The Journey of DDR1 and DDR2 Kinase Inhibitors as Rising Stars in the Fight Against Cancer.
The Journey of DDR1 and DDR2 Kinase Inhibitors as Rising Stars in the Fight Against Cancer.
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DOI：
10.3390/ijms22126535
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发表时间：
2021-06-18
影响因子：
5.6
通讯作者：
Lee K
中科院分区：
文献类型：
--
作者：
Elkamhawy A;Lu Q;Nada H;Woo J;Quan G;Lee K
盘状蛋白结构域受体（disidin domain receptor， DDR）是一种胶原活化受体酪氨酸激酶，在调节细胞的形态发生、分化、增殖、粘附、迁移、侵袭和基质重塑等重要过程中起着至关重要的作用。因此，DDR失调已被归因于多种人类癌症疾病，例如，除了一些炎症和神经退行性疾病外，非小细胞肺癌（NSCLC）、卵巢癌、胶质母细胞瘤和乳腺癌。自20世纪90年代初发现靶点至今，人们一直致力于DDR抑制剂的开发。从药物化学的角度，我们试图揭示最有前途的DDR1和DDR2小分子抑制剂的开发进展，包括它们的设计方法、构效关系（SAR）、生物活性和选择性。
Discoidin domain receptor (DDR) is a collagen-activated receptor tyrosine kinase that plays critical roles in regulating essential cellular processes such as morphogenesis, differentiation, proliferation, adhesion, migration, invasion, and matrix remodeling. As a result, DDR dysregulation has been attributed to a variety of human cancer disorders, for instance, non-small-cell lung carcinoma (NSCLC), ovarian cancer, glioblastoma, and breast cancer, in addition to some inflammatory and neurodegenerative disorders. Since the target identification in the early 1990s to date, a lot of efforts have been devoted to the development of DDR inhibitors. From a medicinal chemistry perspective, we attempted to reveal the progress in the development of the most promising DDR1 and DDR2 small molecule inhibitors covering their design approaches, structure-activity relationship (SAR), biological activity, and selectivity.
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影响因子：
5.7
作者：
Carafoli, Federico;Mayer, Marie Cathrin;Shiraishi, Kazushige;Pecheva, Mira Anguelova;Chan, Lai Yi;Nan, Ruodan;Leitinger, Birgit;Hohenester, Erhard
通讯作者：
Hohenester, Erhard
影响因子：
--
作者：
Al-Kindi A;Kizhakkedath P;Xu H;John A;Sayegh AA;Ganesh A;Al-Awadi M;Al-Anbouri L;Al-Gazali L;Leitinger B;Ali BR
通讯作者：
Ali BR
影响因子：
9.8
作者：
Bargal, Ruth;Cormier-Daire, Valerie;Raas-Rothschild, Annick
通讯作者：
Raas-Rothschild, Annick
影响因子：
3.5
作者：
Dong, Ru;Zhou, Xin;Sun, Li-Ping
通讯作者：
Sun, Li-Ping
影响因子：
4
作者：
Castro-Sanchez, Luis;Soto-Guzman, Adriana;Perez Salazar, Eduardo
通讯作者：
Perez Salazar, Eduardo