• Ning et al showed that LPC

  2021-10-11

  

  Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p

• br Experimental methods br Acknowledgments

  2021-10-11

  

  Experimental methods Acknowledgments We thank all members of the Hermanson lab, especially Ana Teixeira, Shirin Ilkhanizadeh and Karolina Wallenborg, for assistance and discussions, Peter Löw for anti-synaptotagmin antibody, and Lars Björklund, Ole Isacson, Christer Höög, Claes Wahlestedt and

• Next the effects of a

  2021-10-11

  

  Next, the effects of a phenyl group at the 3- and 4-positions of the furan on GCGR affinity were investigated (). Surprisingly, despite the lack of a 4-phenyl group at the furan, compound exhibited almost the same GCGR affinity as compound . On the other hand, when the phenyl group at the 3-positio

• Previous researches about ghrelin focused primarily

  2021-10-11

  

  Previous researches about ghrelin focused primarily on gastrointestinal functions [30], energy balance [31], weight [32], and more recently on anxiety [33], [34], [35] and depression [36]. Here, we provided the first demonstration that chronic peripheral or central ghrelin treatment to CUMS rodents

• Our initial lead optimization started with the modification

  2021-10-11

  

  Our initial lead optimization started with the modification of the indole head group as summarized in . Extensive exploration indicated that there was limited tolerance of structural change in this region of the molecule. All of the modifications to the indole moiety, including N-substitution (), li

• The pharmacokinetic properties of were

  2021-10-09

  

  The pharmacokinetic properties of 12 were amenable to oral dosing allowing in vivo comparison to 6. Compared to a maximum efficacious dose of 6 (60mg/kg), 12 demonstrated improved glycemic control during OGTT in high-fat fed/STZ treated (HF/STZ) and BDF/diet-induced obesity (DIO) mouse models of typ

• br Materials and methods br Results br

  2021-10-09

  

  Materials and methods Results Discussion Protein degradation plays a vital role in nearly all cellular processes, nearly 5% of genes are dedicated to the control of protein stability [31], [32]. The ubiquitin-proteasome system (UPS) represents the major way for degradation of proteins, wher

• FXa is a vitamin K dependent

  2021-10-09

  

  FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 Olomoucine and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102  exhibits the trypsin-like β-barrel structure [12]. The acti

• Expression of p NTR has been linked to

  2021-10-09

  

  Expression of p75NTR has been linked to several aspects of aggressive glioma growth, including migration and invasion, by various mechanisms in a large number of elegant studies [6], [7], [26], [27]. Our study adds to this literature by demonstrating specific roles in hypoxic tumor cells and regulat

• G P also plays a critical role in

  2021-10-09

  

  G6P also plays a critical role in regulating HK2 binding to mitochondria. Elevated levels of intracellular G6P weaken HK2 binding to mitochondria, causing the enzyme to translocate to the cytoplasm and facilitate anabolic glucose metabolism. Acidosis similarly induces HK2 translocation from mitochon

• Studies have demonstrated the paradoxical role

  2021-10-09

  

  Studies have demonstrated the paradoxical role of HO-1 in tumorigenesis. At initial stages of carcinogenesis, it protects DNA by lowering the ROS-mediated mutational rate, but later, HO-1 promotes cancer cell survival and proliferation. One PDAC therapeutic strategy is to increase ROS production and

• br Structural Homology and Functional Implications Amino

  2021-10-09

  

  Structural Homology and Functional Implications Amino Decoquinate sequence analyses of Disp and the Shh receptor Ptch indicate that both proteins share structural homology with a family of bacterial efflux pumps that function in resistance, nodulation, and division (RND) transporter complexes (Fi

• A repertoire of cytotoxic payloads is increasing

  2021-10-09

  

  A repertoire of cytotoxic payloads is increasing; among those, MMAE has been utilized for the highly effective ADC brentuximab vedotin. However, the ADCs which utilized MMAE to target GCC in solid tumors have shown a poor efficacy suggesting that various tumor types respond differently to a given to

• Probenecid We show that pharmacological inactivation of GSTP

  2021-10-09

  

  We show that pharmacological inactivation of GSTP1 over a sustained period does not show any observable toxicity, and not only prevents breast tumor growth but even slows established breast tumor growth in mice. A highly potent GSTP1 inhibitor, ezatiostat (developed by Telik Inc.) has passed phase I

• It appears that different agonists for GPR activate

  2021-10-09

  

  It appears that different agonists for GPR55 activate different signalling pathways [25]. GPR55 activation through LPI has been shown to trigger ERK 1/2 phosphorylation 22, 23, 25, 33. Conversely, endogenous cannabinoid compounds AEA and 2-AG have been shown to have no effect on ERK 1/2 signalling 2

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