NUTLIN-3

活性分子！

Nutlins are cis-imidazoline analogs which inhibit the interaction between mdm2 and tumor suppressor p53, and which were discovered by screening a chemical library by Vassilev et al. Nutlin-1, nutlin-2, and nutlin-3 were all identified in the same screen;^[1] however, Nutlin-3 is the compound most commonly used in anti-cancer studies.^[2] Inhibiting the interaction between mdm2 and p53 stabilizes p53, and is thought to selectively induce a growth-inhibiting state calledsenescence in cancer cells. These compounds are therefore thought to work best on tumors that contain normal or "wild-type" p53.^{[citation needed]} Nutlin-3 has been shown to affect the production of p53 within minutes.^[3]

The more potent of the two enantiomers, (−)-nutlin-3, can be synthesized in a highly enantioselective fashion.^[4]Several derivatives of nutlin, such as RG7112 and RG7388 have been developed and progressed into human studies.