Farnesoid-X-receptor (FXR) and GP-BAR1 are bile acids receptors mainly expressed in entero-hepatic tissues that regulates some metabolic and non-metabolic functions [1]. In the last ten years, this two receptors gained an increasing importance because they are involved in many physiological and physio-pathological human conditions. One of the main problem of these receptors is that bile acids are promiscuous ligand for both receptors. Even if the dual activation could be a promising pharmacological opportunity for several metabolic diseases, often it is associated to several side effects. Starting from the results obtained in several our previous works, [2, 3] in this contest, we decide to manipulate bile acids scaffold in order to produce new selective FXR and GP-BAR1 modulators
Synthesis of new bile acids derivatives as selective FXR/GPBAR1 ligands
MASULLO, DARIO;SEPE, VALENTINA;FESTA, CARMEN;FINAMORE, CLAUDIA;ZAMPELLA, ANGELA
2015
Abstract
Farnesoid-X-receptor (FXR) and GP-BAR1 are bile acids receptors mainly expressed in entero-hepatic tissues that regulates some metabolic and non-metabolic functions [1]. In the last ten years, this two receptors gained an increasing importance because they are involved in many physiological and physio-pathological human conditions. One of the main problem of these receptors is that bile acids are promiscuous ligand for both receptors. Even if the dual activation could be a promising pharmacological opportunity for several metabolic diseases, often it is associated to several side effects. Starting from the results obtained in several our previous works, [2, 3] in this contest, we decide to manipulate bile acids scaffold in order to produce new selective FXR and GP-BAR1 modulatorsI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
