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    • 1. 发明公开
    • Use of monocarboxylate transporter proteins for thyroid hormone transport
    • Verwendung von Monocarboxylat-Transporterproteinen zum Transport von Thyroidhormonen
    • EP1364962A1
    • 2003-11-26
    • EP02077061.6
    • 2002-05-24
    • Stichting tot bevordering van de wetenschap der Endocrinologie
    • Friesema, Edith, Catharina, HendrikaKrenning, Eric, PaulVisser, Theofilus, Johannes
    • C07K14/47A61K38/17A61K45/00A61K48/00G01N33/50A61P5/14
    • C07K14/47
    • The invention provides a use of a monocarboxylate transporter protein or a functional part, derivative and/or analogue thereof for altering transport of a thyroid hormone or a functional part, derivative and/or analogue thereof across a membrane. Said monocarboxylate transporter protein preferably comprises MCT-8. An isolated molecule capable of specifically binding at least part of an MCT protein, or at least part of a ligand of an MCT protein, is also herewith provided. Regulation of the bioavailability of thyroid hormone in a tissue enables interfering with (metabolic) diseases. Hence, the invention also provides pharmaceutical compositions comprising a compound capable of binding said MCT protein, or capable of influencing the binding or transporting of a ligand of said MCT protein. Methods for treatment of a disease such as a disorder of thyroid metabolism, non-thyroidal illness, obesity or cardiovascular illness are also provided, as well as bioassays for identifying or detecting a candidate drug capable of binding to or influencing at least part of said MCT protein.
    • 本发明提供了单羧酸转运蛋白或其功能部分,衍生物和/或类似物用于改变跨膜的甲状腺激素或其功能部分,衍生物和/或类似物的转运的用途。 所述单羧酸转运蛋白优选包含MCT-8。 还提供了能够特异性结合至少部分MCT蛋白或至少部分MCT蛋白质配体的分离的分子。 调节组织中甲状腺激素的生物利用度可以干预(代谢)疾病。 因此,本发明还提供了包含能够结合所述MCT蛋白的化合物或能够影响所述MCT蛋白质的配体的结合或转运的药物组合物。 还提供了治疗诸如甲状腺代谢紊乱,非甲状腺疾病,肥胖或心血管疾病等疾病的方法,以及用于鉴定或检测能够结合或影响所述MCT的至少一部分的候选药物的生物测定 蛋白。