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.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Binding Sites
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DNA-Binding Proteins / chemistry*
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DNA-Binding Proteins / genetics
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DNA-Binding Proteins / metabolism
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Hippo Signaling Pathway
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Humans
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Molecular Targeted Therapy / methods*
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Muscle Proteins / chemistry
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Muscle Proteins / genetics
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Muscle Proteins / metabolism
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Nuclear Proteins / chemistry*
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Nuclear Proteins / genetics
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Nuclear Proteins / metabolism
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Protein Conformation
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Protein Domains
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Protein Serine-Threonine Kinases / metabolism
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Proteins / agonists
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Proteins / antagonists & inhibitors
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Proteins / chemistry
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Proteins / metabolism
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Small Molecule Libraries / chemistry
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Small Molecule Libraries / pharmacology
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TEA Domain Transcription Factors
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Transcription Factors / chemistry*
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Transcription Factors / genetics
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Transcription Factors / metabolism
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Verteporfin / analogs & derivatives
Substances
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DNA-Binding Proteins
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Muscle Proteins
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Nuclear Proteins
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Proteins
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Small Molecule Libraries
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TEA Domain Transcription Factors
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TEAD1 protein, human
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TEAD4 protein, human
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Transcription Factors
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VGLL1 protein, human
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Verteporfin
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Protein Serine-Threonine Kinases