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Abstract

The peptides of formula (I) where: R₁ is the group attached to the N-terminal of the first amino acid of the sequence P, optionally via the ligand X, and is selected from H, CH₃C(═O)—, and maleimide; X is a biradical selected from —NH—(CH₂)_r—C(═O)—, —C(═O)—(CH₂)_r—C(═O)—, —S(CH₂)_r—, —S—(CH₂)_r—C(═O)—, —O—(CH₂)_r—, —S—CH—CH(NH₂)—C(═O)—, —O—(CH₂)_r—C(═O)—, —(CH₂)_r—C(═O)—, —NH—O—CH₂—C(═O)—NH—(CH₂)_r—CH(NH₂)—C(═O)—, —(CH₂)_r—C(═O)—NH—(CH₂)_r—CH(NH₂)—C(═O)—, and —NH—(CH₂)_r—CH(NHC(═O)CH₂NH₂)—C(═O)—; r is 1-5; P is a biradical of an amino acid sequence comprising the sequence D-Pro-D-Trp-D-Val-D-Pro-D-Ser-D-Trp-D-Met-D-Pro-D-Pro-D-Arg-D-His-D-Thr (SEQ ID NO: 1); Y is the group attached to the C-terminal of the last amino acid of the sequence P, and is selected from —NH₂, —OH, —OR₂ and —NHR₂; R₂ is a radical selected from (C₁-C₆)-alkyl and (CH₂)₂—NH—C(═O)—CH₂—O—NH₂; k is 0-2; m is 0-1; with the proviso that when the biradical X is —C(═O)(CH₂)_r—C(═O)—, then R₁ is H; when the N of the amino acid of the sequence P to which is attached the biradical X is a biradical —NH—, then m is 1, and when is a biradical —N—, then m is 0; and when R₁ is maleimide then the biradical X is —C(═O)—(CH₂)_r—C(═O)—, —(CH₂)—C(═O)—, —(CH₂)_r—C(═O)—, and —(CH₂)_r—C(═O)—NH—(CH₂)_r—CH(NH₂)—C(═O)—. The peptides are useful as shuttles through the blood brain barrier (BBB). The constructs BBB-shuttle-cargo, being the cargo of a biologically active substance or for use in a diagnostic method, are useful in therapy and diagnosis.

description='In-line Formulae' end='lead'R₁—(X)_K—P—Y  (I)description='In-line Formulae' end='tail'

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First Claim