Amphipathic Small Molecule AZT Compound Displays Potent Inhibitory Effects in Cancer Cell Proliferation
- Authors
- Gunasekaran, Pethaiah; Han, Ho Jin; Choi, Jung hoon; Ryu, Eun Kyoung; Park, Nam Yeong; Bang, Geul; La, Yeo Kyung; Park, Sunghyun; Hwang, Kyubin; Kim, Hak Nam; Kim, Mi-Hyun; Jeon, Young Ho; Soung, Nak-Kyun; Bang, Jeong Kyu
- Issue Date
- 12월-2021
- Publisher
- MDPI
- Keywords
- anticancer; drug discovery; necrosis; oncosis; small molecule
- Citation
- PHARMACEUTICS, v.13, no.12
- Indexed
- SCIE
SCOPUS
- Journal Title
- PHARMACEUTICS
- Volume
- 13
- Number
- 12
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/135530
- DOI
- 10.3390/pharmaceutics13122071
- ISSN
- 1999-4923
- Abstract
- Cancer has been identified as a leading cause of death worldwide, and the increasing number of cancer cases threatens to shorten the average life expectancy of people. Recently, we reported a 3-azido-3-deoxythymidine (AZT)-based amphipathic small molecule, ADG-2e that revealed a notable potency against tumor metastasis. To evaluate the anticancer potential of ADG-2e, we assessed its anticancer potency in vitro and in vivo. Anticancer screening of ADG-2e against cervical cancer cells, HeLa CCL2, and BT549 mammary gland ductal carcinoma showed significant inhibition of cancer cell proliferation. Furthermore, mechanistic investigations revealed that cancer cell death presumably proceeded through an oncosis mechanistic pathway because ADG-2e treated cells showed severe damage on the plasma membrane, a loss of membrane integrity, and leakage of alpha-tubulin and beta-actin. Finally, evaluation of the antitumorigenic potential of ADG-2e in mouse xenograft models revealed that this compound potentially inhibits cancer cell proliferation. Collectively, these findings suggest that ADG-2e can evolve as an anticancer agent, which may represent a model for nucleoside-based small molecule anticancer drug discovery.
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Collections - College of Pharmacy > Department of Pharmaceutical Science > 1. Journal Articles
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