کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2572719 1129322 2014 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
What is pharmacological ‘affinity’? Relevance to biased agonism and antagonism
ترجمه فارسی عنوان
داروی شیمیایی چیست؟ مربوط به آزار و اذیت و انطباق
کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری علم عصب شناسی علوم اعصاب سلولی و مولکولی
چکیده انگلیسی


• Because receptors are allosteric proteins, affinity estimates are always conditional.
• At present, all known methods to estimate bias utilize functional affinity.
• Binding estimates of affinity can be very different from functional affinity.
• Affinity must be considered when measuring bias.
• Concepts around signaling bias can be extended to development of biased antagonists.

The differences between affinity measurements made in binding studies and those relevant to receptor function are described. There are theoretical and practical reasons for not utilizing binding data and, in terms of the quantification of signaling bias, it is unnecessary to do so. Finally, the allosteric control of ligand affinity through receptor–signaling protein interaction is discussed within the context of biased antagonism. In this regard, it is shown that both the bias and relative efficacy of a ligand are essential data for fully predicting biased effects in vivo.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: - Volume 35, Issue 9, September 2014, Pages 434–441
نویسندگان
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