10.6084/m9.figshare.5123641.v1 Son E.D. Son E.D. Shim J.H. Shim J.H. Choi H. Choi H. Kim H. Kim H. Lim K.M. Lim K.M. Chung J.H. Chung J.H. Byun S.Y. Byun S.Y. Lee T.R. Lee T.R. Supplementary Material for: Cathepsin G Inhibitor Prevents Ultraviolet B- Induced Photoaging in Hairless Mice via Inhibition of Fibronectin Fragmentation Karger Publishers 2012 Cathepsin G Fibronectin Matrix metalloproteinase Skin Photoaging 2012-06-29 00:00:00 Dataset https://karger.figshare.com/articles/dataset/Supplementary_Material_for_Cathepsin_G_Inhibitor_Prevents_Ultraviolet_B-_Induced_Photoaging_in_Hairless_Mice_via_Inhibition_of_Fibronectin_Fragmentation/5123641 <b><i>Background:</i></b> Cathepsin G, a serine protease that is activated by ultraviolet (UV) radiation, increases matrix metalloproteinase-1 (MMP-1) expression in fibroblasts through fibronectin (Fn) fragmentation and promotes the conversion of proMMP-1 to active MMP-1. <b><i>Objectives:</i></b> This study investigated whether [2-[3-[[(1-benzoyl-4-piperidinyl)methylamino]carbonyl]-2-naphthalenyl]-1-(1-naphthalenyl)-2-oxoethyl]-phosphonic acid (KPA), a cathepsin G inhibitor, plays any role in extracellular matrix (ECM) damage in an in vitro 3D dermal equivalent (DE) and an in vivo ultraviolet B (UVB)-irradiated hairless mice. <b><i>Methods:</i></b> We examined the potential ECM-protective effects of a cathepsin G inhibitor in an in vitro 3D DE model and an in vivo UVB-irradiated hairless mouse skin model. <b><i>Results:</i></b> Among five known serine protease inhibitors, KPA showed the strongest potency and selectivity against cathepsin G. KPA inhibited the cathepsin G-mediated MMP-1 increase and alleviated the downregulation of mRNAs encoding collagen and tissue inhibitor of matrix metalloproteinase-1 in an in vitro 3D DE model. Most importantly, topical application of KPA (0.025%) to the dorsal skin of hairless mice enhanced collagen expression and attenuated UVB-induced Fn fragmentation and upregulation of MMP-2 and MMP-9 activities. <b><i>Conclusions:</i></b> Cathepsin G inhibitors may be useful for the prevention of UVB-induced photoaging through amelioration of ECM damage and MMP upregulation.