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Molecular modeling studies also revealed
2022-05-25
Molecular modeling studies also revealed insignificant differences in ligand-receptor interaction energies between R and S enantiomers of LPCs or their 2-OMe-analogues, suggesting that enantiomers of a particular structure should exert similar GPR119-mediated biological effect. Indeed, when studied
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To overcome these limitations investigators have
2022-05-25
To overcome these limitations, investigators have developed novel strategies for identifying and purifying gonadotropes from transgenic mouse models. For example, FSH-producing gonadotropes have been tagged in vivo with a transgenic cell surface antigen (H-2Kk) so that they can be purified in vitro
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Obestatin increased GnRH mRNA expression in the POA
2022-05-25
Obestatin increased GnRH mRNA expression in the POA, being the main place of GnRH synthesis (Goodman, 2015). Simultaneously, obestatin also caused a decrease in the GnRH mRNA expression in ME, without affecting the level of this peptide mRNA in AHA. A lack of differences observed in the mRNA level
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br Acknowledgments This work was supported by the
2022-05-25
Acknowledgments This work was supported by the Slovak grant agency VEGA, Grant 2/0084/13. We would like to thank Dr. J. Bauer for careful reading of the manuscript. Introduction Glycine is an important neurotransmitter which regulates both Kaempferol inhibitory neurotransmission and excitato
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To date glycine receptors have been found in
2022-05-25
To date, glycine receptors have been found in five distinct transmembrane protein subunits (one β subunit and four α subunit (α1–α4)), combining to form two different types of functional receptors [4], [14], either α homomeric, the immature extrasynaptic glycine receptor subtype, or αβ heteromeric,
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The GlyR is pentameric with
2022-05-25
The GlyR is pentameric, with each subunit consisting of an extracellular ligand binding domain (LBD), four transmembrane (TM) segments, and a large intracellular loop between TM3 and TM4. Binding of neurotransmitter produces conformational changes that are rapidly transmitted to the membrane-spannin
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br Conclusion br Conflict of Interest
2022-05-25
Conclusion Conflict-of-Interest JJH has collaborated with several different pharmaceutical companies during the last 30 years; is currently receiving speaker honoraria from NovoNordisk and MSD and is on advisory boards for NovoNordisk. The author is currently supported by an independent grant
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To directly address whether pharmacological attenuation of
2022-05-25
To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N
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br The small conductance Ca
2022-05-25
The small conductance Ca-activated K+ (SKCa; SK, SKCa, KCa2) channels are recognized as a subfamily of KCa channels (Bond, Maylie, & Adelman, 1999). The SKCa channel is encoded by three distinct genes, KCNN1, KCNN2, and KCNN3 with different sensitivities toward apamin. Different with BKCa channels
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Communication through GJ channels is regulated at
2022-05-25
Communication through GJ channels is regulated at different levels and includes GJ plaque internalization into a single cell. Those vesicles contain the membrane of both cells and th assembled Cx43. The C-terminal domain of Cx43 interacts with different peptides and proteins. However, the internaliz
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Syringe services programs SSPs as
2022-05-24
Syringe services programs (SSPs), as well as expanded HIV and hepatitis C virus (HCV) testing, are key components of harm reduction for PWID and can reduce HIV and hepatitis C virus (HCV) transmissions in this epothilone [14], [15], [16]. The number of SSPs has increased in recent years in West Vir
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AEBSF While the dogma of the mainstream considers Hippo path
2022-05-24
While the dogma of the mainstream considers Hippo pathway as a series of size-controlling kinases, there were still some controversial data supporting that YAP, a vital oncoprotein of Hippo downstream, is antagonistic to regenerative proliferation [[20], [21], [22]]. Known for its expansion-driving
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ICLs represent of all generated
2022-05-24
ICLs represent ICL Inducers in Cancer Therapy Nitrogen mustards with aromatic substituents (chlorambucil, melphalan) or a bioactivatable phosphoramide group (cyclophosphamide) were one of the first identified DNA crosslinkers. These agents are still used in combined schemes for the therapy of chr
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br General aspects of HDACs br General aspects of HDAC
2022-05-24
General aspects of HDACs General aspects of HDAC inhibitors Based on the previous elements, inhibitors designed for HDAC have in common a well-admitted pharmacophore model (Fig. 7A). This model is composed of a zinc binding group (ZBG), attached to a linker chain mimicking the lysine side chai
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In mice iNKT cells are
2022-05-24
In mice, iNKT cells are most frequent (20–30%) among liver T lymphocytes, while they only constitute 0.4–1% of the total T cells in thymus, bone marrow, spleen, lymph node, and intraepithelial lymphocytes. In humans, iNKT cells constitute approximately only a 0.1–0.2% of the peripheral blood T lymph
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