• The first rationally designed dual

  2023-04-20

  

  The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic carboxypeptidase b - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been

• Additionally regulation of GPCR heteromerization by specific

  2023-04-20

  

  Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut

• Leflunomide mg br Acknowledgements We thank Dr Stefan Schult

  2023-04-20

  

  Acknowledgements We thank Dr. Stefan Schulte-Merker and his group members at the Hubrecht Institute (Utrecht, the Netherlands) for their invaluable support of the zebrafish studies. Our work is supported by grants from the Dutch Cancer Society (KWF) and the Netherlands Organisation for Scientific

• The identification of novel kinase inhibitor

  2023-04-20

  

  The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y

• Further important evidence for G

  2023-04-20

  

  Further important evidence for G protein signaling on early endosomes has been subsequently obtained for the β2-adrenegic receptor using fluorescently-tagged conformation-sensitive nanobodies selectively recognizing the active receptor and Gs protein [43]. More recently, our group used a combinatio

• Secondly leptin has been shown

  2023-04-20

  

  Secondly, leptin has been shown to enhance aromatase mRNA expression, aromatase content and its enzymatic activity in epithelial breast cancer naloxone hydrochloride by inducing promoters II and I.3 via an enhanced binding of transcription activator protein 1 (AP-1) complex to specific DNA sites in

• Biocytin synthesis In our approach using BRET

  2023-04-20

  

  In our approach using BRET and FRET, there is a substantial increase in BRET and FRET signals between Giα2 or Giα3-YFP and CFP- Gγ2/Rluc-Gγ2 upon apelin-13 activation, indicating that Gαi2, Gαi3 and N-terminus of Gβ1γ2 subunits become closer without subunit dissociation. In contrast, both the FRET a

• br Acknowledgments and Disclosures br Introduction

  2023-04-20

  

  Acknowledgments and Disclosures Introduction Over the last decade, the most visible strategy for the treatment of Alzheimer's disease (AD) has been amyloid β peptide (Aβ) immunotherapy (reviewed in [1]). Although the first efforts with Aβ immunotherapy failed to complete clinical trials [1], A

• br Introduction Hepatocellular carcinoma HCC

  2023-04-20

  

  Introduction Hepatocellular carcinoma (HCC) is the third-leading cause of cancer-related death worldwide and accounts for 70–85% of all liver cancer diagnoses [1]. In East and South-East Asia, the occurrence of HCC and the related number of fatalities have gradually increased in recent decades [2

• br Current therapies for metabolic diseases Inborn errors

  2023-04-20

  

  Current therapies for metabolic diseases Inborn errors of metabolism caused by deficiency of particular enzymes due to loss of function mutations or deletions have been treated by decreasing the intake of the enzymatic substrate, supplementation with an essential cofactor or vitamin, increasing m

• Salivary amylase activity was not significantly

  2023-04-19

  

  Salivary α-amylase activity was not significantly different between bitches with pyometra and healthy bitches, and there were no significant changes after ovariohysterectomy, similar to chromogranin A (Jitpean et al., 2015). Therefore, it is postulated that the SAM axis is not activated in bitches w

• The extent to which GPCR oligomerization is

  2023-04-19

  

  The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or

• In this study we have isolated genes that encode ACL

  2023-04-18

  

  In this study, we have isolated mt t that encode ACL from G. zeae through random mutagenesis by restriction enzyme-mediated integration (REMI). The mutant Z39P186 where the ACL gene had been disrupted showed defects in vegetative growth, asexual and sexual development, virulence, and trichothecene

• br Introduction Throughout early prophase I meiotic cells

  2023-04-18

  

  Introduction Throughout early prophase I, meiotic cells intentionally generate DSBs as part of a stringently controlled process to initiate homologous recombination (HR). HR is a critical DSB repair pathway that ultimately permits the exchange of genetic information between homologous chromosomes

• poly ic Apoptosis signal regulating kinase ASK also referred

  2023-04-18

  

  Apoptosis signal-regulating kinase 1 (ASK1, also referred to as MAP3K5)(Ichijo et al., 1997) participates in many different stress responses, including apoptosis (Chang et al., 1998, Chen et al., 1999, Ichijo et al., 1997, Kanamoto et al., 2000, Noguchi et al., 2008, Saitoh et al., 1998, Tobiume et

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