Method For Induction and Enhancement of Apoptosis In Tumor Cells
AssigneeGeorg-August-UniversitäT GöTtingen Stiftung öFfentlichen Rechts, UniversitäTsmedizin
InventorsCarsten Grundker, Andreas R. Gunthert, Gunter Emons
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Abstract
The present invention relates to methods for inducing and enhancing apoptosis in pathogenic cells. In particular, the present invention relates to the use of GnRH II antagonists for inducing and enhancing apoptosis of specific types of tumor cells, i.e. breast cancer and malignant melanoma as well as gynaecological cancers like endometrial or ovarian cancer, expressing the GnRH II receptor as well as to methods relating thereto. In addition, new GnRH II antagonists are provided.
Claims34
Method for inducing and/or enhancing apoptosis of tumor cells expressing the GnRH II receptor wherein said tumor cells are tumor cells or precursor of tumor cells of breast cancer or malignant melanoma or gynaecological cancers comprising the step of contacting said cells with a GnRH II antagonist.
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A method for the remission of tumor cells or precursors thereof of a breast cancer or malignant melanoma or a gynaecological cancer in a subject comprising the step of contacting the tumor cells or the precursor cells of said cancer with a GnRH II antagonist.
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A compound having the general formula (Seq.-ID No. 46):
- X2—X3-Ser-X4—X5—X6—X7-Pro-X8—NH2
- wherein
- X1=Ac-D-2NaI, Ac-Δ3Pro
- X2=His, D-4 Cpa, Arg, Tyr, Trp, D-4Fpa, D-4 Bpa,
- X3=Trp, D-3 Pal, D-2NaI, Ala, Phe, His
- X4=Tyr, His
- X5=D-Lys, D-Trp, D-3 Pal, D-2NaI
- X6=Trp, Leu, Arg
- X7=Tyr, Leu, Arg
- X8=D-Ala, D-Gly, D-cys, D-Ser, D-Val, D-Thr, D-Pro, D-IIE, D-Leu or derivatives thereof.
A pharmaceutical composition comprising a compound of ‘Seq. ID No. 46 and, optionally, a pharmaceutically acceptable carrier.
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A method for the remission of tumor cells or precursor cells thereof of a breast cancer or malignant melanoma or a gynaecological cancer or a prostate cancer in a subject comprising the step of contacting the tumor cells or the precursor cells thereof of said cancer with a GnRH II antagonist comprising a compound having the general formula (Seq.-ID No. 46):
- X2—X3-Ser-X4—X5—X6—X7-Pro-X8—NH2
- wherein
- X1=Ac-D-2NaI, Ac-Δ3Pro
- X2=His, D-4Cpa, Arg, Tyr, Trp, D-4Fpa, D-4 Bpa,
- X3=Trp, D-3 Pal, D-2NaI, Ala, Phe, His
- X4=Tyr, His
- X5=D-Lys, D-Trp, D-3 Pal, D-2NaI
- X6=Trp, Leu, Arg
- X7=Tyr, Leu, Ara
- X8=D-Ala, D-Gly, D-cys, D-Ser, D-Val, D-Thr, D-Pro, D-IIE, D-Leu or derivatives thereof.
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A method for inducing and/or enhancing apoptosis of tumor cells or precursor cells thereof expressing the GnRH II receptor wherein said tumor cells are tumor cells or precursor cells thereof of prostate cancer, or gynaecological cancer, or a breast cancer or malignant melanoma comprising the step of contacting said cells with a GnRH II antagonist comprising a compound having the general formula (Seq.-ID No. 46):
- X2—X3-Ser-X4—X5—X6—X7-Pro-X8—NH2
- wherein
- X1=Ac-D-2NaI, Ac-Δ3Pro
- X2=His, D-4Cpa, Arg, Tyr, Trp, D-4Fpa, D-4Bpa,
- X3=Trp, D-3 Pal, D-2NaI, Ala, Phe, His
- X4=Tyr, His
- X5=D-Lys, D-Trp, D-3 Pal, D-2NaI
- X6=Trp, Leu, Arg
- X7=Tyr, Leu, Arg
- X8=D-Ala, D-Gly, D-cys, D-Ser, D-Val, D-Thr, D-Pro, D-IIE, D-Leu or derivatives thereof.
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Dependencies are inferred from the claim text.