{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,6]],"date-time":"2026-10-06T04:40:32Z","timestamp":1791261632075,"version":"4.1.0"},"reference-count":109,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2026,7,1]],"date-time":"2026-07-01T00:00:00Z","timestamp":1782864000000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2026,7,1]],"date-time":"2026-07-01T00:00:00Z","timestamp":1782864000000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2026,7,1]],"date-time":"2026-07-01T00:00:00Z","timestamp":1782864000000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2026,7,1]],"date-time":"2026-07-01T00:00:00Z","timestamp":1782864000000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2026,7,1]],"date-time":"2026-07-01T00:00:00Z","timestamp":1782864000000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2026,7,1]],"date-time":"2026-07-01T00:00:00Z","timestamp":1782864000000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2026,7,1]],"date-time":"2026-07-01T00:00:00Z","timestamp":1782864000000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Biochemical Pharmacology"],"published-print":{"date-parts":[[2026,7]]},"DOI":"10.1016\/j.bcp.2026.117916","type":"journal-article","created":{"date-parts":[[2026,3,21]],"date-time":"2026-03-21T00:07:50Z","timestamp":1774051670000},"page":"117916","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":1,"special_numbering":"C","title":["Discovery and research progress of CDK8 inhibitors"],"prefix":"10.1016","volume":"249","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-2028-5026","authenticated-orcid":false,"given":"Menglan","family":"Zou","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kuihua","family":"Zou","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Qianbin","family":"Li","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5434-5747","authenticated-orcid":false,"given":"Zhuo","family":"Chen","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"issue":"11","key":"10.1016\/j.bcp.2026.117916_b0005","doi-asserted-by":"crossref","first-page":"1275","DOI":"10.1038\/ncb1109-1275","article-title":"Cyclin-dependent kinases: a family portrait","volume":"11","author":"Marcos","year":"2009","journal-title":"Nat. Cell Biol."},{"issue":"1","key":"10.1016\/j.bcp.2026.117916_b0010","doi-asserted-by":"crossref","first-page":"17","DOI":"10.1158\/0008-5472.CAN-23-0650","article-title":"Targeting transcriptional regulation with a CDK9 inhibitor suppresses growth of endocrine- and palbociclib-resistant ER+ breast cancers","volume":"84","author":"Arany","year":"2024","journal-title":"Cancer Res."},{"issue":"14","key":"10.1016\/j.bcp.2026.117916_b0015","doi-asserted-by":"crossref","first-page":"7288","DOI":"10.1093\/nar\/gkad538","article-title":"CDK8\/19: positive regulators of signal-induced transcription and negative regulators of mediator complex proteins","volume":"51","author":"Mengqian","year":"2023","journal-title":"Nucleic Acids Res."},{"issue":"2","key":"10.1016\/j.bcp.2026.117916_b0020","doi-asserted-by":"crossref","first-page":"194","DOI":"10.1038\/nsmb.1752","article-title":"CDK8 is a positive regulator of transcriptional elongation within the serum response network","volume":"17","author":"Donner Aaron","year":"2010","journal-title":"Nat. Struct. Mol. Biol."},{"issue":"3","key":"10.1016\/j.bcp.2026.117916_b0025","doi-asserted-by":"crossref","first-page":"275","DOI":"10.1016\/S0092-8674(02)00741-9","article-title":"The conformational plasticity of protein kinases","volume":"109","author":"Morgan","year":"2002","journal-title":"Cell"},{"key":"10.1016\/j.bcp.2026.117916_b0030","article-title":"Binding patterns and structure-activity relationship of CDK8 inhibitors","volume":"96","author":"Duo","year":"2020","journal-title":"Bioorg. Chem."},{"issue":"20","key":"10.1016\/j.bcp.2026.117916_b0035","doi-asserted-by":"crossref","first-page":"8081","DOI":"10.1073\/pnas.1305378110","article-title":"Structure-kinetic relationship study of CDK8\/CycC specific compounds","volume":"110","author":"Schneider","year":"2013","journal-title":"Proc. Natl. Acad. Sci. USA"},{"issue":"6","key":"10.1016\/j.bcp.2026.117916_b0040","doi-asserted-by":"crossref","first-page":"595","DOI":"10.1021\/acsmedchemlett.6b00044","article-title":"Design and development of a series of potent and selective type II inhibitors of CDK8","volume":"7","author":"Philippe","year":"2016","journal-title":"ACS Med. Chem. Lett."},{"issue":"12","key":"10.1016\/j.bcp.2026.117916_b0045","doi-asserted-by":"crossref","first-page":"1208","DOI":"10.1111\/j.1365-2443.2011.01565.x","article-title":"Identification of target genes for the CDK subunits of the mediator complex","volume":"16","author":"Taiki","year":"2011","journal-title":"Genes Cells"},{"issue":"3","key":"10.1016\/j.bcp.2026.117916_b0050","doi-asserted-by":"crossref","first-page":"155","DOI":"10.1038\/nrm3951","article-title":"The mediator complex: a central integrator of transcription","volume":"16","author":"Allen Benjamin","year":"2015","journal-title":"Nat. Rev. Mol. Cell Biol."},{"issue":"43","key":"10.1016\/j.bcp.2026.117916_b0055","doi-asserted-by":"crossref","first-page":"15788","DOI":"10.1073\/pnas.0607483103","article-title":"The cyclin-dependent kinase 8 module sterically blocks mediator interactions with RNA polymerase II","volume":"103","author":"Hans","year":"2006","journal-title":"PNAS"},{"key":"10.1016\/j.bcp.2026.117916_b0060","article-title":"The Cdk8 kinase module regulates interaction of the mediator complex with RNA polymerase II","volume":"296","author":"Sara","year":"2021","journal-title":"J. Biol. Chem."},{"issue":"6800","key":"10.1016\/j.bcp.2026.117916_b0065","doi-asserted-by":"crossref","first-page":"102","DOI":"10.1038\/35024111","article-title":"TFIIH is negatively regulated by cdk8-containing mediator complexes","volume":"407","author":"Akoulitchev","year":"2000","journal-title":"Nature"},{"issue":"1","key":"10.1016\/j.bcp.2026.117916_b0070","doi-asserted-by":"crossref","first-page":"40","DOI":"10.1186\/s43556-023-00151-1","article-title":"JAK-STAT signaling in inflammation and stress-related diseases: implications for therapeutic interventions","volume":"4","author":"Alexey","year":"2023","journal-title":"Mol. Biomed."},{"issue":"2","key":"10.1016\/j.bcp.2026.117916_b0075","doi-asserted-by":"crossref","first-page":"250","DOI":"10.1016\/j.immuni.2012.10.017","article-title":"CDK8 kinase phosphorylates transcription factor STAT1 to selectively regulate the interferon response","volume":"38","author":"Joanna","year":"2013","journal-title":"Immunity"},{"issue":"3","key":"10.1016\/j.bcp.2026.117916_b0080","doi-asserted-by":"crossref","first-page":"437","DOI":"10.1016\/j.celrep.2013.07.012","article-title":"CDK8-mediated STAT1-S727 phosphorylation restrains NK cell cytotoxicity and tumor surveillance","volume":"4","author":"Maria","year":"2013","journal-title":"Cell Rep."},{"issue":"9","key":"10.1016\/j.bcp.2026.117916_b0085","article-title":"STAT1-S727 - the license to kill","volume":"3","author":"Putz Eva","year":"2014","journal-title":"Oncoimmunology"},{"issue":"12","key":"10.1016\/j.bcp.2026.117916_b0090","article-title":"CDK8 fine-tunes IL-6 transcriptional activities by limiting STAT3 resident time at the gene loci","volume":"33","author":"Jonathan","year":"2020","journal-title":"Cell Rep."},{"issue":"4","key":"10.1016\/j.bcp.2026.117916_b0095","doi-asserted-by":"crossref","first-page":"757","DOI":"10.1016\/j.cell.2009.09.035","article-title":"Nuclear CDKs drive smad transcriptional activation and turnover in BMP and TGF-beta pathways","volume":"139","author":"Claudio","year":"2009","journal-title":"Cell"},{"issue":"12","key":"10.1016\/j.bcp.2026.117916_b0100","doi-asserted-by":"crossref","first-page":"1275","DOI":"10.1101\/gad.2060811","article-title":"A smad action turnover switch operated by WW domain readers of a phosphoserine code","volume":"25","author":"Eric","year":"2011","journal-title":"Genes Dev."},{"issue":"7212","key":"10.1016\/j.bcp.2026.117916_b0105","doi-asserted-by":"crossref","first-page":"547","DOI":"10.1038\/nature07179","article-title":"CDK8 is a colorectal cancer oncogene that regulates beta-catenin activity","volume":"455","author":"Ron","year":"2008","journal-title":"Nature"},{"issue":"12","key":"10.1016\/j.bcp.2026.117916_b0110","doi-asserted-by":"crossref","first-page":"2863","DOI":"10.1002\/ijc.24908","article-title":"CDK8 expression in 470 colorectal cancers in relation to beta-catenin activation, other molecular alterations and patient survival","volume":"126","author":"Ron","year":"2010","journal-title":"Int. J. Cancer"},{"issue":"7212","key":"10.1016\/j.bcp.2026.117916_b0115","doi-asserted-by":"crossref","first-page":"552","DOI":"10.1038\/nature07310","article-title":"E2F1 represses beta-catenin transcription and is antagonized by both pRB and CDK8","volume":"455","author":"Morris Erick","year":"2008","journal-title":"Nature"},{"issue":"30","key":"10.1016\/j.bcp.2026.117916_b0120","doi-asserted-by":"crossref","first-page":"3520","DOI":"10.1038\/onc.2012.364","article-title":"CDK8 regulates E2F1 transcriptional activity through S375 phosphorylation","volume":"32","author":"Zhao","year":"2013","journal-title":"Oncogene"},{"key":"10.1016\/j.bcp.2026.117916_b0125","doi-asserted-by":"crossref","unstructured":"B. Zhou, W. Lin, Y. Long, et al. Notch Signaling Pathway: Architecture, Disease, and Therapeutics. Signal transduction and targeted therapy, 2022, 7(1).","DOI":"10.1038\/s41392-022-00934-y"},{"issue":"4","key":"10.1016\/j.bcp.2026.117916_b0130","doi-asserted-by":"crossref","first-page":"509","DOI":"10.1016\/j.molcel.2004.10.014","article-title":"Mastermind recruits CycC:CDK8 to phosphorylate the notch ICD and coordinate activation with turnover","volume":"16","author":"Fryer Christy","year":"2004","journal-title":"Mol. Cell"},{"issue":"3\u20134","key":"10.1016\/j.bcp.2026.117916_b0135","doi-asserted-by":"crossref","first-page":"300","DOI":"10.1016\/j.bbrc.2011.11.030","article-title":"Ubiquitination of Notch1 is regulated by MAML1-mediated P300 acetylation of Notch1","volume":"416","author":"Popko-Scibor Anita","year":"2011","journal-title":"Biochem. Biophys. Res. Commun."},{"issue":"7","key":"10.1016\/j.bcp.2026.117916_b0140","doi-asserted-by":"crossref","first-page":"2417","DOI":"10.1172\/JCI61462","article-title":"Regulation of lipogenesis by cyclin-dependent kinase 8-mediated control of SREBP-1","volume":"122","author":"Xiaoping","year":"2012","journal-title":"J. Clin. Invest."},{"issue":"2","key":"10.1016\/j.bcp.2026.117916_b0145","doi-asserted-by":"crossref","first-page":"62","DOI":"10.1016\/j.ydbio.2018.10.001","article-title":"CDK8 mediates the dietary effects on developmental transition in Drosophila","volume":"444","author":"Xinsheng","year":"2018","journal-title":"Dev. Biol."},{"issue":"11","key":"10.1016\/j.bcp.2026.117916_b0150","article-title":"Cdk8 attenuates lipogenesis by inhibiting SREBP-dependent transcription in Drosophila","volume":"15","author":"Xiao","year":"2022","journal-title":"Dis. Model. Mech."},{"issue":"11","key":"10.1016\/j.bcp.2026.117916_b0155","doi-asserted-by":"crossref","first-page":"2892","DOI":"10.1016\/j.celrep.2019.08.025","article-title":"CDK8 regulates insulin secretion and mediates postnatal and stress-induced expression of neuropeptides in pancreatic \u03b2 cells","volume":"28","author":"Jing","year":"2019","journal-title":"Cell Rep."},{"key":"10.1016\/j.bcp.2026.117916_b0160","doi-asserted-by":"crossref","first-page":"6641","DOI":"10.1038\/ncomms7641","article-title":"Skp2-macroH2A1-CDK8 axis orchestrates G2\/M transition and tumorigenesis","volume":"6","author":"Dazhi","year":"2015","journal-title":"Nat. Commun."},{"key":"10.1016\/j.bcp.2026.117916_b0165","article-title":"Angel or Devil\u00a0? - CDK8 as the new drug target","volume":"213","author":"Dan","year":"2021","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bcp.2026.117916_b0170","article-title":"Unveiling the impact of CDK8 on tumor progression: mechanisms and therapeutic strategies","volume":"15","author":"Xiaomin","year":"2024","journal-title":"Front. Pharmacol."},{"issue":"10","key":"10.1016\/j.bcp.2026.117916_b0175","doi-asserted-by":"crossref","first-page":"7334","DOI":"10.1021\/acs.jmedchem.2c00356","article-title":"Discovery and anti-inflammatory activity evaluation of a novel CDK8 inhibitor through upregulation of IL-10 for the treatment of inflammatory bowel disease in vivo","volume":"65","author":"Yaoyao","year":"2022","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bcp.2026.117916_b0180","article-title":"A novel CDK8 inhibitor with poly-substituted pyridine core: discovery and anti-inflammatory activity evaluation in vivo","volume":"133","author":"Xing","year":"2023","journal-title":"Bioorg. Chem."},{"key":"10.1016\/j.bcp.2026.117916_b0185","article-title":"The discovery of a novel pyrrolo[2,3-b]pyridine as a selective CDK8 Inhibitor offers a new approach against psoriasis","volume":"175","author":"Yao","year":"2024","journal-title":"Biomed. Pharmacother."},{"key":"10.1016\/j.bcp.2026.117916_b0190","article-title":"Design, synthesis, and biological evaluation of indolin-2-one derivatives as novel cyclin-dependent protein kinase 8 (CDK8) inhibitors","volume":"159","author":"Yi","year":"2023","journal-title":"Biomed. Pharmacother."},{"issue":"1","key":"10.1016\/j.bcp.2026.117916_b0195","doi-asserted-by":"crossref","first-page":"378","DOI":"10.1021\/acs.jcim.4c02011","article-title":"Identification of a potent CDK8 inhibitor using structure-based virtual screening","volume":"65","author":"Eight","year":"2025","journal-title":"J. Chem. Inf. Model."},{"key":"10.1016\/j.bcp.2026.117916_b0200","article-title":"Structural optimization and biological evaluation of indolin-2-one derivatives as novel CDK8 inhibitors for idiopathic pulmonary fibrosis","volume":"184","author":"Yi","year":"2025","journal-title":"Biomed. Pharmacother."},{"key":"10.1016\/j.bcp.2026.117916_b0205","article-title":"Identification of pyrazole scaffold inhibitors targeting cyclin-dependent kinase 8 for .s. in pulmonary fibrosis","volume":"237","author":"Eight","year":"2025","journal-title":"Biochem. Pharmacol."},{"issue":"1","key":"10.1016\/j.bcp.2026.117916_b0210","first-page":"285","article-title":"Role of CDK8 and beta-catenin in colorectal adenocarcinoma","volume":"24","author":"Og","year":"2010","journal-title":"Oncol. Rep."},{"key":"10.1016\/j.bcp.2026.117916_b0215","doi-asserted-by":"crossref","first-page":"2233","DOI":"10.2147\/IJGM.S349576","article-title":"CDK3, CDK5 and CDK8 proteins as prognostic and potential biomarkers in colorectal cancer patients","volume":"15","author":"Dan","year":"2022","journal-title":"Int. J. General Med."},{"issue":"1","key":"10.1016\/j.bcp.2026.117916_b0220","doi-asserted-by":"crossref","first-page":"109","DOI":"10.1186\/1756-9966-30-109","article-title":"Effects of cyclin-dependent kinase 8 specific siRNA on the proliferation and apoptosis of colon cancer cells","volume":"30","author":"Bing","year":"2011","journal-title":"J. Exp. Clin. Cancer Res.: CR"},{"issue":"5","key":"10.1016\/j.bcp.2026.117916_b0225","first-page":"2088","article-title":"Tumor-suppressive microRNA-195-5p regulates cell growth and inhibits cell cycle by targeting cyclin dependent kinase 8 in colon cancer","volume":"8","author":"Qifeng","year":"2016","journal-title":"Am. J. Transl. Res."},{"key":"10.1016\/j.bcp.2026.117916_b0230","doi-asserted-by":"crossref","first-page":"153","DOI":"10.1016\/j.biopha.2015.08.015","article-title":"Downregulation of CDK-8 inhibits colon cancer hepatic metastasis by regulating Wnt\/\u03b2-Catenin pathway","volume":"74","author":"Song","year":"2015","journal-title":"Biomed. Pharmacother."},{"issue":"23","key":"10.1016\/j.bcp.2026.117916_b0235","doi-asserted-by":"crossref","first-page":"6594","DOI":"10.1158\/0008-5472.CAN-18-1583","article-title":"CDK8 selectively promotes the growth of colon cancer metastases in the liver by regulating gene expression of TIMP3 and matrix metalloproteinases","volume":"78","author":"Jiaxin","year":"2018","journal-title":"Cancer Res."},{"issue":"1","key":"10.1016\/j.bcp.2026.117916_b0240","first-page":"32","article-title":"MiRNA-107 inhibits proliferation and migration by targeting CDK8 in breast cancer","volume":"7","author":"Li Xiao","year":"2014","journal-title":"Int. J. Clin. Exp. Med."},{"issue":"6","key":"10.1016\/j.bcp.2026.117916_b0245","doi-asserted-by":"crossref","first-page":"8095","DOI":"10.18632\/aging.202595","article-title":"Expression and prognostic value of transcription-associated cyclin-dependent kinases in human breast cancer","volume":"13","author":"Ning","year":"2021","journal-title":"Aging"},{"issue":"8","key":"10.1016\/j.bcp.2026.117916_b0250","doi-asserted-by":"crossref","first-page":"12558","DOI":"10.18632\/oncotarget.14894","article-title":"Inhibition of CDK8 mediator kinase suppresses Estrogen dependent transcription and the growth of Estrogen receptor positive breast cancer","volume":"8","author":"McDermott Martina","year":"2017","journal-title":"Oncotarget"},{"issue":"7","key":"10.1016\/j.bcp.2026.117916_b0255","doi-asserted-by":"crossref","first-page":"1829","DOI":"10.1158\/1078-0432.CCR-16-0094","article-title":"Pan-cancer analysis of the mediator complex transcriptome identifies CDK19 and CDK8 as therapeutic targets in advanced prostate cancer","volume":"23","author":"Johannes","year":"2017","journal-title":"Clin. Cancer Res."},{"issue":"17","key":"10.1016\/j.bcp.2026.117916_b0260","doi-asserted-by":"crossref","first-page":"13474","DOI":"10.18632\/oncotarget.24414","article-title":"CDK8\/19 inhibition induces premature G1\/S transition and ATR-dependent cell death in prostate cancer cells","volume":"9","author":"Akito","year":"2018","journal-title":"Oncotarget"},{"issue":"5","key":"10.1016\/j.bcp.2026.117916_b0265","doi-asserted-by":"crossref","first-page":"813","DOI":"10.1016\/j.ajpath.2022.01.010","article-title":"Inhibition of cyclin-dependent kinase 8\/cyclin-dependent kinase 19 suppresses its pro-oncogenic effects in prostate cancer","volume":"192","author":"Anne","year":"2022","journal-title":"Am. J. Pathol."},{"issue":"4","key":"10.1016\/j.bcp.2026.117916_b0270","doi-asserted-by":"crossref","first-page":"1845","DOI":"10.3892\/mmr.2014.2482","article-title":"MacroH2A suppresses the proliferation of the B16 melanoma cell line","volume":"10","author":"Shaorong","year":"2014","journal-title":"Mol. Med. Rep."},{"issue":"7327","key":"10.1016\/j.bcp.2026.117916_b0275","doi-asserted-by":"crossref","first-page":"1105","DOI":"10.1038\/nature09590","article-title":"The histone variant macroH2A suppresses melanoma progression through regulation of CDK8","volume":"468","author":"Avnish","year":"2010","journal-title":"Nature"},{"issue":"9","key":"10.1016\/j.bcp.2026.117916_b0280","first-page":"711","article-title":"LncRNA HCP5 regulates pancreatic cancer progression by miR-140-5p\/CDK8 Axis","volume":"35","author":"Bo","year":"2020","journal-title":"Cancer Biother. Radiopharm."},{"issue":"2","key":"10.1016\/j.bcp.2026.117916_b0285","doi-asserted-by":"crossref","first-page":"304","DOI":"10.1016\/j.yexcr.2018.05.033","article-title":"CDK8 regulates the angiogenesis of pancreatic cancer cells in part via the CDK8-\u03b2-catenin-KLF2 signal axis","volume":"369","author":"Ran","year":"2018","journal-title":"Exp. Cell Res."},{"issue":"2 Pt B","key":"10.1016\/j.bcp.2026.117916_b0290","first-page":"613","article-title":"Mutated K-Ras activates CDK8 to stimulate the epithelial-to-mesenchymal transition in pancreatic cancer in part via the Wnt\/\u03b2-catenin signaling pathway","volume":"356","author":"Wei","year":"2015","journal-title":"Cancer Lett."},{"key":"10.1016\/j.bcp.2026.117916_b0295","doi-asserted-by":"crossref","first-page":"195","DOI":"10.1186\/s12935-018-0694-9","article-title":"MicroRNA-770 affects proliferation and cell cycle transition by directly targeting CDK8 in glioma","volume":"18","author":"Feng","year":"2018","journal-title":"Cancer Cell Int."},{"issue":"15","key":"10.1016\/j.bcp.2026.117916_b0300","doi-asserted-by":"crossref","first-page":"2803","DOI":"10.1038\/s41388-021-01745-1","article-title":"CDK8 maintains stemness and tumorigenicity of glioma stem cells by regulating the C-MYC pathway","volume":"40","author":"Kazuya","year":"2021","journal-title":"Oncogene"},{"issue":"4","key":"10.1016\/j.bcp.2026.117916_b0305","doi-asserted-by":"crossref","first-page":"3043","DOI":"10.1007\/s11033-012-2378-1","article-title":"Leukemogenesis as a New approach to investigate the correlation between up regulated gene 4\/upregulator of cell proliferation (URG4\/URGCP) and Signal transduction genes in Leukemia","volume":"40","author":"Yavuz","year":"2013","journal-title":"Mol. Biol. Rep."},{"key":"10.1016\/j.bcp.2026.117916_b0310","doi-asserted-by":"crossref","first-page":"112","DOI":"10.1016\/j.ebiom.2017.11.013","article-title":"Mediator kinase phosphorylation of STAT1 S727 promotes growth of neoplasms with JAK-STAT activation","volume":"26","author":"Nitulescu Ioana","year":"2017","journal-title":"EBioMedicine"},{"issue":"7572","key":"10.1016\/j.bcp.2026.117916_b0315","doi-asserted-by":"crossref","first-page":"273","DOI":"10.1038\/nature14904","article-title":"Mediator kinase inhibition further activates super-enhancer-associated genes in AML","volume":"526","author":"Pelish Henry","year":"2015","journal-title":"Nature"},{"issue":"8","key":"10.1016\/j.bcp.2026.117916_b0320","doi-asserted-by":"crossref","first-page":"821","DOI":"10.3390\/cells8080821","article-title":"Identifying cancers impacted by CDK8\/19","volume":"8","author":"Roninson Igor","year":"2019","journal-title":"Cells"},{"issue":"38","key":"10.1016\/j.bcp.2026.117916_b0325","doi-asserted-by":"crossref","first-page":"10208","DOI":"10.1073\/pnas.1710467114","article-title":"CDK8\/19 mediator kinases potentiate induction of transcription by NF\u03baB","volume":"114","author":"Mengqian","year":"2017","journal-title":"PNAS"},{"issue":"3","key":"10.1016\/j.bcp.2026.117916_b0330","doi-asserted-by":"crossref","first-page":"265","DOI":"10.1111\/gtc.12475","article-title":"Mediator cyclin-dependent kinases upregulate transcription of inflammatory genes in cooperation with NF-\u03baB and C\/EBP\u03b2 on stimulation of toll-like receptor 9","volume":"22","author":"Seiji","year":"2017","journal-title":"Genes Cells"},{"issue":"2","key":"10.1016\/j.bcp.2026.117916_b0335","doi-asserted-by":"crossref","first-page":"685","DOI":"10.7150\/ijbs.105826","article-title":"The cyclin-dependent kinase 8 inhibitor E966-0530-45418 attenuates pulmonary fibrosis in vitro and in vivo","volume":"21","author":"Hsuan","year":"2025","journal-title":"Int. J. Biol. Sci."},{"issue":"4","key":"10.1016\/j.bcp.2026.117916_b0340","doi-asserted-by":"crossref","first-page":"1018","DOI":"10.1158\/1535-7163.MCT-19-0789","article-title":"Selective and potent CDK8\/19 inhibitors enhance NK-cell activity and promote tumor surveillance","volume":"19","author":"Hofmann Marco","year":"2020","journal-title":"Mol. Cancer Ther."},{"issue":"6","key":"10.1016\/j.bcp.2026.117916_b0345","doi-asserted-by":"crossref","first-page":"1292","DOI":"10.3390\/v15061292","article-title":"Inhibition of cyclin-dependent kinases 8\/19 restricts bacterial and virus-induced inflammatory responses in monocytes","volume":"15","author":"Kokinos Elena","year":"2023","journal-title":"Viruses"},{"issue":"40","key":"10.1016\/j.bcp.2026.117916_b0350","article-title":"Conversion of antigen-specific effector\/memory T Cells into Foxp3-expressing treg cells by inhibition of CDK8\/19","volume":"4","author":"Masahiko","year":"2019","journal-title":"Sci. Immunol."},{"key":"10.1016\/j.bcp.2026.117916_b0355","article-title":"CDK8\/19 inhibitor enhances arginase-1 expression in macrophages via STAT6 and P38 MAPK activation","volume":"979","author":"Natsumi","year":"2024","journal-title":"Eur. J. Pharmacol."},{"issue":"7","key":"10.1016\/j.bcp.2026.117916_b0360","doi-asserted-by":"crossref","first-page":"1576","DOI":"10.1016\/j.stemcr.2022.06.001","article-title":"The role of CDK8 in mesenchymal stem cells in controlling osteoclastogenesis and bone homeostasis","volume":"17","author":"Takanori","year":"2022","journal-title":"Stem Cell Rep."},{"issue":"9","key":"10.1016\/j.bcp.2026.117916_b0365","doi-asserted-by":"crossref","DOI":"10.1002\/jcp.28321","article-title":"Cyclin-Dependent kinase 8\/19 inhibition suppresses osteoclastogenesis by downregulating RANK and promotes osteoblast mineralization and cancellous bone healing","volume":"234","author":"Amirhosseini","year":"2019","journal-title":"J. Cell. Physiol."},{"issue":"6","key":"10.1016\/j.bcp.2026.117916_b0370","doi-asserted-by":"crossref","first-page":"540","DOI":"10.1021\/acsmedchemlett.8b00011","article-title":"Development of highly potent and selective steroidal inhibitors and degraders of CDK8","volume":"9","author":"Hatcher","year":"2018","journal-title":"ACS Med. Chem. Lett."},{"key":"10.1016\/j.bcp.2026.117916_b0375","doi-asserted-by":"crossref","first-page":"36","DOI":"10.1016\/j.tox.2013.07.013","article-title":"Wogonin induced G1 cell cycle arrest by regulating Wnt\/\u03b2-Catenin signaling pathway and inactivating CDK8 in human colorectal cancer carcinoma cells","volume":"312","author":"He Licheng","year":"2013","journal-title":"Toxicology"},{"issue":"11","key":"10.1016\/j.bcp.2026.117916_b0380","doi-asserted-by":"crossref","first-page":"3140","DOI":"10.1021\/acs.jnatprod.9b00720","article-title":"Antitumor activity of vanicoside B isolated from persicaria dissitiflora by targeting CDK8 in triple-negative breast cancer cells","volume":"82","author":"Donghwa","year":"2019","journal-title":"J. Nat. Prod."},{"issue":"3","key":"10.1016\/j.bcp.2026.117916_b0385","doi-asserted-by":"crossref","first-page":"1078","DOI":"10.1021\/acs.jmedchem.5b01685","article-title":"Discovery of potent, selective, and orally bioavailable small-molecule modulators of the mediator complex-associated kinases CDK8\/19","volume":"59","author":"Aur\u00e9lie","year":"2016","journal-title":"J. Med. Chem."},{"issue":"12","key":"10.1016\/j.bcp.2026.117916_b0390","doi-asserted-by":"crossref","first-page":"973","DOI":"10.1038\/nchembio.1952","article-title":"A selective chemical probe for exploring the role of CDK8\/19 in human disease","volume":"11","author":"Trevor","year":"2015","journal-title":"Nat. Chem. Biol."},{"issue":"6","key":"10.1016\/j.bcp.2026.117916_b0395","doi-asserted-by":"crossref","DOI":"10.1021\/acsmedchemlett.6b00022","article-title":"2,8-disubstituted-1,6-naphthyridines and 4,6-disubstituted-isoquinolines with potent, selective affinity for CDK8\/19","volume":"7","author":"Mallinger","year":"2016","journal-title":"ACS Med. Chem. Lett."},{"key":"10.1016\/j.bcp.2026.117916_b0400","article-title":"Potent and orally bioavailable CDK8 inhibitors: design, synthesis, structure-activity relationship analysis and biological evaluation","volume":"214","author":"Mingfeng","year":"2021","journal-title":"Eur. J. Med. Chem."},{"issue":"7","key":"10.1016\/j.bcp.2026.117916_b0405","doi-asserted-by":"crossref","first-page":"4932","DOI":"10.1021\/acs.jmedchem.2c02045","article-title":"Discovery of LL-K8-22: a selective, durable, and small-molecule degrader of the CDK8-Cyclin C complex","volume":"66","author":"Mingyu","year":"2023","journal-title":"J. Med. Chem."},{"issue":"20","key":"10.1016\/j.bcp.2026.117916_b0410","doi-asserted-by":"crossref","first-page":"9337","DOI":"10.1021\/acs.jmedchem.6b00597","article-title":"Structure-based optimization of potent, selective, and orally bioavailable CDK8 inhibitors discovered by high-throughput screening","volume":"59","author":"Paul","year":"2016","journal-title":"J. Med. Chem."},{"issue":"11","key":"10.1016\/j.bcp.2026.117916_b0415","doi-asserted-by":"crossref","first-page":"1689","DOI":"10.1021\/acsmedchemlett.1c00300","article-title":"Development of highly potent and selective pyrazolopyridine inhibitor of CDK8\/19","volume":"12","author":"Hatcher John","year":"2021","journal-title":"ACS Med. Chem. Lett."},{"issue":"34","key":"10.1016\/j.bcp.2026.117916_b0420","doi-asserted-by":"crossref","first-page":"13799","DOI":"10.1073\/pnas.1206906109","article-title":"Cyclin-dependent kinase 8 mediates chemotherapy-induced tumor-promoting paracrine activities","volume":"109","author":"Porter","year":"2012","journal-title":"Proc. Natl. Acad. Sci. USA"},{"issue":"20","key":"10.1016\/j.bcp.2026.117916_b0425","doi-asserted-by":"crossref","first-page":"33779","DOI":"10.18632\/oncotarget.16810","article-title":"SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains","volume":"8","author":"Tomasz","year":"2017","journal-title":"Oncotarget"},{"issue":"10","key":"10.1016\/j.bcp.2026.117916_b0430","doi-asserted-by":"crossref","first-page":"8161","DOI":"10.1021\/acs.jmedchem.4c00248","article-title":"Discovery of a novel and potent cyclin-dependent kinase 8\/19 (CDK8\/19) inhibitor for the treatment of cancer","volume":"67","author":"Jianyu","year":"2024","journal-title":"J. Med. Chem."},{"issue":"19","key":"10.1016\/j.bcp.2026.117916_b0435","doi-asserted-by":"crossref","first-page":"7099","DOI":"10.1158\/0008-5472.CAN-04-1443","article-title":"43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF\/MEK\/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis","volume":"64","author":"Wilhelm Scott","year":"2004","journal-title":"Cancer Res."},{"key":"10.1016\/j.bcp.2026.117916_b0440","article-title":"Pyrido[2,3-b][1,5]benzoxazepin-5(6H)-one derivatives as CDK8 inhibitors","volume":"201","author":"Sonia","year":"2020","journal-title":"Eur. J. Med. Chem."},{"issue":"19","key":"10.1016\/j.bcp.2026.117916_b0445","doi-asserted-by":"crossref","first-page":"13216","DOI":"10.1021\/acs.jmedchem.2c01042","article-title":"Design and synthesis of a 2-amino-pyridine derivative as a potent CDK8 inhibitor for anti-colorectal cancer therapy","volume":"65","author":"Yao","year":"2022","journal-title":"J. Med. Chem."},{"issue":"3","key":"10.1016\/j.bcp.2026.117916_b0450","doi-asserted-by":"crossref","first-page":"669","DOI":"10.1248\/bpb.b23-00834","article-title":"Osteoblastgenic and osteogenic effects of KY-273 with CDK8\/19 inhibitory activity in bone marrow mesenchymal stem cells and female rats","volume":"47","author":"Megumi","year":"2024","journal-title":"Biol. Pharm. Bull."},{"issue":"17","key":"10.1016\/j.bcp.2026.117916_b0455","doi-asserted-by":"crossref","first-page":"6355","DOI":"10.1080\/07391102.2020.1797537","article-title":"Molecular modeling studies of novel naphthyridine and isoquinoline derivatives as CDK8 inhibitors","volume":"39","author":"Qunlin","year":"2021","journal-title":"J. Biomol. Struct. Dyn."},{"key":"10.1016\/j.bcp.2026.117916_b0460","article-title":"Discovery of a potent, highly selective, and orally bioavailable inhibitor of CDK8 through a structure-based optimisation","volume":"218","author":"Mingfeng","year":"2021","journal-title":"Eur. J. Med. Chem."},{"issue":"8","key":"10.1016\/j.bcp.2026.117916_b0465","doi-asserted-by":"crossref","first-page":"2336","DOI":"10.1016\/j.bmc.2017.02.038","article-title":"Design and synthesis of selective CDK8\/19 dual inhibitors: discovery of 4,5-dihydrothieno[3\u2019,4\u2019:3,4]benzo[1,2-d]isothiazole derivatives","volume":"25","author":"Koji","year":"2017","journal-title":"Bioorg. Med. Chem."},{"issue":"10","key":"10.1016\/j.bcp.2026.117916_b0470","doi-asserted-by":"crossref","first-page":"1102","DOI":"10.1038\/nchembio.2458","article-title":"Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells","volume":"13","author":"Liv","year":"2017","journal-title":"Nat. Chem. Biol."},{"issue":"4","key":"10.1016\/j.bcp.2026.117916_b0475","doi-asserted-by":"crossref","first-page":"1717","DOI":"10.1021\/jm501436m","article-title":"Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen","volume":"58","author":"Aur\u00e9lie","year":"2015","journal-title":"J. Med. Chem."},{"issue":"10","key":"10.1016\/j.bcp.2026.117916_b0480","doi-asserted-by":"crossref","first-page":"1208","DOI":"10.3390\/cells8101208","article-title":"Characterizing CDK8\/19 inhibitors through a NF\u03baB-dependent cell-based assay","volume":"8","author":"Jing","year":"2019","journal-title":"Cells"},{"issue":"18","key":"10.1016\/j.bcp.2026.117916_b0485","doi-asserted-by":"crossref","first-page":"4488","DOI":"10.1016\/j.bmcl.2017.07.080","article-title":"Discovery of potent and selective CDK8 inhibitors through FBDD approach","volume":"27","author":"Xingchun","year":"2017","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"1","key":"10.1016\/j.bcp.2026.117916_b0490","doi-asserted-by":"crossref","first-page":"4741","DOI":"10.1038\/s41467-019-12656-x","article-title":"A kinase-independent role for CDK8 in BCR-ABL1+ Leukemia","volume":"10","author":"Ingeborg","year":"2019","journal-title":"Nat. Commun."},{"issue":"8","key":"10.1016\/j.bcp.2026.117916_b0495","doi-asserted-by":"crossref","first-page":"14095","DOI":"10.1002\/jcb.28685","article-title":"The microRNA-141-3p\/ CDK8 pathway regulates the chemosensitivity of breast cancer cells to trastuzumab","volume":"120","author":"Song Wenqing","year":"2019","journal-title":"J. Cell. Biochem."},{"issue":"32","key":"10.1016\/j.bcp.2026.117916_b0500","article-title":"Inhibition of CDK8\/19 mediator kinase potentiates HER2-targeting drugs and bypasses resistance to these agents in vitro and in vivo","volume":"119","author":"Xiaokai","year":"2022","journal-title":"Proc. Natl. Acad. Sci. USA"},{"issue":"2","key":"10.1016\/j.bcp.2026.117916_b0505","doi-asserted-by":"crossref","first-page":"285","DOI":"10.1158\/0008-5472.CAN-21-4309","article-title":"Transcriptional antagonism by CDK8 inhibition improves therapeutic efficacy of MEK inhibitors","volume":"83","author":"Malone Clare","year":"2023","journal-title":"Cancer Res."},{"issue":"1","key":"10.1016\/j.bcp.2026.117916_b0510","doi-asserted-by":"crossref","first-page":"144","DOI":"10.3390\/cells10010144","article-title":"The inhibition of CDK8\/19 mediator kinases prevents the development of resistance to EGFR-targeting drugs","volume":"10","author":"Sharko Amanda","year":"2021","journal-title":"Cells"},{"issue":"4","key":"10.1016\/j.bcp.2026.117916_b0515","doi-asserted-by":"crossref","first-page":"549","DOI":"10.1016\/j.bmcl.2018.12.065","article-title":"Shape-based virtual screen for the discovery of novel CDK8 inhibitor chemotypes","volume":"29","author":"Jun","year":"2019","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"10.1016\/j.bcp.2026.117916_b0520","article-title":"Identification of 3, 4-disubstituted pyridine derivatives as novel CDK8 inhibitors","volume":"223","author":"Haochao","year":"2021","journal-title":"Eur. J. Med. Chem."},{"issue":"18","key":"10.1016\/j.bcp.2026.117916_b0525","doi-asserted-by":"crossref","first-page":"12095","DOI":"10.1021\/acs.jmedchem.2c00820","article-title":"Discovery of the novel 1H-pyrrolo[2,3-b]pyridine derivative as a potent type II CDK8 inhibitor against colorectal cancer","volume":"65","author":"Xing","year":"2022","journal-title":"J. Med. Chem."},{"issue":"6","key":"10.1016\/j.bcp.2026.117916_b0530","doi-asserted-by":"crossref","first-page":"e5007","DOI":"10.1002\/pro.5007","article-title":"An ensemble machine learning model generates a focused screening library for the identification of CDK8 inhibitors","volume":"33","author":"Eight","year":"2024","journal-title":"Protein Sci."},{"issue":"3","key":"10.1016\/j.bcp.2026.117916_b0535","doi-asserted-by":"crossref","first-page":"413","DOI":"10.1021\/acs.jcim.6b00711","article-title":"In search of novel CDK8 inhibitors by virtual screening","volume":"57","author":"Malika","year":"2017","journal-title":"J. Chem. Inf. Model."},{"issue":"1","key":"10.1016\/j.bcp.2026.117916_b0540","doi-asserted-by":"crossref","first-page":"107","DOI":"10.1002\/cmdc.201800559","article-title":"Discovery of CDK8\/CycC ligands with a new virtual screening tool","volume":"14","author":"Wei","year":"2019","journal-title":"ChemMedChem"},{"issue":"8","key":"10.1016\/j.bcp.2026.117916_b0545","doi-asserted-by":"crossref","first-page":"5439","DOI":"10.1021\/acs.jmedchem.2c01718","article-title":"Discovery of potent, selective, and orally bioavailable small-molecule inhibitors of CDK8 for the treatment of cancer","volume":"66","author":"Yangguang","year":"2023","journal-title":"J. Med. Chem."}],"container-title":["Biochemical Pharmacology"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0006295226002492?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0006295226002492?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2026,5,13]],"date-time":"2026-05-13T22:14:56Z","timestamp":1778710496000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0006295226002492"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2026,7]]},"references-count":109,"alternative-id":["S0006295226002492"],"URL":"https:\/\/doi.org\/10.1016\/j.bcp.2026.117916","relation":{},"ISSN":["0006-2952"],"issn-type":[{"value":"0006-2952","type":"print"}],"subject":[],"published":{"date-parts":[[2026,7]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Discovery and research progress of CDK8 inhibitors","name":"articletitle","label":"Article Title"},{"value":"Biochemical Pharmacology","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.bcp.2026.117916","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2026 Elsevier Inc. All rights are reserved, including those for text and data mining, AI training, and similar technologies.","name":"copyright","label":"Copyright"}],"article-number":"117916"}}