Design of Dimeric Bile Acid Derivatives as Potent and Selective Human NTCP Inhibitors
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https://figshare.com/articles/dataset/Design_of_Dimeric_Bile_Acid_Derivatives_as_Potent_and_Selective_Human_NTCP_Inhibitors/14499791
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资源简介：
Dimeric bile acid derivatives (DBADs)
were developed and tested
for their anti-HBV and anti-HDV activities as sodium taurocholate
cotransporting polypeptide (NTCP) inhibitors. DBADs exhibited strong
and persistent potency of NTCP inhibition, whereas diverse linkers
and constitutions showed distinct inhibition features. Motif aa157–165
on NTCP was shown to be a possible binding site of DBADs; therefore,
we
determined DBADs’ selectivity among NTCPs from different species.
A cyclized DBAD scaffold DBA-41 exhibited a high affinity to human
NTCP (hNTCP). Intraperitoneal administration of DBA-41 to hNTCP-tg
mice induced serum total bile acid elevation. DBA-41 may serve as
a biological tool to study NTCP physiological function.
创建时间：
2021-04-28
