the effects of a phenyl group at the
2022-03-21

Next, the effects of a phenyl group at the 3- and 4-positions of the furan on GCGR affinity were investigated (). Surprisingly, despite the lack of a 4-phenyl group at the furan, compound exhibited almost the same GCGR affinity as compound . On the other hand, when the phenyl group at the 3-position
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Although GLP has greater insulin releasing
2022-03-21

Although GLP-1 has greater insulin-releasing effects at pharmacological concentrations [10], it is apparent that the higher circulating concentrations of GIP combined with more pronounced increase in secretion following feeding make GIP the major physiological incretin [7], [11]. The peptide exerts
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Our initial lead optimization started with the modification
2022-03-21

Our initial lead optimization started with the modification of the indole head group as summarized in . Extensive exploration indicated that there was limited tolerance of structural change in this region of the molecule. All of the modifications to the indole moiety, including N-substitution (), li
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Introduction br Channel activity Since initial reports of th
2022-03-21

Introduction Channel activity Since initial reports of the Ca2+-activated K+ permeability of erythrocytes (see Gardos, 1958), several ‘criteria’ have been established to certify K+ fluxes as being due to the Gárdos channel. For example, the requirement for Ca2+ at the intracellular face of the c
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The structural modelling studies gave a view of arsenic medi
2022-03-21

The structural modelling studies gave a view of arsenic mediated covalent modifications possible in Cx43. In order to look for the biochemical effects of Arsenic on Cx43 and Cx43 mediated GJIC formation, and in order to further decipher the mechanism involved in Arsenic induced decreases in expressi
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br Signals transmitted via MEGJ MEGJ facilitate the direct t
2022-03-21

Signals transmitted via MEGJ MEGJ facilitate the direct transfer of ion currents or small molecules between EC and VSMC. Molecules passing through MEGJ are mainly second messengers such as Ca2+, IP3, and cAMP [31,32,] or endothelium-derived hyperpolarization (EDH) signals [34, 35, 36]. Moreover,
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Galanin was shown to play an important role in
2022-03-21

Galanin was shown to play an important role in pain and pain processing [14] and the involvement of neuropeptides in the development of migraine is well established [[24], [25], [26]], however, so far it has not been examined whether systemic galanin levels correlate with migraine. Therefore, we use
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br Introduction As a fundamental metal
2022-03-21

Introduction As a fundamental metal-dependent hydrolytic enzyme, inorganic pyrophosphatase (PPase) exhibits a specific catalytic ability, in which one molecule of inorganic pyrophosphate (PPi) can be transformed into two orthophosphate (Pi) ions [1,2]. The process of transformation is extremely e
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br Acknowledgments I thank Takeshi Sakaba for critical readi
2022-03-18

Acknowledgments I thank Takeshi Sakaba for critical reading of the manuscript and helpful comments. This work was supported by JSPS/MEXT KAKENHI Grant Numbers 17K19466, 17H03548. Introduction The oral route of drug application is the main route in pharmacology since it is easy to handle and o
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br Results and Discussion The
2022-03-18

Results and Discussion The Set7 sequence is homologous to the other identified histone methyltransferases in S. pombe (Figure S1) and also shares similarity with human HMTases, H3K9 GLP/Ga9, and H4K20 SUV420H1 (Figure S1). Set7 fused with the GFP (Set7-GFP) localized in the nucleus and cytoplasm
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GSK is a critical component of the Wnt signaling pathway
2022-03-18

GSK-3 is a critical component of the Wnt signaling pathway. The Wnt/beta-catenin signal transduction pathway is important in normal growth and development and is also frequently dysregulated in cancer and other diseases. The Wnt/beta-catenin pathway is finely tuned by both positive and negative inte
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Notably we observed that GPR activation induced by
2022-03-18

Notably, we observed that GPR35 activation induced by PA, an in vivo GPR35 agonist [6], significantly decreased DAI, colon weight, and histological score, while increasing colon length in mice with DSS-induced colitis. Furthermore, fibronectin and integrin α5 were co-localized with GPR35 on the colo
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The inhibition of NSAIDs towards GLOI
2022-03-18

The inhibition of NSAIDs towards GLOI provides a direction for the development of novel effective GLOI inhibitors. Although the inhibitory activity of indomethacin was determined and the interactions between it Compstatin receptor and GLOI were probed by NMR titration experiments, no detailed inhib
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br Conclusion br Experimental procedures br Introduction The
2022-03-18

Conclusion Experimental procedures Introduction The glycine receptor (GlyR) is a member of the Cys-loop family of ligand-gated ion channels. It is the primary inhibitory receptor in the brainstem and spinal cord but also plays important roles in higher JNJ 5207852 dihydrochloride regions, i
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