Small-molecule MDM2 antagonists reveal aberrant p53 signaling in cancer: implications for therapy.
By C. Tovar, James A. Rosinski, Z. Filipovic, B. Higgins, K. Kolinsky, Holly Hilton, Xiaolan Zhao, B. Vu, Weiguo Qing, K. Packman and 3 more. Proceedings of the National Academy of Sciences of the United States of America, 2006
720 citations recorded by the source corpus.
Subfields: Molecular Biology, Oncology
View Paper: https://www.semanticscholar.org/paper/63f548734b6d60e8c4c12f504a0255907b7d90b1
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Citations in the corpus
- The Cell-Cycle Arrest and Apoptotic Functions of p53 in Tumor Initiation and Progression. (2016, background): “However, MDM2 inhibition predominantly led to reversible cell-cycle arrest in cell culture and a mouse colon tumor model (Tovar et al. 2006; Huang et al. 2009; Rigatti et al. 2012).”
- Encoding and Decoding Cellular Information through Signaling Dynamics (2013, positive): “Although Nutlin-3 is highly selective for p53 (Tovar et al., 2006), use of more promiscuous agents should be compared with genetic perturbations to substantiate any claims about function.”
- Small-Molecule Inhibitors of the MDM2-p53 Protein-Protein Interaction to Reactivate p53 Function: A Novel Approach for Cancer Therapy (2009, methodology): “In xenograft models of human prostate cancer and osteosarcoma retaining wild-type p53, oral administration of Nutlin-3 and MI-219 induced robust accumulation and activation of p53 in tumor tissues (35,76).”
- Acetylation is indispensable for p53 activation. (2008, background): “Recent studies showed that the treatment of Nutlin-3 strongly induces p53-dependent growth arrest in cancer cells but has a much-reduced ability to activate proapoptotic targets of p53 (Tovar et al., 2006).”
- Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy (2013, methodology): “To determine dissociation constants for peptide–protein interaction, afluorescencepolarization assay (FPA) was used inwhich 10 nMof the fluorescently labeled analog of the linear peptide ATSP-3848 (specifically, FAM-β-Ala-Leu-Thr-Phe-Glu-His-Tyr-Trp-AlaGln-Leu-Thr-Ser-NH2 [FAM-ATSP-3848]) was incuba”
- Standards and Guidelines for the Interpretation and Reporting of Sequence Variants in Cancer: A Joint Consensus Recommendation of the Association for Molecular Pathology, American Society of Clinical Oncology, and College of American Pathologists. (2017, background): “Nutlins, a group of cis-imidazoline small-molecule compounds, have shown selective inhibition of the MDM2:p53 interaction in preclinical studies.(103,104) Nutlins have also been shown in human xenograft models to inhibit wild-type p53 tumor growth in a dose-dependent manner and even exhibited regres”
- Inhibiting NF-κB Activation by Small Molecules As a Therapeutic Strategy (2010, neutral): “Other molecules with similar potential include nutlins [193,194], cisplatin [195,196], leptomycin B [197,198], adenosine-2,3-dialdehyde [199], the NSAID JTE-522 [200], and the cyclindependent kinase inhibitors R-roscovitine [201,202]; and flavopiridol [203,204].”