Antagonists of activin signaling: mechanisms and potential biological applications

• Published in: Trends in endocrinology and metabolism Vol. 16; no. 2; pp. 73 - 78
• Main Authors: Harrison, Craig A., Gray, Peter C., Vale, Wylie W., Robertson, David M.
• Format: Journal Article
• Language: English
• Published: London Elsevier Ltd 01.03.2005; Elsevier
• Subjects: Activins - antagonists & inhibitors; Activins - metabolism; Animals; Apud cells. Peptide and protein hormones. Growth factors; Biological and medical sciences; Cachexia - therapy; Fundamental and applied biological sciences. Psychology; Hormone Antagonists - pharmacology; Hormone Antagonists - therapeutic use; Humans; Neoplasms - therapy; Signal Transduction; Vertebrates: endocrinology; Wound Healing - drug effects; Signal transduction; Endogenous; Antagonist; Review; Activin; Mechanism of action; Biological receptor
• ISSN: 1043-2760; 1879-3061
• DOI: 10.1016/j.tem.2005.01.003

Activins are members of the transforming growth factor-β (TGF-β) superfamily that control many physiological processes such as cell proliferation and differentiation, immune responses, wound repair and various endocrine activities. Activins elicit these diverse biological responses by signaling via type I and type II receptor serine kinases. Recent studies have revealed details of the roles of inhibin, betaglycan, follistatin and its related protein follistatin-related gene (FLRG), Cripto and BAMBI in antagonizing activin action, and exogenous antagonists against the activin type I (SB-431542 and SB-505124) and type II (activin-M108A) receptors have been developed. Understanding how activin signaling is controlled extracellularly is the first step in providing treatment for wound healing and for disorders such as cachexia and cancer, which result from a deregulated activin pathway.