摘要
YAP1和转录共激活因子与PDZ结合基序与许多转录因子一起调控基因转录。YAP1和TAZ由肿瘤抑制性的Hippo病理通路负面地调控,在人类肿瘤中,Hippo通路经常失去控制并且YAP1和TAZ能躲避Hippo通路的抑制,YAP1和TAZ的上调诱导了上皮细胞间质转化与肿瘤细胞耐药性增加。TAZ与肿瘤干细胞有关,结果是与高度表达的YAP1和TAZ肿瘤与临床预后有关。YAP1和TAZ的抑制剂被认为在肿瘤治疗中是有益的。另一方面,因为YAP1和TAZ在各种组织干细胞和组织修复的调节中起着非常重要的角色,YAP1和TAZ的激活物在再生医学中很有用。本文讨论了YAP1和TAZ的抑制剂和激活剂在人类疾病中潜在的应用和综述了检索这些制剂的药物筛选的过程。
关键词: 肿瘤,药物筛选,再生,肌肉减少症,肿瘤抑制剂
图形摘要
Current Drug Targets
Title:The Hippo Pathway as Drug Targets in Cancer Therapy and Regenerative Medicine
Volume: 18 Issue: 4
关键词: 肿瘤,药物筛选,再生,肌肉减少症,肿瘤抑制剂
摘要: Yes-associated protein 1 (YAP1) and transcriptional co-activator with PDZ-binding motif (TAZ) co-operate with numerous transcription factors to regulate gene transcriptions. YAP1 and TAZ are negatively regulated by the tumor suppressive Hippo pathway. In human cancers, the Hippo pathway is frequently deregulated and YAP1 and TAZ escape the inhibition by the Hippo pathway. The upregulation of YAP1 and TAZ induces epithelial-mesenchymal transition and increases drug resistance in cancer cells. TAZ is implicated in cancer stemness. In consequence cancers with hyperactive YAP1 and TAZ are associated with poor clinical prognosis. Inhibitors of YAP1 and TAZ are reasoned to be beneficial in cancer therapy. On the other hand, since YAP1 and TAZ play important roles in the regulation of various tissue stem cells and in tissue repair, activators of YAP1 and TAZ are useful in the regenerative medicine. We discuss the potential application of inhibitors and activators of YAP1 and TAZ in human diseases and review the progress of drug screenings to search for them.
Export Options
About this article
Cite this article as:
The Hippo Pathway as Drug Targets in Cancer Therapy and Regenerative Medicine, Current Drug Targets 2017; 18 (4) . https://dx.doi.org/10.2174/1389450117666160112115641
DOI https://dx.doi.org/10.2174/1389450117666160112115641 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
Related Journals
Related Books
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Structure, Roles and Inhibitors of a Mitotic Protein Kinase Haspin
Current Medicinal Chemistry Thymidine Phosphorylase and Fluoropyrimidines Efficacy: A Jekyl and Hyde Story
Current Medicinal Chemistry - Anti-Cancer Agents Idronoxil as an Anticancer Agent: Activity and Mechanisms
Current Cancer Drug Targets The Bright Future of Radionuclides for Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Editorial [Hot Topic: Akt Pathway in Oncogenesis and as a Target for Anti-Cancer Therapy (Guest Editor: Jin Q. Cheng) ]
Current Cancer Drug Targets High Performance Liquid Chromatographic Approaches to Mass Spectrometry Based Metabolomics
Current Metabolomics Current Major Cancer Targets for Nanoparticle Systems
Current Cancer Drug Targets Glycosylation of Tetraspanin Tspan-1 at Four Distinct Sites Promotes Its Transition Through the Endoplasmic Reticulum
Protein & Peptide Letters Use of Radiopharmaceuticals for Diagnosis, Treatment, and Follow-Up of Differentiated Thyroid Carcinoma
Anti-Cancer Agents in Medicinal Chemistry Green Synthesis and Antioxidant Activity of Novel γ-Cyano-α- hydroxyphosphonate Derivatives
Medicinal Chemistry Mining the Dark Matter of the Cancer Proteome for Novel Biomarkers
Current Cancer Therapy Reviews Therapeutic microRNA Delivery Strategies with Special Emphasis on Cancer Therapy and Tumorigenesis: Current Trends and Future Challenges
Current Drug Metabolism Antitumor Activity of Oxali-Titanocene Y in Xenografted CAKI-1 Tumors in Mice
Letters in Drug Design & Discovery Exfoliated Epithelial Cells: A Non-Invasive way to Evaluate the Physiological State of Gastrointestinal Epithelium
Recent Patents on Biomedical Engineering (Discontinued) The Antiproliferative and Pro-apoptotic Effects of Methoxyamine on Pediatric Medulloblastoma Cell Lines Exposed to Ionizing Radiation and Chemotherapy
Central Nervous System Agents in Medicinal Chemistry An Update of the Review of Neuropsychological Consequences of HIV and Substance Abuse: A Literature Review and Implications for Treatment and Future Research
Current Drug Abuse Reviews Editorial [Hot topic: Imaging Agents for Apoptosis (Guest Editor: Wenbin Zeng)]
Anti-Cancer Agents in Medicinal Chemistry Crotamine, a Small Basic Polypeptide Myotoxin from Rattlesnake Venom with Cell-Penetrating Properties
Current Pharmaceutical Design The c-Met Inhibitors: A New Class of Drugs in the Battle Against Advanced Nonsmall- Cell Lung Cancer
Current Pharmaceutical Design Patent Selections:
Recent Patents on Food, Nutrition & Agriculture