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Journal of Mammary Gland Biology and Neoplasia

Published in:

01-03-2008

Rational Design of Competitive Prolactin/Growth Hormone Receptor Antagonists

Authors: Estelle Tallet, Vincent Rouet, Jean-Baptiste Jomain, Paul A. Kelly, Sophie Bernichtein, Vincent Goffin

Published in: Journal of Mammary Gland Biology and Neoplasia | Issue 1/2008

Abstract

There is increasing evidence that prolactin (PRL) and growth hormone (GH) act as growth-promoters of breast tumors. Recent arguments have accumulated to suggest that when they are locally-produced within the mammary tissue, these hormones, acting by an autocrine-paracrine mechanism may have enhanced, or even specific functions compared to endocrine PRL and GH. Classical drugs blocking pituitary hormone production (dopamine and somatostatin analogs) are ineffective on extrapituitary expression of PRL/GH genes, therefore the undesirable effects of these locally-produced hormones remain a target of interest for alternative strategies. This has encouraged the development of competitive PRL and/or GH receptor antagonists, which involve engineered variants of natural receptor ligands (PRL or GH) aimed at blocking receptor activation rather than hormone production in peripheral tissues. This article overviews the rational design of this new class of molecules, their specific molecular features (receptor specificity, biological properties, etc.) and whenever available, the data that have been obtained in cell or animal models of breast cancer.

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Title: Rational Design of Competitive Prolactin/Growth Hormone Receptor Antagonists
Authors: Estelle Tallet
Vincent Rouet
Jean-Baptiste Jomain
Paul A. Kelly
Sophie Bernichtein
Vincent Goffin
Publication date: 01-03-2008
Publisher: Springer US
Published in: Journal of Mammary Gland Biology and Neoplasia / Issue 1/2008
Print ISSN: 1083-3021
Electronic ISSN: 1573-7039
DOI: https://doi.org/10.1007/s10911-008-9066-8

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