Ephrin Receptor
Eph proteins belong to the superfamily of transmembrane Tyr kinase receptors. They were initially identified in human carcinomas, in which they are significantly overexpressed. One example of a process regulated by ephrin–Eph signalling is developmental cell sorting at tissue compartment boundaries, through which two separate cellular populations sharing a stable border can emerge from initially intermingled populations. Another important ephrin–Eph signalling-mediated process discussed here is axon guidance in neurons, which leads to the collapse or immobilization of axonal growth cones. Cancer, synaptic plasticity and many physiological processes such as vasculogenesis involve short-distance cell–cell communication and also rely on ephrin–Eph signalling.
All Eph receptors are composed of the following domains: an extracellular globular ligand-binding domain; a Cys domain (comprising sushi and epidermal growth factor (EGF)-like motifs); fibronectin domains; a transmembrane domain; an intracellular Tyr kinase domain adjacent to a sterile alpha motif (SAM); and a PDZ domain. Eph receptors have been classified into EphA or EphB subfamilies (there are nine EphA and five EphB rodent members in current genomic databases) depending on whether they preferentially bind to membrane-anchored (glycophosphatidylinositol (GPI)-linked) or transmembrane ephrin ligands, referred to as ephrin-As and ephrin-Bs, respectively. Signals generated by ephrin binding to Eph receptors involve their interaction with specific intracellular proteins, including non-catalytic region of Tyr kinase adaptor protein 1 (Nck1) and Nck2, phosphoinositide 3-kinase (PI3K), Src family kinases, Vav2, Vav3 and ephexin. In turn, these effectors are coupled to Rho GTPases such as Rac1 and RhoA, which can modulate the cytoskeleton.
References
1.Kania A, Klein R. Nat Rev Mol Cell Biol. 2016;17(4):240–256.
All Eph receptors are composed of the following domains: an extracellular globular ligand-binding domain; a Cys domain (comprising sushi and epidermal growth factor (EGF)-like motifs); fibronectin domains; a transmembrane domain; an intracellular Tyr kinase domain adjacent to a sterile alpha motif (SAM); and a PDZ domain. Eph receptors have been classified into EphA or EphB subfamilies (there are nine EphA and five EphB rodent members in current genomic databases) depending on whether they preferentially bind to membrane-anchored (glycophosphatidylinositol (GPI)-linked) or transmembrane ephrin ligands, referred to as ephrin-As and ephrin-Bs, respectively. Signals generated by ephrin binding to Eph receptors involve their interaction with specific intracellular proteins, including non-catalytic region of Tyr kinase adaptor protein 1 (Nck1) and Nck2, phosphoinositide 3-kinase (PI3K), Src family kinases, Vav2, Vav3 and ephexin. In turn, these effectors are coupled to Rho GTPases such as Rac1 and RhoA, which can modulate the cytoskeleton.
References
1.Kania A, Klein R. Nat Rev Mol Cell Biol. 2016;17(4):240–256.
Tyrosine Kinase
Ephrin Receptor
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UniPR505
产品货号 : M36518
cas no: 2938227-14-4
UniPR505 (Compound 14) 是一种 EphA2 拮抗剂,IC50 值为 0.95 μM。UniPR505 表现出抗血管生成特性。 -
KYL
产品货号 : M30656
cas no: 676657-00-4
EphA4 receptor tyrosine kinase inhibitor (Kd = 0.8 μM); inhibits EphA4-EphrinA5 interactions (IC50 = 6.34 μM). Prevents AβO induced synaptic damage, dendritic spine loss and prevents the blocking of LTP in hippocampal CA3-CA1 transmissions. Exhibits a long half life in cell culture media (8 and 12 hours in PC3 and C2C12 media respectively). Neuroprotective. -
123C4
产品货号 : M29586
cas no: 2034159-30-1
123C4 是受体酪氨酸激酶 EPHA4 (Ki=0.65 μM) 的有效、选择性和竞争性激动剂。 -
AWL-II-38.3
产品货号 : M28187
cas no: 1135205-94-5
AWL-II-38.3 是一种有效的肝配蛋白 A 受体 (EphA3) 激酶抑制剂。 AWL-II-38.3 不表现出显着的针对 Src 家族激酶或 b-raf 的细胞活性。 -
NVP-BHG712 isomer
产品货号 : M24025
cas no: 2245892-85-5
NVP-BHG712 异构体显示出与 EPHA2 和 EPHB4 的保守非键合。