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Updated: May 15, 2026

Determination of the Relative Potency of an Anti-TNF Monoclonal Antibody (mAb) by Neutralizing TNF Using an In Vitro Bioanalytical Method
Published on: September 16, 2017
Small-molecule inhibitors of the interaction between TNF and TNFR
Jessica M Davis1, Julie Colangelo
1Fairfield University, 173 North Benson Road, Fairfield, CT 06824, USA. jmdavis@fairfield.edu
Abstract:
The overexpression of TNF has been implicated in a variety of disease conditions including rheumatoid arthritis, Crohn's disease, HIV and cancer. It is presently a therapeutic target for inflammatory diseases. Many of the therapeutics currently used are biologics designed to sequester TNF, preventing it from binding with its receptors. Recent research has been focused on finding small molecules that alter the production of TNF, modulate its signal transduction pathways, or directly inhibit the binding to its receptors. Modulation of a protein-protein interaction with small molecules is an interesting and nontrivial approach. The various strategies used in obtaining small-molecule, nonpeptide, inhibitors of the TNF-TNF receptor interaction through disruption of the TNF trimer or direct inhibition of the TNF-TNF receptor interaction are presented here.
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