Selective delivery molecules and methods of use

摘要

Disclosed herein is a selective delivery molecule comprising: (a) an acidic sequence (portion A) which is effective to inhibit or prevent the uptake into cells or tissue retention, (b) a molecular transport or retention sequence (portion B), and (c) a linker between portion A and portion B, and (d) at least one cargo moiety.

主权项

1. A selective delivery molecule of Formula I, having the structure:
[DA-cA]-A-[cM-M]-X-B-[cB-DB]  Formula Iwherein,
X is a peptide linker cleavable by a protease; A is a peptide with a sequence comprising a series of 5 glutamates (SEQ ID NO:5); B is a peptide with a sequence comprising a series of 8 arginines (SEQ ID NO:6); cA, cB, and cM are each independently 0-1 naturally-occurring amino acid or non-naturally-occurring amino acid; M is a polyethylene glycol (PEG) polymer having an average molecular weight of 500 Da to 10 kDa; and DA and DB are a pair of acceptor and donor fluorescent moieties that are capable of undergoing Försters/fluorescence resonance energy transfer with the other; andwherein [cM-M] is bound to at any position on X, [DA-cA] is bound to any amino acid on A, and [cB-DB] is bound to any amino acid on B.