• Sitagliptin phosphate We recently reported the first cyclopr

  2022-01-15

  

  We recently reported the first cyclopropene-analog of the amino Sitagliptin phosphate neurotransmitter glutamate (Fig. 2A) [27]. This first-generation cyclopropene-glutamate expanded the only other documented report of a cyclopropene-neurotransmitter (cyclopropene-GABA analog by Reissig and coworke

• Here we studied the effects of BZ

  2022-01-15

  

  Here we studied the effects of BZ flurazepam (FZ) at high doses in acute and chronic settings of tolerance and dependence in GluR-A−/− mice (Zamanillo et al., 1999). We used measurements in which the phenomenon of “learning while intoxicated” should play only a minor role in order to find out the s

• As cardiovascular disease accounts for the majority

  2022-01-15

  

  As cardiovascular disease accounts for the majority of deaths in subjects with T2D, it is imperative that we better characterize the cardiovascular risks and benefits of the various therapies we prescribe to these individuals to control their glycemia. Indeed, the potential to identify subsets of di

• Despite potent biological actions the native hormone

  2022-01-15

  

  Despite potent biological actions, the native hormone undergoes degradation by the enzyme dipeptidylpeptidase-IV (DPP-IV) [17] and is rapidly cleared from the bloodstream by renal filtration [18]. One such approach to prolong the biological half-life of GIP is through conjugation with a polyethylene

• ETV plays an important role

  2022-01-15

  

  ETV5 plays an important role in tumorigenesis and metastasis. For example, chromosomal rearrangement of ETV5 which results in increased ETV5 level is believed as a common event driving human prostate cancer (Helgeson et al., 2008; Huang and Waknitz, 2009). Ghrelin/acyl-ghrelin also plays an importan

• A pooled overall survival analysis at

  2022-01-15

  

  A pooled overall survival analysis at 1year showed no difference in survival between the two study arms, although these studies were not designed or powered to demonstrate a survival benefit. Among the 979 total patients in both ROMANA 1 and 2, about 55% continued on to the ROMANA 3 trial. That tria

• CCK-8 receptor br Gap junctions hemichannels and connexins M

  2022-01-15

  

  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

• The highest metabolic stability observed for compound

  2022-01-14

  

  The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou

• In addition to FAK P

  2022-01-14

  

  In addition to FAK, P-38 MAPK (38 kDa polypeptide) serves as cross-talk effector for signal transduction, enabling this factor to play a vital role in numerous biological processes (Cuenda and Rousseau, 2007). Pharmacologically modulation of P-38 has shown to be an effective approach in the orientat

• Hypoxia inducible factors HIFs including HIF HIF

  2022-01-14

  

  Hypoxia-inducible factors (HIFs), including HIF-1α, HIF-1β, HIF-2α and HIF-3α, are important endogenous signaling proteins that contribute to the cellular response to hypoxia. Among these proteins, HIF-1α is involved in many pathophysiological processes, including inflammation, tumor growth and meta

• Screening of the compounds allowed for a

  2022-01-14

  

  Screening of the compounds allowed for a number of interesting SAR observations. First of all, pyridyl analogue demonstrated that a pyridine ring would be beneficial for both log as well as increasing the potency (entry 2 versus entry 1). Electron-poor aryl groups next to the oxadiazolone were detr

• br Concluding remarks Several orphan GPCRs have expression p

  2022-01-14

  

  Concluding remarks Several orphan GPCRs have expression profiles that indicate they are worthy of consideration as therapeutic targets. This view can be supported via various transgenic techniques, and it would be interesting to have wide-ranging phenotypic information on GPR35 knockout mice. Bas

• The precise mechanisms of action of PBA are as yet

  2022-01-14

  

  The precise mechanisms of action of 4-PBA are as yet ambiguous. Its capacity as a chemical chaperone has been thoroughly documented for the ABC transporter family in particular (Prulière-Escabasse et al., 2007; Iram and Cole, 2014; Gordo-Gilart et al., 2016; Pomozi et al., 2017). 4-PBA has been clas

• The sexual dimorphism in dlGALR a and dlGALR b receptors

  2022-01-13

  

  The sexual dimorphism in dlGALR1a and dlGALR1b receptors found in the gonads of adult fish led us to hypothesize that the gene expression difference between female and males might be attributed to the differences in steroid production between female and male gonads. Interestingly we have found that

• Sumoylation is involved in regulating

  2022-01-13

  

  Sumoylation is involved in regulating protein-protein interactions, subcellular protein localization, protein stability, and transcriptional factor activity (reviewed in [29]). The small ubiquitin-like modifier (SUMO) protein is covalently attached to a lysine residue in a Ψ-K-X-D/E consensus sequen

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