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View article: Supplemental Figure S1 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11
Supplemental Figure S1 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11 Open
Supplemental Figure S1 shows BRD4 degradation kinetics in the HiBiT reporter cell line
View article: Data from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11
Data from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11 Open
Targeted protein degradation (TPD) using the ubiquitin proteasome system (UPS) is a rapidly growing drug discovery modality to eliminate pathogenic proteins. Strategies for TPD have focused on heterobifunctional degraders that often suffer…
View article: Supplementary Table S3 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11
Supplementary Table S3 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11 Open
Supplemental Table S3 shows the protein expression plasmids used in these studies
View article: Supplementary Table S1 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11
Supplementary Table S1 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11 Open
Supplementary Table S1 shows CRISPR screen hits
View article: Supplementary Table S4 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11
Supplementary Table S4 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11 Open
Supplementary Table S4 shows information for the antibodies used in these studies
View article: Supplementary Data from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11
Supplementary Data from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11 Open
Supplementary file containing Figures S1-3 and Tables S1-4
View article: Supplemental Figure S2 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11
Supplemental Figure S2 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11 Open
Supplemental Figure S2 shows PLX-3618 binding data to both bromodomains of BRD4
View article: Supplementary Figure S3 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11
Supplementary Figure S3 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11 Open
Supplementary Figure S3 shows megakaryocyte colony formation data
View article: Supplementary Table S2 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11
Supplementary Table S2 from Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11 Open
Supplementary Table S2 show anti-proliferative activity in AML cell lines (n = 2)
View article: Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11
Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11 Open
Targeted protein degradation (TPD) using the ubiquitin proteasome system (UPS) is a rapidly growing drug discovery modality to eliminate pathogenic proteins. Strategies for TPD have focused on heterobifunctional degraders that often suffer…
View article: Supplementary Data from Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A
Supplementary Data from Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A Open
Tables S1-S3, Figures S1-S5
View article: Data from Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A
Data from Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A Open
The PI3K/AKT/mTOR pathway is often activated in lymphoma through alterations in PI3K, PTEN, and B-cell receptor signaling, leading to dysregulation of eIF4A (through its regulators, eIF4B, eIF4G, and PDCD4) and the eIF4F complex. Activatio…
View article: Data from Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A
Data from Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A Open
The PI3K/AKT/mTOR pathway is often activated in lymphoma through alterations in PI3K, PTEN, and B-cell receptor signaling, leading to dysregulation of eIF4A (through its regulators, eIF4B, eIF4G, and PDCD4) and the eIF4F complex. Activatio…
View article: Supplementary Data from Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A
Supplementary Data from Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A Open
Tables S1-S3, Figures S1-S5
View article: Zotatifin, an eIF4A-Selective Inhibitor, Blocks Tumor Growth in Receptor Tyrosine Kinase Driven Tumors
Zotatifin, an eIF4A-Selective Inhibitor, Blocks Tumor Growth in Receptor Tyrosine Kinase Driven Tumors Open
Oncoprotein expression is controlled at the level of mRNA translation and is regulated by the eukaryotic translation initiation factor 4F (eIF4F) complex. eIF4A, a component of eIF4F, catalyzes the unwinding of secondary structure in the 5…
View article: Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A
Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A Open
The PI3K/AKT/mTOR pathway is often activated in lymphoma through alterations in PI3K, PTEN, and B-cell receptor signaling, leading to dysregulation of eIF4A (through its regulators, eIF4B, eIF4G, and PDCD4) and the eIF4F complex. Activatio…
View article: AGER1 downregulation associates with fibrosis in nonalcoholic steatohepatitis and type 2 diabetes
AGER1 downregulation associates with fibrosis in nonalcoholic steatohepatitis and type 2 diabetes Open
Type 2 diabetes is clinically associated with progressive necroinflammation and fibrosis in nonalcoholic steatohepatitis (NASH). Advanced glycation end-products (AGEs) accumulate during prolonged hyperglycemia, but the mechanistic pathways…
View article: Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase
Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase Open
Dysregulation of protein translation is a key driver for the pathogenesis of many cancers. Eukaryotic initiation factor 4A (eIF4A), an ATP-dependent DEAD-box RNA helicase, is a critical component of the eIF4F complex, which regulates cap-d…
View article: Nonphagocytic Activation of NOX2 Is Implicated in Progressive Nonalcoholic Steatohepatitis During Aging
Nonphagocytic Activation of NOX2 Is Implicated in Progressive Nonalcoholic Steatohepatitis During Aging Open
Background and Aims Older patients with obesity/type II diabetes mellitus frequently present with advanced NASH. Whether this is due to specific molecular pathways that accelerate fibrosis during aging is unknown. Activation of the Src hom…
View article: Galectin‐3 regulates inflammasome activation in cholestatic liver injury
Galectin‐3 regulates inflammasome activation in cholestatic liver injury Open
Macrophage activation is an important feature of primary biliary cholangitis (PBC) pathogenesis and other cholestatic liver diseases. Galectin‐3 (Gal3), a pleiotropic lectin, is produced by monocytic cells and macrophages. However, its rol…