Activity-based protein profiling: Recent advances in medicinal chemistry.
Eur J Med Chem
; 191: 112151, 2020 Apr 01.
Article
in En
| MEDLINE
| ID: mdl-32109778
ABSTRACT
Activity-based protein profiling (ABPP) has become an emerging chemical proteomic approach to illustrate the interaction mechanisms between compounds and proteins. This approach has combined organic synthesis, biochemistry, cell biology, biophysics and bioinformatics to accelerate the process of drug discovery in target identification and validation, as well as in the stage of lead discovery and optimization. This review will summarize new developments and applications of ABPP in medicinal chemistry. Here, we mainly described the design principles of activity-base probes (ABPs) and general workflows of ABPP approach. Moreover, we discussed various basic and advanced ABPP strategies and their applications in medicinal chemistry, including competitive and comparative ABPP, two-step ABPP, fluorescence polarization ABPP (FluoPol-ABPP) and ABPs for visualization. In conclusion, this review will give a general overview of the applications of ABPP as a powerful and efficient technique in medicinal chemistry.
Key words
Full text:
1
Database:
MEDLINE
Main subject:
Proteins
Limits:
Animals
/
Humans
Language:
En
Journal:
Eur J Med Chem
Year:
2020
Type:
Article