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Your search keyword '"Benjamin Noll"' showing total 2 results
Start Over Author "Benjamin Noll" Publisher elsevier bv
2 results on '"Benjamin Noll"'

1. Erratum to 'A first-in-class CDK4 inhibitor demonstrates in vitro, ex-vivo and in vivo efficacy against ovarian cancer' [Gynecologic Oncology 159 (2020) 827–838]

Author

Jimma Likisa, Shudong Wang, Solomon Tadesse, Martin K. Oehler, Andrew Beck, Robert W. Milne, Noor A. Lokman, Rupal Pradhan, Carmela Ricciardelli, Mingfeng Yu, Gary K. Heinemann, Benjamin Noll, Hugo Albrecht, and Laychiluh Bantie

Subjects
Oncology, CDK4 Inhibitor, business.industry, In vivo, medicine, Cancer research, Obstetrics and Gynecology, Gynecologic oncology, Ovarian cancer, medicine.disease, business, Ex vivo, In vitro
Published
2021

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

Author

Muhammed H. Rahaman, John D. Hayball, Theodosia Teo, Stephen Philip, Laychiluh B. Mekonnen, Shudong Wang, Yi Long, Man-jun Li, Preethi Eldi, Mingfeng Yu, Benjamin Noll, Gary K. Heinemann, Yuchao Yang, Abel Tesfaye Anshabo, Robert W. Milne, Sarah Diab, Yu, Mingfeng, Teo, Theodosia, Yang, Yuchao, Li, Manjun, Long, Yi, Philip, Stephen, Noll, Benjamin, Heinemann, Gary K, Diab, Sarah, Eldi, Preethi, Mekonnen, Laychiluh, Anshabo, Abel T, Rahaman, Muhammed H, Milne, Robert, Hayball, John D, and Wang, Shudong

Subjects
Male, Cell Survival, Pyridines, Administration, Oral, Biological Availability, Mice, Nude, Antineoplastic Agents, Pharmacology, Rats, Sprague-Dawley, Mice, Structure-Activity Relationship, Mediator, Transcription (biology), Cell Line, Tumor, Drug Discovery, Animals, Humans, Structure–activity relationship, drug-like properties, Kinase activity, Protein Kinase Inhibitors, Transcription factor, Cell Proliferation, Mice, Inbred BALB C, Dose-Response Relationship, Drug, Molecular Structure, Kinase, Chemistry, structure-activity relationship, Organic Chemistry, toxicity, General Medicine, CDK8 inhibitor, Cyclin-Dependent Kinase 8, Rats, Drug Design, Phosphorylation, Cyclin-dependent kinase 8, Female, Drug Screening Assays, Antitumor, pharmacokinetics
Abstract

CDK8 regulates transcription either by phosphorylation of transcription factors or, as part of a four-subunit kinase module, through a reversible association of the kinase module with the Mediator complex, a highly conserved transcriptional coactivator. Deregulation of CDK8 has been found in various types of human cancer, while the role of CDK8 in supressing anti-cancer response of natural killer cells is being understood. Currently, CDK8-targeting cancer drugs are highly sought-after. Herein we detail the discovery of a series of novel pyridine-derived CDK8 inhibitors. Medicinal chemistry optimisation gave rise to 38 (AU1-100), a potent CDK8 inhibitor with oral bioavailability. The compound inhibited the proliferation of MV4-11 acute myeloid leukaemia cells with the kinase activity of cellular CDK8 dampened. No systemic toxicology was observed in the mice treated with 38. These results warrant further pre-clinical studies of 38 as an anti-cancer agent. Refereed/Peer-reviewed

Published
2021

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