Dataset Information

Whole proteome experiment to validate treatment conditions in SJSA-1 cells

ABSTRACT: Navtemadlin is a potent small moeclule inhibitor of the p53-MDM2 protein-protein interaction, that is being tested in Phase II/III clinical trials for the treatment of cancer. The selectivity of this molecule is poorly understood. So we synthesised and validated two photoactivatable clickable probes of Navtemadlin. This data shows the validation of treatment conditions through whole proteome proteomics experiments in order to ensure that the expression of key proteins such as MDM2 is uniform across conditions.

INSTRUMENT(S):

ORGANISM(S): Homo Sapiens (human)

SUBMITTER: Amrita Date

LAB HEAD: Anna Barnadr

PROVIDER: PXD058047 | Pride | 2025-04-28

REPOSITORIES: Pride

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Affinity-based protein profiling of MDM2 inhibitor Navtemadlin.

Date Amrita A Wall Archie A Zhang Peiyu P Houghton Jack W JW Lu Jianan J Thomas Adam M AM Kovačič Tristan T Wilson Andrew J AJ Tate Edward W EW Barnard Anna A

Chemical science 20250312 16

Navtemadlin is a potent inhibitor of the p53-MDM2 protein-protein interaction, which plays a critical role in the proliferation of p53-wildtype tumours. Whilst Navtemadlin has progressed to multiple Phase III clinical trials in oncology, little has been disclosed regarding its selectivity for MDM2 in cells. Here, we report the synthesis and validation of photoactivatable clickable probes of Navtemadlin, and their application to <i>de novo</i> target discovery for Navtemadlin through affinity-bas ...[more]

PMID: 40115185

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