activity-based protein profiling

上次阅读的文献‘An apoplastic peptide activates salicylic acid signalling in maize’中

activity-based protein profiling (ABPP):

ABPP is based on the use of small moleculeprobes that react with the active sites of enzymes in an activity-dependentmanner.

How ABPP Works

Activity-based probes exploit an enzyme’sactivity for labeling and detection. ABPs typically have three main parts

Part 1: A Reactive Group

This part binds to the active site of aparticular enzyme class via a covalent interaction. This ensures that the probesticks to the enzyme it is designed for and that it stays stuck.

Part 2: A Specificity Element

This part helps the probe target aparticular class of enzymes, or even particular enzymes within the class. Forexample: Proteases, esterases, and phospholipases are all serine hydrolases,and you can use a general serine hydrolase ABP to profile all of thissuperfamily. Alternatively, you can use a protease-targeted probe to profilejust the protease subfamily. Cook’s choice.

Part 3: A Reporter Tag

This part allows you to detect your enzymesusing a variety of techniques, typically a fluorophore or an affinity handle.You can also use an azide or an alkyne for a “clickable” ABP. And without thereporter group, you’ll simply have an enzyme inhibitor.

activity-based probes (ABPs)

DCG-04

is an activity-based probe for cysteine cathepsins, enabled fluorescent readout

of its receptor-targeting properties.

E-64：E-64是一种天然的、有效的和不可逆的半胱氨酸蛋白酶（cysteine protease）抑制剂，作用于cathepsins K、S和L。

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