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Title 

Recent advances in protein tyrosine phosphatase detection using chemical probes

 

화학탐침을 이용한 PTP 검출에 대한 최근 연구동향

Authors 

K LeeH J KangY XiaSang Jeon Chung

Publisher 

Bentham Science Publishers

Issue Date 

2011

Citation 

Anti-Cancer Agents in Medicinal Chemistry, vol. 11, no. 1, pp. 54-63

Keywords 

2-fluoromethylphosphotyrosine (FMPT)4-fluoromethylphenylphosphate (FMPP)DiFMUPDual-specificity PTP (DUSP)F?rster resonance energy transfer (FRET)In-gel assayPhosphotyrosine

Abstract 

Protein tyrosine phosphatases (PTPs) are key regulatory enzymes in signal transduction pathways and their aberrancy has been implicated in various diseases such as cancers, metabolic syndrome, and autoimmune disorders. In spite of its great importance, determination of the functional significance of PTPs remains a major challenge, and efficient methodologies are needed to specifically delineate PTP functions. Besides the strategy to use potent and selective PTP inhibitors to study the physiological roles of the enzymes, measurement of PTP activities using specific PTP substrates or activity-based probes (ABPs) has been reported. This review focused on the recent development of small molecular probes to detect PTP activities, consisting of five sub-categories: 1. Conventional fluorescent substrates; 2. Ratiometric fluorescent PTP substrates; 3. Fluorescence substrates with selectivity to a single PTP or a class of PTPs; 4. ABPs specific for PTPs; and 5. A real-time imaging of PTP-substrate complex using a small molecule PTP probe which, offers a measurement of a real-time activity of a certain PTP in cells.

ISSN 

1871-5206

Link 

http://dx.doi.org/10.2174/187152011794941208

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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