Methylcytosine dioxygenase TET1 (TET1)

Methylcytosine dioxygenase TET1 is a member of the ten-eleven translocation (TET) family of enzymes that play a fundamental role in epigenetic regulation through active DNA demethylation [1, 2]. It catalyzes the sequential oxidation of 5-methylcytosine (5mC) to 5-hydroxymethylcytosine (5hmC), 5-formylcytosine (5fC), and 5-carboxylcytosine (5caC), which are subsequently replaced by unmethylated cytosine via the base excision repair pathway [2, 4]. TET1 is essential for maintaining the pluripotency of embryonic stem cells and is involved in various biological processes, including neural plasticity, immune cell development, and genomic imprinting [2, 3, 14]. In human disease, TET1 exhibits a complex, context-dependent role in oncology, acting as a tumor suppressor in some cancers while functioning as an oncogene in others [1, 5, 8, 17]. Pharmacological modulation of TET1 is an emerging area of therapeutic interest, with small molecule inhibitors like Bobcat339 and activators like Vitamin C being explored to correct epigenetic dysregulation in cancer and other chronic conditions [6, 11, 15].

Other names

CXXC6LCXTen-eleven translocation 1CXXC-type zinc finger protein 6KIAA1676bA119F7.1MLL-TET1-MLL

Direct inhibition of catalytic activity, indirect regulation of expression via PARP inhibition, and activation through cofactor supplementation.