用于光控蛋白激酶 C 激活的合成笼状 DAG-内酯。
Synthetic caged DAG-lactones for photochemically controlled activation of protein kinase C.
机构信息
Department of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 2-3-10 Kandasurugadai, Chiyoda-ku, Tokyo 101-0062, Japan.
出版信息
Chembiochem. 2011 Mar 7;12(4):535-9. doi: 10.1002/cbic.201000670. Epub 2011 Jan 18.
Abstract
Switching on kinases: Synthetic caged DAG-lactones have been developed and showed decreases of two orders of magnitude, relative to the corresponding parent compounds, in their binding affinities towards PKC. The caged compounds had no effect on the translocation of PKC until after photoactivation. This approach is a potentially powerful tool for probing the PKC signaling cascade.
摘要
激活蛋白激酶
现已开发出可开关的蛋白激酶 C（protein kinase C，PKC）封端二脂类化合物，与相应的母体化合物相比，其对 PKC 的结合亲和力降低了两个数量级。这些封端化合物在光激活之前对 PKC 的易位没有影响。这种方法是探测 PKC 信号级联的一种潜在强大工具。
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