SLAS2014 Exhibitor tutorial
Now on-demand!

Evaluation of the mechanism of action of allosteric modulators and its application to drug discovery using Back-Scattering Interferometry (BSI)

Presented by Dr. Jeff Reagan,  Scientific Director, Department of Metabolic Disorders, Amgen, Inc.

Hear Dr. Jeff Reagan of Amgen discuss his experience using BSI technology and MSI’s Drug Discovery Services to determine affinity, co-operativity and mechanism of action of allosteric modulators binding to a protein complex drug target enabling critical IND submission decisions.

Allosteric modulators are a class of drugs which bind to a site distinct from the orthosteric binding site on a receptor or enzyme. These types of molecules offer potential benefits in terms of both safety and efficacy for the treatment of various diseases. Calcimimetics are positive allosteric modulators at the calcium sensing receptor.  In this lecture, I will discuss the use of calcimimetics for the treatment of secondary hyperparathyroidism. This presentation will discuss application of an operational model of allosteric agonism/modulation to aid in understanding the mechanism of action of calcimimetics.  In addition, an emerging technology based upon backscattering interferometry will be discussed. This technology allows one to determine both the affinity and cooperativity of allosteric modulators to a receptor using a label free system. The information derived from this assay will allow one to couple it to information obtained from cell-based assays in order to gain a better understanding of the mechanism of action of allosteric modulators.

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