Tīmeklis2024. gada 9. dec. · RBM39(Gly268) also forms a periphery of the hydrophobic pocket. The phenyl-sulfonamide is positioned between several aliphatic side chains, … Tīmeklis2024. gada 13. aug. · RBM39 is indirectly involved in tumor growth and progression by regulating transcription of many tumor-related genes, protein translation, and …
Structural Basis and Kinetic Pathway of RBM39 ... - ScienceDirect
Tīmeklis2024. gada 12. maijs · One recent example of successful chemogenomic screening is the target identification of molecular glue indisulam, RBM39. Indisulam facilitates the interaction of RBM39 with the DCAF15-CUL4-CRL E3 complex, which causes RBM39 polyubiquitination and subsequent degradation [39, 40]. The increased … Tīmeklis2024. gada 1. janv. · The cullin-4 RING ligase (CRL4) substrate receptor DCAF15 is responsible for the pharmacologic degradation of the mRNA splice factor RBM39 induced by the aryl sulfonamide molecular glues indisulam ... night clubs in san jose costa rica
The Rise of Molecular Glues - ScienceDirect
Tīmeklis2024. gada 5. sept. · The structural and kinetic studies confirm aryl sulfonamides as molecular glues in the recruitment of RBM39 and provide a framework for future efforts to utilize DCAF15 to degrade other protein of ... Tīmeklis2024. gada 19. nov. · Indisulam, a “molecular glue” that selectively recruits RBM39 to the CRL4-DCAF15 E3 ubiquitin ligase for proteasomal degradation, is highly efficacious against neuroblastoma, leading to significant responses in multiple high-risk disease models, without overt toxicity. Genetic depletion or indisulam-mediated degradation … Tīmeklis2024. gada 7. janv. · Novel approaches to degrading therapeutic targets using molecular-glue degraders and PROTACs are emerging in pharmaceutical and … nightclubs in philadelphia