• Analogous to all GPCRs the GLP R transduces

  2022-08-17

  

  Analogous to all GPCRs, the GLP-1R transduces signals from the outside of the cell to the inside by allosterically converting a ligand-binding event to activation of intracellular effectors. The GLP-1R couples to several intracellular effectors and this pleiotropic coupling is physiologically releva

• Recent studies suggest that the biological

  2022-08-17

  

  Recent studies suggest that the biological importance of endogenous ghrelin becomes accentuated during exposure to more metabolically-constrained and stressful environments. Indeed, mice lacking either ghrelin or GHSR demonstrate impaired ability to adapt metabolically and/or behaviorally to caloric

• Taken together previous data suggest

  2022-08-17

  

  Taken together, previous data suggest that ghrelin signaling is causally linked to alcohol use and may regulate alcohol seeking and consummatory behaviors [[66], [67], [68]]. As such, the ghrelin system may represent a therapeutic target for AUD. Here, we provide a narrative review of the existing l

• Recent advances in imaging single protein mobility and organ

  2022-08-16

  

  Recent advances in imaging single protein mobility and organization in live organisms such as Drosophila larva motor nerve terminals have initiated this by providing a useful platform to investigate how the dynamic changes in the actomyosin network correlates with vesicle docking and fusion in vivo2

• To efficiently develop bioactive ligands even if

  2022-08-16

  

  To efficiently develop bioactive ligands even if the structural information of the target protein is unknown, we have presented a three-dimensional structural diversity-oriented strategy based on structural properties of a chiral cyclopropane. Our strategy has allowed us to design and synthesize a s

• Ro 31-8220 Mesylate br Methods br Acknowledgements We are gr

  2022-08-16

  

  Methods Acknowledgements We are grateful to Eric Olson for providing Yap/Taz floxed mice, and to members of the Epstein lab for helpful comments and advice. This work was supported by NIH R01 HL118768, R35 HL140018, the Cotswold Foundation and the WW Smith Endowed Chair to J.A.E. The Hippo

• FoxM a downstream target of Gli

  2022-08-16

  

  FoxM1, a downstream target of Gli, has been mainly related to Compound C regulation and cellular proliferation in tumor (Alvarez-Fernandez and Medema, 2013, Halasi and Gartel, 2013, Teh et al., 2002). Especially, FoxM1 is a regulator of G1/S and G2/M transitions and M-phase progression (Wonsey & Fo

• NCSs are helical proteins containing four EF hand

  2022-08-16

  

  NCSs are α-helical proteins containing four EF-hand motifs with EF1 being incapable of Ca-binding throughout the family (atomic-resolution structure was firstly resolved for recoverin [5]; for review on NCS structure, see [6]). Some of the NCS proteins (i.e. recoverin and KChIP3) have two while othe

• Both anxiety like behavior and sucrose preference intake wer

  2022-08-15

  

  Both anxiety-like behavior and sucrose preference/intake were reduced in GPR40/FFAR1 KO male mice, while social behavior was normal in KO mice. These findings indicate that brain GPR40/FFAR1 is involved in the modulation of anxiety- and depression-like behavior in rodents. Previous studies have demo

• br Materials and methods br Results Aberrant

  2022-08-15

  

  Materials and methods Results Aberrant Aβ has been suggested to be an initiating factor for glutamate excitotoxicity in AD pathology. To investigate whether Aβ1-42 alters glutamate uptake in astrocytes, neurons, and astrocyte-neuron co-cultures, we used synthetic Aβ1-42 peptide. Aβ1-42 has fas

• br Central control of GI

  2022-08-13

  

  Central control of GI ghrelin secretion The CNS communicates with the GI tract through the vagus nerve originating in the DMV and sympathetic spinal afferents emanating from the thoracic spinal chord (Bray, 2000). The cells that secrete peripheral ghrelin are under direct control of these two pat

• GSIs were shown to effectively decrease A

  2022-08-13

  

  GSIs were shown to effectively decrease Aβ levels at doses close to or higher than their IC50 values in cell culture models. Surprisingly, they also slightly increase Aβ levels at low doses, (significantly below the IC50) also known as “Aβ rise”, due to various mechanisms including inhibition of cel

• With the identification of small nonpolar

  2022-08-13

  

  With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-methy

• Brain derived neurotrophic factor BDNF is the most abundant

  2022-08-13

  

  Brain-derived neurotrophic factor (BDNF) is the most abundant growth factor in the brain and is critical for neuronal development and synaptic plasticity (Bekinschtein et al., 2008; Lu et al., 2014). Besides playing an important role in mood and cognition, BDNF is also involved in the regulation of

• Although pharmacological studies from the end

  2022-08-13

  

  Although pharmacological studies from the end of the 20th century suggested that β1-AR induces a cAMP-dependent apoptosis [30], more recently it has been demonstrated that cAMP, acting through PKA, may be a crucial anti-apoptotic factor in cardiac myocytes [31]. cAMP can also stimulate PI3K, and the

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