Taebo Sim
Korea University · Medicine
Taebo Sim 교수의 연구실은 신호전달 경로의 이상이 암 발생에 기여하는 분자 기전을 규명하고, 이를 표적으로 하는 표적항암제 개발에 주력하고 있습니다. 특히 FGFR 및 FAK와 같은 티로신 키나제 수용체를 타겟으로 한 신약 후보 물질의 설계와 생물학적 평가를 중심으로 연구를 진행하고 있으며, 암세포의 성장과 전이를 억제하는 다중표적 억제제 개발에 초점을 맞추고 있습니다. 최근에는 자연유래 락톤 유도체의 항암 활성 연구를 통해 새로운 약물 개발 전략을 모색하고 있습니다.
Figures are computed from collected data and may differ slightly.
Aberrant mutational activation of FGFR2 is associated with endometrial cancers (ECs). AP24534 (ponatinib) currently undergoing clinical trials has been known to be an orally available multi-targeted tyrosine kinase inhibitor. Our biochemical kinase assay showed that AP24534 is potent against wild-type FGFR1-4 and 5 mutant FGFRs (V561M-FGFR1, N549H-FGFR2, K650E-FGFR3, G697C-FGFR3, N535K-FGFR4) and possesses the strongest kinase-inhibitory activity on N549H-FGFR2 (IC50 of 0.5 nM) among all FGFRs t
Cancer is one of the leading causes of death globally, accounting for an estimated 8 million deaths each year. As a result, there have been urgent unmet medical needs to discover novel oncology drugs. Natural and synthetic lactones have a broad spectrum of biological uses including anti-tumor, anti-helminthic, anti-microbial, and anti-inflammatory activities. Particularly, several natural and synthetic lactones have emerged as anti-cancer agents over the past decades. In this review, we address
Focal adhesion kinase (FAK) is overexpressed in highly invasive and metastatic cancers. To identify novel FAK inhibitors, we designed and synthesized various thieno[3,2-<i>d</i>]pyrimidine derivatives. An intensive structure-activity relationship (SAR) study led to the identification of <b>26</b> as a lead. Moreover, <b>26</b>, a multitargeted kinase inhibitor, possesses excellent potencies against FLT3 mutants as well as FAK. Gratifyingly, <b>26</b> remarkably inhibits recalcitrant FLT3 mutants
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