Entry Database : PDB / ID : 9eyv Structure visualization Downloads & linksTitle Human PRMT5 in complex with AZ compound 12 ComponentsMethylosome protein WDR77 Protein arginine N-methyltransferase 5, N-terminally processed DetailsKeywords TRANSFERASE / methyl transferase / inhibitorFunction / homology Function and homology informationFunction Domain/homology Component
positive regulation of adenylate cyclase-inhibiting dopamine receptor signaling pathway / peptidyl-arginine N-methylation / oocyte axis specification / type II protein arginine methyltransferase / protein-arginine omega-N symmetric methyltransferase activity / peptidyl-arginine methylation / Golgi ribbon formation / negative regulation of epithelial cell proliferation involved in prostate gland development / histone H4R3 methyltransferase activity / secretory columnal luminar epithelial cell differentiation involved in prostate glandular acinus development ... positive regulation of adenylate cyclase-inhibiting dopamine receptor signaling pathway / peptidyl-arginine N-methylation / oocyte axis specification / type II protein arginine methyltransferase / protein-arginine omega-N symmetric methyltransferase activity / peptidyl-arginine methylation / Golgi ribbon formation / negative regulation of epithelial cell proliferation involved in prostate gland development / histone H4R3 methyltransferase activity / secretory columnal luminar epithelial cell differentiation involved in prostate glandular acinus development / histone arginine N-methyltransferase activity / epithelial cell proliferation involved in prostate gland development / protein-arginine N-methyltransferase activity / methylosome / methyl-CpG binding / endothelial cell activation / histone H3 methyltransferase activity / positive regulation of mRNA splicing, via spliceosome / negative regulation of gene expression via chromosomal CpG island methylation / regulation of mitotic nuclear division / Cul4B-RING E3 ubiquitin ligase complex / histone methyltransferase complex / positive regulation of oligodendrocyte differentiation / histone methyltransferase activity / E-box binding / negative regulation of cell differentiation / ubiquitin-like ligase-substrate adaptor activity / ribonucleoprotein complex binding / spliceosomal snRNP assembly / regulation of ERK1 and ERK2 cascade / nuclear receptor coactivator activity / regulation of signal transduction by p53 class mediator / methyltransferase activity / liver regeneration / DNA-templated transcription termination / circadian regulation of gene expression / Regulation of TP53 Activity through Methylation / RMTs methylate histone arginines / protein polyubiquitination / transcription corepressor activity / p53 binding / snRNP Assembly / ubiquitin-dependent protein catabolic process / chromatin remodeling / protein heterodimerization activity / positive regulation of cell population proliferation / regulation of DNA-templated transcription / chromatin / regulation of transcription by RNA polymerase II / Golgi apparatus / nucleoplasm / identical protein binding / nucleus / cytosol / cytoplasm Similarity search - Function Protein arginine N-methyltransferase PRMT5 / PRMT5 arginine-N-methyltransferase / PRMT5, TIM barrel domain / PRMT5, oligomerisation domain / PRMT5 arginine-N-methyltransferase / PRMT5 TIM barrel domain / PRMT5 oligomerisation domain / Protein arginine N-methyltransferase / SAM-dependent methyltransferase PRMT-type domain profile. / WD40 repeat, conserved site ... Protein arginine N-methyltransferase PRMT5 / PRMT5 arginine-N-methyltransferase / PRMT5, TIM barrel domain / PRMT5, oligomerisation domain / PRMT5 arginine-N-methyltransferase / PRMT5 TIM barrel domain / PRMT5 oligomerisation domain / Protein arginine N-methyltransferase / SAM-dependent methyltransferase PRMT-type domain profile. / WD40 repeat, conserved site / Trp-Asp (WD) repeats signature. / Trp-Asp (WD) repeats profile. / Trp-Asp (WD) repeats circular profile. / WD domain, G-beta repeat / WD40 repeats / WD40 repeat / WD40-repeat-containing domain superfamily / WD40/YVTN repeat-like-containing domain superfamily / S-adenosyl-L-methionine-dependent methyltransferase superfamily Similarity search - Domain/homologyBiological species Homo sapiens (human)Method X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution : 2.15 Å DetailsAuthors Debreczeni, J. Funding support 1items Details Hide detailsOrganization Grant number Country Not funded
CitationJournal : J.Med.Chem. / Year : 2024Title : Discovery and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity.Authors: Smith, J.M. / Barlaam, B. / Beattie, D. / Bradshaw, L. / Chan, H.M. / Chiarparin, E. / Collingwood, O. / Cooke, S.L. / Cronin, A. / Cumming, I. / Dean, E. / Debreczeni, J.E. / Del Barco ... Authors : Smith, J.M. / Barlaam, B. / Beattie, D. / Bradshaw, L. / Chan, H.M. / Chiarparin, E. / Collingwood, O. / Cooke, S.L. / Cronin, A. / Cumming, I. / Dean, E. / Debreczeni, J.E. / Del Barco Barrantes, I. / Diene, C. / Gianni, D. / Guerot, C. / Guo, X. / Guven, S. / Hayhow, T.G. / Hong, T. / Kemmitt, P.D. / Lamont, G.M. / Lamont, S. / Lynch, J.T. / McWilliams, L. / Moore, S. / Raubo, P. / Robb, G.R. / Robinson, J. / Scott, J.S. / Srinivasan, B. / Steward, O. / Stubbs, C.J. / Syson, K. / Tan, L. / Turner, O. / Underwood, E. / Urosevic, J. / Vazquez-Chantada, M. / Whittaker, A.L. / Wilson, D.M. / Winter-Holt, J.J. History Deposition Apr 9, 2024 Deposition site : PDBE / Processing site : PDBERevision 1.0 Aug 14, 2024 Provider : repository / Type : Initial release