p53 is a critical tumor suppressor and is the most frequently inactivated gene in human cancer. Inhibition of the interaction of p53 with its negative regulator MDM2 represents a promising clinical strategy to treat p53 wild-type tumors. AMG 232 is a potential best-in-class inhibitor of the MDM2–p53 interaction and is currently in clinical trials. We characterized the activity of AMG 232 and its effect on p53 signaling in several preclinical tumormodels. AMG232binds theMDM2proteinwith picomolar affinity and robustly inducesp53activity, leading tocell-cycle arrest and inhibition of tumor cell proliferation. AMG 232 treatment inhibited the in vivo growth of several tumor xenografts and led to complete and durable regression of MDM2-amplified ...
International audienceThe gene TP53, encoding transcription factor p53, is mutated or deleted in hal...
Background This open-label, first-in-human, phase 1 study evaluated AMG 232, an oral selective MDM2 ...
We recently reported the discovery of AM-8553 (<b>1</b>), a potent and selective piperidinone inhibi...
The MDM2 inhibitor AMG 232 demonstrates robust anti-tumor efficacy and potentiates the activity of p...
P53 is a recognized tumor suppressor gene, which mainly depends on the activity of its transfer fact...
Inactivation of the function of tumor suppressor p53 is common in human cancers. In approximately ha...
The p53 tumor suppressor is a potent transcription factor that plays a key role in the regulation of...
MDM2 protein are powerful oncogene which is overexpressed in various cancers, including breast cance...
Named as the guardian of the genome, p53 is a tumor suppressor that regulates cell function, often t...
The p53 pathway is disrupted in virtually every human tumor. In similar to 50% of human cancers, the...
Abstract p53, encoded by the tumor suppressor gene TP53, is one of the most important tumor suppress...
Introduction: One of the hallmarks of cancer cells is the inactivation of the p53 pathway either due...
Introduction: One of the hallmarks of cancer cells is the inactivation of the p53 pathway either due...
Cancer cells often depend on multiple pathways for their growth and survival, resulting in therapeut...
A promising new approach in cancer treatment is the inhibition of murine double minute 2 and 4 (MDM2...
International audienceThe gene TP53, encoding transcription factor p53, is mutated or deleted in hal...
Background This open-label, first-in-human, phase 1 study evaluated AMG 232, an oral selective MDM2 ...
We recently reported the discovery of AM-8553 (<b>1</b>), a potent and selective piperidinone inhibi...
The MDM2 inhibitor AMG 232 demonstrates robust anti-tumor efficacy and potentiates the activity of p...
P53 is a recognized tumor suppressor gene, which mainly depends on the activity of its transfer fact...
Inactivation of the function of tumor suppressor p53 is common in human cancers. In approximately ha...
The p53 tumor suppressor is a potent transcription factor that plays a key role in the regulation of...
MDM2 protein are powerful oncogene which is overexpressed in various cancers, including breast cance...
Named as the guardian of the genome, p53 is a tumor suppressor that regulates cell function, often t...
The p53 pathway is disrupted in virtually every human tumor. In similar to 50% of human cancers, the...
Abstract p53, encoded by the tumor suppressor gene TP53, is one of the most important tumor suppress...
Introduction: One of the hallmarks of cancer cells is the inactivation of the p53 pathway either due...
Introduction: One of the hallmarks of cancer cells is the inactivation of the p53 pathway either due...
Cancer cells often depend on multiple pathways for their growth and survival, resulting in therapeut...
A promising new approach in cancer treatment is the inhibition of murine double minute 2 and 4 (MDM2...
International audienceThe gene TP53, encoding transcription factor p53, is mutated or deleted in hal...
Background This open-label, first-in-human, phase 1 study evaluated AMG 232, an oral selective MDM2 ...
We recently reported the discovery of AM-8553 (<b>1</b>), a potent and selective piperidinone inhibi...