p53 Y220C Reactivator NTS071

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable reactivator of the tumor suppressor protein p53 mutation TP53 Y220C, with potential antineoplastic activity. Upon oral administration, p53 Y220C reactivator NTS071 selectively targets and allosterically binds into the Y220C crevice, thereby stabilizing the p53 Y220C protein and restoring the function of wild-type (WT) p53. This restores the ability of p53 to bind to DNA, enables its transcriptional activity, and reactivates p53-mediated signaling. This induces cell cycle arrest and apoptosis in and inhibits the proliferation of tumor cells expressing the TP53 Y220C mutation. p53, a tumor suppressor gene, plays a key role in the regulation of cell cycle arrest, apoptosis, senescence and DNA repair. p53 is often mutated in many tumor cells, resulting in the loss of apoptosis regulation and abnormal cell proliferation. TP53 Y220C is a hotspot loss-of-function mutation.

**Synonyms:** - NTS 071 - NTS-071 - NTS071