Specificity and Speed: Tethered Photopharmacology,Biochemistry

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Specificity and Speed: Tethered Photopharmacology
Biochemistry ( IF 2.9 ) Pub Date : 2017-09-14 00:00:00 , DOI: 10.1021/acs.biochem.7b00687
Philipp Leippe ₁ , Julia Koehler Leman _{2,

3} , Dirk Trauner _{1,

4}

Affiliation

Genetics and pharmacology are often seen as two distinct approaches to interrogating, elucidating, and manipulating biological systems. The former is renowned for its precision whereas the latter for its fast kinetics, reversibility, and practicality. Here, we show that both can be joined as “tethered pharmacology”, wherein a genetically programmed bioconjugation site provides selectivity and a tethered pharmacophore provides function. The speed of onset, and especially cessation, of pharmacological activity can be greatly enhanced by incorporating photoswitches and using light as the trigger (“tethered photopharmacology”). Genetically encoded, tethered photopharmacology is a variant of optogenetics and could even play a role in medicine wherever gene therapy is viable. However, gene therapy may not be necessary if sufficiently selective tethering strategies that operate on wild-type receptors can be developed.

中文翻译：

特异性和速度：束缚光药理学

遗传学和药理学通常被视为审问，阐明和操纵生物系统的两种不同方法。前者以其精确度着称，而后者以快速的动力学，可逆性和实用性而著称。在这里，我们显示了两者都可以作为“栓系药理学”加入，其中基因编程的生物缀合位点提供了选择性，栓系药效团提供了功能。通过合并光开关并使用光作为触发因素，可以大大提高药理活性的发作速度，特别是停止药理活性（“栓系光药理”）。遗传编码的束缚光药理学是光遗传学的一种变体，在可能进行基因治疗的地方，甚至可以在医学中发挥作用。然而，

更新日期：2017-09-15

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