Medical Research Council

Shimoda Biotech (Pty) Ltd

Ardana Bioscience Limited

Robert Peter Millar

Stuart Russell Maudsley

Rakel Lopez De Maturana Garmendia

Henry Nicolas Jabbour

Antonia Kathryn Roseweir

The present invention relates to agents, compositions and methods for use in medicine. In particular, the invention relates to agents related to GnRH peptides.

Methods of treating reproductive cancer

The present invention relates to the use of an antagonist of kisspeptin in the manufacture of a medicament for the treatment of a condition induced and/or worsened by kisspeptin activity in an individual. The invention also provides certain defined peptide molecules, which may act as an antagonist of kisspeptin, which are of use in treating a condition induced and/or worsened by kisspeptin activity in an individual. In addition, the invention provides methods of identifying and/or using antagonists of kisspeptin and/or the defined peptides, and pharmaceutical compositions thereof.

Compound, use and method

The invention describes a retro-inverso (RI) gonadotropin-releasing hormone (GnRH) peptide which is capable of eliciting an immune response directed against GnRH, the peptide having the amino acid sequence GPRLGYSWHX, wherein the amino acids are D-amino acids and X is any amino acid. More particularly, X is E, Q, P or G, and even more particularly, X is E or Q. Thus, a preferred amino acid sequence for the peptide is GPRLGYSWHE. The peptide may optionally include one or more additional D-amino acids at its N- or C-terminus, for example a cysteine residue or a series of linker amino acids, such as a plurality of glycine amino acid residues. Thus, a second preferred amino acid sequence for the peptide is GPRLGYSWHEC, which includes a cysteine residue at the C-terminus for conjugation purposes. The invention also describes a vaccine composition for use in controlling fertility, heat, contraception and/or treating sex hormone-related diseases, and a method for controlling and or treating fertility and sex hormone-related diseases.

Retro-inverso gonadotropin-releasing hormone peptide and vaccine composition

A compound comprising a gonadotrophin releasing hormone analogue conjugated to a hormone moiety, or a derivative thereof, which is able to bind to a plasma hormone binding protein. The compounds may be used to treat hormone-dependent disorders such as cancer, or as a contraceptive. 

Gonadotropin releasing hormone analogues conjugates with steroid hormones

A method of combating menorrhagia, dysmenorrhoea or endometriosis in a female individual that includes administering to the individual at least one agent that reduces the effect of prokineticin 1 on a prokineticin receptor.

Treatment of endometriosis

A method for identifying a test compound that has an anti-tumoral effect whilst not significantly activating unrelated transduction signals, the method comprising the steps of: (a) selecting at least one test compound; (b) assaying the compound for anti-tumoral effect; (c) selecting at least one distinct intracellular event which is modulated, at least partially, by the GnRH receptor; (d) testing for the ability of said test compound not to modulate the selected intracellular event; and (e) selecting the test compound which selectively demonstrates an anti-tumoral effect and does not modulate said other selected intracellular event. A method according to any one of the preceding claims, the method comprising: (a) selecting at least one test compound; (b) determining whether the test compound activates signalling via G&#x3b1;i; (d) testing for the ability of said test compound not to modulate signalling via G&#x3b1;q; and (e) selecting the test compound which selectively activates signalling via G&#x3b1;i and does not modulate signalling via G&#x3b1;q. Compounds selected by the methods, including Ac-D-Nal(2)-D-4-ClPhe-D-Pal-Ser-1-MePal-D-IsopropylLys-Leu-IsopropylLys-Pro-D-AlaNH, are useful in combating cancer and reproductive tissue hyperplasias.

Growing community of inventors

Edinburgh, United Kingdom

Robert Peter Millar