Rbm39 glue
TīmeklisIndisulam is an acts as a molecular glue to induce proteosomal degradation of mRNA splicing factor RBM39 (also designated CAPERα, HCC1, FSAP59, and RNPC2), via binding to DCAF15. Acts as a pre-mRNA splicing modulator (SPLAMs; splicing inhibitor sulfonamides), causes aberrant pre-mRNA splicing. Suppresses proliferation of … TīmeklisdCeMM1 is a RBM39 glue degrader. dCeMM1 can re-direct the activity of the CRL4DCAF15 ligase. dCeMM1 can decrease the expression levels of RBM39 in WT KBM7 cells. 体外活性: dCeMM1 (0-100 µM; 3 days) inhibited cell growth with the EC50 of 3 and 8 µ M for WT and UBE2Mmut KBM7 cells, respectively.
Rbm39 glue
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Tīmeklis2024. gada 15. aug. · Targeted protein degraders: SPLAMs and RBM39: The anticancer sulfonamides chloroquinoxaline sulfonamide (CQS) (15), E7820 (16), indisulam (17) and tasisulam (18) (collectively referred to as SPLAMs, Fig. 8) are molecular glues that promote the degradation of RNA splicing factor RBM39 (CAPERa) through the action … Tīmeklis2024. gada 21. marts · RBM39 (RNA Binding Motif Protein 39) is a Protein Coding gene. Among its related pathways are Processing of Capped Intron-Containing Pre-mRNA and VEGFA-VEGFR2 signaling pathway . Gene Ontology (GO) annotations related to this gene include nucleic acid binding and RNA binding . An important paralog of this …
Tīmeklis2024. gada 1. nov. · To facilitate targeted protein degradation, molecular glues such as immunomodulatory imide drugs (IMiD, e.g., thalidomide, lenalidomide, …
Tīmeklis2024. gada 4. nov. · RBM39 RRM2 packs against an α-helix of DCAF15 and the Gly268 of RBM39, which was previously found to be a dominant position of indisulam resistance mutations 13, 14, packs against the DCAF15... Tīmeklis2016. gada 1. jūn. · Recent studies have revealed that RBM39 is the unexpected target of aryl sulphonamides, which act as molecular glues between RBM39 and the DCAF15‐associated E3 ubiquitin ligase complex leading ...
Tīmeklis2024. gada 3. aug. · Examples of molecular glues that induce proteolysis of targets include the IMiDs (immune modulatory drugs; e.g., thalidomide), which generate a novel interaction between a substrate (e.g.,...
Tīmeklis2024. gada 9. dec. · From RBM39, the interaction is mediated by a helix of the second RNA recognition motif (RRM) domain. Several differences stand out in comparison to … brookings hospital south dakotaTīmeklis2024. gada 1. sept. · DDB1 DCAF15-RBM39. Indisulam 74 and E7820 ... Schematic diagram of the action mechanism of aryl sulfonamides molecular glues. (D) DDB1-DCAF15-E7820-RBM39 co-crystal structure (DDB1 colored in blue, DCAF15 colored in cyan, RBM39 colored in green, DDA1 colored in lightblue; PDB:6Q0R). Hydrogen … care emergency facilitiesTīmeklisAlthough molecules like the ArSulfs, which interfere with splicing decisions, are exciting potential medicines, the molecular glue mechanism of RBM39 degradation introduces complex pleiotropic effects that are difficult to untangle. brookings hospital physical therapyTīmeklis2024. gada 1. jūn. · Molecular glue (MG) compounds are a type of unique small molecule that can change the protein–protein interactions (PPIs) and interactomes by degrading, stabilizing, or activating the target protein after their binging. ... The indisulam-mediated degradation of RBM39 needs the presence of a high-level … brookings india internshipTīmeklisuncovers RBM39 as a regulator of the mitotic kinesin motor proteins KIF20A and KIF20B, which likely plays a role in the antiproliferative activity of ArSulfs. Figure 1. … careem facebookTīmeklis2024. gada 17. nov. · Indisulam, a “molecular glue” that selectively recruits RBM39 to the CRL4-DCAF15 E3 ubiquitin ligase for proteasomal degradation, is highly … brookings inclusive economic growthTīmeklis2024. gada 5. nov. · molecular glue DCAF15 RBM39 E7820 indisulam PROTAC sulfonamide Introduction E7820 and indisulam ( Figure 1A) are aryl sulfonamide … brookings hotels with a pool