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1. (WO2016058547) HIGH ACTIVITY TUMOUR INHIBITOR AND PREPARATION METHOD AND USE THEREOF
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2016/058547 International Application No.: PCT/CN2015/092021
Publication Date: 21.04.2016 International Filing Date: 15.10.2015
IPC:
C07K 7/08 (2006.01) ,C07K 14/00 (2006.01) ,A61K 38/10 (2006.01) ,A61K 38/16 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
7
Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
04
Linear peptides containing only normal peptide links
08
having 12 to 20 amino acids
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
14
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
04
Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
10
Peptides having 12 to 20 amino acids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
16
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
上海宝恒泓康生物技术有限公司 BAO KANG BIOMEDICAL HEALTHCARE INC [CN/CN]; 中国上海市 浦东新区新金桥路27号8号楼2楼 Floor 2, Building No. 8, No. 27 Xinjinqiao Road, Pudong New Area District Shanghai 201206, CN
Inventors:
李康善 LI, Kangshan; CN
Agent:
上海一平知识产权代理有限公司 XU & PARTNERS, LLC.; 中国上海市 普陀区真北路958号天地科技广场1号楼106室 Room No. 106, Building No. 1 Universal High-Tech Plaza 958 Zhen Bei Road, Putuo District Shanghai 200333, CN
Priority Data:
201410555112.317.10.2014CN
Title (EN) HIGH ACTIVITY TUMOUR INHIBITOR AND PREPARATION METHOD AND USE THEREOF
(FR) INHIBITEUR D'ACTIVITÉ DE TUMEUR HAUT ACTIVITÉ ET UTILISATION DE CELUI-CI
(ZH) 高活性的肿瘤抑制剂及其制法和应用
Abstract:
(EN) Provided in the present invention are a YAP protein inhibiting polypeptide and a use thereof. In particular, the present invention obtains a key binding site of a YAP protein and TEAD, screens out a polypeptide with the best YAP inhibitory activity and modifies the polypeptide, for example by adding a disulfide linkage, replacing an amino acid, deleting and/or adding (for example, adding a cell-penetrating fragment), and finally screens, verifies and obtains a series of polypeptides with a YAP protein activity inhibiting effect and good stability. Experiments demonstrate that the polypeptide of the present invention can effectively inhibit the binding activity between YAP protein and TEAD, thus providing a good therapeutic effect on digestive tract tumours (especially liver cancer).
(FR) La présente invention concerne un polypeptide inhibiteur de protéine YAP et son utilisation. La présente invention obtient notamment un site de liaison clé d'une protéine YAP et de TEAD, crible un polypeptide ayant la meilleure activité d'inhibition de YAP et modifie le polypeptide, par exemple, par l'ajout d'une liaison disulfure, le remplacement d'un acide aminé, la suppression et/ou l'ajout (par exemple l'ajout d'un fragment de pénétration cellulaire) et enfin crible, vérifie et obtient une série de polypeptides ayant un effet d'inhibition de l'activité de la protéine YAP et une bonne stabilité. Des expériences montrent que le polypeptide de l'invention permet d'inhiber efficacement l'activité de liaison entre la protéine YAP et TEAD, ce qui donne un bon effet thérapeutique sur les tumeurs du tractus digestif (en particulier le cancer du foie).
(ZH) 本发明提供了YAP蛋白抑制多肽及其应用。具体地,本发明获得了YAP蛋白与TEAD的关键结合位点,筛选出YAP抑制活性最佳的多肽并对其进行改造,例如加入二硫键、对氨基酸进行替换、缺失和/或添加(如加入细胞穿透片段),并最终筛选并验证获得了具有YAP蛋白活性抑制作用且稳定性良好的系列多肽。实验证明,本发明多肽能够有效抑制YAP蛋白与TEAD结合活性,从而对消化道肿瘤(尤其是肝癌)具有良好的治疗作用。
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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, 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 (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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: Chinese (ZH)
Filing Language: Chinese (ZH)