SMARCA2/4 PROTAC for targeted protein degradation and cancer therapy
RB Kargbo - ACS Medicinal Chemistry Letters, 2020 - ACS Publications
Biological Target. SMARCA2 and SMARCA4 Summary. The SMARCA subgroup of genes
belong to the SWI1/SNF1 family that provide instructions for making chromatin remodeling …
belong to the SWI1/SNF1 family that provide instructions for making chromatin remodeling …
Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers
J Cantley, X Ye, E Rousseau, T Januario… - Nature …, 2022 - nature.com
Abstract The mammalian SWItch/Sucrose Non-Fermentable (SWI/SNF) helicase SMARCA4
is frequently mutated in cancer and inactivation results in a cellular dependence on its …
is frequently mutated in cancer and inactivation results in a cellular dependence on its …
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 …
deficiency. Herein, we report the design, synthesis, and biological evaluation of selective …
Potent SMARCA2 targeted degraders induce genetic synthetic lethality in SMARCA4 deleted cancer
SWI/SNF complexes play an important role in controlling gene expression by remodeling
chromatin. SMARCA2 (BRM) and SMARCA4 (BRG1) are the core subunits of the SWI/SNF …
chromatin. SMARCA2 (BRM) and SMARCA4 (BRG1) are the core subunits of the SWI/SNF …
A two-faced selectivity solution to target SMARCA2 for cancer therapy
JD Harling, CP Tinworth - nature communications, 2023 - nature.com
Two new studies exploring PROTAC-mediated degradation of SMARCA2 for cancer therapy
solve an apparently intractable selectivity challenge with SMARCA4 by utilising the …
solve an apparently intractable selectivity challenge with SMARCA4 by utilising the …
Bifunctional Compounds as SMARCA2 Degraders for Treating Cancer
RW Sabnis - ACS Medicinal Chemistry Letters, 2021 - ACS Publications
Disease Area. Cancer Biological Target. SMARCA2 Summary. The field of targeted protein
degradation promoted by small molecules has been intensively studied. Bifunctional …
degradation promoted by small molecules has been intensively studied. Bifunctional …
Synthetic lethality: targeting SMARCA2 ATPase in SMARCA4-deficient tumors–a review of patent literature from 2019–30 June 2023
KD Reichl, ECY Lee, A Gopalsamy - Expert Opinion on …, 2024 - Taylor & Francis
Introduction The multi-subunit SWI/SNF chromatin remodeling complex is a key epigenetic
regulator for many cellular processes, and several subunits are found to be mutated in …
regulator for many cellular processes, and several subunits are found to be mutated in …
[PDF][PDF] Preclinical characterization of PRT3789, a potent and selective SMARCA2 targeted degrader
M Hulse, A Agarwal, M Wang, J Carter, M Sivakumar… - Cancer Res., 2022 - preludetx.com
Background► SWItch/Sucrose Non-Fermentable (SWI/SNF) complexes play an important
role in controlling gene expression by remodeling chromatin. 1► SWI/SNF Related, Matrix …
role in controlling gene expression by remodeling chromatin. 1► SWI/SNF Related, Matrix …
Synthetic lethality: targeting the SMARCA2 bromodomain for degradation in SMARCA4-deficient tumors–a review of patent literature from 2019-June 2023
ECY Lee, KD Reichl, A Gopalsamy - Expert Opinion on …, 2024 - Taylor & Francis
Introduction SMARCA2 and SMARCA4 are subunits of the SWI/SNF complex which is a
chromatin remodeling complex and a key epigenetic regulator that facilitates gene …
chromatin remodeling complex and a key epigenetic regulator that facilitates gene …
Application of Selective SMARCA2/4 PROTAC for Mutant Cancer Therapy
RB Kargbo - ACS Medicinal Chemistry Letters, 2022 - ACS Publications
Bromodomains (BRDs) are epigenetic protein–protein interaction modules that are involved
in gene transcription. Most often, multiple bromodomains are present in nuclear complexes …
in gene transcription. Most often, multiple bromodomains are present in nuclear complexes …