scholarly journals A Comprehensive and Effective Mass Spectrometry-Based Screening Strategy for Discovery and Identification of New Brassinosteroids from Rice Tissues

2016 ◽  
Vol 7 ◽  
Author(s):  
Peiyong Xin ◽  
Jijun Yan ◽  
Bingbing Li ◽  
Shuang Fang ◽  
Jinshi Fan ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Effective Mass ◽  
Screening Strategy ◽  
Rice Tissues

scholarly journals Native mass spectrometry can effectively predict PROTAC efficacy

2019 ◽  
Author(s):  
Rebecca Beveridge ◽  
Dirk Kessler ◽  
Klaus Rumpel ◽  
Peter Ettmayer ◽  
Anton Meinhart ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Protein Interactions ◽  
High Throughput Screening ◽  
Native Mass Spectrometry ◽  
Screening Strategy ◽  
Great Promise ◽  
Pharmaceutical Drugs ◽  
Label Free ◽  
Single Experiment ◽  
Multiple Substrate

Protein degraders, also known as proteolysis targeting chimeras (PROTACs), are bifunctional small molecules that bring an E3 ubiquitin ligase and a protein of interest (POI) into proximity, thus promoting ubiquitination and degradation of the targeted POI [1–3]. Despite their great promise as next-generation pharmaceutical drugs, the development of new PROTACs is challenged by the complexity of the system, which involves binary and ternary interactions between components. Here, we demonstrate the strength of native mass spectrometry (nMS), a label-free technique, to provide novel insight into PROTAC-mediated protein interactions. We show that nMS can monitor the formation of ternary E3-PROTAC-POI complexes and detect various intermediate species in a single experiment. A unique benefit of the method is its ability to reveal preferentially formed E3-PROTAC-POI combinations in competition experiments with multiple substrate proteins, thereby positioning it as an ideal high-throughput screening strategy during the development of new PROTACs.

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