Results 61 to 70 of about 7,268 (227)
On the mechanism of action of SJ-172550 in inhibiting the interaction of MDM4 and p53. [PDF]
PLoS ONE, 2012 SJ-172550 (1) was previously discovered in a biochemical high throughput screen for inhibitors of the interaction of MDMX and p53 and characterized as a reversible inhibitor (J. Biol. Chem. 2010; 285:10786).
Michal Bista +15 more
doaj +1 more source
Hinokiflavone Inhibits MDM2 Activity by Targeting the MDM2-MDMX RING Domain
Biomolecules, 2022 The proto-oncogene MDM2 is frequently amplified in many human cancers and its overexpression is clinically associated with a poor prognosis. The oncogenic activity of MDM2 is demonstrated by its negative regulation of tumor suppressor p53 and the ...
Viktoria K. Ilic +6 more
doaj +1 more source
Clinical Cancer Research, 2021 Purpose: We describe the first-in-human dose-escalation trial for ALRN-6924, a stabilized, cell-permeating peptide that disrupts p53 inhibition by mouse double minute 2 (MDM2) and MDMX to induce cell-cycle arrest or apoptosis in TP53-wild-type (WT ...
M. Saleh +18 more
semanticscholar +1 more source
Searching for novel MDM2/MDMX dual inhibitors through a drug repurposing approach
, 2023 Disruption of p53-MDM2/MDMX interaction by smaller inhibitors is a promising therapeutic intervention gaining tremendous interest. However, no MDM2/MDMX inhibitors have been marketed so far.
Bo Wang (86769) +7 more
core +1 more source
Methoxyphenyl Imidazolines as Potential Activators of p53
Medical Sciences Forum, 2022 The use of p53-MDM2/X inhibitors is a prospective strategy in anti-cancer therapy for tumors with wild type p53 protein. In our study, new low-molecular-weight inhibitors of the p53-mdm2 interaction have been proposed.
Daniil R. Bazanov +3 more
doaj +1 more source
Design of stapled peptide-based PROTACs for MDM2/MDMX atypical degradation and tumor suppression
Theranostics, 2022 Rationale: Although stapled peptides offer a powerful solution to overcome the susceptibility of linear peptides to proteolytic degradation and improve their ability to cross membranes, an efficient and durable disease treatment strategy has not yet been
Si Chen +10 more
semanticscholar +1 more source
, 2019 The study of the p53-MDMX/MDM2 binding sites is a research hotspot for tumor drug design. The inhibition of p53-targeted MDMX/MDM2 has become an effective approach in anti-tumor drug development.
Yuchen Li (1501165) +6 more
core +1 more source
, 2013 The molecular marker of well-differentiated/de-differentiated liposarcomas is MDM2 gene amplification coupled with protein overexpression and wild-type TP53. MDMX is a recently identified MDM2 homolog and its presence in this tumor is unexplored. Our aim
F. Bozzi +14 more
core +2 more sources
Theranostics, 2021 As alternatives to small-molecular proteolysis-targeting chimeras (PROTAC), peptide-based molecular glues (MG) are a broad range of dual-functional ligands that simultaneously bind with targetable proteins and E3 ligases by mimicking proteinprotein ...
Siqi Yan +11 more
semanticscholar +1 more source
Protecting the Genome from Mdm2 and Mdmx [PDF]
Genes & Cancer, 2012 The contribution of Mdm2, and its recently identified family member Mdmx (Mdm4), to tumorigenesis has primarily focused on their negative regulation of the p53 tumor suppressor. Although Mdm2 and Mdmx clearly inhibit p53, which can lead to tumor development, both have also been shown to affect tumorigenesis independent of p53.
Alexia N, Melo, Christine M, Eischen
openaire +2 more sources