autophagy-targeting chimeras

TSPO ligand-2 (Carbonic acid) is a ligand of AUTAC1 which contains a p-fluorobenzylguanine and a Fumagillol moiety.

J22352, a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM, enhances anticancer effects in glioblastoma by promoting HDAC6 degradation. It does so by inhibiting autophagy and stimulating the antitumor immune response, further restoring host antitumor activity through the reduction of PD-L1's immunosuppressive activity.

Cys-C-cGMP serves as an autophagy tag for AUTACs (autophagy-targeting chimeras). It enhances K63-linked ubiquitination of mitochondria within HeLa cells [1].

2G-HaloAUTAC (Compound tt44), a second-generation autophagy-targeting chimera (2G-HaloAUTAC), enhances the activity of autophagy-targeting chimeras (AUTAC) by substituting the L-Cysteine (L-Cys) linker with alternative structures. This compound demonstrates degradative activity against EGFP-HaloTag protein through an autophagy mechanism.