Methods and reagents for efficient and targeted delivery of therapeutic molecules to CXCR4 cells
AssigneesUniversitat Autonoma De Barcelona, Institut Recerca Hospital De La Santa Creu I Sant Pau, Centro De Investigacion Biomedica En Red En Bioingenieria Biomateriales Y Nanomedicina (Ciber Bbn)
InventorsAntonio Pedro Villaverde Corrales, Esther Vazquez Gomez, Maria Virtudes Cespedes Navarro, Isolda Casanova Rigat, Neus Ferrer Miralles, Ramon Mangues Bafalluy, Ugutz Unzueta Elorza
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Abstract
Conjugates comprising a targeting moiety specific for the CXCR4 and based on the polyphemusin-derived peptide and a therapeutic or imaging agent are provided. Therapeutic and diagnostic methods with the conjugates which require specific targeting to CXCR4+cells are provided as well.
Claims11
A conjugate comprising
- (i) a targeting peptide comprising the sequence RRWCYRKCYKGYCYRKCR (SEQ ID NO:
- 5) or
- a peptide with at least one conservative amino acid substitution in the sequence SEQ ID NO:
- 5, wherein the conservative amino acid substitution is selected from the following six groups each contain amino acids that are conservative substitutions for one another:
- 1Alanine (A), Serine (S);
- Threonine (T);
- 2Aspartic acid (D), Glutamic acid (E);
- 3Asparagine (N), Glutamine (Q);
- 4Arginine (R), Lysine (K);
- 5Isoleucine (I), Leucine (L), Methionine (M), Valine (V);
- and
- 6Phenylalanine (F), Tyrosine (Y), Tryptophan (W), and
- (ii) a therapeutic agent,
- wherein the targeting peptide specifically binds to chemokine receptor type 4 (CXCR4) and promotes internalization of the therapeutic agent in a cell expressing CXCR4 and wherein the therapeutic agent is a polypeptide or protein.
Dependencies are inferred from the claim text.