• HCC is one of the most prevalent malignant tumors and

  2022-01-19

  

  HCC is one of the most prevalent malignant tumors and a leading cause of cancer-related death, globally [[11], [12], [13]]. Hepatitis B virus (HBV) infection is closely related to the development of liver diseases [[14], [15], [16], [17]]. More than 350 million people are chronically infected with H

• Recently a G protein coupled receptor GPR a was identified

  2022-01-19

  

  Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of

• In the latent inhibition model a conditioned

  2022-01-19

  

  In the latent inhibition model, a conditioned stimulus (CS) is pre-exposed alone without any consequences (i.e., unconditioned stimulus [US]) in the pre-exposure phase. The CS is then associated with a US to form a CS-US association. The strength of the CS-induced response in the pre-exposure group

• The rapid actions of glucocorticoids range

  2022-01-19

  

  The rapid actions of glucocorticoids range from the production of endocannabinoid as a retrograde messenger [9], to regulation of ion channels [10], [11], to inhibitory effects on immune AT-101 [12], [13], [14]. Many different kinase signaling pathways have been implicated in the rapid actions of g

• The in vivo biological activity of

  2022-01-19

  

  The in vivo biological activity of the four novel analogues was then systematically assessed in three animal models including normal control, high fat fed and ob/ob mice. As expected from earlier in vitro studies, all four glucagon receptor antagonists had minor effects on glucose or insulin concent

• br Gap junctions hemichannels and

  2022-01-19

  

  Gap junctions, hemichannels and connexins: Molecular characteristics and function Cell-to-cell communication is of extreme importance in tissue homeostasis, which is maintained by transmission of regulatory signals (Fig. 1). Intercellular communication via gap junctions (GJs) represents one of th

• br Introduction Hepatocyte injury initiates and

  2022-01-19

  

  Introduction Hepatocyte injury initiates and facilitates inflammation in the course of liver disease progression. Thus, understanding the regulatory basis for sensing and responding to damage-associated inflammatory processes in the liver’s parenchymal cells is a primary issue in liver pathophysi

• Wnt-C59 Several observations about structure activity relati

  2022-01-19

  

  Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic Wnt-C59 class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkage of

• This profound cell type specificity of G a GLP

  2022-01-19

  

  This profound cell-type specificity of G9a/GLP complex modulation of neuronal plasticity is accentuated by studies employing genetic ablation of G9a in dopamine 1 receptor (Drd1)- and dopamine 2 receptor (Drd2)-expressing medium spiny neurons (MSNs) in the nucleus accumbens (NAc). Conditional G9a kn

• An important example of a

  2022-01-18

  

  An important example of a frame is the lattice of open subsets of any topological space X. The correspondence is clearly functorial (by taking inverse images), and consequently one has a contravariant functor with the category of topological spaces and continuous maps as domain category. The functor

• br Clinical development of anti NASH drug therapies

  2022-01-18

  

  Clinical development of anti-NASH drug therapies The current understanding of NASH pathogenesis has led to broad efforts to target several features of the disease, alone or in combination, even in the absence of liver-guided therapies. Therefore, drug development in NASH is a rapidly changing fie

• Most excitingly we found the increased

  2022-01-18

  

  Most excitingly, we found the increased δ-cells hold the ability to trans-differentiate into β-cells in T1D mice. It has been shown that after near-total β-cell loss, juvenile mice display δ-to-β-cell conversion to recover diabetes, involving de-differentiation, proliferation and re-expression of is

• The findings in this study

  2022-01-18

  

  The findings in this study may represent an example of a more general phenomenon, namely that the exquisite specificity of the G protein-coupled receptors that mediate the physiological actions of the R 59-022 synthesis family hormones in mammals may have arisen relatively late in evolution. In non

• However ghrelin has a short half life of min

  2022-01-18

  

  However, ghrelin has a short half-life of 15–20 min, because it is a natural peptide containing 28-amino acids, its clinical usefulness as a therapeutic agent may be limited (Mosińska et al., 2017; Vestergaard et al., 2007). Hence, many efforts have been made to elucidate the smallest segment of ghr

• CaCl was from the Radiochemical Centre

  2022-01-18

  

  45CaCl2 was from the Radiochemical Centre (Amersham, UK), NaVO3 was from Reachim (Moscow, Russia). Tetrodotoxin was purchased from Calbiochem, DTNB from Merck, Darmstadt, Germany. Nifedipine was synthesized in the Institute of Drug Research, Modra, Slovakia and was kindly provided by Dr. Zdeno Mahrl

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