DNA polymerase θ (POLθ) plays a central role in microhomology-mediated end joining (MMEJ), an error-prone DSB repair pathway. Under normal conditions, MMEJ acts as a backup repair mechanism. However, in HRR-deficient tumors, reliance on POLlθ-driven MMEJ is markedly increased, making POLθ essential for cancer cell survival. Researchers from Astrazeneca plc reported the discovery and characterization of AZD-4956, a POLθ inhibitor that can be used in combination with PARP inhibitors and other DNA-damaging agents.
Avelos Therapeutics Inc. has divulged new sulfur or selenium-containing compounds acting as DNA polymerase θ (POLθ; POLQ) inhibitors potentially useful for the treatment of cancer.
Hangzhou Synrx Therapeutics Technology Co. Ltd. has divulged crystalline salts of DNA polymerase θ (POLθ) inhibitors reported to be useful for the treatment of cancer.
Shanghai Apeiron Biotechnology Co. Ltd. has reported selenium-containing heterocyclic compounds acting as DNA polymerase theta (POLθ, POLQ) inhibitors potentially useful for the treatment of cancer.
