The <i>S</i>-palmitoylated signal-transducing rat sarcoma GTPase, which plays important roles in cellular growth, division, and differentiation, is frequently mutated in various types of cancer. Dynamic palmitoylation and depalmitoylation of RAS confers proper localization and signaling in cells. So far, only two enzymes have been characterized as being involved in depalmitoylation: including acyl protein thioesterase 1 and acyl protein thioesterase 2. To decipher the physiological functions of the enzymes involved in <i>S</i>-depalmitoylation, we have designed a clickable activity-based probe for acyl protein thioesterases. The probe consists of a palmitoylated serine substrate linked to a trapping moiety that becomes reactive after enzymatic hydrolysis. This activity based probe will be critical for profiling the activities of acyl protein thioesterases in biological systems and also for inhibitor screening.

Activity-based probe for acyl protein thioesterases

249th National Meeting (2015)

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