COMPOUND FOR INHIBITING TANKYRASE, AND MEDICAL USE THEREOF

• Main Authors: AHN, Ji-Yeon, KIM, Young Hoon, BAE, Su Yeal, KIM, Jae-Sung, SONG, Jie Young, SEO, Hye-Ran, HWANG, Sang Gu, KIM, Hyo Jeong, RYU, Hwani, CHOI, Na Young, KIM, Bo Kyoung
• Format: Patent
• Language: English; French; Korean
• Published: 25.05.2023
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention relates to a compound for inhibiting tankyrase, and medical use thereof. Since the compound according to the present invention inhibits the activity of enzyme tankyrase (TNKS), inhibits target β-catenin gene expression and active β-catenin protein expression, stabilizes the AXIN2 protein level, and exhibits anti-cancer activity in human colon cancer cell lines, the compound can be used as an anti-cancer agent. In addition, when coadministered with a conventional anti-cancer agent 7-ethyl-10-hydroxycamptothecin (SN-38) or fluorouracil (5-FU), the compound exhibits synergistic effects in anti-cancer activity, and thus can be used in a combination therapy with a conventional anti-cancer agent. La présente invention concerne un composé pour inhiber la tankyrase, et son utilisation médicale. Comme le composé selon la présente invention inhibe l'activité de l'enzyme tankyrase (TNKS), inhibe l'expression du gène de la β-caténine cible et l'expression de la protéine β-caténine active, stabilise le niveau de protéine AXIN2, et présente une activité anticancéreuse dans les lignées cellulaires du cancer du côlon humain, le composé peut être utilisé en tant qu'agent anticancéreux. De plus, lorsqu'il est co-administré avec un agent anticancéreux classique 7-éthyle-10-hydroxycamptothécine (SN-38) ou le fluorouracile (5-FU), le composé présente des effets synergiques dans l'activité anticancéreuse, et peut donc être utilisé dans une polythérapie avec un agent anticancéreux classique. 본 발명은 탄키라제 억제용 화합물 및 이의 의학적 용도에 관한 것으로, 본 발명에 따른 화합물은 탄키라제(TNKS) 효소 활성을 억제하며, 베타-카테닌(β-catenin) 타겟 유전자 발현과 활성 베타-카테닌 단백질 발현을 억제하고, AXIN2 단백질 수준을 안정화 시키며, 인체 대장암 세포주에서 항암활성을 나타내므로, 상기 화합물을 항암제로 활용할 수 있고, 또한, 상기 화합물은 기존 항암제인 7-에틸-10-하이드록시캄프토테신(7-Ethyl-10-hydroxycamptothecin; SN-38] 또는 플루오로우라실(fluorouracil; 5-FU)과 병용 시 항암활성에서 시너지 효과를 나타내므로, 기존 항암제와의 병용요법으로 활용할 수 있다.