Peptide clearing agents

摘要

A peptide clearing agent is provided for clearance of a conjugate of an enzyme and a binding molecule which binds specifically at a target location from a non-target location in a subject. The peptide clearing agent binds the active site of the enzyme. The peptide also binds to the asialoglycoprotein receptor expressed by hepatic cells to facilitate clearance through the liver. The peptide may be glycosylated to facilitate clearance through the liver by binding to hepatic cells expressing an asialoglycoprotein receptor. Typically, the peptide prevents or inhibits enzyme activity upon binding to the enzyme and is not substantially modified by the enzyme activity. The peptide may be based upon the dipeptide amino-naphthoic acid (ANA)-glutamate (GIu) and may comprise the amino acid sequence serine (Ser)-Alanine (Ala)-amino-naphthoic acid (ANA)-glutamate (GIu). In such cases, the enzyme of interest is typically CPG2.

主权项

1. A peptide clearing agent for clearance of a conjugate of
a. an enzyme; and b. a binding molecule which binds specifically at a target location,from a non-target location in a subject comprising a first domain which binds to the active site of the enzyme and a second domain, which binds to the asialoglycoprotein receptor expressed by hepatic cells to facilitate clearance of the conjugate, bound via the first domain, through the liver wherein the peptide is no more than 30 amino acids in length and comprises the dipeptide amino-naphtoic (ANA)-glutamate (Glu).