Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15

TB Faust, H Yoon, RP Nowak, KA Donovan, Z Li… - Nature chemical …, 2020 - nature.com
… to promote RBM39 degradation by CRL4 DCAF15 . We find that DCAF15 adopts a structure
… and engages the second RRM domain of RBM39 with an extended, non-conserved surface …

Investigations around RBM39 degrading arylsulfonamides

S Coomar - 2020 - edoc.unibas.ch
… The following chapter summarizes our structural investigations around the RBM39-ArSulf-DCAF15
interaction. We conduct immunoprecipitation and pull-down experiments with the …

[HTML][HTML] A molecular glue RBM39-degrader induces synthetic lethality in cancer cells with homologous recombination repair deficiency

S Kohsaka, S Yagishita, Y Shirai, Y Matsuno… - NPJ Precision …, 2024 - nature.com
… Interestingly, E7820-mediated double-strand breaks in DNA … complex assembly between
RBM39 and DCAF15, an adapter … represses cassette exon inclusion and promotes intron …

Insights on the biological functions and diverse regulation of RNA-binding protein 39 and their implication in human diseases

M Eléouët, C Lu, Y Zhou, P Yang, J Ma, G Xu - Biochimica et Biophysica …, 2023 - Elsevier
… glues to recruit RBM39 to the CRL4 DCAF15 E3 ubiquitin … Most protein isoforms for RBM39
contain all four structural … Abl/ABL1, facilitating the transcription coactivation of RBM39 on the …

Targeting the E3 ubiquitin ligases DCAF15 and cereblon for cancer therapy

KM Nguyen, L Busino - Seminars in Cancer Biology, 2020 - Elsevier
… that thalidomide promotes proteasomal degradation of the Sal-… -EM structure of the
DDB1–DCAF15–DDA1 bound to RBM39DCAF15 or RBM39, and formation of the …

Targeting the spliceosome through RBM39 degradation results in exceptional responses in high-risk neuroblastoma models

S Singh, W Quarni, M Goralski, S Wan, H Jin… - Science …, 2021 - science.org
… of DCAF15, and … RBM39 dependence and DCAF15 expression. Here, we demonstrate that
neuroblastoma is both dependent on RBM39 and expresses relatively high levels of DCAF15

[PDF][PDF] Characterization of Ubiquitin Ligase Targeting by Anticancer Sulfonamides

TCY Ting - 2020 - utswmed-ir.tdl.org
… Inducing proximity among these proteins facilitates the transfer … degron within RBM39 as
well as the residues in DCAF15 that … system for structural and functional studies of RBM39, we …

Unlocking DCAFs To Catalyze Degrader Development: An Arena for Innovative Approaches

Q Miao, VD Kadam, A Mukherjee, Z Tan… - Journal of Medicinal …, 2023 - ACS Publications
… an allosteric stabilizer of DCAF15RBM39 complex or act as … The structural model of
the human DCAF15–E7820–RBM39 … -type way, but rather facilitated the degradation of off-target …

Arylsulfonamide mediated RBM39 degradation causes aberrant splicing of mitotic kinesins

S Coomar, A Penson, J Schwaller, O Abdel-Wahab… - bioRxiv, 2021 - biorxiv.org
… of RBM39 degradation introduces complex pleiotropic effects that are difficult to untangle. For
example, DCAF15 inhibition, RBM39 degradation, … 1B) are structurally related to indisulam …

E3-specific degrader discovery by dynamic tracing of substrate receptor abundance

A Hanzl, E Barone, S Bauer, H Yue… - Journal of the …, 2023 - ACS Publications
DCAF15 (Figure 4C). Upon docking of dRRM-1 to a published crystal structure of
DDB1ΔB-DDA1-DCAF15-E7820-RBM39, … E3 ligases of interest and facilitate the de novo …