Advertisement

 

 

Competitive affinity-based proteome profiling and imaging to reveal potential cellular targets of betulinic acid.

Competitive affinity-based proteome profiling and imaging to reveal potential cellular targets of betulinic acid.
Author Information (click to view)

Guo H, Xu J, Hao P, Ding K, Li Z,


Guo H, Xu J, Hao P, Ding K, Li Z, (click to view)

Guo H, Xu J, Hao P, Ding K, Li Z,

Advertisement

Chemical communications (Cambridge, England) 53(69) 9620-9623 doi 10.1039/c7cc04190j

Abstract

Betulinic acid (BA), a pentacyclic triterpenoid natural product, has received considerable attention owing to the broad spectrum of biological activities such as anti-HIV, anti-inflammatory, and especially, antitumor. Despite numerous studies on the antitumor mechanisms over the past decade, the cellular targets in cancer cells remain obscure. Here, we developed two photoprobes, BA-1/BA-2, by attaching terminal alkyne-containing "minimalist" tetrazole/diazirine photo-crosslinkers (L3 and L7) at the C-3 and C-28 positions of BA, respectively, based on well-established structure-activity relationships. The potential cellular targets were identified via competitive proteome profiling and bioimaging approaches.

Submit a Comment

Your email address will not be published. Required fields are marked *

fifteen − 11 =

[ HIDE/SHOW ]