4.7 Review

Advances of targeting the YAP/TAZ-TEAD complex in the hippo pathway for the treatment of cancers

Related references

Note: Only part of the references are listed.
Review Medicine, Research & Experimental

The Hippo pathway in cancer: YAP/TAZ and TEAD as therapeutic targets in cancer

Richard Cunningham et al.

Summary: This article discusses the importance of the Hippo signaling pathway in cancer research and explores recent discoveries on how this pathway influences cancer progression. It also focuses on the latest efforts to target the key effectors of the pathway for therapeutic purposes in both preclinical and clinical settings.

CLINICAL SCIENCE (2022)

Article Biochemistry & Molecular Biology

Identification of Small-molecule YAP-TEAD inhibitors by High-throughput docking for the Treatment of colorectal cancer

Lijun Li et al.

Summary: The YAP-TEAD transcriptional complex plays a crucial role in cancer cell growth, proliferation, and apoptosis, and dysregulation of the Hippo pathway due to YAP overexpression has been observed in various cancers. Inhibiting TEAD has shown promise in suppressing the expression of associated genes, making it a valuable transcription factor for the development of anti-cancer therapies. Through virtual screening, compound L06 was identified as a potent TEAD4 inhibitor, inhibiting TEAD autopalmitoylation, disrupting YAP-TEAD interaction, and reducing their transcriptional activity. L06 also demonstrated the ability to reduce CTGF expression and inhibit the proliferation, migration, and invasion of colorectal cancer cells.

BIOORGANIC CHEMISTRY (2022)

Review Biochemistry & Molecular Biology

Hippo Signaling in Embryogenesis and Development

Zhengming Wu et al.

Summary: The Hippo pathway, known for its role in controlling organ size, also plays diverse functions in development, tissue homeostasis, immunity, and tumorigenesis. It is involved in differential gene expression during embryogenesis and plays a crucial role in tissue specification and organ development during organogenesis.

TRENDS IN BIOCHEMICAL SCIENCES (2021)

Review Biochemistry & Molecular Biology

YAP and TAZ Are Not Identical Twins

Francesca Reggiani et al.

Summary: YAP and TAZ are paralog transcriptional regulators that play roles in cell growth and differentiation by integrating mechanical, metabolic, and signaling inputs. They have both common and distinctive structural features and regulatory mechanisms, interacting with different transcriptional partners and controlling nonidentical transcriptional programs. Despite being considered functionally redundant in most literature, they have distinct or even contrasting roles in different contexts, implying significant implications for mechanistic and translational studies.

TRENDS IN BIOCHEMICAL SCIENCES (2021)

Article Oncology

Small Molecule Inhibitors of TEAD Auto-palmitoylation Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma

Tracy T. Tang et al.

Summary: Mutations in the NF2 gene leading to dysfunctional Merlin are common in malignant mesothelioma. Compounds selectively inhibiting YAP/TAZ-TEAD gene transcription have been discovered, providing a novel way to target the dysregulated Hippo-YAP pathway in mesothelioma and other YAP-driven cancers and diseases.

MOLECULAR CANCER THERAPEUTICS (2021)

Article Pharmacology & Pharmacy

Discovery of a subtype-selective, covalent inhibitor against palmitoylation pocket of TEAD3

Tian Lu et al.

Summary: The TEAD family proteins play crucial roles in controlling cell differentiation and organ size in the Hippo pathway. Subtype selective inhibitors have been identified, providing important chemical probes for the study of TEAD-related functions in development and diseases. The development of a novel TEAD1/3 covalent inhibitor and subsequent optimization led to the discovery of a selective TEAD3 inhibitor with significant activity.

ACTA PHARMACEUTICA SINICA B (2021)

Article Biotechnology & Applied Microbiology

The interaction of TEA domain transcription factor 4 (TEAD4) and Yes-associated protein 1 (YAP1) promoted the malignant process mediated by serum/glucocorticoid regulated kinase 1 (SGK1)

Songlin He et al.

Summary: The study revealed that the TEAD4/YAP complex promotes the malignant progression of ESCC cells, while interference with SGK1 can inhibit this effect.

BIOENGINEERED (2021)

Review Oncology

The metabolism of cancer cells during metastasis

Gabriele Bergers et al.

Summary: This review discusses the metabolic rewiring in cancer cells during the metastatic cascade and the distinct metabolic features of primary tumors and metastases. Metastasis is the leading cause of death in most cancer patients, and targeting metastatic seeding and colonization remains a significant challenge. Adjusting metabolism may provide therapeutic opportunities to prevent or reduce metastasis, and targeting the new metabolic traits in established metastases could lead to their eradication.

NATURE REVIEWS CANCER (2021)

Review Biotechnology & Applied Microbiology

Targeting the Hippo pathway in cancer, fibrosis, wound healing and regenerative medicine

Anwesha Dey et al.

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Article Chemistry, Medicinal

Discovery of Covalent Inhibitors Targeting the Transcriptional Enhanced Associate Domain Central Pocket

Hacer Karatas et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

Article Multidisciplinary Sciences

A new perspective on the interaction between the Vg/VGLL1-3 proteins and the TEAD transcription factors

Yannick Mesrouze et al.

SCIENTIFIC REPORTS (2020)

Review Biochemistry & Molecular Biology

Protein-Protein Interaction Disruptors of the YAP/TAZ-TEAD Transcriptional Complex

Ajaybabu V. Pobbati et al.

MOLECULES (2020)

Review Medicine, Research & Experimental

Analysis of the role of the Hippo pathway in cancer

Yanyan Han

JOURNAL OF TRANSLATIONAL MEDICINE (2019)

Review Cell Biology

The Hippo Signaling Pathway in Development and Disease

Yonggang Zheng et al.

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Article Biochemistry & Molecular Biology

Identification of Quinolinols as Activators of TEAD-Dependent Transcription

Ajaybabu V. Pobbati et al.

ACS CHEMICAL BIOLOGY (2019)

Article Medicine, Research & Experimental

Targeting YAP to overcome acquired resistance to ALK inhibitors in ALK-rearranged lung cancer

Mi Ran Yun et al.

EMBO MOLECULAR MEDICINE (2019)

Editorial Material Oncology

The Epithelial-to-Mesenchymal Transition in Cancer

Joelle Roche

CANCERS (2018)

Article Biochemistry & Molecular Biology

Yap regulates glucose utilization and sustains nucleotide synthesis to enable organ growth

Andrew G. Cox et al.

EMBO JOURNAL (2018)

Review Biochemistry & Molecular Biology

Regulation of the Hippo Pathway Transcription Factor TEAD

Kimberly C. Lin et al.

TRENDS IN BIOCHEMICAL SCIENCES (2017)

Article Multidisciplinary Sciences

Crystal structure of TAZ-TEAD complex reveals a distinct interaction mode from that of YAP-TEAD complex

Hung Yi Kristal Kaan et al.

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Article Biochemistry & Molecular Biology

A Potential Structural Switch for Regulating DNA-Binding by TEAD Transcription Factors

Dong-Sun Lee et al.

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Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration

Fuqin Fan et al.

SCIENCE TRANSLATIONAL MEDICINE (2016)

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Hippo Pathway in Organ Size Control, Tissue Homeostasis, and Cancer

Fa-Xing Yu et al.

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Nuclear TAZ expression associates with the triple-negative phenotype in breast cancer

Juan Diaz-Martin et al.

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YAP/TAZ for cancer therapy: Opportunities and challenges

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Genome-wide association between YAP/TAZ/TEAD and AP-1 at enhancers drives oncogenic growth

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Targeting the Central Pocket in Human Transcription Factor TEAD as a Potential Cancer Therapeutic Strategy

Ajaybabu V. Pobbati et al.

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Article Multidisciplinary Sciences

MAP4K family kinases act in parallel to MST1/2 to activate LATS1/2 in the Hippo pathway

Zhipeng Meng et al.

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Article Gastroenterology & Hepatology

YAP activation is an early event and a potential therapeutic target in liver cancer development

Andrea Perra et al.

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Article Chemistry, Medicinal

Structure-Based Design and Synthesis of Potent Cyclic Peptides Inhibiting the YAP-TEAD Protein-Protein Interaction

Zhisen Zhang et al.

ACS MEDICINAL CHEMISTRY LETTERS (2014)

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The Hippo pathway and human cancer

Kieran F. Harvey et al.

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Structural and Functional Similarity between the Vgll1-TEAD and the YAP-TEAD Complexes

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Structural insights into the YAP and TEAD complex

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Discovery of Small Molecule Inhibitors of Protein-Protein Interactions Using Combined Ligand and Target Score Normalization

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Tead4 is required for specification of trophectoderm in pre-implantation mouse embryos

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Elucidation of a universal size-control mechanism in Drosophila and mammals

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Mob as tumor suppressor is activated by Hippo kinase for growth inhibition in Drosophila

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