Relocalizing transcriptional kinases to activate apoptosis

Kinases are critical regulators of cellular function that are commonly implicated in the mechanisms underlying disease. Most drugs that target kinases are molecules that inhibit their catalytic activity, but here we used chemically induced proximity to convert kinase inhibitors into activators of th...

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Veröffentlicht in:	Science (American Association for the Advancement of Science) 2024-10, Vol.386 (6717), p.eadl5361
Hauptverfasser:	Sarott, Roman C, Gourisankar, Sai, Karim, Basel, Nettles, Sabin, Yang, Haopeng, Dwyer, Brendan G, Simanauskaite, Juste M, Tse, Jason, Abuzaid, Hind, Krokhotin, Andrey, Zhang, Tinghu, Hinshaw, Stephen M, Green, Michael R, Crabtree, Gerald R, Gray, Nathanael S
Format:	Artikel
Sprache:	eng
Schlagworte:	Ablation Animals Apoptosis Apoptosis - drug effects Bcl-6 protein Binders Biodegradation Cancer Catalytic activity Cell death Cell Line, Tumor Cell membranes Cell proliferation Chemical activity Chemical properties Cyclin-dependent kinase Cyclin-Dependent Kinase 9 - metabolism Cyclin-dependent kinases Cytotoxicity Deregulation DNA - metabolism DNA-directed RNA polymerase Drug delivery Drug development Elongated structure Enzyme inhibitors Epigenetics Gene expression Genes Germinal centers Humans Immunization Inhibitors Kinases Ligands Lymphocytes Lymphocytes B Lymphoma Lymphoma, Large B-Cell, Diffuse - genetics Lymphoma, Large B-Cell, Diffuse - metabolism Mice Mice, Inbred C57BL Mortality Pharmacology Phosphorylation Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use Proteins Proto-Oncogene Proteins c-bcl-6 - genetics Proto-Oncogene Proteins c-bcl-6 - metabolism Quorum sensing Ribonucleic acid RNA RNA polymerase RNA polymerase II RNA Polymerase II - metabolism Therapeutic applications Therapeutic targets Transcription factors Transcription, Genetic Transcriptomics Tumor cell lines
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