The present invention provides a manufacturing process for preparing a peptide, preferably a decapeptide, such as degarelix, by incorporating p-nitro-phenylalanin in the amino acid sequence preferably during stepwise solid phase synthesis, and converting these into the required amino acids Aph(Hor) and/or D-Aph(Cbm), preferably while attached to a solid phase. The invention further provides intermediates useful in the manufacturing process.

Compositions and methods for treating a medical condition are provided. Accordingly, there is provided a composition comprising a polypeptide comprising a GnRH receptor binding protein and a polynucleotide coding a therapeutic agent, wherein said polypeptide is in association with said polynucleotide via a linker comprising a cleavage motif that can be cleaved by a proteolytic enzyme secreted by a cell expressing said GnRH receptor. Also provided is a nucleic acid construct comprising a nucleic acid sequence encoding a fusion protein comprising a DNA binding domain (DBD) of a transcription factor that binds a regulatory region of a gonadotropin gene attached to a chromatin modifying domain that represses transcription upon association with the DBD. Also provided are methods of use thereof.

Compositions and methods for treating a medical condition are provided. Accordingly, there is provided a composition comprising a polypeptide comprising a GnRH receptor binding protein and a polynucleotide coding a therapeutic agent, wherein said polypeptide is in association with said polynucleotide via a linker comprising a cleavage motif that can be cleaved by a proteolytic enzyme secreted by a cell expressing said GnRH receptor. Also provided is a nucleic acid construct comprising a nucleic acid sequence encoding a fusion protein comprising a DNA binding domain (DBD) of a transcription factor that binds a regulatory region of a gonadotropin gene attached to a chromatin modifying domain that represses transcription upon association with the DBD. Also provided are methods of use thereof.

Conjugating LHRH to curcumin (LHRH-Curcumin) substantially enhances the bioavailability of curcumin, targets it to cells expressing LHRH receptors, facilitates intravenous administration, and increases the anti-cancer efficacy of curcumin. The conjugate may be used against cancer cells that express the LHRH receptor: pancreas, prostate, breast, testicular, uterine, ovarian, melanoma. LH-Curcumin conjugates may be used against cancer cells that express the LH receptor: prostate, breast, ovary, testis, uterus, pancreas, and melanoma.

Conjugating LHRH to curcumin (LHRH-Curcumin) substantially enhances the bioavailability of curcumin, targets it to cells expressing LHRH receptors, facilitates intravenous administration, and increases the anti-cancer efficacy of curcumin. The conjugate may be used against cancer cells that express the LHRH receptor: pancreas, prostate, breast, testicular, uterine, ovarian, melanoma. LH-Curcumin conjugates may be used against cancer cells that express the LH receptor: prostate, breast, ovary, testis, uterus, pancreas, and melanoma.

The conjugation of luteinizing hormone-releasing hormone (LHRH) with activated cisplatin using a malonate linker gives rise to a new Platinum-LHRH conjugate that effectively targets tumor cells that express the LHRH receptor. The Pt-LHRH conjugate may be used in a method for killing or inhibiting the growth of a tumor cell, especially in late state, highly invasive and aggressive stage IV tumors and in reoccurring tumors.

The conjugation of luteinizing hormone-releasing hormone (LHRH) with activated cisplatin using a malonate linker gives rise to a new Platinum-LHRH conjugate that effectively targets tumor cells that express the LHRH receptor. The Pt-LHRH conjugate may be used in a method for killing or inhibiting the growth of a tumor cell, especially in late state, highly invasive and aggressive stage IV tumors and in reoccurring tumors.

The conjugation of luteinizing hormone-releasing hormone (LHRH) with activated cisplatin using a malonate linker gives rise to a new Platinum-LHRH conjugate that effectively targets tumor cells that express the LHRH receptor. The Pt-LHRH conjugate may be used in a method for killing or inhibiting the growth of a tumor cell, especially in late state, highly invasive and aggressive stage IV tumors and in reoccurring tumors.

The conjugation of luteinizing hormone-releasing hormone (LHRH) with activated cisplatin using a malonate linker gives rise to a new Platinum-LHRH conjugate that effectively targets tumor cells that express the LHRH receptor. The Pt-LHRH conjugate may be used in a method for killing or inhibiting the growth of a tumor cell, especially in late state, highly invasive and aggressive stage IV tumors and in reoccurring tumors.

Disclosed is a method for preparing ganirelix acetate. The method includes the following steps: respectively replacing Fmoc-HArg(Et).sub.2-OH and Fmoc-D-HArg(Et).sub.2-OH by employing Fmoc-Lys(Boc)-OH and Fmoc-D-Lys(Boc)-OH or Fmoc-Lys(Alloc)-OH and Fmoc-D-Lys(Alloc)-OH; synthesizing a ganirelix precursor I or ganirelix precursor II-peptide resin in advance; and then respectively performing modifications and treatments on side chain amino groups of Lys and D-Lys in the precursor I or the precursor II-peptide resin to obtain ganirelix acetate. The ganirelix acetate synthesized therefrom is high in purity, has few impurities and a relatively low cost, and is suitable for large-scale production.