[en] Activation of the estrogen receptor alpha (ERa) is of prime importance for the development of hormone-dependent breast cancers. Hence, drugs able to impede the emergence of an active folding of ERa have been used for a long time as a first line therapeutic strategy. Aromatase inhibitors that block estradiol synthesis and / or antiestrogens that compete with hormone binding to the receptor are routinely prescribed. Unfortunately, emergence of tumor resistance almost invariably results from currently used antihormonal approaches. One may anticipate that a 'multi-target' strategy affecting key regulatory domains distinct from ligand binding pocket of ERa may help to circumvent this problem. To reach this goal, the synthesis of peptides that may specifically inhibit intra- or inter-molecular interactions has been proposed. This paper describes functional motifs potentially suitable for the design of such antagonists. Activity of available peptidic and non-peptidic mimics of these motifs is also reviewed.
Disciplines :
Oncology
Author, co-author :
Leclercq, Guy
Gallo, Dominique
Cossy, Janine
Laïos, Ioanna
Larsimont, Denis
Laurent, Guy ; Université de Mons > Faculté de Médecine et de Pharmacie > Histologie
Jacquot, Yves
Language :
English
Title :
Peptides targeting estrogen receptor alpha - Potential applications for breast cancer treatment
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