• Although pharmacological studies from the

  2021-12-24

  

  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

• Recently results obtained by our group have demonstrated tha

  2021-12-24

  

  Recently, results obtained by our group have demonstrated that hEECs are able to secrete NPY into the extracellular medium and that this peptide can induce an increase in the [Ca]i of these cells (Jacques et al., 2003b). In light of these results and those obtained in this study, we can speculate th

• The comparatively low number of H

  2021-12-24

  

  The comparatively low number of H1R agonists is contrasted by the high number of diverse H1R antagonists. Based on pharmacological classification, they are grouped into different generations by considering their target as well as side effects profile. The first generation “antihistamines” consist of

• MAP Ks act at the level of

  2021-12-24

  

  MAP4Ks act at the level of MST1/2 to phosphorylate LATS1/2 and regulate the Hippo pathway (Box 1). Of particular interest is the involvement of MAP4K4, a key metabolic regulator [88] and common polymorphisms in the MAP4K4 locus are associated with T2D and insulin resistance [89] in adipogenesis. In

• The effect of microtubule inhibitors on HBV

  2021-12-24

  

  The effect of microtubule inhibitors on HBV infection and replication were reported previously. In the study by Dr. Ai-Long Huang's group, microtubule inhibitors promoted HBV replication in Hep2.2.15 and HepG2-HBV1.1, in which HBV DNA is integrated into the chromosomal DNA (Xu et al., 2015). Integra

• Pharmacologic approaches of inhibiting GSNOR activity have r

  2021-12-24

  

  Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications

• Apart from the different assays used biased agonism could

  2021-12-24

  

  Apart from the different assays used, biased agonism could also explain the inconsistent pharmacology of GPR55. Indeed, one study compared the effect of LPIs and Virodhamine in HEK293 WS 3 stably transfected with human GPR55. They found that the effect of both ligands on intracellular Ca2+ was bloc

• In order to investigate whether this off target activity

  2021-12-24

  

  In order to investigate whether this off-target activity was related to a particular structural feature of this igf1r inhibitor or was characteristic of the series, compounds , and were selected as being matched pairs with compound but with structural variation in terms of the R, R and R groups, res

• Acknowledgments This research was supported

  2021-12-24

  

  Acknowledgments This research was supported by the Korea Research Institute of Chemical Technology (KRICT) funded by the Ministry of Science, ICT & Future Planning (KK1703-G00, KK1707-C05, SI1707-02, KK-1607-C09, and SKO1707C05) and a grant of the Korea Health Technology R&D Project through the Kor

• Besides its established insulinotropic actions GIP has

  2021-12-24

  

  Besides its established insulinotropic actions, GIP has been shown to possess other direct beneficial effects on the beta cell, including stimulation of growth, differentiation, proliferation and survival.21, 22, 23 It has also been shown to stimulate proinsulin gene transcription and translation. M

• Zn is the second most abundant trace metal in

  2021-12-23

  

  Zn2+ is the second most abundant trace metal in many cells and neurons in the brain. It regulates cellular functions such as gene expression, epigenetic enzymatic activity, protein structural stability, and neuronal plasticity. Zn2+ is particularly abundant in the cortex and limbic system, includin

• The first FPR ligand described is the fMLF peptide which

  2021-12-23

  

  The first FPR1 ligand described is the fMLF peptide, which binds with high affinity (in the nM range) to and activates FPR1. Formylated peptides derived from Listeria monocytogenes also selectively activate FPR1 [10] (Table 1). Formylation of peptides also occurs in mitochondria. Thus, the release o

• uPAR promotes cell associated proteolysis by binding

  2021-12-23

  

  uPAR promotes cell-associated proteolysis by binding to uPA which locally converts plasminogen into active plasmin [10]. Ligand-engaged uPAR also acts as a potent regulator of cell migration and matrix attachment. Being a membrane receptor, uPAR needs to interact with extracellular matrix (ECM) prot

• br Conclusions GPCRs are versatile signaling molecules regul

  2021-12-23

  

  Conclusions GPCRs are versatile signaling molecules regulating almost all physiological processes, including energy homeostasis and glucose homeostasis.105, 106 They also prove to be important therapeutic targets. Drugs targeting GPCRs account for 30% of current pharmaceutical sales. GPR40 is a m

• Recently the classical view of the compartmentalization of t

  2021-12-23

  

  Recently, the classical view of the compartmentalization of the plant isoprenoid metabolism has been re-evaluated, following the demonstration of the partial peroxisomal localization of the mevalonic Cholesterol (MVA) pathway, generally regarded as cytosolic. Using GFP-tagging approaches, the last

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