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Journal: Modeling the Effect of Cooperativity in Ternary Complex Formation and Targeted Protein Degradation Mediated by Heterobifunctional Degraders. (Pubmed Central) - Apr 27, 2023
We also develop a statistical inference model for determining cooperativity in intracellular ternary complex formation from cellular assay data and demonstrate it by quantifying the change in cooperativity due to site-directed mutagenesis at the POI-ligase interface of the SMARCA2-ACBI1-VHL ternary complex. Our pharmacodynamic model provides a quantitative framework to dissect the complex HBF-mediated TPD process and may inform the rational design of effective HBF degraders.
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[VIRTUAL] A mutation characteristics analysis of SMARCA4defSMARCA2wt in lung cancer () - Jul 22, 2021 - Abstract #ESMO2021ESMO_2478;
Selective SMARCA2 degrading agents (such as ACBI1, one of PROTAC drugs) can induce the death of SMARCA4-deficient cancer cells... Our analysis indicate the medication-related mutation characteristics of SMARCA4defSMARCA2wt in lung cancer, and may contribute to medication guidance.
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