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ProteomicsStructural complementarity offsets low receptor affinity in E7820-mediated RBM39 degradation by CRL4DCAF15
The investigational drugs E7820, indisulam and tasisulam (aryl-sulfonamides) promote the degradation of the splicing factor RBM39 in a proteasome and CRL4DCAF15 ubiquitin ligase-dependent mechanism, however the molecular details of this activity remain elusive. Here we present the cryo-EM structure ...
ORGANISM(S): Homo sapiens (Human) 
2019-07-10 | PXD014536 | Pride
Dcaf15 E7820 Crl4 Sulfonamide Ubiquitin Cullin Rbm39 
UnknownThe small-molecule protein ligand interface stabiliser E7820 induces differential cell line specific responses of integrin α2 expression.
Not available
S-EPMC8132423 | biostudies-literature
UnknownStructural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15.
Not available
S-EPMC6917914 | biostudies-literature
GenomicsE7820, an Anti-Cancer Sulfonamide, Degrades RBM39 in Patients with Splicing Factor Mutant Myeloid Malignancies: A Phase II Clinical Trial
E7820, an Anti-Cancer Sulfonamide, Degrades RBM39 in Patients with Splicing Factor Mutant Myeloid Malignancies: A Phase II Clinical Trial
PRJNA944678 | ENA
TranscriptomicsE7820, an Anti-Cancer Sulfonamide, Degrades RBM39 in Patients with Splicing Factor Mutant Myeloid Malignancies: A Phase II Clinical Trial
Mutations in RNA splicing factor genes (SF3B1, SRSF2, and U2AF1) are common in AML and MDS and recent studies demonstrate pharmacologic degradation of the RNA splicing factor RBM39 results in preferential killing of splicing factor mutant cells. We therefore conducted a phase II clinical trial (NCT0...
ORGANISM(S): Homo sapiens 
2024-09-30 | GSE227343 | GEO
UnknownA molecular glue RBM39-degrader induces synthetic lethality in cancer cells with homologous recombination repair deficiency.
Not available
S-EPMC11126574 | biostudies-literature
ClinicalA Phase II Study of the Safety and Efficacy of E7820 Plus Cetuximab in Colorectal Cancer, Preceded by a Run-in Study in Advanced Solid Tumors
This study proposes to determine the safety of the administration of E7820 plus cetuximab and explore the MTD of the combination in a Phase Ib study. In addition, the efficacy of this combination will be explored in patients with colorectal cancer in the Phase II proof of concept phase of the study.
2027665 | ecrin-mdr-crc
UnknownE7820, an anti-cancer sulfonamide, degrades RBM39 in patients with splicing factor mutant myeloid malignancies: a phase II clinical trial.
Not available
S-EPMC10681888 | biostudies-literature
UnknownThe Neutrophil: The Underdog That Packs a Punch in the Fight against Cancer.
Not available
S-EPMC7659937 | biostudies-literature
UnknownL-cysteine transporter-PCR to detect hydrogen sulfide-producing Campylobacter fetus.
Not available
S-EPMC6839519 | biostudies-literature
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