title: Peptides targeting estrogen receptor alpha-potential applications for breast cancer treatment.
abstract: Activation of the estrogen receptor alpha (ERα) is of prime importance for the development of hormone-dependent breast cancers. Hence, drugs able to impede the emergence of an active folding of ERα 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 ERα 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.
authors: Laboratoire J-C Heuson de Cancérologie Mammaire - Université Libre de Bruxelles, Institut Jules Bordet, 1 rue Héger-Bordet, B-1000 Brussels, Belgium. lcanmamm@ulb.ac.be
authors: Guy
authors: G
authors: Leclercq
authors: Dominique
authors: D
authors: Gallo
authors: Janine
authors: J
authors: Cossy
authors: Ioanna
authors: I
authors: Laïos
authors: Denis
authors: D
authors: Larsimont
authors: Guy
authors: G
authors: Laurent
authors: Yves
authors: Y
authors: Jacquot
mesh_terms: D000818:Animals; D047072:Aromatase Inhibitors / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D015195:Drug Design; D019008:Drug Resistance, Neoplasm; D004965:Estrogen Antagonists / Q000494:pharmacology*; D047628:Estrogen Receptor alpha / Q000037:antagonists & inhibitors / Q000378:metabolism; D005260:Female; D006801:Humans; D008024:Ligands; D010455:Peptides / Q000494:pharmacology*; D017510:Protein Folding
chemical_list: D047072:Aromatase Inhibitors; D004965:Estrogen Antagonists; D047628:Estrogen Receptor alpha; D008024:Ligands; D010455:Peptides