Title : Knocking on FXR's door: the "hammerhead"-structure series of FXR agonists - amphiphilic isoxazoles with potent in vitro and in vivo activities.

Pub. Date : 2014

PMID : 25388536






3 Functional Relationships(s)
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1 The quest for synthetic non-steroidal FXR agonists with general drug likeliness and improved pharmacokinetic and - dynamic properties has started more than a decade ago: The first non-steroidal and selective FXR agonist with decent submicromolar potency, GW4064, was patented in 1998 and published in 2000. GW 4064 nuclear receptor subfamily 1 group H member 4 Homo sapiens
2 The quest for synthetic non-steroidal FXR agonists with general drug likeliness and improved pharmacokinetic and - dynamic properties has started more than a decade ago: The first non-steroidal and selective FXR agonist with decent submicromolar potency, GW4064, was patented in 1998 and published in 2000. GW 4064 nuclear receptor subfamily 1 group H member 4 Homo sapiens
3 Since then, many pharmaceutical companies have taken GW4064 as a structural template for their efforts in identifying novel patentable FXR agonists with the GW-derived trisubstituted isoxazole general structure. GW 4064 nuclear receptor subfamily 1 group H member 4 Homo sapiens