Identification of vibsanin A analog as a novel HSP90 inhibitor |
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| Institution: | 1. Department of Pharmaceutical Chemistry, Gokaraju Rangaraju College of Pharmacy, Bachupally, Kukatpally, Hyderabad 500090, India;2. Department of Pharmacology, National Institute of Pharmaceutical Education and Research, Balanagar, Hyderabad 500042, India;3. Department of Chemistry, University College of Science and Faculty of Pharmacy, Osmania University, Hyderabad 500007, India;1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The British University in Egypt, Al-Sherouk City, Cairo-Suez Desert Road, 11837 Cairo, Egypt;2. Faculty of Pharmacy, The British University in Egypt, Egypt;3. Department of Pharmacology, Faculty of Pharmacy, The British University in Egypt, Al-Sherouk City, Cairo-Suez Desert Road, 11837 Cairo, Egypt;4. Department of Chemistry, University of Waterloo, 200 University Avenue West, Waterloo, Ontario N2L 3G, Canada;1. College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea;2. School of Pharmacy, Sungkyunkwan University, Suwon, Gyeonggi-do 16419, Republic of Korea;3. Division of Medical Oncology, Department of Internal Medicine, Korea University College of Medicine, Korea University, Seoul 08308, Republic of Korea;4. Brain Korea 21 Program for Biomedical Science, Korea University College of Medicine, Korea University, Seoul 08308, Republic of Korea;5. Department of Biomedical Research Center, Korea University Guro Hospital, Korea University, Seoul 08308, Republic of Korea;1. State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China;2. State Key Laboratory of Chemical Biology and Drug Discovery, and Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Kowloon, Hong Kong;3. Division of Molecular Therapeutics & Formulation, School of Pharmacy, The University of Nottingham, University Park Campus, Nottingham NG7 2RD, UK;1. Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, PR China;2. Department of Pharmacy, Shandong Provincial Hospital Affiliated to Shandong University, Jinan 250021, PR China;3. State Key Laboratory of Microbial Technology, School of Life Sciences, Shandong University, Jinan, Shandong 250100, PR China |
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| Abstract: | Vibsanin A is the first natural product isolated from Viburnum awabuki and has several biological activities. We have reported that a vibsanin A analog, obtained from process of total synthesis of vibsanin A, has anti-proliferative activity against human cancer cell lines. In this study, we evaluated anti-proliferative effect of the vibsanin A analogs against various human cancer cell lines and examined molecular target of the analog in human cells. Among the vibsanin A analogs, vibsanin A analog C (VAC) showed anti-proliferative effect against various cancer cell lines, and the anti-proliferative activity was strongest among the vibsanin A analogs. Additionally, VAC fluctuated amounts of HSP90-related proteins in cells and inhibited HSP90-mediated protein refolding of luciferase in vitro. These results suggest that the anti-proliferative activity of VAC is due to HSP90 inhibition, and VAC has a potential as novel anti-cancer drug as HSP90 inhibitor. |
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| Keywords: | Vibsanin A Natural product Anti-cancer activity HSP90 inhibitor |
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