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. Author manuscript; available in PMC: 2014 Mar 1.
Published in final edited form as: Pflugers Arch. 2013 Jan 8;465(3):427–440. doi: 10.1007/s00424-012-1201-0

Figure 2. Examples of selective enzyme inhibitors found through competitive ABPP.

Figure 2

a) Structures of selective inhibitors for enzymes (in parentheses) that have been found through competitive ABPP platforms. b) To ascertain selectivity of these inhibitors outside of their cognate enzyme classes, these small-molecules can themselves be turned into activity-based probes by appending a chemoorthogonal handle (such as an alkyne or azide). PF-3845yne and ABL112 are alkyne-appended ABP analogs of PF-3845 and ABL127, respectively. These probes can be reacted with proteomes in vitro, in situ, or even in vivo and proteomes can be subjected to click chemistry with biotin or rhodamine-azide and detected by ABPP-MudPIT or gel-based approaches, respectively.