肺癌可用靶点——CDH17

一、靶点介绍

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]

+ f0 E+ f3 I7 x) P  B3 e( O$ {

二、可用药物

  B; N9 ~2 j6 L. r3 {/ ?% ^$ `, ]BI 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。
3 ~/ d2 H) H: c: [! P+ W5 j
7 q3 I6 s/ f- ~, T: ~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] 

) j! E' ], U+ _, g

三、参考文献

[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
[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/