title: The Hippo Pathway and YAP/TAZ-TEAD Protein-Protein Interaction as Targets for Regenerative Medicine and Cancer Treatment.
abstract: The Hippo pathway is an important organ size control signaling network and the major regulatory mechanism of cell-contact inhibition. Yes associated protein (YAP) and transcriptional co-activator with PDZ-binding motif (TAZ) are its targets and terminal effectors: inhibition of the pathway promotes YAP/TAZ translocation to the nucleus, where they interact with transcriptional enhancer associate domain (TEAD) transcription factors and coactivate the expression of target genes, promoting cell proliferation. Defects in the pathway can result in overgrowth phenotypes due to deregulation of stem-cell proliferation and apoptosis; members of the pathway are directly involved in cancer development. The pharmacological regulation of the pathway might be useful in cancer prevention, treatment, and regenerative medicine applications; currently, a few compounds can selectively modulate the pathway. In this review, we present an overview of the Hippo pathway, the sequence and structural analysis of YAP/TAZ, the known pharmacological modulators of the pathway, especially those targeting YAP/TAZ-TEAD interaction.
authors.affiliation: †Department of Life Sciences, University of Modena and Reggio Emilia, Via Giuseppe Campi 183, Modena 41125, Italy.
authors.forename: Matteo
authors.initials: M
authors.lastname: Santucci
authors.affiliation: †Department of Life Sciences, University of Modena and Reggio Emilia, Via Giuseppe Campi 183, Modena 41125, Italy.
authors.forename: Tatiana
authors.initials: T
authors.lastname: Vignudelli
authors.affiliation: †Department of Life Sciences, University of Modena and Reggio Emilia, Via Giuseppe Campi 183, Modena 41125, Italy.
authors.forename: Stefania
authors.initials: S
authors.lastname: Ferrari
authors.affiliation: ‡Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/A, Parma 43124, Italy.
authors.forename: Marco
authors.initials: M
authors.lastname: Mor
authors.affiliation: ‡Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/A, Parma 43124, Italy.
authors.forename: Laura
authors.initials: L
authors.lastname: Scalvini
authors.affiliation: §Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, Bologna 40126, Italy.
authors.forename: Maria Laura
authors.initials: ML
authors.lastname: Bolognesi
authors.affiliation: §Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, Bologna 40126, Italy.
authors.forename: Elisa
authors.initials: E
authors.lastname: Uliassi
authors.affiliation: †Department of Life Sciences, University of Modena and Reggio Emilia, Via Giuseppe Campi 183, Modena 41125, Italy.
authors.forename: Maria Paola
authors.initials: MP
authors.lastname: Costi
mesh_terms: D000217:Acyltransferases; D048868:Adaptor Proteins, Signal Transducing / Q000737:chemistry / Q000378:metabolism*; D000595:Amino Acid Sequence; D000818:Animals; D004268:DNA-Binding Proteins / Q000737:chemistry / Q000378:metabolism*; D055808:Drug Discovery; D000090683:Hippo Signaling Pathway; D006801:Humans; D008958:Models, Molecular; D008969:Molecular Sequence Data; D058990:Molecular Targeted Therapy / Q000379:methods; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D009687:Nuclear Proteins / Q000737:chemistry / Q000378:metabolism*; D010750:Phosphoproteins / Q000737:chemistry / Q000378:metabolism*; D060066:Protein Interaction Maps / Q000187:drug effects; D017346:Protein Serine-Threonine Kinases / Q000737:chemistry / Q000378:metabolism*; D044968:Regenerative Medicine / Q000379:methods; D016415:Sequence Alignment; D015398:Signal Transduction / Q000187:drug effects; D013234:Stem Cells / Q000378:metabolism; D000091262:TEA Domain Transcription Factors; D014157:Transcription Factors / Q000737:chemistry / Q000378:metabolism*; D000091102:YAP-Signaling Proteins
chemical_list: D048868:Adaptor Proteins, Signal Transducing; D004268:DNA-Binding Proteins; D009687:Nuclear Proteins; D010750:Phosphoproteins; D000091262:TEA Domain Transcription Factors; C057182:TEAD1 protein, human; D014157:Transcription Factors; D000091102:YAP-Signaling Proteins; C088374:YAP1 protein, human; D000217:Acyltransferases; C108675:TAFAZZIN protein, human; D017346:Protein Serine-Threonine Kinases