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Small-Molecule Inhibition of TNF-α

by Cachero, Teresa G. , Choong, Ingrid C. , Oslob, Johan D. , Braisted, Andrew C. , Cancilla, Mark T. , Day, Eric S. , Whitty, Adrian , Lugovskoy, Alexey A. , Wang, Jun , Yoburn, Josh C. , Fung, Amy D. , Miller, Stephan K. , Smith, Annemarie Stroustrup , Eldredge, John K. , He, Molly M. , Cruz, Leslie A. , Flanagan, William M. , Cunningham, Brian C. , Friedman, Jessica E. , Farrington, Graham

in Analysis / Binding sites / Biological and medical sciences / Biotinylation / Bones, joints and connective tissue. Antiinflammatory agents / Chemical Phenomena / Chemistry, Physical / Crystal structure / Crystallography, X-Ray / Dimerization / Dimers / Fluorescence / Hydrogen / Hydrogen - chemistry / Hydrophobic and Hydrophilic Interactions / Indoles - chemical synthesis / Indoles - chemistry / Indoles - pharmacology / Kinetics / Mass Spectrometry / Medical sciences / Models, Chemical / Models, Molecular / Molecular Conformation / Molecular Structure / Molecules / Monomers / Pharmacology. Drug treatments / Protein Conformation / Protein Subunits - chemistry / Receptors / Receptors, Tumor Necrosis Factor, Type I - metabolism / Trimers / Tumor Necrosis Factor-alpha - antagonists & inhibitors / Tumor Necrosis Factor-alpha - chemistry / Tumor Necrosis Factor-alpha - metabolism

2005

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2005

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2005

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Journal Article

Small-Molecule Inhibition of TNF-α

Cachero, Teresa G.,

Choong, Ingrid C.,

Oslob, Johan D.,

Braisted, Andrew C.,

Cancilla, Mark T.,

Day, Eric S.,

Whitty, Adrian,

Lugovskoy, Alexey A.,

Wang, Jun,

Yoburn, Josh C.,

Fung, Amy D.,

Miller, Stephan K.,

Smith, Annemarie Stroustrup,

Eldredge, John K.,

He, Molly M.,

Cruz, Leslie A.,

Flanagan, William M.,

Cunningham, Brian C.,

Friedman, Jessica E.,

Farrington, Graham

2005

Overview

We have identified a small-molecule inhibitor of tumor necrosis factor α (TNF-α) that promotes subunit disassembly of this trimeric cytokine family member. The compound inhibits TNF-α activity in biochemical and cell-based assays with median inhibitory concentrations of 22 and 4.6 micromolar, respectively. Formation of an intermediate complex between the compound and the intact trimer results in a 600-fold accelerated subunit dissociation rate that leads to trimer dissociation. A structure solved by x-ray crystallography reveals that a single compound molecule displaces a subunit of the trimer to form a complex with a dimer of TNF-α subunits.

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Publisher

American Association for the Advancement of Science

Subject

Analysis

/ Binding sites

/ Biological and medical sciences

/ Biotinylation

/ Bones, joints and connective tissue. Antiinflammatory agents

/ Chemical Phenomena

/ Chemistry, Physical