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1. (WO2018026236) METHOD FOR SCREENING ANTICANCER DRUG INHIBITING BINDING OF AIMP2-DX2 AND K-RAS
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.:    WO/2018/026236    International Application No.:    PCT/KR2017/008449
Publication Date: 08.02.2018 International Filing Date: 04.08.2017
IPC:
G01N 33/50 (2006.01), A61K 39/395 (2006.01), A61K 48/00 (2006.01), A61K 39/00 (2006.01)
Applicants: MEDICINAL BIOCONVERGENCE RESEARCH CENTER [KR/KR]; (Iui-dong) 8th Fl., B-dong Advanced Institutes of Convergence Technology, 145 Gwanggyo-ro, Yeongtong-gu, Suwon-si Gyeonggi-do 16229 (KR)
Inventors: KIM, Sunghoon; (KR).
KIM, Dae Gyu; (KR).
ROH, Youn Ah; (KR).
LIM, Semi; (KR)
Agent: LEE, Hee Sook; (JS Building, Yeoksam-dong) 9th Fl. 11, Teheran-ro 33 gil, Gangnam-gu Seoul 06141 (KR)
Priority Data:
10-2016-0099352 04.08.2016 KR
Title (EN) METHOD FOR SCREENING ANTICANCER DRUG INHIBITING BINDING OF AIMP2-DX2 AND K-RAS
(FR) MÉTHODE DE CRIBLAGE D'AGENTS ANTICANCÉREUX INHIBANT LA LIAISON ENTRE AIMP2-DX2 ET K-RAS
(KO) AIMP2-DX2와 K-RAS의 결합을 저해하는 항암제 스크리닝 방법
Abstract: front page image
(EN)The present invention relates to a method for screening an anticancer drug inhibiting the binding of AIMP2-DX2 and K-Ras and, more specifically, to a method for screening an anticancer drug and an anticancer composition containing, as an active ingredient, an anticancer drug selected by the method, wherein the method comprises the steps of: (a) contacting AIMP2-DX2 or a fragment thereof with K-Ras or a fragment thereof in the presence or absence of a test substance; (b) measuring the binding of AIMP2-DX2 and K-Ras in the presence or absence of the test substance; (c) comparing the binding of AIMP2-DX2 and K-Ras in the presence of the test substance with the binding of AIMP2-DX2 and K-Ras in the absence of the test substance, thereby determining a change in the binding level of AIMP2-DX2 and K-Ras due to the test substance; (d) selecting a test substance that reduces the binding level of AIMP2-DX2 and K-Ras; and (e) investigating anticancer activity of the selected test substance in cells or an animal. A compound inhibiting the binding of K-Ras and AIMP2-DX2, which is selected by the screening method of the present invention, has excellent effects of lowering the level of K-Ras protein in a cancer and inhibiting the occurrence and progression of cancer.
(FR)La présente invention concerne une méthode de criblage de médicaments anticancéreux inhibant la liaison entre AIMP2-DX2 et K-Ras, et plus spécifiquement, une méthode de criblage de médicaments anticancéreux et une composition anticancéreuse contenant comme principe actif un médicament anticancéreux sélectionné par cette méthode, la méthode comprenant les étapes consistant : (a) à mettre en contact AIMP2-DX2 ou un fragment de ce dernier avec K-Ras ou un fragment de ce dernier, en présence ou en l'absence d'une substance expérimentale ; (b) à mesurer la liaison formée entre AIMP2-DX2 et K-Ras en présence ou en l'absence de la substance expérimentale ; (c) à comparer la formation de la liaison entre AIMP2-DX2 et K-Ras en présence de la substance expérimentale avec la formation de la liaison entre AIMP2-DX2 et K-Ras en l'absence de la substance expérimentale, permettant ainsi d'estimer le changement du niveau de liaison entre AIMP2-DX2 et K-Ras dû à la substance expérimentale ; (d) à sélectionner les substances expérimentales qui diminuent le niveau de liaison entre AIMP2-DX2 et K-Ras ; et (e) à étudier l'activité anticancéreuse de la substance expérimentale sélectionnée dans des cellules ou chez l'animal. Un composé inhibant la liaison entre K-Ras et AIMP2-DX2 sélectionné par la méthode de criblage de la présente invention possède d'excellents effets qui diminuent le niveau de la protéine K-Ras au sein d'un cancer, et inhibent l’occurrence et la progression du cancer.
(KO)본 발명은 AIMP2-DX2와 K-Ras의 결합을 저해하는 항암제 스크리닝 방법에 관 한 것으로, 보다 상세하게는 (a) 시험 물질의 존재 또는 부존재하에서 AIMP2-DX2 또는 이의 단편과 K-Ras 또는 이의 단편을 접촉시키는 단계; (b) 시험 물질의 존재 또는 부존재하에서의 AIMP2-DX2와 K-Ras의 결합을 측정하는 단계; (c) 시험 물질 존재하에서의 AIMP2-DX2와 K-Ras의 결합과 시험 물질 부존재하에서의 AIMP2-DX2와 K-Ras의 결합을 비교하여 시험 물질에 의한 AIMP2-DX2와 K-Ras의 결합 수준의 변화 를 판단하는 단계; (d) AIMP2-DX2와 K-Ras의 결합 수준을 감소시키는 시험 물질을 선별하는 단계; 및 (e) 선별된 시험 물질의 항암 활성을 세포 또는 동물에서 확인 하는 단계를 포함하는 항암제 스크리닝 방법과 상기 방법으로 선별된 항암제를 유 효성분으로 포함하는 항암용 조성물에 관한 것이다. 본 발명에 상기 스크리닝 방법에 따라 선별된 K-Ras와 AIMP2-DX2의 결합을 억제하는 화합물은 암에서 K-Ras 단백질의 수준을 낮추고 암의 발생과 진행을 억제 하는 효과가 뛰어나다.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG).
Publication Language: Korean (KO)
Filing Language: Korean (KO)