Abstract
Abstract Epigenetic modifications are dynamic and reversible processes that regulate gene expression without altering the underlying sequence of the DNA. Gene expression is instead controlled by modification to the chromatin including DNA methylation, histone modifications, and chromatin remodeling. The proteins that perform these epigenetic modifications can be divided into three classes: writers, which perform the modifications; readers, which recognize the modifications; and erasers, which remove the modifications. While essential for normal cellular function, abnormal expression or alteration of the proteins involved in epigenetic regulation can lead to disease, such as cancer. As a result, epigenetic modifiers present attractive targets for the discovery and development of novel therapeutics. At Reaction Biology we offer a suite of services to enable epigenetic drug including the largest panel for epigenetic screening and profiling in the industry and biochemical and biophysical technologies to evaluate inhibition, potency, target occupancy, and even binding modes. Here we highlight our biophysical platform surface plasmon resonance (SPR) using the epigenetic target PRMT5 as an example. SPR was used to measure the binding kinetics of several small molecule inhibitors of PRMT5 and explore their distinct binding modes. Citation Format: Rebecca Eells, Lynn K. Baker, Christopher Bray, Haiching Ma. Probing PRMT5 inhibitors with distinct binding modes using surface plasmon resonance [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2022; 2022 Apr 8-13. Philadelphia (PA): AACR; Cancer Res 2022;82(12_Suppl):Abstract nr 2921.
Published Version
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