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Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists

Yingnan Zhang,Mark Ultsch,Nicholas J Skelton,Daniel J Burdick,Maureen H Beresini,Wei Li,Monica Kong-Beltran,Andrew Peterson,John Quinn,Cecilia Chiu,Yan Wu,Steven Shia,Paul Moran,Paola Di Lello,Charles Eigenbrot,Daniel Kirchhofer

NATURE STRUCTURAL & MOLECULAR BIOLOGY（2017）

Cited 52|Views40
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Abstract
PCSK9 binds to and promotes degradation of LDLR, thus regulating serum levels of LDL. An accessible groove in PCSK9, adjacent to the LDLR-binding site, can be targeted by peptides that disrupt the LDLR interaction.
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Key words
Drug discovery,Peptides,Structural biology,Life Sciences,general,Biochemistry,Protein Structure,Membrane Biology,Biological Microscopy
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