Short peptides from the ‘2nd loop’ of 7 transmembrane receptor which selectively modulate signal transduction

A compound which has the property of modulation of signal transduction of a seven transmembrane (7TM) receptor consisting of:

• at least one moiety for transport across cellular membranes, in association with a peptide sequence of 5-20 amino acid residues selected from the group consisting of:
• (a) a peptide sequence which is a continuous stretch of at least 5 amino acids present in the 7TM receptor in positions corresponding to the positions 143-151 of bovine rhodopsin when the 2nd intracellular region of the 7TM receptor is aligned with the 2nd intracellular region of rhodopsin;
• (b) a variant of the peptide sequence according to (a) wherein up to 40% of the amino acids of the native sequence have been replaced with a naturally or non-naturally occurring amino acid or with a peptidomimetic moiety;
• and/or up to 40% of the amino acids have their side chains chemically modified;
• and/or up to 20% of the amino acids have been deleted, provided that, when the 2nd intracellular region of the 7TM receptor is aligned with the corresponding 2nd intracellular region of bovine rhodopsin, at least 50% of the amino acids corresponding to positions 143-151 of parent bovine rhodopsin sequence of (a) are maintained unaltered in the variant;
• (c) a peptide sequence according to (a) or (b) wherein at least one of the amino acids is replaced with a corresponding D-amino acid;
• (d) a peptide sequence according to any one of (a)-(c) wherein at least one of the peptidic backbones has been altered to a non-naturally occurring peptidic backbone;
• (e) a peptide sequence being the sequence of any one of (a)-(d) in reverse order;
• and
• (f) a combination of two or more of the peptide sequences of (a) to (e).