Target intelligence / Profile preview

A Disintegrin And Metalloprotease 17 (ADAM17)

Target
ADAM17
Molecular classification
Metalloprotease, Sheddase, Type I transmembrane protein
01

Overview

ADAM17, also known as TACE, is a transmembrane metalloprotease responsible for cleaving the extracellular domains of various membrane proteins, including TNF-alpha and IL-6R. This proteolytic activity regulates diverse biological processes such as inflammation, immune response, cell proliferation, and vascular biology. Dysregulation of ADAM17 is implicated in several diseases, including chronic inflammatory conditions, cancer, and metabolic disorders.

Other names
TACETumor Necrosis Factor-α Converting Enzyme
02

Mechanism of action

ADAM17 inhibitors block the shedding of various substrates, preventing their activation or release.

03

Biological functions

Shedding of cytokinesProteolytic processingInflammationImmune response modulationCell proliferationCell differentiationVascular remodelingMetabolic regulationEmbryonic development
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Disease associations

Chronic inflammatory diseasesCancer progressionVascular disordersHypertensionAneurysm formationMetabolic syndromesInsulin resistancePsoriasis
05

Safety considerations

Loss-of-function mutations are lethal during embryogenesisOveractivity contributes to disease states

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