Discovery of YAP1/TAZ pathway inhibitors through phenotypic screening with potent anti-tumor activity via blockade of Rho-GTPase signaling.

doi:10.1016/j.chembiol.2024.02.013

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Article

Discovery of YAP1/TAZ pathway inhibitors through phenotypic screening with potent anti-tumor activity via blockade of Rho-GTPase signaling.

Cell chemical biology - 18 Jul 2024

Graham Keith, Lienau Philip, Bader Benjamin, Prechtl Stefan, Naujoks Jan, Lesche Ralf, Weiske Joerg, Kuehnlenz Julia, Brzezinka Krzysztof, Potze Lisette, Zanconato Francesca, Nicke Barbara, Montebaur Anna, Bone Wilhelm, Golfier Sven, Kaulfuss Stefan, Kopitz Charlotte, Pilari Sabine, Steuber Holger, Hayat Sikander, Kamburov Atanas, Steffen Andreas, Schlicker Andreas, Buchgraber Philipp, Braeuer Nico, Font Nuria Aiguabella, Heinrich Tobias, Kuhnke Lara, Nowak-Reppel Katrin, Stresemann Carlo, Steigemann Patrick, Walter Annette O, Blotta Simona, Ocker Matthias, Lakner Ashley, von Nussbaum Franz, Mumberg Dominik, Eis Knut, Piccolo Stefano, Lange Martin

Abstract excerpt

This study describes the identification and target deconvolution of small molecule inhibitors of oncogenic Yes-associated protein (YAP1)/TAZ activity with potent anti-tumor activity in vivo. A high-throughput screen (HTS) of 3.8 million compounds was conducted using a cellular YAP1/TAZ reporter assay. Target deconvolution studies identified the geranylgeranyltransferase-I (GGTase-I) complex as the direct target...

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PMID: 38537632
DOI: 10.1016/j.chembiol.2024.02.013

Genes

YAP1

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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