APROTININ POLYPEPTIDES FOR TRANSPORTING A COMPOUND ACROSS THE BLOOD-BRAIN BARRIER

摘要

The invention relates to improvements in the field of drug delivery. More particularly, the invention relates to polypeptides derived from aprotinin and from aprotinin analogs as well as conjugates and pharmaceutical compositions comprising these polypeptides or conjugates. The present invention also relates to the use of these polypeptides for transporting a compound or drug across the blood-brain barrier of a mammal and in the treatment and diagnosis of neurological diseases.

主权项

1. A method for treating a mammal having a neurological disease, said method comprising administering to said mammal a conjugate comprising:
(a) a polypeptide comprising an amino acid sequence having at least 80% identity to the sequence of Angiopep-1 (SEQ ID NO:67), wherein said polypeptide has a substitution at the position corresponding to the cysteine at position 7 of the Angiopep-1 sequence; and (b) an agent for treating said neurological disease, wherein said agent is conjugated to said polypeptide, wherein said conjugate is capable of crossing the blood-brain barrier or an in vitro model thereof.