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We have isolated various bioactive peptides acting by bindin
2022-10-02

We have isolated various bioactive 6-Chloromelatonin synthesis acting by binding to the receptors of endogenous bioactive peptides such as opioid, bradykinin, neurotensin, and complements C3a and C5a etc. [24]. Rubimetide is the first example of an agonist peptide of the FPR2 of exogenous origin.
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2-APB Several small molecules such as erastin and
2022-10-02

Several small molecules, such as erastin and RSL3, are reported to induce ferroptosis in both normal and cancer 2-APB [21,22]. We confirmed that erastin-induced growth inhibition is an ideal ferroptosis model for cardiomyocytes. The erastin inhibits the growth of H9c2 cells in a Fe-dependent manner
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3254 The main consequence of glucose catabolism is
2022-10-02

The main consequence of glucose catabolism is the elevation of ATP concentration, which in turn suppresses the ATP sensitive potassium (KATP) channels gating function. The KATP channels are octamers composed of the tetrameric inward-rectifying potassium channels (with Kir6.1 and Kir6.2 subunits), th
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We also investigated fat depots in mesenteric
2022-10-01

We also investigated fat depots in mesenteric and retroperitoneal adipose tissues as well as in the liver and verified a reduction in lipid droplets following exercise or exercise and FS oil treatments in the liver from obese mice. Potential molecular candidates in the modulation of adipose tissue b
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Because AM had limited efficacy
2022-09-30

Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to
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LbGlcK crystallized as a ligandless
2022-09-30

LbGlcK crystallized as a ligandless dimer in the asymmetric unit of space group P21 (Fig. 1a) with two identical subunits stabilized by a large contact surface area of 2295 Å2 (13% of the total surface area) as determined by the Protein Interfaces, Surfaces, and Assemblies (PISA) server [18]. Each m
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Olanzapine has been reported to attenuate insulin secretion
2022-09-30

Olanzapine has been reported to attenuate insulin secretion, cause insulin resistance (Chintoh et al., 2008) and reduce whole body carbohydrate oxidation (Klingerman et al., 2014). However, a blunting of these effects in Gcgr−/− mice would not appear to explain the protection against olanzapine-indu
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br STAR Methods br Acknowledgments We would like to
2022-09-30

STAR★Methods Acknowledgments We would like to thank Dr. Xiping Cheng for help with the immunohistochemistry staining, Qi Su for help with gene expression analysis, and Dr. Chaoying Liang at the UTSW Genomics Microarray Core facility for assistance on RNA-seq. W.-H.L. was supported by grant awa
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br Conclusion In conclusion we discovered a
2022-09-30

Conclusion In conclusion, we discovered a pair of novel epimers CBC and CBD from plant C. bungei. These two natural compounds inhibit Hh pathway by blocking signaling at the level of Gli. They are effective in suppressing Hh pathway-dependent medulloblastoma growth in vitro and in vivo. Furthermo
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Recently unimolecular multi functional peptides that combine
2022-09-30

Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with azilsartan medoxomil and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control
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Last we demonstrate that the role
2022-09-29

Last, we demonstrate that the role of EZH2 as a transcriptional activator, with AR being a key target, coexists with its conventional catalytic role in gene repression and plays important oncogenic functions in AR-driven PCa (Figure 7F). Enzymatic EZH2 inhibitors such as EPZ and GSK126, although eff
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br Introduction Currently HIV infection treatment
2022-09-29

Introduction Currently, HIV-1 infection treatment guidelines adopted in USA and EU provide for the simultaneous administration of three antiretroviral drugs (HAART “Highly Active Anti-Retroviral Therapy”) in severely compromised patients [[1], [2], [3]]. Coupling at least two different mechanisms
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Acetylation of histones by histone acetyltransferases stimul
2022-09-29

Acetylation of histones by histone acetyltransferases stimulates gene expression by relaxing Streptomycin sulfate structure, allowing access of transcription factors to DNA, whereas deacetylation of histones by histone deacetylases promotes chromatin condensation and transcriptional repression. Rec
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In tumor cells HK II induction is mediated by
2022-09-29

In tumor cells HK-II induction is mediated by Akt/mTOR pathway [6], [11]. HK-II dynamically shuttles between the mitochondria and cytoplasm under different metabolic conditions. In cardiomyocytes, Akt enhances HK-II binding to mitochondria, setting the heart at a state resistant to ischemic injury [
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An isoflavone type secondary metabolite Glabrescione B GlaB
2022-09-29

An isoflavone type secondary metabolite, Glabrescione B (GlaB), from Derris glabrescens (Benth.) J.F. Macbr. from the family Fabaceae, was found to possess the capacity to bind the Gli1 zinc finger domain and to further block DNA binding capacity [118]. Pyrvinium, an anthelmintic drug approved by th
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