登录 | 注册    关注公众号  
搜索
 > 【TIE2】

TIE2信息

英文名称:TEK receptor tyrosine kinase
中文名称:泰克酪氨酸激酶
靶点别称:EC:2.7.10.1,Endothelial Tyrosine Kinase,Tyrosine-protein kinase receptor TEK,Tunica interna endothelial cell kinase,Angiopoietin-1 receptor,p140 TEK,Tyrosine kinase with Ig and EGF homology domains-2,TEK,TEK Receptor Tyrosine Kinase,Tyrosine-Protein Kinase Receptor TIE-2,TEK Tyrosine Kinase, Endothelial,VMCM1,VMCM,TIE2,Venous Malformations, Multiple Cutaneous And Mucosal,CD202b Antigen,EC 2.7.10.1,CD202B,GLC3E,TIE-2,HTIE2,Receptor, TIE-2,EC 2.7.10
上市药物数量:4
临床药物数量:8
最高研发阶段:批准上市

TIE2 分子别名

TIE2,Tie-2,TEK,VMCM, VMCM1,CD202b,Angiopoietin-1 receptor

TIE2 分子背景

Tyrosine-protein kinase that acts as cell-surface receptor for ANGPT1, ANGPT2 and ANGPT4 and regulates angiogenesis, endothelial cell survival, proliferation, migration, adhesion and cell spreading, reorganization of the actin cytoskeleton, but also maintenance of vascular quiescence. Has anti-inflammatory effects by preventing the leakage of proinflammatory plasma proteins and leukocytes from blood vessels. Required for normal angiogenesis and heart development during embryogenesis. Required for post-natal hematopoiesis. After birth, activates or inhibits angiogenesis, depending on the context. Inhibits angiogenesis and promotes vascular stability in quiescent vessels, where endothelial cells have tight contacts. In quiescent vessels, ANGPT1 oligomers recruit TEK to cell-cell contacts, forming complexes with TEK molecules from adjoining cells, and this leads to preferential activation of phosphatidylinositol 3-kinase and the AKT1 signaling cascades. In migrating endothelial cells that lack cell-cell adhesions, ANGT1 recruits TEK to contacts with the extracellular matrix, leading to the formation of focal adhesion complexes, activation of PTK2/FAK and of the downstream kinases MAPK1/ERK2 and MAPK3/ERK1, and ultimately to the stimulation of sprouting angiogenesis. ANGPT1 signaling triggers receptor dimerization and autophosphorylation at specific tyrosine residues that then serve as binding sites for scaffold proteins and effectors. Signaling is modulated by ANGPT2 that has lower affinity for TEK, can promote TEK autophosphorylation in the absence of ANGPT1, but inhibits ANGPT1-mediated signaling by competing for the same binding site. Signaling is also modulated by formation of heterodimers with TIE1, and by proteolytic processing that gives rise to a soluble TEK extracellular domain. The soluble extracellular domain modulates signaling by functioning as decoy receptor for angiopoietins. TEK phosphorylates DOK2, GRB7, GRB14, PIK3R1; SHC1 and TIE1.

TIE2 前沿进展

TIE2上市药物信息

英文名称 中文名称 研发代码 研发阶段 公司 最早商品名 最早批准国家 最早适应症 最早批准公司 最早批准日期 适应症 临床试验
Ponatinib Hydrochloride 盐酸普纳替尼 AP24534 hydrochloride; AP24534-HCL; AP24534 HCl; INCB-84344; AP-24534 批准上市 Ariad Iclusig Japan 急性淋巴细胞白血病, 慢性髓细胞白血病 Otsuka Holdings Co Ltd 2012-12-14 急性淋巴细胞白血病, 非小细胞肺癌, 双表型急性白血病, 淋巴瘤, 急性髓细胞样白血病, 慢性髓样白血病, 胃肠道间质瘤, 费城染色体, 甲状腺髓样癌, 慢性髓细胞白血病, 原始细胞危象, 小细胞肺癌, 肺腺癌, 实体瘤, 髓系白血病加速期, 白血病, 血液肿瘤 详情
Ripretinib 瑞派替尼 DCC-2618 批准上市 Deciphera 擎乐, Qinlock United Kingdom 胃肠道间质瘤 Deciphera Pharmaceuticals Llc 2020-05-15 肿瘤, 系统性肥大细胞增多症, 胃肠道间质瘤 详情
Regorafenib 瑞戈非尼 DAST; BAY-73-4506 批准上市 拜耳 Stivarga, Resihance Mainland China 胃肠道间质瘤 Bayer Pharma Ag 2012-09-27 急性髓细胞样白血病, 肉瘤, 胃泌素瘤, 结直肠癌, 胃肠道间质瘤, 胆道癌, 腹膜癌, 非霍奇金淋巴瘤, 肺癌, 腺样囊性癌, 甲状腺瘤, 输卵管癌, 肝细胞癌, 黑色素瘤, 转移癌, 胃肠道癌症, 生长抑制素瘤, 实体瘤, 胰高血糖素瘤, 多发性骨髓瘤, 胰腺癌, 卵巢上皮癌, 移行细胞癌, 肿瘤, 胶质母细胞瘤, 结肠癌, 血管肉瘤, 胰岛细胞癌, 胰岛素瘤, 类癌瘤, 直肠癌, 肾细胞癌, 卵巢癌 详情
Cabozantinib S-malate 苹果酸卡博替尼 XL-184; BMS-907351 批准上市 Exelixis Inc Cometriq, Cabometyx Japan 肾细胞癌 Takeda 2012-11-29 甲状腺瘤, 滤泡性腺癌, 脑癌, 肉瘤, 神经母细胞瘤, 丛状神经纤维瘤, 前列腺癌, 胆管上皮癌, 结直肠癌, 星形细胞瘤, 肝功能衰退, 胆道癌, 中枢神经系统肿瘤, 淋巴瘤, 急性髓细胞样白血病, 胶质瘤, 神经内分泌癌, 肝细胞癌, 生殖细胞和胚胎肿瘤, 非小细胞肺癌, 腺癌, 甲状腺乳头状瘤, 脑膜瘤, 移行细胞癌, 肾肿瘤, 卵巢生殖细胞肿瘤, 骨转移, 肾细胞癌, 肝脏移植排斥, 食道癌, 疼痛, 胃癌, Merkel细胞癌, 胶质母细胞瘤, 精原细胞瘤, 实体瘤, 神经纤维瘤病, 肿瘤, 唾腺癌, 乳头状癌, 皮肤肿瘤, 肾脏疾病, 神经内分泌瘤, 肾上腺皮质细胞癌, 去势抵抗性前列腺肿瘤, 多发性骨髓瘤 详情

TIE2临床药物信息

英文名称 研发代码 研发阶段 公司 适应症 临床试验
CEP-11981 ESK-981; CEP-11981; SSR-106462; BOL-303213X 临床二期 赛诺菲 前列腺癌 详情
Gersizangitide AXT-107 AsclepiX Therapeutics Inc 详情
Altiratinib DP-5164; DCC-2701; DCC-22701; T-678746713 Deciphera 详情
Trebananib AMG-386; 20060439 安进, Takeda Pharmaceutical Co Ltd 详情
Pexmetinib ARRY-614 Array Biopharma 详情
Razuprotafib AKB-9778 Akebia Therapeutics Inc 详情
Rebastinib Tosylate DP-1919; DCC-2036; DP-1919.TO Deciphera 详情
QBH-196 QBH-196 临床一期 沈阳药科大学 实体瘤, 胃癌 详情
Sitravatinib IND-155305; MG-516; MG-91516; MGCD-516 临床三期 Mirati Therapeutics 输尿管肿瘤, 黑色素瘤, 胃肠道癌症, 非小细胞肺癌, 肝细胞癌, 肺癌, 口腔癌, 鳞状细胞癌, 子宫内膜癌, 食管鳞状细胞癌, 肝功能衰退, 实体瘤, 乳腺癌, 脂肪肉瘤, 肺疾病, 三阴性乳腺肿瘤, 移行细胞癌, 肿瘤, 肾细胞癌, 转移性上皮癌, 头颈部鳞状细胞癌, 胆管癌 详情

消息提示

请输入您的联系方式,再点击提交!

确定