{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Galvan ML"],"funding":["NIH","NIAMS NIH HHS"],"pagination":["115993"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8217219"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["150"],"pubmed_abstract":["Skeletal development and bone formation are regulated by epigenetic mechanisms that either repress or enhance osteogenic commitment of mesenchymal stromal/stem cells and osteoblasts. The transcriptional suppressive trimethylation of histone 3 lysine 27 (H3K27me3) hinders differentiation of pre-committed osteoblasts. Osteoblast maturation can be stimulated by genetic loss of the H3K27 methyltransferase Ezh2 which can also be mimicked pharmacologically using the classical Ezh2 inhibitor GSK126. Identification of other Ezh2 inhibitors (iEzh2) that enhance osteogenic potential would increase chemical options for developing new bone stimulatory compounds. In this study, we examined a panel of iEzh2s and show that all eight inhibitors we tested are capable of accelerating osteoblast differentiat"],"journal":["Bone"],"pubmed_title":["Multiple pharmacological inhibitors targeting the epigenetic suppressor enhancer of zeste homolog 2 (Ezh2) accelerate osteoblast differentiation."],"pmcid":["PMC8217219"],"funding_grant_id":["R01 AR049069"],"pubmed_authors":["Khani F","Kubrova E","Jerez S","Thaler R","Galvan ML","Dudakovic A","van Wijnen AJ","Paradise CR"],"additional_accession":[]},"is_claimable":false,"name":"Multiple pharmacological inhibitors targeting the epigenetic suppressor enhancer of zeste homolog 2 (Ezh2) accelerate osteoblast differentiation.","description":"Skeletal development and bone formation are regulated by epigenetic mechanisms that either repress or enhance osteogenic commitment of mesenchymal stromal/stem cells and osteoblasts. The transcriptional suppressive trimethylation of histone 3 lysine 27 (H3K27me3) hinders differentiation of pre-committed osteoblasts. Osteoblast maturation can be stimulated by genetic loss of the H3K27 methyltransferase Ezh2 which can also be mimicked pharmacologically using the classical Ezh2 inhibitor GSK126. Identification of other Ezh2 inhibitors (iEzh2) that enhance osteogenic potential would increase chemical options for developing new bone stimulatory compounds. In this study, we examined a panel of iEzh2s and show that all eight inhibitors we tested are capable of accelerating osteoblast differentiat","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 Sep","modification":"2025-04-27T00:07:52.859Z","creation":"2025-04-06T17:49:00.423Z"},"accession":"S-EPMC8217219","cross_references":{"pubmed":["33940225"],"doi":["10.1016/j.bone.2021.115993"]}}