TAPI 1

TAPI-1 is a specific TACE (TNF-α-converting enzyme) inhibitor.IC50 value:Target: TAPI-1 inhibited LL-37-induced TGF-α production, EGFR activation and subsequent MUC5AC mucin production, whereas TGF-α-neutralizing antibody, but not AR- or HB-EGF-neutralizing antibody, inhibited LL-37-induced EGFR activation and subsequent MUC5AC mucin production in NCI-H292 cells [1]. Using the TNF-alpha converting enzyme (TACE) inhibitor, TAPI-1, TPA-stimulated TNFalpha shedding could be completely prevented in PKCepsilon transgenic mice and isolated keratinocytes [2]. Pretreatment with antibody against FcγRII or with CD32 siRNA, p47(phox) siRNA, apocynin, N-acetylcysteine, tumor necrosis factor-α protease inhibitor 1 (TAPI-1) or TACE siRNA attenuated sLOX-1 release induced by CRP. CRP also elevated serum sLOX-1 levels in a rabbit model of atherosclerosis [3].

Signaling Pathways >> Metabolic Enzyme/Protease >> MMP

Research Areas >> Cancer

[1]. Zhang Y, et al. The human Cathelicidin LL-37 induces MUC5AC mucin production by airway epithelial cells via TACE-TGF-α-EGFR pathway. Exp Lung Res. 2014 Jun 5.

[2]. Wheeler DL, et al. Protein kinase Cepsilon is linked to 12-O-tetradecanoylphorbol-13-acetate-induced tumor necrosis factor-alpha ectodomain shedding and the development of metastatic squamous cell carcinoma in protein kinase Cepsilon transgenic mice. Canc

[3]. Zhao XQ, et al. CRP enhances soluble LOX-1 release from macrophages by activating TNF-α converting enzyme. J Lipid Res. 2011 May;52(5):923-33.

GM 6001 | T-5224 | SB-3CT | Batimastat | Astragaloside IV | Marimastat (BB-2516) | edaravone | TAPI-2 | ISOGINKGETIN | Arctigenin | CTS-1027 | GI254023X | JNJ 0966 | CL-82198 | Incyclinide