TGF-β1 is a cytokine transforming growth factor β Polypeptide member of the superfamily. Specifically, it is a secretory protein with a variety of cellular functions, including the control of cell growth, cell proliferation, cell differentiation, and apoptosis. Besides, TGF-β Superfamily regulates cell growth and differentiation. At least four kinds of TGF have been found in mammals-β subtypes, including TGF-β1、TGF-β2、TGF-β3, and TGF-β1β2. Moreover, it plays a key role in the chronic inflammation of various tissues. Furthermore, it is relevant to organ fibrosis caused by inflammation, epithelial-mesenchymal transformation (EMT), and extracellular deposition matrix (ECM).
Meanwhile, TGF-β1 treatment activated the TGF/Smad signaling pathway during the transformation from BMEC to EMT phenotype. In addition, TGF-β1 enhanced the gene expression of MMP2, MMP7, and fibronectin. Nonetheless, TGF-β Injection induced mammary gland infection and fibrosis in mice. TGF-β1-induced phenotypic changes cause functional changes leading to cell proliferation, ECM deposition, and liver fibrosis. Importantly, TGF-β1 increases collagen expression in LF cells. Particularly, TGF-β binding with connective tissue growth factor (cTGF) can regulate cell proliferation and the synthesis of ECM components. Here, we will introduce a potent TGFβ1 antagonist, IMM-H007.
IMM-H007 is a Potent TGFβ1 Antagonist.
First of all, IMM-H007 has protective effects in cardiovascular diseases via activation of AMPK (AMP-activated protein kinase). In particular, IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling.
In the second place, IMM-H007 inhibits ABCA1 degradation. IMM-H007 resolves hepatic steatosis in HFD-fed hamsters by the regulation of lipid metabolism. Obviously, IMM-H007 can be used for the research of nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis.
Last but not the least, IMM-H007 inhibits fatty acid import into hepatocytes and liver lipogenesis. Additionally, IMM-H007 concomitantly stimulates fatty acid oxidation, autophagy, and the export of hepatic lipids.
All in all, IMM-H007 is a potent TGFβ1 antagonist.