Table 1.
List of inhibitors targeting REV1/Polζ-associated TLS.
| Inhibitor | Screening Target | Mechanism | Effect | References |
|---|---|---|---|---|
| JH-RE-06 | REV1 CTD-REV7 PPI | Promote REV1 dimerization Disrupt REV1-REV7 PPI |
Inhibition of cisplatin-induced mutagenic TLS Enhancement of cisplatin, BPDE, 4-NQO, and MMS cytotoxicity in vitro Enhancement of cisplatin chemosensitivity in vivo |
[105,106] |
| Compound 7 | REV3-REV7 PPI | Disrupt REV3-REV7 PPI | Inhibition of interstrand cross-link repair Enhancement of cisplatin cytotoxicity in vitro |
[107] |
| ZINC97017995, ZINC25496030 | REV7 homodimer | Disrupt REV1-REV7 PPI | Enhancement of cisplatin and doxorubicin cytotoxicity in vitro | [108] |
| Thiophene, piperazine, piperidine, and aryl piperazine compounds | REV1 CTD-Polκ RIR PPI | Disrupt REV1 CTD-RIR PPI | Enhancement of cisplatin and UV cytotoxicity in vitro Inhibition of cisplatin-induced mutagenesis |
[109,110] |
| Phenazopyridine compounds | REV1 CTD | Disrupt REV1 CTD-RIR PPI | Enhancement of cisplatin cytotoxicity in vitro | [111,112,113] |
CTD: C terminal domain, PPI: protein–protein interaction, RIR: REV1-interacting region, TLS: translesion DNA synthesis, BPDE: benzo[a]pyrene diol epoxide, 4-NQO: 4-nitroquinolone 1-oxide, MMS: methyl methanesulfonate, UV: ultraviolet.