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. 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 deseases, often it is associated to several side effects. Starting from the results obtained in several our previous works, in this contest, we decide to manipulate bile acids scaffold in order to produce new selective FXR and GP-BAR1 modulators.

Bile acids derivatives in the selective modulation of FXR and GPBAR1

MASULLO, DARIO;FINAMORE, CLAUDIA;SEPE, VALENTINA;FESTA, CARMEN;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. 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 deseases, often it is associated to several side effects. Starting from the results obtained in several our previous works, in this contest, we decide to manipulate bile acids scaffold in order to produce new selective FXR and GP-BAR1 modulators.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/647627
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