Abstract A046: Identification of paralog selective degraders of SMARCA2 and SMARCA4 for treatment of various cancers

C Abbineni, K Aithal, L Khare, SD V, B Kuila… - Molecular Cancer …, 2023 - AACR
Abstract Background: The BAF (SWI/SNF) chromatin remodeling complex comprises of two
mutually exclusive ATPases, SMARCA2 (BRM) and SMARCA4 (BRG1), that affect the …
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Discovery of orally bioavailable SMARCA2/4 dual degraders for treatment of acute myeloid leukemia

C Abbineni, L Khare, B Kuila, AR Khaji, DB Mahadeo… - Cancer Research, 2022 - AACR
Abstract Background: The BAF (SWI/SNF) chromatin remodeling complex comprises of two
mutually exclusive ATPases, SMARCA2 (BRM) and SMARCA4 (BRG1), that affect the …
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Orally bioavailable SMARCA2 degraders with exceptional selectivity and potency

C Abbineni, LK Satyam, B Kuila, A Ettam, KA Rawoof… - Cancer Research, 2021 - AACR
Abstract Background: SMARCA2 (BRM) and SMARCA4 (BRG1) are two mutually exclusive
DNA-dependent ATPases of the SWI/SNF complex, which function in mobilizing …
被引用次数：1 相关文章

Discovery of potent, highly selective and orally efficacious SMARCA2 degraders

L Leng, L Yang, W Tu, R Rej, SR Allu, L Huang… - Cancer Research, 2024 - AACR
In human non-small cell lung cancer, melanoma and other types of human cancers, the
mammalian SWItch/Sucrose Non-Fermentable (SWI/SNF) helicase SMARCA4 is frequently …
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Abstract B113: Discovery of PRT3789, a first-in-class potent and selective SMARCA2 degrader in clinical trials for the treatment of patients with SMARCA4 mutated …

K Ito, M Hulse, A Agarwal, J Carter, M Sivakumar… - Molecular Cancer …, 2023 - AACR
SWI/SNF complexes play an important role in controlling gene expression by remodeling
chromatin. SMARCA2 (BRM) and SMARCA4 (BRG1) are the core catalytic subunits of the …
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Preclinical characterization of PRT7732: A highly potent, selective, and orally bioavailable targeted protein degrader of SMARCA2

A Shvartsbart, K Ito, J Rager, M Hulse, A Agarwal… - Cancer Research, 2024 - AACR
Abstract SWI/SNF (BAF) complexes play an important role in controlling gene expression by
remodeling chromatin. SMARCA2 (BRM) and SMARCA4 (BRG1) are the core catalytic …
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[PDF] preludetx.com

[PDF][PDF] Selective and orally bioavailable SMARCA2 targeted degraders induce synthetic lethality in SMARCA4-deficient solid tumor

K Ito, A Shvartsbart, J Rager, A Agarwal, M Hulse… - Cancer …, 2023 - preludetx.com
Conclusions▸ We have identified the first orally bioavailable bivalent molecules that
selectively degrade SMARCA2 over SMARCA4 by> 100 fold▸ Our SMARCA2 oral degrader …
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Discovery of SMD-3040 as a Potent and Selective SMARCA2 PROTAC Degrader with Strong in vivo Antitumor Activity

L Yang, W Tu, L Huang, B Miao… - Journal of Medicinal …, 2023 - ACS Publications
SMARCA2 is an attractive synthetic lethality target for human cancers with SMARCA4
deficiency. Herein, we report the design, synthesis, and biological evaluation of selective …
被引用次数：11 相关文章 所有 2 个版本

Development of potent, highly selective and efficacious SMARCA2 degraders

L Yang, W Tu, L Huang, L Leng, W Jiang, M Wang… - Cancer Research, 2024 - AACR
In human lung, melanoma and other types of human cancers, the mammalian
SWItch/Sucrose Non-Fermentable (SWI/SNF) helicase SMARCA4 is frequently mutated …
被引用次数：1 相关文章

713TiP A phase I study of PRT3789, a potent and selective degrader of SMARCA2 in patients with advanced or metastatic solid tumors and a SMARCA4 mutation

I Dagogo-Jack, A Dowlati, R Guo… - Annals of …, 2023 - annalsofoncology.org
Background Genes encoding subunits of the switch/sucrose non-fermentable (SWI/SNF)
chromatin remodeling complex are often mutated in cancer, occurring in 20% of all human …
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