Definition

An orally bioavailable inhibitor of human DNA methyltransferase 1 (DNMT1), with potential antineoplastic activity. Upon oral administration, DNMT1 inhibitor NTX-301 targets ad binds to DNMT1, thereby inhibiting the activity of DNMT1. This may prevent DNA methylation, induce DNA hypomethylation, and activate tumor suppressor genes silenced by hypermethylation. This may inhibit tumor cell proliferation. DNMT1, a member of the DNA methyltransferase (DNMT) family, plays an important role in maintaining the DNA methylation pattern. Dysregulation of DNMT1 has been associated with a number of cancers.