Drug intelligence / Profile preview

TAPI-0

Development stage
Unknown
Lead developer
Amgen
Modality
Small Molecules
Administration
Parenteral
01

Overview

TAPI-0 (TNF-alpha processing inhibitor-0) is a synthetic, hydroxamate-based small molecule inhibitor of tumor necrosis factor-alpha converting enzyme (TACE/ADAM17) and various matrix metalloproteinases (MMPs), including collagenase and gelatinase. It acts as a sheddase inhibitor, blocking the proteolytic cleavage and release of cell-surface proteins such as pro-TNF-alpha, L-selectin, and soluble TNF receptors (sTNFR1 and sTNFR2). TAPI-0 is widely utilized as a research tool to study cell signaling, protein shedding, and inflammatory processes, particularly in the context of macrophage migration and tumor microenvironment modulation. It has also been shown to inhibit bacterial peptide deformylase (PDF).

Other names
N-[(2R)-2-[2-(Hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]-3-(2-naphthalenyl)-L-alanyl-L-alaninamideN-(R)-[2-(Hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-naphthylalanyl-L-alanine AmideTNF-alpha protease inhibitor-0TNF-alpha processing inhibitor-0
02

Targets

ADAM17 (A disintegrin and metalloprotease 17)MMP9 (Matrix metalloproteinase-9)MMP12 (Macrophage Metalloelastase)PDF (Peptide deformylase, mitochondrial)MMP1 (Matrix metalloproteinase-1)MMP13 (Matrix metalloproteinase-13)MMP2 (Matrix metalloproteinase-2)MMP8 (Neutrophil collagenase)

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