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Interrogration of impacts on Hydrogen Deuterium Exchange of ligand binding using heterobifunctional molecules ACBi1(SiTX-0038406), PROTAC1(SiTX-0038404) and PROTAC2(SiTX-0038405) on target proteins SMARCA2 and VHL both in the binary and Ternary modes.
ORGANISM(S): Homo sapiens (Human) 
2022-10-12 | PXD033849 | Pride
The mammalian SWI/SNF helicase SMARCA4 is frequently mutated in cancer and inactivation results in a cellular dependence on its paralog, SMARCA2, thus making SMARCA2 an attractive synthetic lethal target. However, published data indicates that achieving a high degree of SMARCA2 selectivity is likely...
ORGANISM(S): Homo sapiens (Human) 
2022-09-22 | PXD036865 | Pride
Genome binding of SMARCA2 and SMARCA4 in lung cancer cells reconstituted with SMARCA4 WT with and without SMARCA2 depletion
In this work, we characterise novel SMARCA2/4 degraders using a robust cell biology and structural workflow and reveal for the first time, the recruitment of two E3 ligase substrate receptors: FBXO22 and DCAF16 by the same degradation tail. Furthermore, we were able to chemically fine-tune this dual...
ORGANISM(S): Homo sapiens (Human) 
2026-05-16 | PXD065523 | Pride
Heterozygous mutations in SMARCA2 lead to impaired neurogenesis due to global retargeting of SMARCA4
In this work, we characterise novel SMARCA2/4 degraders using a robust cell biology and structural workflow and reveal for the first time, the recruitment of two E3 ligase substrate receptors: FBXO22 and DCAF16 by the same degradation tail. Furthermore, we were able to chemically fine-tune this dual...
ORGANISM(S): Homo sapiens (Human) 
2026-05-16 | PXD065445 | Pride
Chromatin accessibility in response to knockdown of GLI1 and SMARCA2 in GLI1-mediated gene expression.
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