PMID- 25719868
OWN - NLM
STAT- MEDLINE
DCOM- 20150914
LR  - 20211203
IS  - 1520-4804 (Electronic)
IS  - 0022-2623 (Linking)
VI  - 58
IP  - 12
DP  - 2015 Jun 25
TI  - The Hippo Pathway and YAP/TAZ-TEAD Protein-Protein Interaction as Targets for 
      Regenerative Medicine and Cancer Treatment.
PG  - 4857-73
LID - 10.1021/jm501615v [doi]
AB  - 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.
FAU - Santucci, Matteo
AU  - Santucci M
AD  - daggerDepartment of Life Sciences, University of Modena and Reggio Emilia, Via 
      Giuseppe Campi 183, Modena 41125, Italy.
FAU - Vignudelli, Tatiana
AU  - Vignudelli T
AD  - daggerDepartment of Life Sciences, University of Modena and Reggio Emilia, Via 
      Giuseppe Campi 183, Modena 41125, Italy.
FAU - Ferrari, Stefania
AU  - Ferrari S
AD  - daggerDepartment of Life Sciences, University of Modena and Reggio Emilia, Via 
      Giuseppe Campi 183, Modena 41125, Italy.
FAU - Mor, Marco
AU  - Mor M
AD  - double daggerDepartment of Pharmacy, University of Parma, Parco Area delle Scienze 27/A, 
      Parma 43124, Italy.
FAU - Scalvini, Laura
AU  - Scalvini L
AD  - double daggerDepartment of Pharmacy, University of Parma, Parco Area delle Scienze 27/A, 
      Parma 43124, Italy.
FAU - Bolognesi, Maria Laura
AU  - Bolognesi ML
AD  -  section signDepartment of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 
      6, Bologna 40126, Italy.
FAU - Uliassi, Elisa
AU  - Uliassi E
AD  -  section signDepartment of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 
      6, Bologna 40126, Italy.
FAU - Costi, Maria Paola
AU  - Costi MP
AD  - daggerDepartment of Life Sciences, University of Modena and Reggio Emilia, Via 
      Giuseppe Campi 183, Modena 41125, Italy.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
DEP - 20150311
PL  - United States
TA  - J Med Chem
JT  - Journal of medicinal chemistry
JID - 9716531
RN  - 0 (Adaptor Proteins, Signal Transducing)
RN  - 0 (DNA-Binding Proteins)
RN  - 0 (Nuclear Proteins)
RN  - 0 (Phosphoproteins)
RN  - 0 (TEA Domain Transcription Factors)
RN  - 0 (TEAD1 protein, human)
RN  - 0 (Transcription Factors)
RN  - 0 (YAP-Signaling Proteins)
RN  - 0 (YAP1 protein, human)
RN  - EC 2.3.- (Acyltransferases)
RN  - EC 2.3.1.- (TAFAZZIN protein, human)
RN  - EC 2.7.11.1 (Protein Serine-Threonine Kinases)
SB  - IM
MH  - Acyltransferases
MH  - Adaptor Proteins, Signal Transducing/chemistry/*metabolism
MH  - Amino Acid Sequence
MH  - Animals
MH  - DNA-Binding Proteins/chemistry/*metabolism
MH  - Drug Discovery
MH  - Hippo Signaling Pathway
MH  - Humans
MH  - Models, Molecular
MH  - Molecular Sequence Data
MH  - *Molecular Targeted Therapy/methods
MH  - Neoplasms/*drug therapy/metabolism
MH  - Nuclear Proteins/chemistry/*metabolism
MH  - Phosphoproteins/chemistry/*metabolism
MH  - Protein Interaction Maps/drug effects
MH  - Protein Serine-Threonine Kinases/chemistry/*metabolism
MH  - *Regenerative Medicine/methods
MH  - Sequence Alignment
MH  - Signal Transduction/drug effects
MH  - Stem Cells/metabolism
MH  - TEA Domain Transcription Factors
MH  - Transcription Factors/chemistry/*metabolism
MH  - YAP-Signaling Proteins
EDAT- 2015/02/27 06:00
MHDA- 2015/09/15 06:00
CRDT- 2015/02/27 06:00
PHST- 2015/02/27 06:00 [entrez]
PHST- 2015/02/27 06:00 [pubmed]
PHST- 2015/09/15 06:00 [medline]
AID - 10.1021/jm501615v [doi]
PST - ppublish
SO  - J Med Chem. 2015 Jun 25;58(12):4857-73. doi: 10.1021/jm501615v. Epub 2015 Mar 11.