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137 条记录 (耗时 0.04 秒)

    A METHOD FOR REGULATING CANCER STEM CELL GROWTH BY INHIBITING PHOSPHORYLATION OF 120TH THREONINE RESIDUE OF TSPYL5 PROTEIN, A COMPOSITION CONTAINING THE PEPTIDE SEQUENCE FUNCTIONING TO INHIBIT THE PHOSPHORYLATION AND A USE THEREOF
    13.
    发明申请
    A METHOD FOR REGULATING CANCER STEM CELL GROWTH BY INHIBITING PHOSPHORYLATION OF 120TH THREONINE RESIDUE OF TSPYL5 PROTEIN, A COMPOSITION CONTAINING THE PEPTIDE SEQUENCE FUNCTIONING TO INHIBIT THE PHOSPHORYLATION AND A USE THEREOF 审中-公开
    一种通过抑制TSPYL5蛋白质的第120位残基的磷酸化来调节癌症干细胞生长的方法，所述TSPYL5蛋白质是一种含肽功能抑制磷酸化作用的肽组合物及其用途

    公开(公告)号：WO2017217782A1

    公开(公告)日：2017-12-21

    申请号：PCT/KR2017/006240

    申请日：2017-06-15

    申请人： KOREA ATOMIC ENERGY RESEARCH INSTITUTE

    发明人： KIM, In Gyu ,  KIM, Seo Yeon ,  LEE, Jei Ha ,  CHOI, Soo Im ,  KIM, Min Sik ,  KIM, Jung Yul ,  SHIN, Byungchul ,  JUNG, Uhee

    IPC分类号： C07K7/08 ,  C12N5/095 ,  A61K38/10

    CPC分类号： A61K38/02 ,  A61K38/00 ,  A61P35/04 ,  C07K7/08 ,  C07K14/4702

    摘要： The present invention relates to a peptide suppressing the phosphorylation of threonine(T120), the 120th residue of TSPYL5(testis-specific Y-like protein 5), which is specifically as follows. The present inventors constructed T120D, the mutant of the 120th residue threonine(T120) of TSPYL5, and T120A-TSPYL5 gene and then transfected cells with them in order to investigate the effect of phosphorylation on T120 residue. As a result, wild-type TSPYL5 and T120D moved into nucleus and stayed there. But in the case of T120A-TSPYL5, TSPYL5 did not move into nucleus and instead it was expressed only in cytoplasm. The protein could not bind to AKT, either. Instead, ubiquitination of TSPYL5 was increased but SUMOylation was inhibited. Also, the expressions of ALDH1-A1, -A3, CD44 gene and protein were reduced, and thereby the growth and metastasis of lung cancer cells were suppressed and sphere formation was reduced. Based on the observation above, the inventors constructed the peptide composed of the amino acid sequences represented by SEQ. ID. NO: 43 or NO: 44 that could inhibit phosphorylation of the 120th residue threonine of TSPYL5. The said peptide can be effectively used as a composition for the inhibition of cancer cell growth, metastasis, and cancer stem cell growth.

    摘要翻译： 本发明涉及抑制TSPYL5（睾丸特异性Y样蛋白5）的第120个残基苏氨酸（T120）磷酸化的肽，具体如下。 本发明人构建了T120D，TSPYL5的第120个残基苏氨酸（T120）和T120A-TSPYL5基因的突变体，然后用它们转染细胞以研究磷酸化对T120残基的影响。 结果，野生型TSPYL5和T120D进入细胞核并停留在那里。 但在T120A-TSPYL5的情况下，TSPYL5不进入细胞核，而是仅在细胞质中表达。 蛋白质也不能与AKT结合。 相反，TSPYL5泛素化增加，但SUMO化受到抑制。 此外，ALDH1-A1，-A3，CD44基因和蛋白质的表达降低，由此肺癌细胞的生长和转移受到抑制并且球形成减少。 基于上述观察，本发明人构建了由SEQ.ID.No.1所代表的氨基酸序列组成的肽。 ID。 NO：43或NO：44可抑制TSPYL5的第120位苏氨酸的磷酸化。 所述肽可以有效地用作抑制癌细胞生长，转移和癌症干细胞生长的组合物。

    MODULATORS OF THE P70S6 KINASE FOR USE IN THE TREATMENT OF BRAIN DISORDERS AND TRIPLE-NEGATIVE BREAST CANCER
    17.
    发明申请
    MODULATORS OF THE P70S6 KINASE FOR USE IN THE TREATMENT OF BRAIN DISORDERS AND TRIPLE-NEGATIVE BREAST CANCER 审中-公开
    用于治疗脑梗塞和三阴性乳腺癌的P70S6激酶的调节剂

    公开(公告)号：WO2016131776A1

    公开(公告)日：2016-08-25

    申请号：PCT/EP2016/053172

    申请日：2016-02-15

    申请人： SENTINEL ONCOLOGY LIMITED

    发明人： BOYLE, Robert George ,  WALKER, David Winter

    IPC分类号： C07D403/04 ,  A61K31/498 ,  A61K31/53 ,  A61P35/00 ,  A61P25/00

    CPC分类号： C07D403/12 ,  A61K31/498 ,  A61K31/53 ,  A61P35/04 ,  C07D403/04

    摘要： The invention provides compounds for use in the treatment of a disease or condition selected from brain disorders and triple-negative breast cancer, the compounds being of the formula (1) or a salt or tautomer thereof; wherein: X 1 is N or N+(O'); X 2 is N or CH; Q is selected from a C1-3 alkylene group, cyclopropane-1,1-diyl and cyclobutane- 1,1-diyl; R 1 is selected from hydrogen and C 1-4 alkyl;R 2 , R 3 and R 4 are the same or different and each is selected from hydrogen and fluorine; Ar 1 is a benzene, thiophene, naphthyl or pyridine ring optionally substituted with 1, 2 or 3 substituents selected from fluorine; chlorine; bromine; CM hydrocarbyl; C 1-4 hydrocarbyloxy; trifluoromethyl; difluoromethyl; cyano; trifluoromethoxy; difluoromethoxy; Ar 2 is a monocyclic 5- or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S and being optionally substituted with 1, 2 or 3 substituents selected from fluorine; C 1-4 hydrocarbyl; amino; mono-C 1-4 hydrocarbylamino and di-C 1-4 hydrocarbylamino; and wherein, in each substituent consisting of or containing C 1-4 hydrocarbyl, the C 1-4 hydrocarbyl is selected from C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, cyclopropyl, cyclobutyl and cyclopropylmethyl.

    摘要翻译： 本发明提供了用于治疗选自脑疾病和三阴性乳腺癌的疾病或病症的化合物，所述化合物为式（1）或其盐或互变异构体; 其中：X1是N或N +（O'）; X2是N或CH; Q选自C 1-3亚烷基，环丙烷-1,1-二基和环丁烷-1,1-二基; R1选自氢和C1-4烷基; R2，R3和R4相同或不同，各自选自氢和氟; Ar1是任选被1,2或3个选自氟取代的取代基的苯，噻吩，萘基或吡啶环; 氯; 溴; CM烃基; C 1-4烃氧基; 三氟甲基; 二氟; 氰基; 三氟甲氧基; 二氟甲氧基; Ar2是含有1,2或3个选自O，N和S的杂原子环成员并且任选被1,2或3个选自氟取代的取代基的单环5或6元杂芳基环; C 1-4烃基; 氨基; 单-C 1-4烃基氨基和二-C 1-4烃基氨基; 并且其中，在由或含有C 1-4烃基的每个取代基中，C 1-4烃基选自C 1-4烷基，C 2-4烯基，C 2-4炔基，环丙基，环丁基和环丙基甲基。