[HTML][HTML] 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 …

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 …

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 …

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 …

[HTML][HTML] The aryl sulfonamide indisulam inhibits gastric cancer cell migration by promoting the ubiquitination and degradation of the transcription factor ZEB1

J Lu, D Li, H Jiang, Y Li, C Lu, T Chen, Y Wang… - Journal of Biological …, 2023 - ASBMB
… experiments reveal that indisulam promotes the interaction between … DCAF15 and the
neosubstrate RNA-binding protein RBM39, which was subsequently ubiquitinated and degraded

Molecular glues for targeted protein degradation: from serendipity to rational discovery

G Dong, Y Ding, S He, C Sheng - Journal of medicinal chemistry, 2021 - ACS Publications
… (a) Chemical structures of indisulam, E7820, CQS, and … of DCAF15, while RBM39 has low
binding affinity with DCAF15. … subsequently promotes cyclin K ubiquitination and degradation. …

[HTML][HTML] Aryl sulfonamides induce degradation of aryl hydrocarbon receptor nuclear translocator through CRL4DCAF15 E3 ligase

SA Kim, SH Jo, JH Cho, MY Yu, HC Shin, JA Kim… - Molecules and cells, 2020 - Elsevier
… proteasomal degradation of ARNT through CRL4 DCAF15 … examined whether degradation
of both RBM39 and RBM23 … proteins and DCAF15 facilitates ARNT degradation. However…

Profiling the landscape of drug resistance mutations in neosubstrates to molecular glue degraders

PM Gosavi, KC Ngan, MJR Yeo, C Su, J Li… - ACS Central …, 2022 - ACS Publications
… (h) Structural view of the E7820-DCAF15-RBM39(RRM2) ternary complex showing the …
evaluated RBM39 degradation using a fluorescent reporter system, in which wt or mutant RBM39