Pharmacological blockade of TEAD–YAP reveals its therapeutic limitation in cancer cells

Yang Sun; Lu Hu; Zhipeng Tao; Gopala K. Jarugumilli; Hannah Erb; Alka Singh; Qi Li; Jennifer L. Cotton; Patricia Greninger; Regina K. Egan; Y. Tony Ip; Cyril H. Benes; Jianwei Che; Junhao Mao; Xu Wu

doi:10.1038/s41467-022-34559-0

Nature Communications (Nov 2022)

Pharmacological blockade of TEAD–YAP reveals its therapeutic limitation in cancer cells

Yang Sun,
Lu Hu,
Zhipeng Tao,
Gopala K. Jarugumilli,
Hannah Erb,
Alka Singh,
Qi Li,
Jennifer L. Cotton,
Patricia Greninger,
Regina K. Egan,
Y. Tony Ip,
Cyril H. Benes,
Jianwei Che,
Junhao Mao,
Xu Wu

Affiliations

Yang Sun: Cutaneous Biology Research Center, Massachusetts General Hospital, Harvard Medical School, Charlestown
Lu Hu: Cutaneous Biology Research Center, Massachusetts General Hospital, Harvard Medical School, Charlestown
Zhipeng Tao: Cutaneous Biology Research Center, Massachusetts General Hospital, Harvard Medical School, Charlestown
Gopala K. Jarugumilli: Cutaneous Biology Research Center, Massachusetts General Hospital, Harvard Medical School, Charlestown
Hannah Erb: Cutaneous Biology Research Center, Massachusetts General Hospital, Harvard Medical School, Charlestown
Alka Singh: Department of Molecular, Cell and Cancer Biology, University of Massachusetts Chan Medical School, Worcester
Qi Li: Department of Molecular, Cell and Cancer Biology, University of Massachusetts Chan Medical School, Worcester
Jennifer L. Cotton: Department of Molecular, Cell and Cancer Biology, University of Massachusetts Chan Medical School, Worcester
Patricia Greninger: Massachusetts General Hospital Cancer Center, and Department of Medicine, Harvard Medical School, Charlestown
Regina K. Egan: Massachusetts General Hospital Cancer Center, and Department of Medicine, Harvard Medical School, Charlestown
Y. Tony Ip: Program in Molecular Medicine, University of Massachusetts Chan Medical School, Worcester
Cyril H. Benes: Massachusetts General Hospital Cancer Center, and Department of Medicine, Harvard Medical School, Charlestown
Jianwei Che: Department of Cancer Biology, Dana Farber Cancer Institute, and Harvard Medical School, Boston
Junhao Mao: Department of Molecular, Cell and Cancer Biology, University of Massachusetts Chan Medical School, Worcester
Xu Wu: Cutaneous Biology Research Center, Massachusetts General Hospital, Harvard Medical School, Charlestown

DOI: https://doi.org/10.1038/s41467-022-34559-0
Journal volume & issue: Vol. 13, no. 1
pp. 1 – 18

Abstract

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Previously, the small molecule inhibitor of transcriptional enhanced associate domain (TEAD) MGH-CP1 has been described in stem cells. Here, the authors demonstrate the utility of MGH-CP1 in cancer therapy and find treatment to increase Akt pathway activation via TEAD-Vgll3 activation, presenting a rationale for combination with Akt inhibition.

Published in Nature Communications

ISSN: 2041-1723 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Science
Website: https://www.nature.com/ncomms/

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