Small molecule RITA binds to p53, blocks p53–HDM-2 interaction and activates p53 function in tumors
By N. Issaeva, P. Bozko, M. Enge, Marina Protopopova, L. G. Verhoef, M. Masucci, A. Pramanik, G. Selivanova. Nature Medicine, 2004
809 citations recorded by the source corpus.
Subfields: Molecular Biology, Oncology
View Paper: https://www.semanticscholar.org/paper/470836e5945ff6a384b1158e83a52006cc3976b4
How researchers see this paper
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In Molecular Biology
- Moshe Oren
- Magali Olivier
- M. Hollstein
- Pierre Hainaut
- D. Meek
- Arnold J. Levine
- Daniela Hoeller
- Wenyi Wei
In Oncology
- Magali Olivier
- Moshe Oren
- M. Hollstein
- Pierre Hainaut
- D. Meek
- Arnold J. Levine
- Daniela Hoeller
- Ivan Dikic
Citations in the corpus
- The role of ubiquitination in tumorigenesis and targeted drug discovery (2020, background): “The same shortcomings are also found in RITA (reactivation of p53 and induction of tumor cell apoptosis), a small molecule inhibitor preventing the interaction between p53 and Mdm2 both in vitro and in vivo.(383) Guided by the interactions among the p53 peptide, nutlin and Mdm2, a new class of inhib”
- Targeting the ubiquitin system in cancer therapy (2009, background): “In the case of p53, small compounds called RITA (2,5-bis(5-hydroxymethyl-2-thienyl)furan) have been shown to bind the amino terminus of p53 and promote growth arres”
- TP53 mutations in human cancers: origins, consequences, and clinical use. (2010, background): “…that target broad classes of mutants to reactivate suppressive functions in tumor cells (PRIMA, RITA, scFv) (Caron de Fromentel et al. 1999; Issaeva et al. 2004; Bykov et al. 2005), or compounds that specifically target particular missense mutants to restore wild-type-like structure…”
- Tumour suppression by p53: a role for the DNA damage response? (2009, background): “Small molecules that interfere with the p53–MDM2 interaction are sufficient to robustly induce p53 in the absence of a stress stimulus, underscoring the central importance of this even”
- The first 30 years of p53: growing ever more complex (2009, positive): “A complementary approach led to the identification of the small-molecule inhibitor RITA (reactivation of p53 and induction of tumour cell apoptosis); whereas Nutlins bind to MDM2, RITA binds to p53 and prevents it from being attacked by MDM2 (Ref”