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Literature DB >> 29251924

Targeting Transcriptional Enhanced Associate Domains (TEADs).

Floriane Gibault¹, Manon Sturbaut¹, Fabrice Bailly¹, Patricia Melnyk¹, Philippe Cotelle^1,2.

Abstract

Transcriptional enhanced associate domain (TEAD) proteins are the downstream effectors of the Hippo signaling pathway that regulate cell proliferation and stem cell functions. TEADs are unable to activate transcription and require the help of coactivators such as YAP, TAZ, VgLL, and p160 proteins. The expression of TEAD family is up-regulated in many cancer types including gastric, colorectal, breast, and prostate cancers, which is correlated with poor survival in patients. Pharmacological modulators of TEADs could therefore find application in cancer treatment and regenerative medicine. In this review, we present the very recent available structures of TEADs with or without coactivators or inhibitors and discuss the potential therapeutic application of their ligands.

Entities: Disease Gene Species

Mesh：

Substances：

Year: 2017 PMID： 29251924 DOI： 10.1021/acs.jmedchem.7b00879

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

24 in total

Review 1. Targeting the Hippo pathway in cancer, fibrosis, wound healing and regenerative medicine.

Authors: Anwesha Dey; Xaralabos Varelas; Kun-Liang Guan
Journal: Nat Rev Drug Discov Date: 2020-06-17 Impact factor: 84.694

Review 2. YAP/TAZ Signaling and Resistance to Cancer Therapy.

Authors: Chan D K Nguyen; Chunling Yi
Journal: Trends Cancer Date: 2019-03-27

3. SRC-RAC1 signaling drives drug resistance to BRAF inhibition in de-differentiated cutaneous melanomas.

Authors: Eliot Y Zhu; Jesse D Riordan; Marion Vanneste; Michael D Henry; Christopher S Stipp; Adam J Dupuy
Journal: NPJ Precis Oncol Date: 2022-10-21

4. Fluorescence polarization assay for the identification and evaluation of inhibitors at YAP-TEAD protein-protein interface 3.

Authors: Wei Zhou; Yiping Li; Jinhua Song; Chenglong Li
Journal: Anal Biochem Date: 2019-08-31 Impact factor: 3.365

5. Targeting the YAP-TEAD interaction interface for therapeutic intervention in glioblastoma.

Authors: Jacquelyn T Saunders; Brent Holmes; Angelica Benavides-Serrato; Sunil Kumar; Robert N Nishimura; Joseph Gera
Journal: J Neurooncol Date: 2021-01-28 Impact factor: 4.130

6. Toward the Discovery of a Novel Class of YAP⁻TEAD Interaction Inhibitors by Virtual Screening Approach Targeting YAP⁻TEAD Protein⁻Protein Interface.

Authors: Floriane Gibault; Mathilde Coevoet; Manon Sturbaut; Amaury Farce; Nicolas Renault; Frédéric Allemand; Jean-François Guichou; Anne-Sophie Drucbert; Catherine Foulon; Romain Magnez; Xavier Thuru; Matthieu Corvaisier; Guillemette Huet; Philippe Chavatte; Patricia Melnyk; Fabrice Bailly; Philippe Cotelle
Journal: Cancers (Basel) Date: 2018-05-08 Impact factor: 6.639

Targeting Transcriptional Enhanced Associate Domains (TEADs).

Review 1. Targeting the Hippo pathway in cancer, fibrosis, wound healing and regenerative medicine.

Review 2. YAP/TAZ Signaling and Resistance to Cancer Therapy.

3. SRC-RAC1 signaling drives drug resistance to BRAF inhibition in de-differentiated cutaneous melanomas.

4. Fluorescence polarization assay for the identification and evaluation of inhibitors at YAP-TEAD protein-protein interface 3.

5. Targeting the YAP-TEAD interaction interface for therapeutic intervention in glioblastoma.

6. Toward the Discovery of a Novel Class of YAP⁻TEAD Interaction Inhibitors by Virtual Screening Approach Targeting YAP⁻TEAD Protein⁻Protein Interface.

Review 7. Targeting the Hippo Pathway and Cancer through the TEAD Family of Transcription Factors.

Review 8. YAP/TAZ Activation as a Target for Treating Metastatic Cancer.

9. A Drosophila model of oral peptide therapeutics for adult intestinal stem cell tumors.

Review 10. Repurposing of Drugs Targeting YAP-TEAD Functions.