Targeting the Hippo pathway in cancer, fibrosis, wound healing and regenerative medicine
Open accessAbstract
The Hippo pathway is an evolutionarily conserved signalling pathway with key roles in organ development, epithelial homeostasis, tissue regeneration, wound healing and immune modulation. Many of these roles are mediated by the transcriptional effectors YAP and TAZ, which direct gene expression via control of the TEAD family of transcription factors. Dysregulated Hippo pathway and YAP/TAZ-TEAD activity is associated with various diseases, most notably cancer, making this pathway an attractive target for therapeutic intervention. This Review highlights the key findings from studies of Hippo pathway signalling across biological processes and diseases, and discusses new strategies and therapeutic implications of targeting this pathway.
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Hagenbeek and colleagues developed allosteric TEAD inhibitors and showed that they block adaptive resistance to G12C inhibitor treatment.
“Hagenbeek et al. (56) reported the development of allosteric TEAD inhibitors and demonstrated their ability to block adaptive resistance to G12Ci treatment”
From Genome-Wide CRISPR Screens Identify Multiple Synthetic Lethal Targets That Enhance KRASG12C Inhibitor Efficacy (2023) · cites this paper as [56]
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References 219 · Cited by 860
- Authors
- Dey, A., Varelas, X., & Guan, K.-L.
- Affiliations
- Genentech (US)
- Boston University (US)
- University of California San Diego (US)
- Corresponding author
- Dey, Anwesha
- Varelas, Xaralabos
- Venue
- Nature Reviews Drug Discovery
- Published
- 2020-06-17
- Volume
- 19
- Issue
- 7
- Pages
- 480-494
- ISSN
- 1474-1776 (ISSN-L)
- 1474-1784
- PMC
- PMC7880238
- OpenAlex
- W3036513507
- Cited by
- 860
- References
- 219
- Citations by year
- 2026: 105 · 2025: 164 · 2024: 192 · 2023: 168 · 2022: 127 · 2021: 90 · 2020: 12 · 2012: 1
- FWCI
- 11.59
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Nature Reviews Drug Discovery (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Heart, Lung, and Blood Institute (R01HL124392)
- National Cancer Institute (R35CA196878, R01CA217642)
- National Institute of General Medical Sciences (R01GM051586)
- Eunice Kennedy Shriver National Institute of Child Health and Human Development (R21HD094012)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › Hippo pathway signaling and YAP/TAZ
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › TGF-β signaling in diseases
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer-related molecular mechanisms research
- Keywords
- Hippo signaling pathway, YAP, TAZ, TEAD transcription factors, cancer, fibrosis, wound healing, tissue regeneration, organogenesis, epithelial homeostasis, immunomodulation, therapeutic targeting
- MeSH terms
- Hippo Signaling Pathway, YAP-Signaling Proteins, TEA Domain Transcription Factors, Acyltransferases, Animals, DNA-Binding Proteins, Fibrosis, Gene Expression Regulation, Humans, Neoplasms, Nuclear Proteins, Transcription Factors, Wound Healing, Signal Transduction, Protein Serine-Threonine Kinases, Regenerative Medicine, Adaptor Proteins, Signal Transducing
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