Title : E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: structural development study and separation from farnesoid X receptor-agonistic activity.

Pub. Date : 2012 Jun 15

PMID : 22583617






5 Functional Relationships(s)
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1 E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: structural development study and separation from farnesoid X receptor-agonistic activity. GW 4064 ATP binding cassette subfamily B member 11 Homo sapiens
2 E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: structural development study and separation from farnesoid X receptor-agonistic activity. GW 4064 ATP binding cassette subfamily B member 11 Homo sapiens
3 We previously found that compounds based on GW4064, a representative farnesoid X receptor (FXR) agonist, enhanced E297G BSEP transport activity. GW 4064 ATP binding cassette subfamily B member 11 Homo sapiens
4 Here, we conducted a structure-activity relationship analysis of GW4064 derivatives aimed at separating E297G BSEP-function-promoting activity and FXR-agonistic activity. GW 4064 ATP binding cassette subfamily B member 11 Homo sapiens
5 Among newly synthesized reversed-amide derivatives of previously reported GW4064 analogs 2a-2f, we identified 7c as a selective BSEP function enhancer. GW 4064 ATP binding cassette subfamily B member 11 Homo sapiens