Discoidin domain receptor 1 (DDR1) kinase as target for structure-based drug discovery.
Discoidin domain receptor 1 (DDR1) kinase as target for structure-based drug discovery.
复制标题
DOI：
10.1016/j.drudis.2014.09.025
复制
发表时间：
2015-02
影响因子：
7.4
通讯作者：
Meiler, Jens
中科院分区：
文献类型：
--
作者：
Kethiwale, Sandeepkumar;Borza, Corina M.;Lowe, Edward W., Jr.;Pozzi, Ambra;Meiler, Jens
盘状结构域受体(DDR)1和2是属于受体酪氨酸激酶(RTK)家族的跨膜受体。在胶原结合的基础上，DDRs转导参与多种细胞功能的细胞信号，包括细胞黏附、增殖、分化、迁移和基质动态平衡。突变或过度表达引起的DDR功能改变与多种疾病有关，包括动脉粥样硬化、炎症、癌症和组织纤维化。几种公认的抑制剂，如伊马替尼、达沙替尼和尼洛替尼，最初是作为Abelson小鼠白血病(Abl)激酶抑制剂开发的，已被发现抑制DDR激酶活性。正如我们在这里回顾的那样，最近发现的新型抑制剂及其与DDR1激动域的共晶结构使基于结构的DDR1药物发现变得顺从。
Discoidin domain receptor (DDR) 1 and 2 are transmembrane receptors that belong to the family of receptor tyrosine kinases (RTK). Upon collagen binding, DDRs transduce cellular signaling involved in various cell functions, including cell adhesion, proliferation, differentiation, migration, and matrix homeostasis. Altered DDR function resulting from either mutations or overexpression has been implicated in several types of disease, including atherosclerosis, inflammation, cancer, and tissue fibrosis. Several established inhibitors, such as imatinib, dasatinib, and nilotinib, originally developed as Abelson murine leukemia (Abl) kinase inhibitors, have been found to inhibit DDR kinase activity. As we review here, recent discoveries of novel inhibitors and their co-crystal structure with the DDR1 kinase domain have made structure-based drug discovery for DDR1 amenable.
登录
查看更多内容
影响因子：
2.9
作者：
Kaufmann, Kristian W.;Lemmon, Gordon H.;DeLuca, Samuel L.;Sheehan, Jonathan H.;Meiler, Jens
通讯作者：
Meiler, Jens
影响因子：
7.3
作者：
Gao, Mingshan;Duan, Lei;Ding, Ke
通讯作者：
Ding, Ke
影响因子：
4.6
作者：
Roarty, Kevin;Serra, Rosa
通讯作者：
Serra, Rosa
影响因子：
14.8
作者：
Liu, Y;Gray, NS
通讯作者：
Gray, NS
影响因子：
20.3
作者：
Rix, Uwe;Hantschel, Oliver;Superti-Furga, Giulio
通讯作者：
Superti-Furga, Giulio