In some cases, receptor activation caused by ligand binding to a receptor is directly coupled to the cell's response to the ligand. For example, the neurotransmitter GABA can activate a cell surface receptor that is part of an ion channel. GABA binding to a GABAA receptor on a neuron opens a chloride-selective ion channel that is part of the receptor. GABAA receptor activation allows negatively charged chloride ions to move into the neuron, which inhibits the ability of the neuron to produce action potentials.
Zabedosertib (BAY1834845)是一种具有免疫调节潜力的白介素-1受体相关激酶4 (Interleukin-1 receptor-activated kinase 4, IRAK4)抑制剂,IRAK4是一种参与蛋白激酶信号Toll样受体先天免疫反应的蛋白激酶
MoreEmavusertib (CA-4948) 是一种有效的、口服生物可利用的 interleukin-1 receptor-associated kinase 4/FMS-like Tyrosine Kinase 3 (IRAK4/FLT3) 的抑制剂,具有抗肿瘤活性
MoreACBI3 是一种选择性强效的泛 KRAS PROTAC 降解剂,能够促进 VHL 结合、三元复合物形成以及 E3 连接酶依赖的 KRAS 降解,且在蛋白质组范围内具有高选择性。它表现出强大的抗肿瘤活性,可在 KRAS 驱动的癌症中实现持久的通路调控和肿瘤消退
MoreRMC-7977 是一种强效、可逆、三重复合口服抑制剂,可选择性靶向活性(GTP 结合)形式的 KRAS、HRAS 和 NRAS,对突变型和野生型变体均具有广谱活性(RASMULTI (ON) 抑制剂)。它还对胰腺导管腺癌 (PDAC) 表现出显著的抗肿瘤功效
MoreZoldonrasib (RMC-9805) 是一种有效且具有口服活性的 KRAS G12D 抑制剂。Zoldonrasib 可诱导KRAS G12D 突变型癌细胞凋亡 (apoptosis)。Zoldonrasib 具有研究 KRAS G12D 突变癌症的潜力
More
