Recent progress in TGF-β inhibitors for cancer therapy

Cheng-Yi Huang; Chih-Ling Chung; Tsung-Hui Hu; Jih-Jung Chen; Pei-Feng Liu; Chun-Lin Chen

doi:10.1016/j.biopha.2020.111046

Recent progress in TGF-β inhibitors for cancer therapy

Biomed Pharmacother. 2021 Feb:134:111046. doi: 10.1016/j.biopha.2020.111046. Epub 2020 Dec 16.

Authors

Cheng-Yi Huang¹, Chih-Ling Chung², Tsung-Hui Hu³, Jih-Jung Chen⁴, Pei-Feng Liu⁵, Chun-Lin Chen⁶

Affiliations

¹ Department of Biological Sciences, National Sun Yat-sen University, Kaohsiung 80424, Taiwan, ROC; Department of Pathology, Kaohsiung Armed Forces General Hospital, Kaohsiung 80284, Taiwan, ROC.
² Department of Biological Sciences, National Sun Yat-sen University, Kaohsiung 80424, Taiwan, ROC.
³ Division of Hepato-Gastroenterology, Department of Internal Medicine, Kaohsiung Chang Gung Memorial Hospital, Kaohsiung 83301, Taiwan, ROC.
⁴ Faculty of Pharmacy, School of Pharmaceutical Sciences, National Yang-Ming University, Taipei 11221, Taiwan, ROC; Department of Medical Research, China Medical University Hospital, China Medical University, Taichung 40402, Taiwan.
⁵ Department of Biomedical Science and Environmental Biology, Kaohsiung Medical University, Kaohsiung 80708, Taiwan ROC.
⁶ Department of Biological Sciences, National Sun Yat-sen University, Kaohsiung 80424, Taiwan, ROC; Department of Biotechnology, Kaohsiung Medical University, Kaohsiung 80708, Taiwan ROC; Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 80708, Taiwan ROC. Electronic address: chunlinchen@mail.nsysu.edu.tw.

PMID: 33341049
DOI: 10.1016/j.biopha.2020.111046

Abstract

Transforming growth factor-β (TGF-β) is a multifunctional cytokine that is involved in proliferation, metastasis, and many other important processes in malignancy. Inhibitors targeting TGF-β have been considered by pharmaceutical companies for cancer therapy, and some of them are in clinical trial now. Unfortunately, several of these programs have recently been relinquished, and most companies that remain in the contest are progressing slowly and cautiously. This review summarizes the TGF-β signal transduction pathway, its roles in oncogenesis and fibrotic diseases, and advancements in antibodies and small-molecule inhibitors of TGF-β.

Keywords: Cancer therapy; Endocytosis; Lipid raft; Small-molecule inhibitor; TGF-β inhibitor.

Publication types

Review

MeSH terms

Animals
Antibodies, Neutralizing / therapeutic use
Antineoplastic Agents / therapeutic use*
Aptamers, Peptide / therapeutic use
Cancer Vaccines / therapeutic use
Carcinogenesis / drug effects
Clinical Trials as Topic
Endocytosis / drug effects
Fibrosis / drug therapy
Humans
Membrane Microdomains / metabolism
Mice
Neoplasms / drug therapy*
Oligonucleotides, Antisense / therapeutic use
Receptors, Transforming Growth Factor beta / antagonists & inhibitors
Receptors, Transforming Growth Factor beta / metabolism
Signal Transduction / drug effects
Transforming Growth Factor beta / antagonists & inhibitors*
Transforming Growth Factor beta / metabolism*

Substances

Antibodies, Neutralizing
Antineoplastic Agents
Aptamers, Peptide
Cancer Vaccines
Oligonucleotides, Antisense
Receptors, Transforming Growth Factor beta
Transforming Growth Factor beta