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2012558-47-1

2012558-47-1 Structure

2012558-47-1 Structure
IdentificationBack Directory
[Name]

Bulevirtide
[CAS]

2012558-47-1
[Synonyms]

Bulevirtide
Chemical PropertiesBack Directory
[form ]

Solid
[color ]

White to off-white
Hazard InformationBack Directory
[Description]

Bulevirtide (BLV), the first-in-class entry inhibitor, is a 47-amino acid synthetic liner lipopeptide derived from the preS1 domain of the HBV large surface that targets the NTCP, the entry receptor for HBV/HDV. By blocking this receptor, new infections are prevented, and infected hepatocytes are replaced by naive cells that will be protected from infection. Consequently, viral spread in the liver is prevented.
[Biological Activity]

The sequence of Bulevirtide (BLV) is derived from that of preS1 from HBV genotype C (residues Gly2-Gly48) with a shortening of the 11 additional N-terminal amino acids and one amino acid substitution, Gln46Lys. BLV exhibits a remarkably high inhibitory constant (IC50?=?140 pM) against HBV and HDV in primary human hepatocytes and HepaRG cells. BLV has also been demonstrated to inhibit the NTCP-mediated uptake of bile salts but at an IC50 in the nanomolar range[1].
[References]

[1] Liu, Hongtao et al. “Structure of antiviral drug bulevirtide bound to hepatitis B and D virus receptor protein NTCP.” Nature Communications 22 1 (2024).
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