The bioactive lipid sphingosine-1-phosphate (S1P) and its receptors (S1P1-5) play critical roles in many pathologic processes, including cancer. The S1P axis has become a bona fide therapeutic target in cancer. JTE-013 [N-​(2,​6-​dichloro-​4-​pyridinyl)-​2-​[1,​3-​dimethyl-​4-​(1-​methylethyl)-​1H-​pyrazolo[3,​4-​b]pyridin-​6-​yl]-​hydrazinecarboxamide], a known S1P2 antagonist, suffers from in...

Previously we demonstrated that sphingosine 1-phosphate receptor 1 (S1PR(1)) played a prominent, but not exclusive, role in enhancing the excitability of small-diameter sensory neurons, suggesting that other S1PRs can modulate neuronal excitability. To examine the potential role of S1PR(2) in regulating neuronal excitability we used the established selective antagonist of S1PR(2), JTE-013. Here...

Drugs that exhibit insurmountable antagonism are proposed to provide improved clinical efficacy through extended receptor blockade. Long-term suppression of the gonadotropin-releasing hormone receptor (GnRHR) is an important therapeutic approach for a number of sex hormone-dependent diseases. In this study, we describe the mechanism and structural components required for insurmountable activity...

aUniversité de Pau et des Pays de l’Adour LMAP UMR 5142 and Inria CAGIRE Team – Avenue de l’Université – 64 013 Pau, France bInria CAGIRE Team, Université de Pau et des Pays de l’Adour LMAP UMR 5142 – Avenue de l’Université – 64 013 Pau, France cCNRS, Université de Pau et des Pays de l’Adour LMAP UMR 5142 and Inria CAGIRE Team – Avenue de l’Université – 64 013 Pau, France dGhent University – De...

There have been various laboratory methods for the microbiological diagnosis of periodontal disease. However, there have been some disadvantages in these methods. In this study of the application of a chair-side test for microbiological diagnosis, the activity of peptidases in periodontal pockets of patients was examined by using the assay system SK-013. SK-013 consists of synthetic substrates ...

Introduction Sarcoidosis is a granulomatous disease possibly affecting all organ systems. Less than 10% of sarcoidosis patients develop symptomatic neurological involvement. Although muscular non-caseating granulomas (NCGs) can be found in up to 75% of sarcoidosis patients, muscular symptoms develop only in less than 0.5% of sarcoidosis patients. Corticosteroids (CS) are the mainstay of medical...

Pedometer-determined physical activity (PA) levels in Belgian adults were provided and compared to PA scores reported in the International Physical Activity Questionnaire (IPAQ). The representative sample (N=1239) of the Belgian population took on average 9655 (4526) steps/day. According to pedometer indices 58.4% were insufficiently active. Steps/day differed significantly between gender (F = ...