The potential for selective pharmacological therapies through biased receptor signaling.

The potential for selective pharmacological therapies through biased receptor signaling.
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DOI:
10.1186/2050-6511-13-3
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发表时间:
2012-08-13
影响因子:
2.9
通讯作者:
Kenakin T
Kenakin T
中科院分区:
医学4区
文献类型:
--
作者:
Kenakin T

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并非所有激动剂都均匀地激活细胞信号传导途径(偏置信号传导)的发现极大地改变了激动剂的药物发现过程和用激动剂治疗疾病的策略。技术进步使得复杂的受体行为能够被独立地观察,并且通过这些测定,可以量化对激动剂的偏倚。据预测,治疗表型将通过转化研究与量化的偏倚尺度相联系,以指导药物化学家进行药物发现。
The discovery that not all agonists uniformly activate cellular signaling pathways (biased signaling) has greatly changed the drug discovery process for agonists and the strategy for treatment of disease with agonists. Technological advances have enabled complex receptor behaviors to be viewed independently and through these assays, the bias for an agonist can be quantified. It is predicted that therapeutic phenotypes will be linked, through translational studies, to quantified scales of bias to guide medicinal chemists in the drug discovery process.
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