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TEAD inhibitor K-975 enhances KRASG12C inhibitor adagrasib-mediated cancer cell proliferation inhibition via dual cell cycle arrest

ABSTRACT: Here we investigate the effect of the dual inhibition, in KRASG12C mutated NSCLC cells, using the KRASG12Ci adagrasib (MRTX849) and the pan-TEAD inhibitor (TEADi) K-975. We show that K-975 enhances adagrasib-induced tumor cell growth inhibition in cancer cells. Mechanistically, we detect a downregulation of MYC and E2F signatures and a downregulation of the G2/M checkpoint regulation, which result in the increase of G1 and the decrease of the G2/M cell cycle phases. These data suggest that the co-inhibition of KRASG12C and YAP1-TEAD leads to a specific switch in the mechanism of cancer cell killing.

ORGANISM(S): Homo Sapiens (human)

SUBMITTER: Iris Valtingojer

PROVIDER: PXD039726 | JPOST Repository | Fri May 12 00:00:00 BST 2023

REPOSITORIES: jPOST

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TEAD Inhibitors Sensitize KRASG12C Inhibitors via Dual Cell Cycle Arrest in KRASG12C-Mutant NSCLC.

Tammaccaro Salvina Laura SL Prigent Philippe P Le Bail Jean-Christophe JC Dos-Santos Odette O Dassencourt Laurent L Eskandar Myriam M Buzy Armelle A Venier Olivier O Guillemot Jean-Claude JC Veeranagouda Yaligara Y Didier Michel M Spanakis Emmanuel E Kanno Tokuwa T Cesaroni Matteo M Mathieu Stephane S Canard Luc L Casse Alhassan A Windenberger Fanny F Calvet Loreley L Noblet Laurence L Sidhu Sukhvinder S Debussche Laurent L Moll Jurgen J Valtingojer Iris I

Pharmaceuticals (Basel, Switzerland) 20230406 4

KRASG12C is one of the most common mutations detected in non-small cell lung cancer (NSCLC) patients, and it is a marker of poor prognosis. The first FDA-approved KRASG12C inhibitors, sotorasib and adagrasib, have been an enormous breakthrough for patients with KRASG12C mutant NSCLC; however, resistance to therapy is emerging. The transcriptional coactivators YAP1/TAZ and the family of transcription factors TEAD1-4 are the downstream effectors of the Hippo pathwa ...[more]

PMID: 37111311

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Dataset Information

TEAD inhibitor K-975 enhances KRASG12C inhibitor adagrasib-mediated cancer cell proliferation inhibition via dual cell cycle arrest

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Publications

TEAD Inhibitors Sensitize KRAS<sup>G12C</sup> Inhibitors via Dual Cell Cycle Arrest in KRAS<sup>G12C</sup>-Mutant NSCLC.

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