College of Pharmacy, Dongguk University-Seoul, Goyang 10326, Korea.
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
Int J Mol Sci. 2021 Jun 18;22(12):6535. doi: 10.3390/ijms22126535.
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.
Discoidin domain receptor (DDR) 是一种胶原蛋白激活的受体酪氨酸激酶，在调节细胞的形态发生、分化、增殖、黏附、迁移、侵袭和基质重塑等基本过程中发挥着关键作用。因此，DDR 的失调与多种人类癌症疾病有关，例如非小细胞肺癌 (NSCLC)、卵巢癌、胶质母细胞瘤和乳腺癌，以及一些炎症和神经退行性疾病。自 20 世纪 90 年代初发现靶点以来，人们投入了大量精力开发 DDR 抑制剂。从药物化学的角度来看，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。
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