GNRH (gonadotropin-releasing hormone) peptide variants

A technology of drugs and peptide sequences, applied in the directions of luteinizing hormone-releasing hormone, biochemical equipment and methods, and microbial determination/inspection, etc., can solve the problem of not finding functional alternative subtypes, etc.

Inactive Publication Date: 2013-03-20
MEDICAL RESEARCH COUNCIL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although type II receptors have been cloned in some primates, no functional alternative isoform has been identified in humans (Morgan et al., 2003)

Method used

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  • GNRH (gonadotropin-releasing hormone) peptide variants
  • GNRH (gonadotropin-releasing hormone) peptide variants
  • GNRH (gonadotropin-releasing hormone) peptide variants

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0254] Embodiment 1-experimental data

[0255] Materials and methods

[0256] Material

[0257] GnRH I and GnRH II were purchased from Sigma-Aldrich Co. Ltd. (Poole, Dorset, UK). Modified GnRH analogs were purchased from Roger Roeske (University of Indiana, Indianapolis, USA). Anti-phospho-ERK1 / 2 and anti-ERK2 antisera were purchased from New England Biolabs (UK) Ltd. (NEB; Hitchin, Herts, UK). Anti-cleaved poly[ADPribose] polymerase (PARP) antibody (Asp214 / Gly215; human specific) was purchased from Cell Signaling Technology, Inc. (Beverly, MA, USA). All secondary antibodies were purchased from Sigma. Chemical inhibitors JNK inhibitor II, PD98059 (MEK inhibitor), SB203580 (p38MAPK inhibitor), wortmannin (PI-3K inhibitor), herbimycin A (tyrosine kinase Inhibitor), PP2 (Src Inhibitor), AG1478 (EGFR Inhibitor), U-73122 (PLC Inhibitor), Ro-31-8220 (PKC Inhibitor) and (PKC inhibitor) was purchased from Calbiochem (Calbiochem / Merck Biosciences Ltd.; Nottingham, East Midland...

Embodiment 2

[0308] Example 2 Exemplary Pharmaceutical Composition

[0309] While it is possible to use the agents of the invention alone, it is preferred to present them as pharmaceutical compositions together with one or more acceptable carriers. The carrier must be "acceptable" in the sense of being compatible with the agents of the invention and not deleterious to its recipients. Usually, the carrier is sterile and pyrogen-free water or saline.

[0310] The following examples illustrate medicaments and pharmaceutical compositions according to the present invention, wherein the active ingredient is an agent of the present invention.

[0311] Preferably, the agent of the invention is provided in an amount ranging from 10 μg to 500 mg. It should be recognized that the following exemplary medicaments and pharmaceutical compositions can be formulated with 10 [mu]g to 500 mg of the agents described herein. For example, the agents of the invention may be presented in one-tenth or one-hundr...

Embodiment 3

[0367] Example 3 - Treatment of Proliferative Disorders Using Agents of the Invention

[0368] According to the method of the present invention, 1 mg of the agent of the present invention is administered intramuscularly per day to a patient with prostate cancer unresponsive to antiandrogen therapy.

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Abstract

The inventors have discovered that substituting amino acid residues at positions 5 and / or 7 and / or 8 of the GnRH I (gonadotropin-releasing hormone) peptide sequence, and particularly removal of the arginine residue at position 8, results in elevated antiproliferative activitey. Furthermore, the introduction of certain D-amino acid residues at position 6 of the GnRH II peptide sequence results in elevated antiproliferative activity. This surprising discovery provides potent and selective agents for use in treating antiproliferative disorders, such as cancer.

Description

[0001] This application is a divisional application of the Chinese patent application with the application number 200780026537.3, the application date is May 1, 2007, and the invention title is "GnRH (Gonadotropin-releasing Hormone) Peptide Derivatives". technical field [0002] The present application relates to reagents, compositions and methods for use in medicine. In particular, the invention relates to agents related to GnRH peptides. Background technique [0003] At least two forms of gonadotropin-releasing hormone (GnRH) exist in humans. Although little is known about the biological role of GnRH II, GnRH I is known to be a central regulator of neuroendocrine control of mammalian reproduction. GnRH I released from hypothalamic neurons binds to its specific, G protein-coupled receptor (GPCR) in the anterior pituitary, ultimately promoting gonadotropin synthesis and release (Kaiser et al. , 1997; Millar et al., 2004). GnRH additionally has effects on extra-pituitary t...

Claims

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Application Information

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IPC IPC(8): C07K7/06C12N5/07C12Q1/02A61K38/08A61P35/00
CPCC07K7/23A61K38/00A61P35/00
Inventor R·P·米勒S·R·莫兹利R·洛佩斯德马图拉纳加门迪亚
Owner MEDICAL RESEARCH COUNCIL
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