Systemic Toxicity Reported for CDK8/19 Inhibitors CCT251921 and MSC2530818 Is Not Due to Target Inhibition

A small molecule–kinase interaction map for clinical kinase inhibitors

Fabian, M. A., Biggs, W., Treiber, D. K., Atteridge, C. E., Azimioara, M. D., Benedetti, M. G., Carter, T. A., Ciceri, P., Edeen, P. T., Floyd, M. B., et al. (2005) · Nature Biotechnology · doi:10.1038/nbt1068 · Cited by 1,901 · see citing works

Mediator kinase inhibition further activates super-enhancer-associated genes in AML

Pelish, H. E., Liau, B. B., Nitulescu, I. I., Tangpeerachaikul, A., Poss, Z. C., Silva, D. H. D., Caruso, B., Arefolov, A., Fadeyi, O., Christie, A. L., et al. (2015) · Nature · doi:10.1038/nature14904 · Cited by 397 · see citing works

Making Waves: New Developments in Toxicology With the Zebrafish

Horzmann, K. A., & Freeman, J. L. (2018) · Toxicological Sciences · doi:10.1093/toxsci/kfy044 · Cited by 336 · see citing works

CDK8 Kinase Phosphorylates Transcription Factor STAT1 to Selectively Regulate the Interferon Response

Bancerek, J., Poss, Z. C., Steinparzer, I., Sedlyarov, V., Pfaffenwimmer, T., Mikulic, I., Dölken, L., Strobl, B., Müller, M., Taatjes, D. J., et al. (2013) · Immunity · doi:10.1016/j.immuni.2012.10.017 · Cited by 297 · see citing works

The mammalian phosphatidylinositol 3-phosphate 5-kinase (PIKfyve) regulates endosome-to-TGN retrograde transport

Rutherford, A. C., Traer, C. J., Wassmer, T., Pattni, K., Bujny, M. V., Carlton, J. G., Stenmark, H., & Cullen, P. J. (2006) · Journal of Cell Science · doi:10.1242/jcs.03153 · Cited by 279 · see citing works

CDK8

Galbraith, M. D., Donner, A. J., & Espinosa, J. M. (2010) · Transcription · doi:10.4161/trns.1.1.12373 · Cited by 214 · see citing works

Cyclin-dependent kinase 8 mediates chemotherapy-induced tumor-promoting paracrine activities

Porter, D. C., Farmaki, E., Altilia, S., Schools, G. P., West, D. K., Chen, M., Chang, B.-D., Puzyrev, A. T., Lim, C., Rokow-Kittell, R., et al. (2012) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1206906109 · Cited by 175 · see citing works

Molecular Pathways: Revisiting Glycogen Synthase Kinase-3β as a Target for the Treatment of Cancer

Walz, A. L., Ugolkov, A. V., Chandra, S., Kozikowski, A. P., Carneiro, B. A., O’Halloran, T. V., Giles, F. J., Billadeau, D. D., & Mazar, A. P. (2017) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-15-2240 · Cited by 162 · see citing works

CDK8/19 Mediator kinases potentiate induction of transcription by NFκB

Chen, M., Liang, J., Ji, H., Yang, Z., Altilia, S., Hu, B., Schronce, A., McDermott, M. S. J., Schools, G. P., Lim, C., et al. (2017) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1710467114 · Cited by 141 · see citing works

Inhibition of CDK8 mediator kinase suppresses estrogen dependent transcription and the growth of estrogen receptor positive breast cancer

McDermott, M. S. J., Chumanevich, A. A., Lim, C., Liang, J., Chen, M., Altilia, S., Oliver, D., Rae, J. M., Shtutman, M. S., Kiaris, H., et al. (2017) · Oncotarget · doi:10.18632/oncotarget.14894 · Cited by 137 · see citing works

CDK8-Mediated STAT1-S727 Phosphorylation Restrains NK Cell Cytotoxicity and Tumor Surveillance

Putz, E. M., Gotthardt, D., Hoermann, G., Csiszar, A., Wirth, S., Berger, A., Straka, E., Rigler, D., Wallner, B., Jamieson, A. M., et al. (2013) · Cell Reports · doi:10.1016/j.celrep.2013.07.012 · Cited by 132 · see citing works

Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening

Czodrowski, P., Mallinger, A., Wienke, D., Esdar, C., Pöschke, O., Busch, M., Rohdich, F., Eccles, S. A., Ortiz-Ruiz, M.-J., Schneider, R., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00597 · Cited by 123 · see citing works

Regulatory functions of the Mediator kinases CDK8 and CDK19

Fant, C. B., & Taatjes, D. J. (2018) · Transcription · doi:10.1080/21541264.2018.1556915 · Cited by 122 · see citing works

Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19

Mallinger, A., Schiemann, K., Rink, C., Stieber, F., Calderini, M., Crumpler, S., Stubbs, M., Adeniji-Popoola, O., Poeschke, O., Busch, M., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01685 · Cited by 117 · see citing works

SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains

Rzymski, T., Mikuła, M., Żyłkiewicz, E., Dreas, A., Wiklik, K., Gołas, A., Wójcik, K., Masiejczyk, M., Wróbel, A., Dolata, I., et al. (2017) · Oncotarget · doi:10.18632/oncotarget.16810 · Cited by 117 · see citing works

Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?

Philip, S., Kumarasiri, M., Teo, T., Yu, M., & Wang, S. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00901 · Cited by 111 · see citing works

Cortistatin A is a High‐Affinity Ligand of Protein Kinases ROCK, CDK8, and CDK11

Cee, V. J., Chen, D. Y. ‐., Lee, M. R., & Nicolaou, K. C. (2009) · Angewandte Chemie International Edition · doi:10.1002/anie.200904778 · Cited by 106 · see citing works

Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases

Clarke, P. A., Ortiz-Ruiz, M.-J., Poele, R. T., Adeniji-Popoola, O., Box, G., Court, W., Czasch, S., Bawab, S. E., Esdar, C., Ewan, K., et al. (2016) · eLife · doi:10.7554/elife.20722 · Cited by 99 · see citing works

CDK8 Selectively Promotes the Growth of Colon Cancer Metastases in the Liver by Regulating Gene Expression of TIMP3 and Matrix Metalloproteinases

Liang, J., Chen, M., Hughes, D. T., Chumanevich, A. A., Altilia, S., Kaza, V., Lim, C., Kiaris, H., Mythreye, K., Peña, M. M. O., et al. (2018) · Cancer Research · doi:10.1158/0008-5472.can-18-1583 · Cited by 91 · see citing works

Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen

Mallinger, A., Crumpler, S., Pichowicz, M., Waalboer, D., Stubbs, M., Adeniji-Popoola, O., Wood, B., Smith, E. L., Thai, C., Henley, A. T., et al. (2015) · Journal of Medicinal Chemistry · doi:10.1021/jm501436m · Cited by 83 · see citing works

Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells

Koehler, M. F. T., Bergeron, P., Blackwood, E. M., Bowman, K. K., Clark, K., Firestein, R., Kiefer, J. R., Maskos, K., McCleland, M. L., Orren, L., et al. (2016) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.5b00278 · Cited by 81 · see citing works

Mediator kinase CDK8/CDK19 drives YAP1-dependent BMP4-induced EMT in cancer

Serrao, A., Jenkins, L. M., Chumanevich, A. A., Horst, B., Liang, J., Gatza, M. L., Lee, N. Y., Roninson, I. B., Broude, E. V., & Mythreye, K. (2018) · Oncogene · doi:10.1038/s41388-018-0316-y · Cited by 64 · see citing works

Stereodivergent Synthesis of 17‐α and 17‐β‐Aryl Steroids: Application and Biological Evaluation of D‐Ring Cortistatin Analogues

Shi, J., Shigehisa, H., Guerrero, C. A., Shenvi, R. A., Li, C., & Baran, P. S. (2009) · Angewandte Chemie International Edition · doi:10.1002/anie.200901116 · Cited by 64 · see citing works

Identifying Cancers Impacted by CDK8/19

Roninson, I. B., Győrffy, B., Mack, Z. T., Shtil, A. A., Shtutman, M. S., Chen, M., & Broude, E. V. (2019) · Cells · doi:10.3390/cells8080821 · Cited by 63 · see citing works

CDK8/19 inhibition induces premature G1/S transition and ATR-dependent cell death in prostate cancer cells

Nakamura, A., Nakata, D., Kakoi, Y., Kunitomo, M., Murai, S., Ebara, S., Hata, A., & Hara, T. (2018) · Oncotarget · doi:10.18632/oncotarget.24414 · Cited by 48 · see citing works

Discovery and structure–activity relationship of thienopyridine derivatives as bone anabolic agents

Saito, K., Nakao, A., Shinozuka, T., Shimada, K., Matsui, S., Oizumi, K., Yano, K., Ohata, K., Nakai, D., Nagai, Y., et al. (2013) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2013.01.071 · Cited by 37 · see citing works

Preclinical Toxicity of AZD7969

Hall, A. P., Escott, K. J., Sanganee, H. J., & Hickling, K. (2014) · Toxicologic Pathology · doi:10.1177/0192623314544468 · Cited by 25 · see citing works

Cyclin‐dependent kinase 8/19 inhibition suppresses osteoclastogenesis by downregulating RANK and promotes osteoblast mineralization and cancellous bone healing

Amirhosseini, M., Bernhardsson, M., Lång, P., Andersson, G., Flygare, J., & Fahlgren, A. (2019) · Journal of Cellular Physiology · doi:10.1002/jcp.28321 · Cited by 25 · see citing works

Characterizing CDK8/19 Inhibitors through a NFκB-Dependent Cell-Based Assay

Li, J., Ji, H., Porter, D. C., Broude, E. V., Roninson, I. B., & Chen, M. (2019) · Cells · doi:10.3390/cells8101208 · Cited by 21 · see citing works

CDK8 as the STAT1 serine 727 kinase?

Staab, J., Herrmann‐Lingen, C., & Meyer, T. (2013) · JAK-STAT · doi:10.4161/jkst.24275 · Cited by 14 · see citing works

CDK8 and CDK19: positive regulators of signal-induced transcription and negative regulators of Mediator complex proteins

Chen, M., Li, J., Zhang, L., Wang, L., Cheng, C., Ji, H., Altilia, S., Ding, X., Cai, G., Altomare, D., et al. (2023) · Nucleic Acids Research · doi:10.1093/nar/gkad538 · Cited by 73 · see citing works

Proline metabolism and transport in retinal health and disease

Du, J., Zhu, S., Lim, R. R., & Chao, J. R. (2021) · Amino Acids · doi:10.1007/s00726-021-02981-1 · Cited by 63 · see citing works

Angel or Devil ? - CDK8 as the new drug target

Wu, D., Zhang, Z., Chen, X., Yan, Y., & Liu, X. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.113043 · Cited by 53 · see citing works

Inhibition of CDK8/19 Mediator kinase potentiates HER2-targeting drugs and bypasses resistance to these agents in vitro and in vivo

Ding, X., Sharko, A. C., McDermott, M. S. J., Schools, G. P., Chumanevich, A. A., Ji, H., Li, J., Zhang, L., Mack, Z. T., Sikirzhytski, V., et al. (2022) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2201073119 · Cited by 49 · see citing works

CDK8 Fine-Tunes IL-6 Transcriptional Activities by Limiting STAT3 Resident Time at the Gene Loci

Martínez‐Fábregas, J., Wang, L., Pöhler, E., Cozzani, A., Wilmes, S., Kazemian, M., Mitra, S., & Moraga, I. (2020) · Cell Reports · doi:10.1016/j.celrep.2020.108545 · Cited by 47 · see citing works

Transcription associated cyclin-dependent kinases as therapeutic targets for prostate cancer

Constantin, T. A., Greenland, K. K., Varela‐Carver, A., & Bevan, C. L. (2022) · Oncogene · doi:10.1038/s41388-022-02347-1 · Cited by 40 · see citing works

Discovery of LL-K8-22: A Selective, Durable, and Small-Molecule Degrader of the CDK8-Cyclin C Complex

Wang, M., Lin, R., Li, J., Suo, Y., Gao, J., Liu, L., Zhou, L., Ni, Y., Yang, Z., Zheng, J., et al. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c02045 · Cited by 42 · see citing works

A Selective and Orally Bioavailable Quinoline-6-Carbonitrile-Based Inhibitor of CDK8/19 Mediator Kinase with Tumor-Enriched Pharmacokinetics

Zhang, L., Cheng, C., Li, J., Wang, L., Chumanevich, A. A., Porter, D. C., Mindich, A., Gorbunova, S., Roninson, I. B., Chen, M., et al. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01951 · Cited by 40 · see citing works

PYCR, a key enzyme in proline metabolism, functions in tumorigenesis

Li, Y., Bie, J., Song, C., Liu, M., & Luo, J. (2021) · Amino Acids · doi:10.1007/s00726-021-03047-y · Cited by 39 · see citing works

The Inhibition of CDK8/19 Mediator Kinases Prevents the Development of Resistance to EGFR-Targeting Drugs

Sharko, A. C., Lim, C., McDermott, M. S. J., Hennes, C., Philavong, K. P., Aiken, T., Tatarskiy, V. V., Roninson, I. B., & Broude, E. V. (2021) · Cells · doi:10.3390/cells10010144 · Cited by 36 · see citing works

Hydrophobic tag tethering degrader as a promising paradigm of protein degradation: Past, present and future perspectives

Ha, S., Zhu, J., Xiang, H., & Luo, G. (2023) · Chinese Chemical Letters · doi:10.1016/j.cclet.2023.109192 · Cited by 34 · see citing works

Chemical inhibitors of transcription-associated kinases

Clopper, K. C., & Taatjes, D. J. (2022) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2022.102186 · Cited by 28 · see citing works

CDK8 and CDK19 regulate intestinal differentiation and homeostasis via the chromatin remodeling complex SWI/SNF

Dannappel, M., Zhu, D., Sun, X., Chua, H. K., Poppelaars, M., Suehiro, M., Khadka, S., Sian, T. C. C. L. K., Sooraj, D., Loi, M., et al. (2022) · Journal of Clinical Investigation · doi:10.1172/jci158593 · Cited by 24 · see citing works

CDK8 and CDK19 act redundantly to control the CFTR pathway in the intestinal epithelium

Prieto, S., Dubra, G., Camasses, A., Simboeck, E., Aznar, A. B., Begon‐Pescia, C., Pirot, N., Gerbe, F., Angevin, L., Jay, P., et al. (2022) · EMBO Reports · doi:10.15252/embr.202154261 · Cited by 22 · see citing works

Mediator kinase inhibition reverses castration resistance of advanced prostate cancer

Li, J., Hilimire, T. A., Liu, Y., Wang, L., Liang, J., Győrffy, B., Sikirzhytski, V., Ji, H., Zhang, L., Chen, C., et al. (2024) · Journal of Clinical Investigation · doi:10.1172/jci176709 · Cited by 22 · see citing works

Design and Synthesis of a 2-Amino-pyridine Derivative as a Potent CDK8 Inhibitor for Anti-colorectal Cancer Therapy

Yan, Y. Y., Zhang, X. X., Xiao, Y., Shen, X. B., Jian, Y. J., Wang, Y., She, Z. H., Liu, M. M., & Liu, X. H. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01042 · Cited by 21 · see citing works

Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation

Yu, M., Teo, T., Yang, Y., Li, M., Long, Y., Philip, S., Noll, B. D., Heinemann, G. K., Diab, S., Eldi, P., et al. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113248 · Cited by 21 · see citing works

Transcriptional Antagonism by CDK8 Inhibition Improves Therapeutic Efficacy of MEK Inhibitors

Malone, C. F., Kim, M., Alexe, G., Engel, K. L., Forman, A. B., Robichaud, A. L., Conway, A. S., Goodale, A. B., Meyer, A., Khalid, D., et al. (2022) · Cancer Research · doi:10.1158/0008-5472.can-21-4309 · Cited by 19 · see citing works

CDK8 inhibitors antagonize HIV-1 reactivation and promote provirus latency in T cells

Horvath, R. M., Brumme, Z. L., & Sadowski, I. (2023) · Journal of Virology · doi:10.1128/jvi.00923-23 · Cited by 17 · see citing works

Genetically Engineered Mice Unveil In Vivo Roles of the Mediator Complex

Ilchuk, L. A., Kubekina, M. V., Okulova, Y. D., Silaeva, Y. Y., Tatarskiy, V. V., Filatov, M. A., & Bruter, A. V. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms24119330 · Cited by 16 · see citing works

Design, synthesis, and biological evaluation of indolin-2-one derivatives as novel cyclin-dependent protein kinase 8 (CDK8) inhibitors

Hsu, J., Hsu, K., Sun, C., Chou, C.-H., Lin, T. E., Sung, T.-Y., Tseng, H.-J., Yen, S., Yang, C., & Huang, W. (2023) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2023.114258 · Cited by 15 · see citing works

Super-Enhancers in the Regulation of Gene Transcription: General Aspects and Antitumor Targets

Bruter, A. V., Rodionova, M. D., Varlamova, E. A., & Shtil, A. A. (2021) · Acta Naturae · doi:10.32607/actanaturae.11067 · Cited by 14 · see citing works

The Cyclin-Dependent Kinase 8 (CDK8) Inhibitor DCA Promotes a Tolerogenic Chemical Immunophenotype in CD4 + T Cells via a Novel CDK8-GATA3-FOXP3 Pathway

Arnett, A., Moo, K. G., Flynn, K. J., Sundberg, T. B., Johannessen, L. H., Shamji, A. F., Gray, N. S., Decker, T., Zheng, Y., Gersuk, V. H., et al. (2021) · Molecular and Cellular Biology · doi:10.1128/mcb.00085-21 · Cited by 13 · see citing works

MK256 is a novel CDK8 inhibitor with potent antitumor activity in AML through downregulation of the STAT pathway

Lee, J., Liu, S., Wang, Y., You, L., & Jablons, D. M. (2022) · Oncotarget · doi:10.18632/oncotarget.28305 · Cited by 12 · see citing works

Development of Highly Potent and Selective Pyrazolopyridine Inhibitor of CDK8/19

Hatcher, J. M., Vatsan, P. S., Wang, E., Jiang, J., & Gray, N. S. (2021) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.1c00300 · Cited by 12 · see citing works

Mediator kinase inhibitors suppress triple-negative breast cancer growth and extend tumor suppression by mTOR and AKT inhibitors

Ding, X., Liang, J., Sharko, A. C., Hilimire, T. A., Li, J., Loskutov, J., Mack, Z. T., Ji, H., Schools, G. P., Cai, C., et al. (2024) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2414501121 · Cited by 11 · see citing works

Cyclin-Dependent Kinase 8 Represents a Positive Regulator of Cytomegalovirus Replication and a Novel Host Target for Antiviral Strategies

Obergfäll, D., Wild, M. R., Sommerer, M., Dahm, M. B., Kicuntod, J., Tillmanns, J., Kögler, M., Lösing, J., Dhotre, K., Müller, R., et al. (2024) · Pharmaceutics · doi:10.3390/pharmaceutics16091238 · Cited by 9 · see citing works

Binding patterns and structure–activity relationship of CDK8 inhibitors

Ma, D., Chen, X., Shen, X., Sheng, L., & Liu, X. H. (2020) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2020.103624 · Cited by 9 · see citing works

CDK8/19 inhibition attenuates G1 arrest induced by BCR-ABL antagonists and accelerates death of chronic myelogenous leukemia cells

Khamidullina, A. I., Yastrebova, M. A., Bruter, A. V., Nuzhina, J., Vorobyeva, N. E., Khrustaleva, A. M., Varlamova, E. A., Tyakht, A., Abramenko, Y. E., Ivanova, E. S., et al. (2025) · Cell Death Discovery · doi:10.1038/s41420-025-02339-6 · Cited by 8 · see citing works

Knockout of cyclin-dependent kinases 8 and 19 leads to depletion of cyclin C and suppresses spermatogenesis and male fertility in micePreprint

Bruter, A. V., Varlamova, E. A., Stavskaya, N. I., Antysheva, Z., Манских, В. Н., Tvorogova, A. V., Korshunova, D. S., Khamidullina, A. I., Utkina, M. V., Bogdanov, V. P., et al. (2024) · eLife · doi:10.7554/elife.96465 · Cited by 8 · see citing works

Inhibition of Cyclin-Dependent Kinases 8/19 Restricts Bacterial and Virus-Induced Inflammatory Responses in Monocytes

Kokinos, E. K., Tsymbal, S. A., Galochkina, A. V., Bezlepkina, S. A., Nikolaeva, J. V., Vershinina, S. O., Андреевна, Ш. А., Tatarskiy, V. V., Shtil, A. A., Broude, E. V., et al. (2023) · Viruses · doi:10.3390/v15061292 · Cited by 6 · see citing works

The Cyclin-Dependent Kinase 8 Inhibitor E966-0530-45418 Attenuates Pulmonary Fibrosis In Vitro and In Vivo

Chou, C.-H., Huang, W.-J., Hsu, K., Hsu, J., Lin, T. E., & Yang, C. (2024) · International Journal of Biological Sciences · doi:10.7150/ijbs.105826 · Cited by 6 · see citing works

Cyclin-dependent kinase 8 is an independent prognosticator in uterine leiomyosarcoma

Yasutake, N., Iwasaki, T., Yamamoto, H., Sonoda, K., Kodama, K., Okugawa, K., Asanoma, K., Yahata, H., Kato, K., & Oda, Y. (2022) · Pathology - Research and Practice · doi:10.1016/j.prp.2022.153920 · Cited by 4 · see citing works

Immunogenic antitumor potential of Prakasine nanoparticles in zebrafish by gene expression stimulation

Prakash, S. K. (2023) · Artificial Cells Nanomedicine and Biotechnology · doi:10.1080/21691401.2023.2173217 · Cited by 3 · see citing works

CDK8 fine-tunes IL-6 transcriptional activities by limiting STAT3 resident time at the gene loci

Martinez-Fabregas, J., Wang, L., Pohler, E., Cozzani, A., Kazemian, M., Mitra, S., & Moraga, I. (2020) · doi:10.1101/2020.03.19.998351 · Cited by 2 · see citing works

Knockout of cyclin-dependent kinases 8 and 19 leads to depletion of cyclin C and suppresses spermatogenesis and male fertility in mice

Bruter, A. V., Varlamova, E. A., Stavskaya, N. I., Antysheva, Z., Манских, В. Н., Tvorogova, A. V., Korshunova, D. S., Khamidullina, A. I., Utkina, M. V., Bogdanov, V. P., et al. (2025) · eLife · doi:10.7554/elife.96465.4 · Cited by 2 · see citing works

Structural optimization and biological evaluation of indolin-2-one derivatives as novel CDK8 inhibitors for idiopathic pulmonary fibrosis

Hsu, J., Hsu, K., Chou, C.-H., He, T.-Y., Lin, T. E., Sung, T.-Y., Yen, S., Hsieh, J., Yang, C., & Huang, W. (2025) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2025.117891 · Cited by 2 · see citing works

Anoikis resistance and metastasis of ovarian cancer can be overcome by CDK8/19 mediator kinase inhibition

Monavarian, M., Rajkarnikar, R., Page, E. F., Kumari, A., Quintero-Macías, L., Massicano, F., Lee, N. Y., Sahoo, S., Hempel, N., Jolly, M. K., et al. (2026) · JCI Insight · doi:10.1172/jci.insight.192113 · Cited by 3 · see citing works

Targeting Mediator Kinase Cyclin-Dependent Kinases 8/19 Potentiates Chemotherapeutic Responses, Reverses Tumor Growth, and Prolongs Survival from Ovarian Clear Cell Carcinoma

Barton, W. C., Kumari, A., Mack, Z. T., Schools, G. P., Quintero-Macías, L., Choi, A. S., Rangavajhula, K., Arend, R. C., Broude, E. V., & Mythreye, K. (2025) · Cancers · doi:10.3390/cancers17060941 · Cited by 1 · see citing works

Inhibition of CDK8 rescues impaired ischemic fracture healing

Capobianco, C. A., Song, M. J., Farrell, E. C., Knights, A. J., Kessell, K., Donneys, A., Schmanski, J. T., Schroeder, L. R., Chen, M., Roninson, I. B., et al. (2026) · npj Regenerative Medicine · doi:10.1038/s41536-026-00456-z · Cited by 1 · see citing works

Design and synthesis of a 1,3,6-trimethyl-1H-benzo[d]imidazole-5-sulfonamide derivative as a type I CDK8 inhibitor against colorectal cancer

Du, J., Zhang, Y., Shi, D., Chang, C., Zhou, F., Dong, J., Yan, Y., & Liu, X. (2025) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2025.109297 · Cited by 1 · see citing works

CDK8/19 Inhibition Attenuates the Tolerance of Leukemia Cells to BCR-ABL1 Blockers in the Medium Conditioned by Bone Marrow Fibroblasts

Savin, A. M., Levchuk, D. P., Ilchenko, A. D., Ivanova, E. S., & Shtil, A. A. (2026) · Cell and Tissue Biology · doi:10.1134/s1990519x26600675 · Cited by 1 · see citing works

CDK8/19 in Stress Response in Mouse Embryonic Fibroblast Model

Varlamova, E. A., Kirukhina, T. A., Isagulieva, A. K., Khamidullina, A. I., Sorokina, M. Y., Silaeva, Y. Y., Tatarskiy, V. V., & Bruter, A. V. (2025) · Molecular Biology · doi:10.1134/s0026893325700098 · Cited by 1 · see citing works

CDK8 inhibitors antagonize HIV-1 reactivation and promote provirus latency in T cellsPreprint

Horvath, R. M., Brumme, Z. L., & Sadowski, I. (2023) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2023.06.07.544021 · Cited by 1 · see citing works

The CDK8 inhibitor DCA promotes a tolerogenic chemical immunophenotype in CD4 + T cells via a novel CDK8-GATA3-FOXP3 pathwayPreprint

Arnett, A., Moo, K. G., Flynn, K. J., Sundberg, T. B., Johannessen, L. H., Shamji, A. F., Gray, N. S., Decker, T., Zheng, Y., Gersuk, V. H., et al. (2019) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/855429

Transcriptomic and Proteomic Effects of CDK8 and CDK19 Mediator KinasesPreprint

Chen, M., Li, J., Wang, L., Zhang, L., Cheng, C., Ji, H., Altilia, S., Ding, X., Cai, G., Altomare, D., et al. (2022) · SSRN Electronic Journal · doi:10.2139/ssrn.4169247

Knockout of cyclin dependent kinases 8 and 19 leads to depletion of cyclin C and suppresses spermatogenesis and male fertility in micePreprint

Bruter, A. V., Varlamova, E. A., Stavskaya, N. I., Antysheva, Z., Манских, В. Н., Tvorogova, A. V., Korshunova, D. S., Khamidullina, A. I., Utkina, M. V., Bogdanov, V. P., et al. (2024) · eLife · doi:10.7554/elife.96465.1

Knockout of cyclin dependent kinases 8 and 19 leads to depletion of cyclin C and suppresses spermatogenesis and male fertility in micePreprint

Bruter, A. V., Varlamova, E. A., Stavskaya, N. I., Antysheva, Z., Манских, В. Н., Tvorogova, A. V., Korshunova, D. S., Khamidullina, A. I., Utkina, M. V., Bogdanov, V. P., et al. (2025) · eLife · doi:10.7554/elife.96465.2

Knockout of cyclin dependent kinases 8 and 19 leads to depletion of cyclin C and suppresses spermatogenesis and male fertility in micePreprint

Bruter, A. V., Varlamova, E. A., Stavskaya, N. I., Antysheva, Z., Манских, В. Н., Tvorogova, A. V., Korshunova, D. S., Khamidullina, A. I., Utkina, M. V., Bogdanov, V. P., et al. (2025) · eLife · doi:10.7554/elife.96465.3

Selective Dual Inhibition of TNKS1 and CDK8 by TCS9725 Attenuates STAT1/β-Catenin/TGFβ1 Signaling in Renal Cancer

Fayi, M. S. A., & Alshyarba, M. (2025) · Current Issues in Molecular Biology · doi:10.3390/cimb47060463

Discovery and Chemical Biology of CDK8 Inhibitors Reveals Insights for Kinase Inhibitor DevelopmentPreprint

Borel, F., Bihan, Y. V. L., Josselin, B., Robert, T., Duez, J., Angevin, L., Simboeck, E., Prieto, S., Hodimont, E., Ferrer, J.-L., et al. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.11.06.686927

Transcriptional kinase CDK8, but not CDK19, promotes the development of atherosclerotic lesions in mice

Незнамов, А. Н., Байкова, Ю. П., Korshunov, E. N., Isaeva, E., Bruter, A. V., & Kubekina, M. V. (2025) · Bulletin of Russian State Medical University · doi:10.24075/brsmu.2025.078

The Mediator Complex: From Transcriptional Regulation to Disease Pathogenesis

Iyer, S., Ito, T., Nakagawa, T., & Hattori, N. (2026) · International Journal of Molecular Sciences · doi:10.3390/ijms27052221

A novel CDK8/19 inhibitor RO8323 mitigates allograft rejection through dual mechanisms of action to modulate regulatory T cell and myeloid cell

Shen, F., Xie, R., Gan, Y., Ren, P., Wu, R.-R., Yan, J.-W., Bian, Y.-Y., Liu, C.-C., Yang, S., Han, X.-C., et al. (2026) · Acta Pharmacologica Sinica · doi:10.1038/s41401-026-01773-1

Rôle des kinases du Médiateur CDK8 et CDK19 dans la physiologie cellulaire et la réponse au stress environnemental

Angevin, L. (2022) · doi:10.70675/354d1c5fza872z406ezb94ez534c4f73354d

Inhibition of cyclin-dependent kinase 8 modulates chondrocyte transition to hypertrophy and provides in vivo protection against spontaneous osteoarthritis

Wells, L. M., Keen, J. A. C., Sharma, A., Marr, N., Hansen, R., Pereira, J. S., Roe, T., Roberts, L. D., Oppermann, U. C. T., Clarke, P. A., et al. (2026) · Bone Research · doi:10.1038/s41413-026-00551-3

A guide to transcriptional cyclin‐dependent kinases in cancer

Devlin, J. R., Kyheröinen, S., & Johnstone, R. W. (2026) · FEBS Journal · doi:10.1111/febs.70731

BindingDB Entry 50013163: Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.

BindingDB (2022) · UC San Diego · doi:10.7270/q2930xw8

BindingDB Entry 50015816: Design and Synthesis of a 2-Amino-pyridine Derivative as a Potent CDK8 Inhibitor for Anti-colorectal Cancer Therapy.

BindingDB (2023) · UC San Diego · doi:10.7270/q28w3j8d

BindingDB Entry 50015341: A Selective and Orally Bioavailable Quinoline-6-Carbonitrile-Based Inhibitor of CDK8/19 Mediator Kinase with Tumor-Enriched Pharmacokinetics.

BindingDB (2023) · UC San Diego · doi:10.7270/q2wd44g8

BindingDB Entry 50014191: Development of Highly Potent and Selective Pyrazolopyridine Inhibitor of CDK8/19.

BindingDB (2022) · UC San Diego · doi:10.7270/q29w0k80

Discovery and Chemical Biology of CDK8 Inhibitors Reveals Insights for Kinase Inhibitor DevelopmentPreprint

Borel, F., Bihan, Y. V. L., Josselin, B., Robert, T., Duez, J., Angevin, L., Simboeck, E., Prieto, S., Hodimont, E., Ferrer, J.-L., et al. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.11.06.686927

Abstract 129: Assessing the mechanism and therapeutic potential of modulators of the human mediator complex-associated protein kinases CDK8 and CDK19

Clarke, P. A., Ortiz-Ruiz, M.-J., Poele, R. T., Adeniji-Popoola, O., Box, G., Esdar, C., Ewan, K., Gowan, S. M., Brandon, A. D. H., Hewitt, P., et al. (2017) · Cancer Research · doi:10.1158/1538-7445.am2017-129

Discovery of a Novel and Potent Cyclin-Dependent Kinase 8/19 (CDK8/19) Inhibitor for the Treatment of Cancer

Xu, J., Qi, H., Wang, Z., Wang, L., Steurer, B., Cai, X., Liu, J., Aliper, A., Zhang, M., Ren, F., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c00248 · Cited by 15 · see citing works

The Development of Novel CDK8 and CDK19 Inhibitors and Degraders as Potential Anti-cancer Agents

Zhang, L. (2021) · Scholar Commons (University of South Carolina)

Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases

Clarke, P. A., Ortiz-Ruiz, M.-J., Poele, R. T., Adeniji-Popoola, O., Box, G., Court, W., Czasch, S., Bawab, S. E., Esdar, C., Ewan, K., et al. (2016) · eLife · doi:10.7554/elife.20722 · Cited by 99 · see citing works