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Aminopyrazole based CDK9 PROTAC sensitizes pancreatic cancer cells to venetoclax

التفاصيل البيبلوغرافية
العنوان: Aminopyrazole based CDK9 PROTAC sensitizes pancreatic cancer cells to venetoclax
المؤلفون: Hannah M. King, Edward L. Ezell, Smitha Kizhake, Muhammad Zahid, Sydney P. Kubica, Michael J. Naldrett, Jayapal Reddy Mallareddy, Amarnath Natarajan, Henry C.-H. Law, Sophie Alvarez, Nicholas T. Woods, Sandeep Rana
المصدر: Bioorg Med Chem Lett
بيانات النشر: Elsevier BV, 2021.
سنة النشر: 2021
مصطلحات موضوعية: Clinical Biochemistry, Pharmaceutical Science, Antineoplastic Agents, 01 natural sciences, Biochemistry, Article, Structure-Activity Relationship, chemistry.chemical_compound, Cyclin-dependent kinase, Drug Discovery, Humans, Kinome, Protein Kinase Inhibitors, Molecular Biology, Cell Proliferation, Sulfonamides, Dose-Response Relationship, Drug, Molecular Structure, biology, 010405 organic chemistry, Venetoclax, Kinase, Organic Chemistry, Proteolysis targeting chimera, Bridged Bicyclo Compounds, Heterocyclic, Cyclin-Dependent Kinase 9, 0104 chemical sciences, Pancreatic Neoplasms, 010404 medicinal & biomolecular chemistry, chemistry, Proteolysis, Cancer research, biology.protein, Pyrazoles, Molecular Medicine, Oncogene MYC, Cyclin-dependent kinase 9, Drug Screening Assays, Antitumor, Growth inhibition
الوصف: Cyclin-dependent kinase 9 (CDK9) is a member of the cyclin-dependent kinase (CDK) family which is involved in transcriptional regulation of several genes, including the oncogene Myc, and is a validated target for pancreatic cancer. Here we report the development of an aminopyrazole based proteolysis targeting chimera (PROTAC 2) that selectively degrades CDK9 (DC50 = 158 ± 6 nM). Mass spectrometry-based kinome profiling shows PROTAC 2 selectively degrades CDK9 in MiaPaCa2 cells and sensitizes them to Venetoclax mediated growth inhibition.
تدمد: 0960-894X
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56ee918f658efcc3aacbc3e5dfd20d20
https://doi.org/10.1016/j.bmcl.2021.128061
حقوق: OPEN
رقم الأكسشن: edsair.doi.dedup.....56ee918f658efcc3aacbc3e5dfd20d20
قاعدة البيانات: OpenAIRE
الوصف
تدمد:0960894X