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Given the actions of GIP analogues
2022-03-30
Given the actions of GIP analogues administered as a single dose to ob/ob mice, studies were performed to assess their ability to act in vivo as antagonists of GIP-induced insulinotropic and antihyperglycaemic actions. (Ala3)GIP, (Phe3)GIP, (Tyr3)GIP and (Pro3)GIP all counteracted the glucose-loweri
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Fig a and b illustrates a slow inhibition by PMA
2022-03-30
Fig. 3a and b illustrates a slow inhibition by PMA in 2 μM Ca2+. Moreover, channel inhibition was reversed by addition of PKC19–31, a peptide inhibitor specific for PKC, as shown in Fig. 3c. In three experiments, Im was reduced to 14.5±0.6% of the control value by PMA to increase to 207.6±73.6% by a
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br Structures of human secretase Before the
2022-03-30
Structures of human γ-secretase Before the near-atomic resolution structures, the highest resolutions achieved for γ-secretase were 15 and 12Å [19, 21]. The 15-Å structure revealed a SC-10 mg chamber in the transmembrane domain and two pores at the top and bottom of γ-secretase, which were specu
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We have previously designed an azobenzene based molecule
2022-03-30
We have previously designed an azobenzene-based molecule, Razo, which could switch the conformations of G-quadruplex structures by photoregulation. 12, 13, 14, 15 However, it lacks selectivity to different G-quadruplexes. Therefore, we want to find a way to modify this molecule so that it could be u
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Xylazine HCl The extensive worldwide research efforts in
2022-03-30
The extensive worldwide research efforts in the decade following FFA1 de-orphaning aimed at developing clinically useful FFA1 agonists were nearly halted after Takeda’s first-in-class agent fasiglifam (TAK-875) was discontinued in phase III of human trials. On the date of submission of this manuscri
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Prion diseases are transmissible and result in fatal
2022-03-30
Prion diseases are transmissible and result in fatal neurodegenerative disorders, which, similar to AD, also involve the infiltration and activation of mononuclear phagocytes in Andarine mg lesions (reviewed in [61]). A 21 amino-acid fragment of the aberrant human prion protein, Prp106–126, can for
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Sensitivity to EphB TKI was also demonstrated in
2022-03-30
Sensitivity to EphB3 TKI was also demonstrated in a colon cancer cell line, COLO 205, with high expression of EphB3. We found not only exogenous but also endogenous EphB3 protein was expressed in the COLO 205 Acarbose receptor after transient transfection of pCMV6-AC-GFP/EphB3, and both were demons
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Recently Bristol Myers Squibb and Merck reported their GPR a
2022-03-30
Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic Manidipine 2HCl derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GPR40 ago
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Through experimental models and clinical
2022-03-30
Through experimental models and clinical experiments, those four drugs above can shown efficacy-enhancing and toxicity-reducing effects after compatibility. Our preclinical studies showed that XFC has a definite effect on relieving joint symptoms in RA patients. XFC can improve joint pain, swelling,
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To enhance the impact of GD as
2022-03-30
To enhance the impact of GD2 as an immune target in this cancer, we investigated a novel strategy to upregulate expression on the cell surface of EwS cells by an epigenetic agent, based on the following rationale. Biosynthesis of GD2 and other gangliosides during organ development is driven by stage
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br Dynamic Localization of Hippo
2022-03-30
Dynamic Localization of Hippo Pathway Components The observation that Wts normally localizes with an inhibitor, Jub, raised the question of how and where Wts normally becomes activated. Under conditions of pathway activation in Drosophila imaginal discs, Wts relocalized from Jub to Ex, where it i
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br Acknowledgments The authors gratefully acknowledge
2022-03-30
Acknowledgments The authors gratefully acknowledge the financial support of this study by STCU Project 6052 “Enzyme multibiosensor system for renal dysfunction diagnosis and hemodialysis control”. Furthermore, this study was supported by NASU in the frame of Scientific and Technical Program “Sens
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We have previously reported on the
2022-03-30
We have previously reported on the effects of replacing the isoquinoline P2∗ moiety with a naphthalene ring and modifying the connectivity for this element to the P2 proline ring, as demonstrated by compounds – (). Therein, it was hypothesized that the reduced potency observed with – when compared t
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br Conclusion and future perspectives The nicotinic acid rec
2022-03-29
Conclusion and future perspectives The nicotinic m-Chlorophenylbiguanide hydrochloride receptor GPR109A and its close relatives GPR109B and GPR81 are primarily expressed in adipocytes and are coupled to Gi-type G proteins. Recently, the ketone body β-hydroxy-butyrate, the β-oxidation intermediat
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TDG furthermore is inhibited in its excision of U on
2022-03-29
TDG, furthermore, is inhibited in its excision of U on the NCP relative to duplex, though not to the same extent as SMUG1. There is no significant difference between TDGFL and TDG82−308, consistent with a previous report that the N- and C-termini missing from TDG82−308 do not affect the excision of
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