ArticleMethods in molecular biology (Clifton, N.J.)2026
Biophysical and Cellular Assays for the Evaluation of Peptidomimetic Inhibitors Based on Degron Sequences.
Article in Methods in molecular biology (Clifton, N.J.), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Scientific research in drug discovery relies on robust, versatile, and well-established methodologies. One effective strategy for targeting disease-relevant proteins, such as E3 ligases, involves rational drug design using degron peptides as starting points for compound development. Here, we present a comprehensive set of complementary assays for the evaluation of degron-based binders, enabling their integration into an efficient drug discovery pipeline. We introduce screening strategies such as Differential Scanning Fluorimetry (DSF) and Fluorescence Polarization (FP), alongside both solution-based and immobilization-based biophysical techniques, including Isothermal Titration Calorimetry (ITC) and Surface Plasmon Resonance (SPR) for reliable affinity determination. To assess intracellular interactions with full-length target proteins, we also employ Nano Bioluminescence Resonance Energy Transfer (NanoBRET). Together, these methods establish a robust framework for the discovery and characterization of degron-based peptidomimetic compounds.
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