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Last update 02 Mar 2026
TEAD4 x VGLL4
Last update 02 Mar 2026
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100 Clinical Results associated with TEAD4 x VGLL4
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100 Translational Medicine associated with TEAD4 x VGLL4
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0 Patents (Medical) associated with TEAD4 x VGLL4
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16
Literatures (Medical) associated with TEAD4 x VGLL401 Feb 2026·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Stapled peptide inhibitors target VGLL4/TEAD4 interactions to accelerate cutaneous wound healing
Article
Author: Gai, Conghao ; Zhang, Pei-Chao ; Dong, Peng ; Xue, Hongjuan ; Zhao, Qingjie ; Wang, Guangyao ; Chai, Xiaoyun ; Zhuo, Xiaobin ; Su, Juan ; Zou, Yan ; Zhang, Wenwen ; Chen, Shuai
Cutaneous wound healing is a crucial biological process for tissue repair, with skin fibroblasts acting as key cellular mediators in this regenerative cascade. The TEAD family, a downstream effector of the Hippo signaling pathway, plays a crucial role in maintaining tissue homeostasis, regulating cell proliferation, and promoting organ growth. Inhibiting TEAD4-VGLL4 interactions can initiate tissue repair and regeneration. Peptides have been created to modulate PPIs with varying success. In particular, stapling peptides can improve their ability to penetrate cell membranes and their stability, showing high specificity and activity compared to linear peptides, which highlights their broad potential in drug development. Based on the crystal structure of the VGLL4-mTEAD4 complex, we designed and synthesized a series of stapled peptides derived from the key motif of the VGLL4 protein. Among these peptides, the stapled peptides SHip2-5 and SHip2-6 effectively bind to the mTEAD4 protein, promote the proliferation and migration of skin fibroblasts, upregulate the expression levels of YAP and its downstream target genes, and present high α-helical content, stability, and membrane permeability. Moreover, SHip2-5 and SHip2-6 promote skin wound healing in rats. As novel VGLL4-mTEAD4 stapled peptide inhibitors, SHip2-5 and SHip2-6 serve as lead compounds for effective skin wound treatment, providing a new perspective and theoretical basis for the functional regeneration of damaged skin tissues. It also demonstrates strong potential for application and significant research value.
01 Dec 2024·JOURNAL OF ETHNOPHARMACOLOGY
Bu-Sui-Dan Enhances Osteoblast Differentiation by Upregulating VGLL4 to Counteract TEAD4-Mediated RUNX2 Transcription Suppression in Ovariectomized Rats
Article
Author: Liao, Yitao ; Fan, Zhihong ; Zhang, Jiayan ; Li, Chao ; Liu, Xiaofeng ; Chen, Xi ; Zhang, Xian
ETHNOPHARMACOLOGICAL RELEVANCE:
Postmenopausal osteoporosis (PMOP) has been considered as a major causative factor for bone-joint pain and inducing pathologic fractures. Bu-Sui-Dan (BSD), a classic ancient herbal formula, has been shown to exhibit osteoprotective effects by promoting bone marrow development and bone growth. However, the exact mechanism of BSD are still unexplored.
AIM OF STUDY:
The study aimed to investigate the protective effect of BSD against osteoporotic injury, and to explore whether BSD regulated BMSCs' osteogenic differentiation by targeting VGLL4, which in turn improved PMOP.
MATERIALS AND METHODS:
The anti-osteoporotic effect of BSD was studied in ovariectomized (OVX) rats and bone marrow mesenchymal stem cells (BMSCs). Micro-CT imaging and HE staining were performed, and the levels of osteogenic protein RUNX2 and osteogenesis-related factor VGLL4 were determined. Co-immunoprecipitation (Co-IP) was further employed to delve into the effects of BSD on the interactions between TEAD4 and RUNX2. The key osteogenic factors 1ALP, COLl1A1, and Osterix expression were detected by RT-qPCR. Co-IP and proximity ligation assay (PLA) were employed to scrutinize the influence of BSD on TEAD4 and RUNX2 inter-binding. Moreover, VGLL4 knockdown in BMSCs was conducted to confirm the role of VGLL4 in the therapeutic mechanism of BSD.
RESULTS:
BSD showed a dose-dependent protective effect against osteoporotic injury, as evidenced by improvement in bone volume, bone microarchitecture, and histomorphometry. Additionally, BSD treatment increased the levels of RUNX2 and its downstream target genes including ALP, COL1A1, and Osterix. Moreover, BSD upregulated VGLL4 expression and lessened TEAD4-RUNX2 interactions. In BMSCs experiment, BSD-containing serum could promote osteogenic differentiation of BMSCs, boosted the expression of osteogenesis-related factors and VGLL4 level. The knockdown of VGLL4 in BMSCs diminished the promotion effect of BSD in osteoblast differentiation, suggesting that VGLL4 play a vital role in the therapeutic effects exerted by BSD.
CONCLUSION:
BSD ameliorated osteoporosis injury and promoted osteoblast differentiation through upregulation of VGLL4 levels, which in turn antagonized TEAD4-mediated RUNX2 transcriptional repression. Our study implied that BSD may be an osteoporosis therapeutic agent.
01 May 2024·FEBS letters
Article
Author: Hyo Jin Kim ; Yunsik Choi ; Mi Hwangbo ; Jongchan Kim ; Yuri Lee
TEAD transcription factors play a central role in the Hippo signaling pathway. In this study, we focused on transcriptional enhancer factor TEF‐3 (TEAD4), exploring its regulation by the deubiquitinase OTU domain‐containing protein 6A (OTUD6A). We identified OTUD6A as a TEAD4‐interacting deubiquitinase, positively influencing TEAD‐driven transcription without altering TEAD4 stability. Structural analyses revealed specific interaction domains: the N‐terminal domain of OTUD6A and the YAP‐binding domain of TEAD4. Functional assays demonstrated the positive impact of OTUD6A on the transcription of YAP–TEAD target genes. Despite no impact on TEAD4 nuclear localization, OTUD6A selectively modulated nuclear interactions, enhancing YAP–TEAD4 complex formation while suppressing VGLL4 (transcription cofactor vestigial‐like protein 4)–TEAD4 interaction. Critically, OTUD6A facilitated YAP–TEAD4 complex binding to target gene promoters. Our study unveils the regulatory landscape of OTUD6A on TEAD4, providing insights into diseases regulated by YAP–TEAD complexes.
1
News (Medical) associated with TEAD4 x VGLL406 Mar 2024
HOUSTON--(BUSINESS WIRE)-- Sporos BioDiscovery, Inc. (a portfolio company of Sporos Bioventures, LLC.), a precision oncology company developing a diversified pipeline of small molecule therapeutic programs targeting cancer vulnerabilities in the tumor and tumor microenvironment, today announced that it will present two posters highlighting preclinical data from the company’s novel TEAD1 / TEAD4 isoform selective inhibitor, SPR1, at the American Association for Cancer Research (AACR) Annual Meeting 2024, taking place April 5-10, 2024, in San Diego, CA.
“We look forward to presenting two posters at this year’s AACR meeting that highlight the significant preclinical work we have done to characterize SPR1 as a potential best-in-class TEAD inhibitor. In addition, our team’s expert biological analysis has uncovered a new therapeutic vulnerability that could broaden the potential use of SPR1, a TEAD1/4 inhibitor, to a new subset of cancers with certain homozygous deletions,” said Stephen Rubino, Ph.D., President of Sporos BioDiscovery.
Presentation Details:
Title: TEAD1/4 inhibitors exhibit deeper biological impact and broader activity compared to TEAD1-only inhibitors in both monotherapy and combination without additional kidney toxicity
Session Category: Experimental and Molecular Therapeutics
Session Title: New Targets
Session Date and Time: Tuesday Apr 9, 2024, 1:30 p.m. - 5:00 p.m. PT
Abstract Number: 5913
Poster Number: 27
Title: VGLL4 is the target of the 3p25 homozygous deletion and presents a novel therapeutic vulnerability for TEAD1/4 but not TEAD1 inhibitors
Session Category: Experimental and Molecular Therapeutics
Session Title: YAP/TAZ/TEAD Modulators
Session Date and Time: Wednesday Apr 10, 2024, 9:00 a.m. - 12:30 p.m. PT
Abstract Number: 7266
Poster Number: 3
About Sporos BioDiscovery
Sporos BioDiscovery, Inc. is a biotechnology research & development company with a diversified pipeline of several small molecule precision oncology therapeutic programs in development, including its lead candidate SPR1, a novel TEAD inhibitor program. Sporos BioDiscovery, Inc. is a portfolio company of Sporos Bioventures, LLC, a private biotechnology company focused on transforming the drug development process across oncology.
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