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| Type |
Poster Presentation |
| Area |
의약화학 |
| Room No. |
포스터발표장 |
| Time |
4월 20일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-451 |
| Subject |
Novel EGFR kinase inhibitors against EGFR T790M mutation |
| Authors |
류희윤, 손정범, 강동욱1,*, 최환근*
대구경북첨단의료산업진흥재단 신약개발지원센터, Korea
1대구가톨릭대학교 제약산업공학과, Korea
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| Abstract |
Kinase inhibitors have been playing an important role in the treatment of cancer and other diseases. However numerous reports indicate that patients end up gaining drug resistance towards those widely used drug. Among those, approximately 60% of the first generation of EGFR TKI (Epidermal Growth Factor Receptor Tyrosine Kinase inhibitor) for the treatment of non-small cell lung carcinoma (NSCLC), such as Gefitinib and Erlotinib, lost significant efficacy due to the emergence of EGFR-T790M gatekeeper mutation. In oreder to overcome this disturbing phenomenon, one needs to come up with a new agent that could not only be potent against EGFR-T790M, but also be selective over wild type EGFR. With respect to this, most of the second and third generation EGFR TKI ( Afatinib, AZD-9291, CO1686, HM61713 and etc) possess acryl amide moiety that could form an irreversible bond with the cystein residue(C797). In the study, we report new type of irreversible inhibitors could form a covalent bond with EGFR-C797. Particularly, compound 2 has EGFR-T790M enzyme activity in EGFR-T790M (IC50: 5nM). |
| E-mail |
kanu0611@naver.com |
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119th General Meeting of the KCS