• The overall very satisfactory potency profile of compounds a

  2022-08-29

  

  The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic RGDfK core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly sensiti

• Oxaliplatin mg Ning et al showed that LPC

  2022-08-29

  

  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

• individuals with variants in the codon

  2022-08-26

  

  13 individuals with variants in the codon 1031–1159 region had global developmental delay and apparent ID, ranging from speech delay and learning difficulties to markedly impaired basic life functions (Table 2 and Table S3). The last available occipitofrontal-circumference measurements revealed micr

• Oltipraz has been shown to inhibit

  2022-08-26

  

  Oltipraz has been shown to inhibit the growth of HCC gemsa australia and is being evaluated in clinical trials as a potential anti-cancer drug for HCC (Mann et al., 2009; Piton et al., 2005; Yates and Kensler, 2007). The present observation that pre-treatment of tumorigenic liver cells with oltipra

• Following our initial observation of an unexpected increase

  2022-08-26

  

  Following our initial observation of an unexpected increase in the maximal rates of cGMP formation by NO-stimulated sGC in the presence of cytosolic PCA preparations [15], we attempted to purify, identify and characterize the responsible protein(s). The purification protocol described in the present

• Lactate as administered in these models is metabolized rapid

  2022-08-26

  

  Lactate as administered in these models is metabolized rapidly and it appears that transient engagement of GPR81 with lactate serum concentrations in the range of moderate exercise physiology, as measured here at 3–4 mmol/L, are sufficient to suppress tissue macrophage NF-κB activation in our models

• br Acknowledgments br Introduction Obesity and type

  2022-08-26

  

  Acknowledgments Introduction Obesity and type 2 diabetes (T2D) are two major chronic non-communicable diseases that are increasing worldwide at an alarming rate; the majority of people with T2D are overweight or obese, and T2D associated with obesity is expected to have doubled by 2030 (Chen e

• br Declaration of interest br

  2022-08-26

  

  Declaration of interest Acknowledgments This work was supported by grants from the Polish National Science Centre (PRELUDIUM grant no. 2013/11/N/NZ5/00270) and the European Commission FP7 Project Beta-JUDO (grant number 279 153), European Union EIT Health project DeTecT2D, Swedish Diabetes A

• Hair loss in women is polygenic

  2022-08-26

  

  Hair loss in women is polygenic and multifactorial with the additional influence of environmental factors. Several studies focused on the importance of several genes related to alopecia (Carey et al., 1993, Hillmer et al., 2008, Randall, 2008). FPHL involves progressive hair follicle miniaturization

• Several studies have found that GPR possesses a distinct pha

  2022-08-26

  

  Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected STF 31 expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Rimona

• With the administration of OM

  2022-08-26

  

  With the administration of OM3 fatty acids, it has previously been shown that the activation of GPR120 is linked to the secretion and circulating levels of the adipokine adiponectin [123] promoting anti-inflammation (downregulation of NF-κB) and insulin sensitivity [124]. Interestingly, Nrf2 also d

• br Author contributions br Acknowledgements The work was fin

  2022-08-26

  

  Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa

• GnRH ant have been designed to obtain pharmacological

  2022-08-26

  

  GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p

• Given that we planned to

  2022-08-26

  

  Given that we planned to isolate the GluN1/GluN3A receptor by immunoaffinity chromatography using a Myc epitope tag on GluN3A, we first checked that the tag does not affect the functional properties of the receptor. To do this we co-transfected HEK-293 cells with DNA encoding WT GluN1 and either WT

• Excessive extracellular glutamate may induce excitotoxic neu

  2022-08-26

  

  Excessive extracellular glutamate may induce excitotoxic neuronal damage in disorders of the CNS (Schwartz et al., 2003). EAATs are considered to contribute to prevention of excitotoxicity by glutamate uptake. Our data revealed that expression levels of membrane EAAT proteins in astrocytes are much

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