Etanercept is a TNF-α antagonist composed of the dimeric fusion protein of extracellular ligand-binding portion of...

Etanercept is a TNF-α antagonist composed of the dimeric fusion protein of extracellular ligand-binding portion of the soluble 75-kDa TNF-α receptor II and the fragment-crystallisable (Fc) portion of human immunoglobulin (IgG).” Based on this quote, what does etanercept compete with? Where does etanercept and its competitor bind?

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ANSWER

Etanercept is a soluble p75 TNF-alpha receptor fusion protein that binds TNF-alpha and has a longer half life than the native soluble receptor.Etanercept, a fully soluble, human dimeric fusion protein, functions as a TNF inhibitor by competitively binding to TNF and preventing its activation of the inflammatory cascade. Etanercept is composed of 2 extracellular ligand-binding domains of the TNF p75 receptor linked to the Fc portion of human immunoglobulin G1 (IgG1) by 3 disulfide bonds. Etanercept is a soluble form of the p75 receptor that inhibits TNF-α, and to some extent TNF-β, by blocking its interaction with cell-surface TNF receptors. Etanercept is different from adalimumab and infliximab, which are monoclonal antibodies to TNF. The dimeric structure of etanercept allows it to bind TNF at an affinity that is 50 to 1000 times greater than naturally occurring TNF receptors.By binding and sequestering TNF, etanercept modulates biologic responses involved in the pathogenesis of psoriasis, such as the expression of adhesion molecules that function in leukocyte migration (E-selectin and intercellular adhesion molecule-1), serum cytokine levels, and serum matrix metalloproteinase-3 levels

gladiator answered 1 year ago

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