Ontology highlight
ABSTRACT:
SUBMITTER: Warner WA
PROVIDER: S-EPMC3448857 | biostudies-literature | 2012 Oct
REPOSITORIES: biostudies-literature
Warner Wayne A WA Sanchez Ricardo R Dawoodian Alex A Li Esther E Momand Jamil J
Chemical biology & drug design 20120723 4
The integrity of the p53 tumor suppressor pathway is compromised in the majority of cancers. In 7% of cancers p53 is inactivated by abnormally high levels of MDM2--an E3 ubiquitin ligase that polyubiquitinates p53, marking it for degradation. MDM2 engages p53 through its hydrophobic cleft, and blockage of that cleft by small molecules can re-establish p53 activity. Small molecule MDM2 inhibitors have been developed, but there is likely to be a high cost and long time period before effective drug ...[more]