Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex
DE Bussiere, L Xie, H Srinivas, W Shu, A Burke… - Nature Chemical …, 2020 - nature.com
The anticancer agent indisulam inhibits cell proliferation by causing degradation of RBM39,
an essential mRNA splicing factor. Indisulam promotes an interaction between RBM39 and …
an essential mRNA splicing factor. Indisulam promotes an interaction between RBM39 and …
Structural basis and kinetic pathway of RBM39 recruitment to DCAF15 by a sulfonamide molecular glue E7820
X Du, OA Volkov, RM Czerwinski, HL Tan, C Huerta… - Structure, 2019 - cell.com
E7820 and indisulam are two examples of aryl sulfonamides that recruit RBM39 to Rbx-Cul4-
DDA1-DDB1-DCAF15 E3 ligase complex, leading to its ubiquitination and degradation by …
DDA1-DDB1-DCAF15 E3 ligase complex, leading to its ubiquitination and degradation by …
Aryl sulfonamides degrade RBM39 and RBM23 by recruitment to CRL4-DCAF15
Indisulam and related sulfonamides recruit the splicing factor RBM39 to the CRL4-DCAF15
E3 ubiquitin ligase, resulting in RBM39 ubiquitination and degradation. Here, we used a …
E3 ubiquitin ligase, resulting in RBM39 ubiquitination and degradation. Here, we used a …
Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15
The investigational drugs E7820, indisulam and tasisulam (aryl-sulfonamides) promote the
degradation of the splicing factor RBM39 in a proteasome-dependent mechanism. While the …
degradation of the splicing factor RBM39 in a proteasome-dependent mechanism. While the …
Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15
INTRODUCTION Indisulam is an aryl sulfonamide drug that inhibits the proliferation of
certain human cancer cell lines. Its mechanism of action and the mechanism underlying its …
certain human cancer cell lines. Its mechanism of action and the mechanism underlying its …
[HTML][HTML] Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders
Small molecules that induce protein-protein interactions to exert proximity-driven
pharmacology such as targeted protein degradation are a powerful class of therapeutics 1 …
pharmacology such as targeted protein degradation are a powerful class of therapeutics 1 …
CRISPR screen reveals BRD2/4 molecular glue-like degrader via recruitment of DCAF16
AG Shergalis, VL Marin, DY Rhee… - ACS chemical …, 2023 - ACS Publications
Molecular glues (MGs) are monovalent small molecules that induce an interaction between
proteins (native or non-native partners) by altering the protein–protein interaction (PPI) …
proteins (native or non-native partners) by altering the protein–protein interaction (PPI) …
Targeting the spliceosome through RBM39 degradation results in exceptional responses in high-risk neuroblastoma models
Aberrant alternative pre-mRNA splicing plays a critical role in MYC-driven cancers and
therefore may represent a therapeutic vulnerability. Here, we show that neuroblastoma, a …
therefore may represent a therapeutic vulnerability. Here, we show that neuroblastoma, a …
RNA‐binding motif protein 39 (RBM39): an emerging cancer target
RNA‐binding motif protein 39 (RBM39) is an RNA‐binding protein involved in transcriptional
co‐regulation and alternative RNA splicing. Recent studies have revealed that RBM39 is the …
co‐regulation and alternative RNA splicing. Recent studies have revealed that RBM39 is the …
Dual targeting of DDX3 and eIF4A by the translation inhibitor rocaglamide A
M Chen, M Asanuma, M Takahashi, Y Shichino… - Cell chemical …, 2021 - cell.com
The translation inhibitor rocaglamide A (RocA) has shown promising antitumor activity
because it uniquely clamps eukaryotic initiation factor (eIF) 4A onto polypurine RNA for …
because it uniquely clamps eukaryotic initiation factor (eIF) 4A onto polypurine RNA for …