کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
4333876 1294756 2008 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Novel pharmacological targets based on receptor heteromers
موضوعات مرتبط
علوم زیستی و بیوفناوری علم عصب شناسی علوم اعصاب (عمومی)
پیش نمایش صفحه اول مقاله
Novel pharmacological targets based on receptor heteromers
چکیده انگلیسی

Studies performed in the last 10 years have provided solid evidence indicating that G-protein-coupled receptors are expressed on the plasma membrane as homo and heterodimers. The first consequence of this fact is that homo and heterodimers are the true targets of natural (hormones, neurotransmitters) and synthetic drugs. Furthermore a given receptor in a heteromer may display a different functional and/or pharmacological profile than the same receptor characterized as monomer or as homodimer. Recent evidence indicates that receptor heteromers are sensors that lead to a fine-tuning in neurotransmission or hormone regulation; mainly this is achieved by a modification of the signaling pathways activated via a given receptor when it is forming a given heteromer. Quite often antagonists display variable affinities when a given receptor is expressed with different heteromeric partners. This fact should be taken into account in the development of new drugs. Finally it should be pointed out that radioligand binding data has to be analyzed by a model that considers receptors as dimers and not as monomers. This model provides a novel approach to characterize drugs interacting with the orthosteric center (agonists/antagonists) or with allosteric centers (allosteric regulators).

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Brain Research Reviews - Volume 58, Issue 2, August 2008, Pages 475–482
نویسندگان
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