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The objective of this study is to design
2022-03-15

The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of
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The recent identification of new mechanisms for
2022-03-15

The recent identification of new mechanisms for triggering ferroptosis, by compounds termed FIN56 and FINO2, provided new insights into regulation of ferroptosis. FINO2 acts through a distinct mechanism: it promotes lipid peroxidation by oxidizing iron and indirectly inactivating GPX4 [180]. FIN56 w
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Integrin engagement triggers activation of several
2022-03-15

Integrin engagement triggers activation of several signaling pathway including Fak, which is recognized as the key signal transduction factor in the integrin signaling pathway that functions by activating downstream signaling in focal adhesion plaques. Whether changes in integrin-FAK signaling pathw
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br Introduction br Results br Discussion br Experimental br
2022-03-15

Introduction Results Discussion Experimental Acknowledgment Introduction Endocannabinoids, N-arachidonoylethanolamine (AEA) and 2-arachidonoylglycerol (2-AG) have been found in most mammalian tissues and they stimulate cannabinoid CB1 and CB2 receptor activity thereby modulating se
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Dual H H receptor antagonists developed by GlaxoSmithKline h
2022-03-15

Dual H1/H3 receptor antagonists developed by GlaxoSmithKline have also reached clinical trials at various stages. These candidates are useful for alleviating the symptoms associated with allergic rhinitis(Daley-Yates et al., 2012). GSK-1004723, 4-[(4-chlorophenyl)methyl]-2-( (2R)-1-[4-(4- [3-(hexahy
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br Conclusion In conclusion HER CTCs can be detected
2022-03-15

Conclusion In conclusion, HER2+ CTCs can be detected using the LiquidBiopsy system. Among the patients with histologically HER2+ breast cancer, 41.9% had ≥ 1 HER2+ CTC/4 mL of blood. The cell lines experiments showed high sensitivity (100%) and specificity (99.9%) using a HER2/CD45 fluorescence r
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Type IIIa b the ligand dependent oncogenic
2022-03-15

Type IIIa/b – the ligand dependent oncogenic Hh pathway (paracrine or reverse paracrine mode) is mediated by paracrine activation and is usually encountered in embryonic development, but also in installation and progression of cancer [58]. Specifically, Hh ligands secreted by malignant NVP-ADW742 a
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br The serine threonine kinase
2022-03-15

The serine/threonine kinase haspin (ploid Germ Cell-pecific Nuclear rote Kinase, also known as erm Cell-pecific ene-2; Gsg2) functions in mitosis, where it phosphorylates histone H3 at Thr-3 (H3T3ph). During mitosis, this phosphorylation generates a binding site on H3 for Survivin and thereby posi
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GSK can function in regulating insulin signaling and glucose
2022-03-15

GSK-3 can function in regulating insulin signaling and glucose metabolism. Inactivation of GSK-3 activity results in dephosphorylation and activation of GS that leads to improved glucose tolerance. However, there are additional mechanisms that can lead to increases in GS activity and improve insulin
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br Materials and methods br Results br Discussion
2022-03-15

Materials and methods Results Discussion Metabolic abnormalities and systemic immune dysfunctions are common during HIV infection and/or antiretroviral therapy. Although some transcriptomic studies of HIV infection have revealed global changes in the mRNA and microRNA expression profiles (R
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br Materials and methods br Results br Discussion
2022-03-15

Materials and methods Results Discussion To understand the molecular basis for how ghrelin secretion is regulated at the cellular level, we identified the full repertoire of 7TM receptors and G proteins in gastric ghrelin bcl-2 inhibitor and functionally characterized the majority of the re
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br Results and discussion br
2022-03-15

Results and discussion Conclusions In summary, we generated analogues of the hit compounds 1–3, studied their structure–activity relationships, and created a series of highly potent GPR55 agonists. The most potent agonists among the series were 17a-b, 17e, 17g and 17l with EC50 values below 10
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There is abundant literature about
2022-03-15

There is abundant literature about different functional aspects of the cannabinoid system (Badal et al., 2017, Balenga et al., 2011, Henderson-Redmond et al., 2016, Nair et al., 2015); however, not a great deal is known about the mechanism by which ethanol impacts its function in connection to the i
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br Funding This work was partially supported by the National
2022-03-15

Funding This work was partially supported by the National Institute on Alcohol Abuse and Alcoholism, award R00AA021264, startup funds from the Department of Immunology, Herbert Wertheim College of Medicine, and the Office of Research and Economic Development at FIU, and pilot funds from Dr. Werth
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Typically upon chronic agonist exposure GPCRs undergo desens
2022-03-15

Typically, upon chronic agonist exposure GPCRs undergo desensitization and internalization resulting in a loss of receptor responsiveness over time (Drake et al., 2006, Kelly et al., 2008). However, not all GPCR systems conform to this model of acute agonist-mediated regulation. Some receptors have
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