Identification of quinoline-based compounds with dual activity against CysLT1R and GPBAR1 for the treatment of metabolic fatty liver disease

Pharmacological therapy based on dual receptor modulators represents an attractive opportunity for the modulation of the same cellular process by acting on different pathways. This study presents the discovery of new ligands with dual activity against the two membrane receptors, the cysteinyl leukotriene receptor 1 (CysLT1R) and the G-protein coupled bile acid receptor 1 (GPBAR1). The new series with quinoline scaffold has been designed starting from the structure of REV5901 - the first r...

Identification of molecular basis of praja2 and TBC1D31 interaction

OFD1 is a component of the centrosome/basal body playing a key role in cilium biogenesis, and, therefore, in the control of cell differentiation, growth and development. Mutations of the OFD1 cause ciliopathies with several implications in the development determining severe malformations [1]. In this work, we investigated the role of the ubiquitin system in the control of OFD1 activity and stability. In particular, we discovered that praja2 is the E3 ligase responsible for OFD1 ubiquitination...

Identification of quinoline-based compounds with dual activity against CysLT1R and GPBAR1

Pharmacological therapy based on dual receptor modulators represents an attractive opportunity for the modulation of the same cellular process by acting on different pathways. In this work, the discovery of new ligands with dual activity against two membrane receptors is presented: the cysteinyl leukotriene receptor 1 (CysLT1R) and the G protein coupled bile acid receptor 1 (GPBAR1). The novel quinoline series has been designed starting from the structure of REV5901, the first dual compound r...

LENTAMENTE GIOCANDO. S.L.O.W. is CHI.C.: SLOW LIFE ORIENTERING WAY is CHILDREN CITY. Il modo di orientare la vita lenta è la città dei bambini.