Ng KangBo, Bland Tom, Hirani Nisha, Goehring Nathan W
Francis Crick Institute, London, NW1 1AT, UK.
Institute for the Physics of Living Systems, University College London, WC1E 6BT, UK.
MicroPubl Biol. 2022 Aug 4;2022. doi: 10.17912/micropub.biology.000610. eCollection 2022.
Engineered analog sensitive kinases provide a highly effective method for acute, controllable, and highly selective inhibition of kinase activity. Here we describe the design and characterization of an analog sensitive allele of the polarity kinase, PKC-3. This allele supports normal function as measured by its ability to exclude PAR-2 from the anterior membrane of zygotes, and is rapidly and reversibly inhibited in a dose-dependent manner by the ATP analog 1NA-PP1. This allele provides a new tool to explore the role of PKC-3 in diverse contexts within , particularly those in which acute and reversible control of PKC-3 kinase activity may be desired.
工程化的模拟敏感激酶为急性、可控且高度选择性地抑制激酶活性提供了一种高效方法。在此,我们描述了极性激酶PKC-3的模拟敏感等位基因的设计与特性。通过其将PAR-2排除在受精卵前膜之外的能力来衡量,该等位基因支持正常功能,并且被ATP类似物1NA-PP1以剂量依赖性方式快速且可逆地抑制。该等位基因为探索PKC-3在多种情况下的作用提供了一种新工具,特别是那些可能需要对PKC-3激酶活性进行急性和可逆控制的情况。