1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. Discoidin Domain Receptor

Discoidin Domain Receptor (盘状结构域受体)

盘状蛋白结构域受体 (DDR) 是跨膜受体酪氨酸激酶 (RTK) 超家族的成员,与其他受体的区别在于,盘状蛋白结构域中存在盘状蛋白基序,并且利用胶原蛋白作为内部配体。已鉴定出两种类型的 DDR,即 DDR1 和 DDR2,具有不同的表达谱和配体特异性。

与胶原蛋白结合后,DDR 会传导涉及各种细胞功能的细胞信号,包括细胞粘附、增殖、分化、迁移和基质稳态。由突变或过表达导致的 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。DDR 已被视为药物发现的新型潜在分子靶点,并且人们正在加大力度,以识别针对该受体的新型小分子抑制剂。

Discoidin domain receptors (DDRs) are members of the transmembrane receptor tyrosine kinase (RTK) superfamily which are distinguished from others by the presence of a discoidin motif in the extracellular domain and their utilization of collagens as internal ligands. Two types of DDRs, DDR1 and DDR2, have been identified with distinct expression profiles and ligand specificities.

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. DDRs have been considered as novel potential molecular targets for drug discovery and increasing efforts are being devoted to the identification of new small molecule inhibitors targeting the receptors.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-176849
    DDR1-IN-12 Inhibitor
    DDR1-IN-12 (Compound 7t) 是一种高选择性的盘状结构域受体 1 (DDR1) 抑制剂 (IC50=0.126 μM)。DDR1-IN-12 能够阻断受体酪氨酸激酶的自身磷酸化以及下游信号传导 (例如抑制 TGF-β1 诱导的成纤维细胞活化),从而抑制肿瘤细胞迁移和肺纤维化进展。DDR1-IN-12 有望用于肺癌 (尤其是肺腺癌) 的研究。
    DDR1-IN-12
  • HY-162540
    LLC355 Degrader
    LLC355 是一种盘状结构域受体 1 (DDR1) ATTEC 降解剂。LLC355 可有效降解 DDR1 蛋白,在非小细胞肺癌 NCI-H23 细胞中的 DC50 值为 150.8 nM。LLC355 通过溶酶体介导的自噬诱导 DDR1 降解。LLC355 可有效抑制癌细胞的致瘤性、迁移和侵袭。
    LLC355
  • HY-162102
    DDR1-IN-8 Inhibitor
    DDR1-IN-8 (compound 7s) 是一种有效的 DDR1/2 抑制剂,IC50 值分别为 0.045 μM 和 0.126 μM,DDR1-IN-8 具有抗肿瘤活性。
    DDR1-IN-8
  • HY-122848
    DDR1/2 inhibitor-3 Inhibitor
    DDR1/2 inhibitor-3 (5n) 是 DDR1/2 的抑制剂,IC50 值分别为 9.4 和 20.4 nM。DDR1/2 inhibitor-3 可用于抗炎研究。
    DDR1/2 inhibitor-3
  • HY-W778154
    O,O-Dimethyl dithiophosphate-13C2 ammonium Inhibitor
    O,O-Dimethyl dithiophosphate-13Csub>2 ammonium 是 O,O-Dimethyl dithiophosphate ammonium 的 13C 标记的同位素。
    O,O-Dimethyl dithiophosphate-<sup>13</sup>C<sub>2</sub> ammonium
  • HY-13979A
    DDR1-IN-1 dihydrochloride Inhibitor
    DDR1-IN-1 dihydrochloride是DDR1受体酪氨酸激酶抑制剂,IC50 值为105 nM,而对 DDR2 的 IC50 为413 nM。
    DDR1-IN-1 dihydrochloride
目录号 产品名 / 同用名 种属 表达系统
目录号 产品名 / 同用名 应用 反应物种

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.