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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Event Hall |
| Time |
4월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-629 |
| Subject |
Synthetic aryloxazole derivative acts
as a strong anti-glioblastoma agent by inhibiting P-gp
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| Authors |
HyeanJeong Jeong, Yun Kyung Kim1,*
Korea University, Korea
1Korea Institute of Science and Technology, Korea
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| Abstract |
Glioblastoma (GBM) is the most maliganat type of glioma which is arising from glial cells. Despite the aggressive treatment such as surgical resection with chemo-.and radiation therapy, most patients develop recurrent glioblastoma. The survival time of the patients bearing reccurent glioblastoma is merely 6 months on average. To increase the survival rate, more effective anti-glioblastoma agents that suppress tumor growth and migration are urgently required. However the conventional anti-cancer agents have been difficult to be applied for targeting glioblastoma effectively due to their low blood brain-barrier (BBB) penetration. P-glycoprotein, an efflux hemembrane transporter, is responsible for limiting brain uptake of small and hydrophobic drug substances.
To develope brain-penetrable anti-tumor agents, an aryloxazole moiety, which is known to inhibit P-glycoprotein, have been introduced to colchicine derivatives. This synthetic aryloxazole derivative, named KIST-G1, showed the strongest anti-tumor effect, together P-glycoprotein inhibitory activity. With the aid of BBB-permeable properties, KIST-G1 inhibits glioblastoma cell growth and migration almost completely in the orthotopic glioblastoma xenograft models. This results demonstrate the effectiveness of an aryloxazole moiety to targeting brain tumor and suggest KIST-G1 as a potent anti-glioblastoma agent.
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| E-mail |
guswjd7979@kist.re.kr |
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121st General Meeting of the KCS