Cited by 148Hippo pathway signaling and YAP/TAZMicrotubule and mitosis dynamicsCancer-related molecular mechanisms research

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Therapeutic targeting of TEAD transcription factors in cancer

Pobbati, Ajaybabu V., Kumar, Ramesh, Rubin, Brian P., Hong, Wanjin·2023·Trends in Biochemical Sciences

DOI 10.1016/j.tibs.2022.12.005

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Abstract

The Hippo signaling pathway inhibits the activity of the oncogenic YAP (Yes-associated protein)/TAZ (transcriptional co-activator with PDZ-binding motif)-TEAD (TEA/ATTS domain) transcriptional complex. In cancers, inactivating mutations in upstream Hippo components and/or enhanced activity of YAP/TAZ and TEAD have been observed. The activity of this transcriptional complex can be effectively inhibited by targeting the TEAD family of transcription factors. The development of TEAD inhibitors has been driven by the discovery that TEAD has druggable hydrophobic pockets, and is currently at the clinical development stage. Three small molecule TEAD inhibitors are currently being tested in Phase I clinical trials. In this review, we highlight the role of TEADs in cancer, discuss various avenues through which TEAD activity can be inhibited, and outline the opportunities for the administration of TEAD inhibitors.

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eLife Assessment: VGLL2 and TEAD1 fusion proteins drive YAP/TAZ-independent transcription and tumorigenesis by engaging p300
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Authors: Pobbati, A. V., Kumar, R., Rubin, B. P., & Hong, W.
Affiliations: Cleveland Clinic (US)
Agency for Science, Technology and Research (SG)
Corresponding author: Hong, Wanjin
ORCID: Pobbati, Ajaybabu V.
Kumar, Ramesh
Rubin, Brian P.
Hong, Wanjin
Venue: Trends in Biochemical Sciences
Publisher: Elsevier BV
Published: 2023-05
Volume: 48
Issue: 5
Pages: 450-462
ISSN: 0968-0004 (ISSN-L)
DOI: 10.1016/j.tibs.2022.12.005
OpenAlex: W4318451216
Cited by: 147
References: 108
Citations by year: 2026: 41 · 2025: 42 · 2024: 41 · 2023: 23
FWCI: 4.77
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
doi.org/10.15223/policy-017 (stm-asf)
doi.org/10.15223/policy-037 (stm-asf)
doi.org/10.15223/policy-012 (stm-asf)
doi.org/10.15223/policy-029 (stm-asf)
doi.org/10.15223/policy-004 (stm-asf)
Locations: Trends in Biochemical Sciences (publishedVersion)
PubMed (publishedVersion)
Funders: Agency for Science, Technology and Research
National Medical Research Council (OF-IRG19may-0011)
Margie and Robert E. Petersen Foundation
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › Hippo pathway signaling and YAP/TAZ
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › Microtubule and mitosis dynamics
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer-related molecular mechanisms research
Keywords: TEAD transcription factors, Hippo signaling pathway, YAP/TAZ, TEAD inhibitors, small molecule inhibitors, cancer therapy, drug development
MeSH terms: Hippo Signaling Pathway, TEA Domain Transcription Factors, Humans, Neoplasms, Transcription Factors

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Therapeutic targeting of TEAD transcription factors in cancer

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