Advances of targeting the YAP/TAZ-TEAD complex in the hippo pathway for the treatment of cancers.
Eur J Med Chem
; 244: 114847, 2022 Dec 15.
Article
in En
| MEDLINE
| ID: mdl-36265280
ABSTRACT
The Hippo pathway is an evolutionarily conserved signaling pathway that plays critical roles in the tumorigenesis and progression of breast cancer, oral cancer, rectal cancer, colloid cancer, and so on. YAP/TAZ-TEAD complex is a key knot in the Hippo pathway regulating cell proliferation and stem cell functions. Activation or overexpression of this complex has been proved to lead to cell transformation, proliferation and eventually cancerization. In this review, the association between the alterations of hippo pathway and tumorigenesis of various cancer had been elucidated. The structural basis of YAP/TAZ-TEAD complex is analyzed, and the targeting inhibitors are summarized within the medicinal chemistry classification. Moreover, we have also discussed the clinical status and current challenges of these drug candidates, and provide guidance for the future development of inhibitors targeting this pathway, especially YAP/TAZ-TEAD complex.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Carcinogenesis
/
Hippo Signaling Pathway
/
YAP-Signaling Proteins
/
TEA Domain Transcription Factors
/
Transcriptional Coactivator with PDZ-Binding Motif Proteins
/
Neoplasms
/
Antineoplastic Agents
Type of study:
Guideline
Limits:
Humans
Language:
En
Journal:
Eur J Med Chem
Year:
2022
Document type:
Article