A Small‐Molecule Probe for Selective Profiling and Imaging of Monoamine Oxidase B Activities in Models of Parkinson’s Disease

Li, Lin; Zhang, Chengwu; Ge, Jingyan; Qian, Linghui; Chai, Bing-Han; Zhu, Qing; Lee, Jung Hoon; Lim, Kah‐Leong; Yao, Shao Q.

doi:10.1002/ange.201504441

Cited by 24 publications

(1 citation statement)

References 31 publications

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“…Activity‐based probes can also be used for the cellular imaging of MAOs [53] . The group of Yao designed a highly MAO B‐selective activity‐based probe, which found use for the ABPP of MAO B and live cell bioimaging of MAO B activity in cell and tissue models of Parkinson's disease [54] …”

Section: Introductionmentioning

confidence: 99%

Activity‐Based Protein Profiling of Oxidases and Reductases

Krammer

Breinbauer

2023

Israel Journal of Chemistry

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Section: Introductionmentioning

confidence: 99%

Activity‐Based Protein Profiling of Oxidases and Reductases

Krammer

Breinbauer

2023

Israel Journal of Chemistry

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A Strategy for Specific Fluorescence Imaging of Monoamine Oxidase A in Living Cells

2017

Angewandte Chemie

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Monoamine oxidase (MAO) has two isoforms, MAO-A and MAO-B,which showdifferent functions,and thus selective fluorescence imaging is important for biological studies.C urrently,h owever,s pecific detection of MAO-A remains ag reat challenge.H erein, we report an ew strategy for specific imaging of MAO-A through the design of fluorogenic probes combining the characteristic structure of an inhibitor of the target enzyme along with propylamine as arecognition moiety.The high specificity of our representative probe is demonstrated by imaging MAO-A in different live cells such as SH-SY5Y (high levels of MAO-A) and HepG2 (high levels of MAO-B), and further validated by western blot analyses.T he superior specificity of the probe may enable the accurate detection of MAO-A in complex biosystems.I mportantly,the use of the characteristic structure of an inhibitor,a s demonstrated in this work, mays erve as ag eneral strategy to design specific recognition moieties for fluorogenic probes for enzymes.

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A Vinyl Sulfone‐Based Fluorogenic Probe Capable of Selective Labeling of PHGDH in Live Mammalian Cells

et al. 2017

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Chemical probes are powerful tools for interrogating small molecule‐target interactions. With additional fluorescence Turn‐ON functionality, such probes might enable direct measurements of target engagement in live mammalian cells. DNS‐pE (and its terminal alkyne‐containing version DNS‐pE2) is the first small molecule that can selectively label endogenous 3‐phosphoglycerate dehydrogenase (PHGDH) from various mammalian cells. Endowed with an electrophilic vinyl sulfone moiety that possesses fluorescence‐quenching properties, DNS‐pE/DNS‐pE2 became highly fluorescent only upon irreversible covalent modification of PHGDH. With an inhibitory property (in vitro Ki=7.4 μm) comparable to that of known PHGDH inhibitors, our probes thus offer a promising approach to simultaneously image endogenous PHGDH activities and study its target engagement in live‐cell settings.

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A Small‐Molecule Probe for Selective Profiling and Imaging of Monoamine Oxidase B Activities in Models of Parkinson’s Disease

Cited by 24 publications

References 31 publications

Activity‐Based Protein Profiling of Oxidases and Reductases

Activity‐Based Protein Profiling of Oxidases and Reductases

A Strategy for Specific Fluorescence Imaging of Monoamine Oxidase A in Living Cells

A Vinyl Sulfone‐Based Fluorogenic Probe Capable of Selective Labeling of PHGDH in Live Mammalian Cells

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