Abstract:
:Within our efforts in the discovery of novel potent and selective ligands for the FXR receptor, 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine was synthesized and evaluated for its ability to activate and modulate the biological response of the receptor. Alphascreen and RT-PCR revealed that the 6α-ethyl-24-norcholanyl-23-amine derivate behaves as full FXR agonist endowed with high binding affinity and efficacy, representing a promising lead candidate for further optimization. In addition, docking studies provide new insights into the molecular basis governing the partial and full agonist activity at FXR.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Gioiello A,Macchiarulo A,Carotti A,Filipponi P,Costantino G,Rizzo G,Adorini L,Pellicciari Rdoi
10.1016/j.bmc.2011.03.004subject
Has Abstractpub_date
2011-04-15 00:00:00pages
2650-8issue
8eissn
0968-0896issn
1464-3391pii
S0968-0896(11)00185-4journal_volume
19pub_type
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