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一、靶点介绍
9 ~+ l7 [, j. T5 d7 O% U1 ]人类肝肠黏着蛋白(human liver-intestine cadherin protein,CDH17)也被称为肠肽相关转运子 HPT-1,肝肠钙粘蛋白(liver-intestine cadherin,Licadherin),最初是在小鼠肝脏发现的一类钙依赖性粘附分子。[1] |
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共2条精彩回复,最后回复于 2022-5-24 10:05
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本帖最后由 小方 于 2022-5-24 11:30 编辑
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二、可用药物
/ N( E/ X0 e' aBI 905711是一种同时靶向TRAILR2和CDH17的新型四价双特异性抗体,是一种专为克服先前策略缺点而设计的新型保肝TRAILR2激动剂。BI 905711能在体外有效地触发CDH17阳性的CRC肿瘤细胞的凋亡。
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BI 905711在CDH17阳性的CRC移植瘤中证明了单药肿瘤消退,与伊立替康联合使用后效果进一步增强。BI 905711以顺式(同一细胞)和反式(相邻细胞)两种方式诱导细胞凋亡,即使在CDH17表达异质的异种移植模型中也转化为显著的抗肿瘤活性。[2] |
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尚未签到
本帖最后由 小方 于 2022-5-24 11:30 编辑
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三、参考文献 7 A1 \- d7 _7 R2 z( T) I
[1]王前玉,戚玉芹,高晓,毛学源,仲竹娟,时潇洋.CDH 17在胃癌组织中的表达及其临床病理诊断价值[J].交通医学,2020,34(05):455-457.DOI:10.19767/j.cnki.32-1412.2020.05.005. http://kns-cnki-net-443.webvpn.y ... KIYT9CbsM-Si00PUSI4
4 ]: {! C* J' I( s: f w3 w[2]Garcia-Martinez Juan Manuel Department of Cancer Cell Signaling, Boehringer Ingelheim RCV GmbH & Co KG juan_manuel.garcia-martinez@boehringer-ingelheim.com. Wang Shirley Boehringer Ingelheim RCV GmbH & Co KG. Weishaeupl Cordula Boehringer Ingelheim RCV GmbH & Co KG. Wernitznig Andreas Boehringer Ingelheim RCV GmbH & Co KG. Chetta Paolo Boehringer Ingelheim RCV GmbH & Co KG. Pinto Catarina Cancer Immunology and Immune Modulation, Boehringer Ingelheim RCV GmbH & CoKG. Ho Jason Biotherapeutics, Boehringer Ingelheim Pharmaceuticals, Inc. Dutcher Darrin Boehringer Ingelheim Pharmaceuticals, Inc. Gorman Philip N Biotherapeutics Discovery, Boehringer Ingelheim Pharmaceuticals, Inc. Kroe-Barrett Rachel Biotherapeutics Molecule Discovery, Boehringer Ingelheim Pharmaceuticals, Inc. Rinnenthal Joerg Department of Cancer Cell Signaling, Boehringer Ingelheim RCV GmbH & Co KG. Giragossian Craig Boehringer Ingelheim Pharmaceuticals, Inc. Impagnatiello Maria Antonietta Translational Research/Pharmacology, Boehringer Ingelheim RCV GmbH & Co KG. Tirapu Iñigo Cancer Immunology and Immune Modulation, Boehringer Ingelheim RCV GmbH & CoKG. Hilberg Frank R&D, Department of Pharmacology, Boehringer Ingelheim RCV GmbH & Co KG. Kraut Norbert Global Department of Cancer Research, Boehringer Ingelheim RCV GmbH & Co KG. Pearson Mark Boehringer Ingelheim RCV GmbH & Co KG. Kuenkele Klaus-Peter NBE Vienna, Boehringer-Ingelheim Gmbh & Co KG. . Selective tumor cell apoptosis and tumor regression in CDH17-positive colorectal cancer models using BI 905711, a novel liver-sparing TRAILR2 agonist.[J]. Molecular cancer therapeutics,2020. https://pubmed.ncbi.nlm.nih.gov/33037135/ |
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