使用IBT-16plex通过热蛋白质组分析鉴定药物靶点。
Identifying drug targets with thermal proteome profiling using IBT-16plex.
作者信息
Shi Zhaomei, Ren Yan, Li Shuwei, Hao Piliang
机构信息
School of Life Science and Technology, ShanghaiTech University, Shanghai, China.
Experiment Center for Science and Technology, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
出版信息
Rapid Commun Mass Spectrom. 2024 Jan 15;38(1):e9673. doi: 10.1002/rcm.9673.
RATIONALE
Thermal proteome profiling (TPP) has been widely used for the identification of drug targets for several years, and TMTpro-16plex has recently been evaluated for TPP of vehicle- and drug-treated samples in a single labeling process to reduce missing values and save instrument time. A novel isobaric labeling reagent, IBT-16plex, was developed with slightly better performance in protein identification and quantification than the commercially available TMTpro-16plex.
METHODS
In this study, we applied the newly developed IBT-16plex for target identification of methotrexate and panobinostat using TPP.
RESULTS
The known targets of these two drugs were successfully identified with elevated melting temperatures, and some known off-targets and potential new off-targets were also identified.
CONCLUSIONS
IBT-16plex can be a cost-effective replacement for TMTpro-16plex for TPP applications.
原理
热蛋白质组分析（TPP）已被广泛用于药物靶点鉴定数年，并且最近对TMTpro-16plex进行了评估，以便在单一标记过程中对载体处理和药物处理的样品进行TPP，以减少缺失值并节省仪器时间。一种新型的等压标记试剂IBT-16plex被开发出来，其在蛋白质鉴定和定量方面的性能略优于市售的TMTpro-16plex。
方法
在本研究中，我们应用新开发的IBT-16plex通过TPP进行甲氨蝶呤和帕比司他的靶点鉴定。
结果
这两种药物的已知靶点通过升高的解链温度被成功鉴定，同时还鉴定出了一些已知的脱靶和潜在的新脱靶。
结论
对于TPP应用，IBT-16plex可以作为TMTpro-16plex的一种经济高效的替代品。
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