1D05 PCSK9 ANTAGONISTS

摘要

Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.

主权项

1. An isolated PCSK9-specific antagonist which comprises:
(a) a heavy chain variable region comprising a CDR3 domain comprising SEQ ID NO: 17 or an equivalent thereof, said equivalent characterized as having one or more conservative amino acid substitutions in the CDR3 domain; and/or (b) a light chain variable region comprising a CDR3 domain comprising SEQ ID NO: 7 or an equivalent thereof, said equivalent characterized as having one or more conservative amino acid substitutions in the CDR3 domain; wherein said PCSK9-specific antagonist antagonizes PCSK9's inhibition of cellular LDL uptake.