Targeted therapeutics

摘要

The present invention relates to compositions, methods and kits for delivery of active agents (X) to cells or tissues that express proteoglycans. More specifically, the present invention relates to conjugates comprising (HB-linker)n-Xm-(linker-HB)o, where HB is a heparin binding protein, X is an active agents such as a therapeutic protein (including a functional fragment or variant thereof), or a therapeutic small molecule, linker is a linker entity and m is an integer of at least 1, and n+o is an integer of at least 1. Other aspects relate to use of a HB-X conjugate in methods to deliver active agents to cartilage for the treatment of cartilage related disease and disorders, the use of the HB-X conjugate in methods to deliver active agents to neuronal tissues (e.g., brain and spinal cord) for the treatment of neurological disorders, and the use of the HB-X conjugates in methods for the treatment of eye conditions and disorders and inflammatory conditions and disorders.

主权项

1. A composition comprising:
at least one heparin binding (HB) peptide selected from the group consisting of KRKKKGKGLGKKRDPRLRKYK (SEQ ID NO:2) and KRKKKGKGLGKKRDPKLRKYK (SEQ ID NO:3); and an active agent (X) linked to the HB peptide, wherein X is selected from the group consisting of a chemical entity to be administered to a subject to treat a condition and a biological product to be administered to a subject to treat a condition.