Pharmacologic activation of p53 by small-molecule MDM2 antagonists

H Shen, CG Maki - Current pharmaceutical design, 2011 - ingentaconnect.com
H Shen, CG Maki
Current pharmaceutical design, 2011ingentaconnect.com
Restoring p53 activity by inhibiting the interaction between p53 and MDM2 represents an
attractive approach for cancer therapy. To this end, a number of small-molecule p53-MDM2
binding inhibitors have been developed during the past several years. Nutlin-3 is a potent
and selective small-molecule MDM2 antagonist that has shown considerable promise in pre-
clinical studies. This review will highlight recent advances in the development of small-
molecule MDM2 antagonists as potential cancer therapeutics, with special emphasis on …
Restoring p53 activity by inhibiting the interaction between p53 and MDM2 represents an attractive approach for cancer therapy. To this end, a number of small-molecule p53-MDM2 binding inhibitors have been developed during the past several years. Nutlin-3 is a potent and selective small-molecule MDM2 antagonist that has shown considerable promise in pre-clinical studies. This review will highlight recent advances in the development of small-molecule MDM2 antagonists as potential cancer therapeutics, with special emphasis on Nutlin-3.
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