Probable global transcription activator SNF2L2 is a protein that in humans is encoded by the SMARCA2 gene. [5] [6]

2024年12月25日 · Complete information for SMARCA2 gene (Protein Coding), SWI/SNF Related BAF Chromatin Remodeling Complex Subunit ATPase 2, including: function, proteins, disorders, pathways, orthologs, and expression.

Herein, we present development of a potent and selective SMARCA2 degrader, structurally unrelated to known chemotypes with first in class potential selectively targeting SMARCA4 mutant cells. SMARCA2/4, core members of SWI/SNF complex, are two mutually exclusive ATP-dependent engines that function in mobilizing nucleosomes to regulate

2022年11月10日 · Selective SMARCA2 degradation is achieved in the absence of selective SMARCA2/4 PROTAC binding and translates to potent in vitro growth inhibition and in vivo efficacy in SMARCA4 mutant...

SMARCA2 has been identified as a key synthetic lethal target in SMARCA4-deficient cancers, yet the mechanism underlying the synthetic lethal relationship is unclear.

The SMARCA2 gene provides instructions for making one piece (subunit) of a group of similar protein complexes known as SWI/SNF complexes. These complexes regulate gene activity (expression) by a process known as chromatin remodeling.

6 天之前 · SMARCA2 is an ATPase that regulates chromatin structure via ATP pathways, controlling cell division and differentiation. SMARCA2's bromodomain and ATPase domain, crucial for chromatin remodeling and cell regulation, are therapeutic targets in cancer treatment.

BAF requires either SMARCA2 (BRM) or SMARCA4 (BRG1), mutually exclusive ATPase subunits, for chromatin remodeling to occur. Inhibiting SMARCA2 in SMARCA4-deficient cancer is expected to cause synthetic lethality. 2 SMARCA4 mutations are observed in multiple tumor types, including up to 11% in non-small cell lung cancers. 7

Using the TPD approach, Prelude is developing highly potent and selective SMARCA2 protein degraders designed to specifically inhibit SMARCA4-deficient tumors.

• Selective SMARCA2 degradation modulates gene expression via transcriptional regulation in sensitive cell lines, enabling the identification of robust biomarkers