Instituto Gulbenkian de Ciência, Oeiras, Portugal.
Faculty of Veterinary Medicine, Lusofona University, Lisbon, Portugal.
Life Sci Alliance. 2023 Jan 31;6(4). doi: 10.26508/lsa.202201644. Print 2023 Apr.
The metalloprotease ADAM17 is a sheddase of key molecules, including TNF and epidermal growth factor receptor ligands. ADAM17 exists within an assemblage, the "sheddase complex," containing a rhomboid pseudoprotease (iRhom1 or iRhom2). iRhoms control multiple aspects of ADAM17 biology. The FERM domain-containing protein iTAP/Frmd8 is an iRhom-binding protein that prevents the precocious shunting of ADAM17 and iRhom2 to lysosomes and their consequent degradation. As pathophysiological role(s) of iTAP/Frmd8 have not been addressed, we characterized the impact of iTAP/Frmd8 loss on ADAM17-associated phenotypes in mice. We show that iTAP/Frmd8 KO mice exhibit defects in inflammatory and intestinal epithelial barrier repair functions, but not the collateral defects associated with global ADAM17 loss. Furthermore, we show that iTAP/Frmd8 regulates cancer cell growth in a cell-autonomous manner and by modulating the tumor microenvironment. Our work suggests that pharmacological intervention at the level of iTAP/Frmd8 may be beneficial to target ADAM17 activity in specific compartments during chronic inflammatory diseases or cancer, while avoiding the collateral impact on the vital functions associated with the widespread inhibition of ADAM17.
金属蛋白酶 ADAM17 是 TNF 和表皮生长因子受体配体等关键分子的脱落酶。ADAM17 存在于一个集合体中,即“脱落酶复合物”,其中包含一个菱形假蛋白酶(iRhom1 或 iRhom2)。iRhoms 控制 ADAM17 生物学的多个方面。含有 FERM 结构域的蛋白 iTAP/Frmd8 是一种 iRhom 结合蛋白,可防止 ADAM17 和 iRhom2 过早分流到溶酶体并随之降解。由于尚未解决 iTAP/Frmd8 的病理生理作用,我们在小鼠中描述了 iTAP/Frmd8 缺失对 ADAM17 相关表型的影响。我们表明,iTAP/Frmd8 KO 小鼠在炎症和肠道上皮屏障修复功能方面存在缺陷,但不存在与全局 ADAM17 缺失相关的次要缺陷。此外,我们表明 iTAP/Frmd8 通过调节肿瘤微环境以细胞自主的方式调节癌细胞生长。我们的工作表明,在慢性炎症性疾病或癌症期间,在 iTAP/Frmd8 水平进行药理学干预可能有益于靶向特定部位的 ADAM17 活性,同时避免对与广泛抑制 ADAM17 相关的重要功能产生次要影响。