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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Exhibition Hall 2 |
| Time |
4월 18일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-406 |
| Subject |
Design, synthesis and biological evaluation of phenoxazine derivatives as clathrin inhibitors |
| Authors |
Eunyeong Rim, Seung Kyu Kang1, Chijung Kim1, Navin Pandit, Kwan-Young Jung1,*
Department of Medicinal Chemistry & Pharmacology, University of Science & Technology, Korea
1Therapeutics & Biotechnology Division, Korea Research Institute of Chemical Technology, Korea
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| Abstract |
Clathrin regulates various physiological processes, including internalization of growth factors and receptors, synaptic transmission, and entry of pathogens. Clathrin functions as a central organizing platform for coated pit assembly and dissociation within the endocytic network through its terminal domain. To inhibit clathrin, a series of phenoxazine compounds were synthesized and evaluated for their clathrin inhibitory effect by measuring transferrin uptake and change of puncta. Among the phenoxazine derivatives, 3-(10H-phenoxazin-10-yl)-N,N-bis(2-((tetrahydro-2H-pyran-2-yl)oxy)ethyl)propan-1-amine (3t) was identified as the best clathrin inhibitor with IC50 = 6.8 µM. |
| E-mail |
wydl3796@krict.re.kr |
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123rd General Meeting of the KCS