While targeted protein degraders such as PROTACs are a clinically proven therapeutic strategy, the discovery of novel degraders remains hampered by trial-and-error process. To address this challenge, we developed the AIMSTM platform, which combines structural proteomics with AI models for rational PROTAC design. AIMSTM is an end-to-end toolkit for PROTAC optimization, encompassing structure solving using proteomics and AI, prediction of ADME and degradation properties, and prospective ranking of compound design ideas. Altogether, this integrated platform successfully enabled the multi-parameter optimization of a potent and bioavailable in vivo validated KAT6A degrader, establishing a versatile framework for PROTAC development across various targets.
Arad, G., Simchi, N., Brodsky, S., Shtrikman, A., Kedem, Y., Alchanati, I., Otonin, G., Shenoy, A., Kovalerchik, D., Ran Shchory, M., Ben Shoshan-Galeczki, Y., Cohen, N., Lange, K., Seger, E., Pevzner, K.
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