A gastrin analogue shows high uptake in CCK-2 receptor positive tumors and simultaneously a very low accumulation in the kidneys. This is achieved by a mini-gastrin analogue PP-F11 having the formula: PP-F11-X-DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-Ala-Tyr-Gly-Trp-Y-Asp-Phe-NH.sub.2, wherein Y is an amino acid replacing methionine and X is a chemical group attached to the peptide for diagnostic and/or therapeutic intervention at CCK-2 receptor relevant diseases. Very suitable compounds with respect to a high tumor to kidney ratio are mini-gastrin analogues with six D-glutamic acids or six glutamines. These compounds still possess a methionine which can be oxidized easily which is a disadvantage for clinical application under GMP due to the forms which may occur. The elimination of the methionine leads to a lower affinity to oxidation which in general favors the tumor-kidney-ratio. Ideally, the methionine is replaced by norleucine. This PP-F11N mini gastrin exhibits currently the best tumor-kidney-ratio and is the most promising candidate.

A gastrin analog shows high uptake in CCK-2 receptor positive tumors and simultaneously a very low accumulation in the kidneys. This is achieved by a mini-gastrin analog PP-F11 having the formula: PP-F11-X-DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-Ala-Tyr-Gly-Trp-Y-Asp-Phe-NH.sub.2, wherein Y is an amino acid replacing methionine and X is a chemical group attached to the peptide for diagnostic and/or therapeutic intervention at CCK-2 receptor relevant diseases. Very suitable compounds with respect to a high tumor to kidney ratio are mini-gastrin analogs with six D-glutamic acids or six glutamines. These compounds still possess a methionine which can be oxidized easily which is a disadvantage for clinical application under GMP due to the forms which may occur. The elimination of the methionine leads to a lower affinity to oxidation which in general favors the tumor-kidney-ratio. Ideally, the methionine is replaced by norleucine. This PP-F11N mini gastrin exhibits currently the best tumor-kidney-ratio and is the most promising candidate.

A gastrin analog shows high uptake in CCK-2 receptor positive tumors and simultaneously a very low accumulation in the kidneys. This is achieved by a mini-gastrin analog PP-F11 having the formula: PP-F11-X-DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-Ala-Tyr-Gly-Trp-Y-Asp-Phe-NH.sub.2, wherein Y is an amino acid replacing methionine and X is a chemical group attached to the peptide for diagnostic and/or therapeutic intervention at CCK-2 receptor relevant diseases. Very suitable compounds with respect to a high tumor to kidney ratio are mini-gastrin analogs with six D-glutamic acids or six glutamines. These compounds still possess a methionine which can be oxidized easily which is a disadvantage for clinical application under GMP due to the forms which may occur. The elimination of the methionine leads to a lower affinity to oxidation which in general favors the tumor-kidney-ratio. Ideally, the methionine is replaced by norleucine. This PP-F11N mini gastrin exhibits currently the best tumor-kidney-ratio and is the most promising candidate.

A connector of a helical coiled coil-type structure connecting a first and a second molecule, wherein the first molecule comprises a peptidic first alpha-helix and the second molecule comprises a peptidic second alpha-helix, which second alpha-helix is coiled to the first alpha-helix. The first alpha-helix comprises a C-terminal region consisting of a repeat of an amino acid motif a-x.sub.1 and the C-terminal motif a-x.sub.1-x.sub.2, or an N-terminal region consisting of a repeat of an amino acid motif x.sub.1-a and the N-terminal motif x.sub.2-x.sub.1-a, where a is a motif sequence of 4-8 amino acids, x.sub.1 is Lysin, and x.sub.2 is an extension of the motif. The extension consists of 1-10 amino acids and does not comprise more than 4 consecutive amino acids incorporated in said motif a-x.sub.1 or x.sub.1-a. In a multimeric protein, two polypeptide chains can be connected to each other by such connector.

A connector of a helical coiled coil-type structure connecting a first and a second molecule, wherein the first molecule comprises a peptidic first alpha-helix and the second molecule comprises a peptidic second alpha-helix, which second alpha-helix is coiled to the first alpha-helix. The first alpha-helix comprises a C-terminal region consisting of a repeat of an amino acid motif a-x.sub.1 and the C-terminal motif a-x.sub.1-x.sub.2, or an N-terminal region consisting of a repeat of an amino acid motif x.sub.1-a and the N-terminal motif x.sub.2-x.sub.1-a, where a is a motif sequence of 4-8 amino acids, x.sub.1 is Lysin, and x.sub.2 is an extension of the motif. The extension consists of 1-10 amino acids and does not comprise more than 4 consecutive amino acids incorporated in said motif a-x.sub.1 or x.sub.1-a. In a multimeric protein, two polypeptide chains can be connected to each other by such connector.

The present invention relates, inter alia, to certain peptide conjugates, and to the use of the conjugates in the treatment of a variety of diseases or disorders, including diabetes (type 1 and/or type 2) and diabetes related diseases or disorders.

The invention relates to methods for obtaining liposomes externally modified with a targeting peptide able to selectively drive liposomal doxorubicin on membrane receptors over expressed in tumours.

The invention is based on a kit containing a first vial filled with a sterile, translucent, red dispersion of the liposomal doxorubicin drug; a second vial filled with a modified phospholipid with a reactive function such as DSPEPegmaleimide in lyophilized form; and a third vial filled with a peptide modified with an appropriate reactive function, in a 1:1 stoichiometric amount respect to modified phospholipid and in lyophilized form.

The kit could also contain an additional fourth vial with the targeting peptide modified with a chelating agent able to complex radioactive metal ions for diagnostic and imaging purposes. The patients to be treated with the peptide modified liposomal doxorubicin could be selected on the basis of the over expression of the targeting receptors.

The present invention relates, inter alia, to certain peptide conjugates, and to the use of the conjugates in the treatment of a variety of diseases or disorders, including diabetes (type 1 and/or type 2) and diabetes-related diseases or disorders.

The present invention relates, inter alia, to certain peptide conjugates, and to the use of the conjugates in the treatment of a variety of diseases or disorders, including diabetes (type 1 and/or type 2) and diabetes-related diseases or disorders.

There is provided peptidic compounds of Formula I, A or B(R.sup.rad.sub.n6-[linker]-R.sup.L-Xaa.sup.1-Xaa.sup.2-Xaa.sup.3-Xaa.sup.4-Xaa.sup.5-Xaa.sup.6-Xaa.sup.7-Xaa.sup.8--Xaa.sup.9-NH.sup.2). Xaa.sup.1 is D-Phe, Cpa, D-Cpa, Nal, D-Nal, 2-Nal, or D-2-Nal; Xaa.sup.2 is Asn, Gln, Hse, Cit or His. Xaa.sup.3 is Trp, Bta, Trp(Me), Trp(7-Me), Trp(6-Me), Trp(5-Me), Trp(4-Me), Trp(2-Me), Trp(7-F), Trp(6-F), Trp(5-F), Trp(4-F), Trp(5-OH), or Me-Trp. Xaa.sup.4 is Ala or Ser. Xaa.sup.5 is Val, Cpg, or Tle. Xaa.sup.6 is Gly, NMe-Gly, or D-Ala. Xaa.sup.7 is His or NMe-His. Xaa.sup.8 is Leu or Phe. Xaa.sup.9-NH.sub.2 is a C-terminally amidated amino acid residue selected from Pro, 4-oxa-L-Pro, Me.sub.2 Thz, or Thz. represents a peptide bond or reduced peptide bond joining Xaa.sup.8 to Xaa.sup.9. R.sup.rad.sub.n6 is 1-5 radiolabeling groups. There is also provided the use of such compounds as imaging agents or therapeutic agents.