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.
Tucatinib (Irbinitinib, ONT-380, ARRY-380) 是一种具有口服活性、可逆的、ATP竞争性的的ErbB2(HER2)小分子抑制剂。在细胞实验中,ARRY-380对ErbB-2和p95 HER2的IC50s分别为8 nM和7 nM,对HER2的选择性是对EGFR的500倍。具有潜在的抗肿瘤活性。
MoreSD-36 是一种强效、选择性和有效的 PROTAC 降解剂,可降解 STAT3 蛋白,Kd 约为 50 nM。它还能有效降解细胞中突变的 STAT3 蛋白并抑制 STAT3 的转录活性,IC50 为 10 nM。它还具有抗肿瘤活性。
More一种口服有效的STAT6抑制剂,IC50为1.9nM。AS1810722显示出良好的CYP3A4抑制作用,一种稠合双环嘧啶衍生物,具有用于过敏性疾病,例如哮喘和特应性疾病研究的潜力。
MoreKT-333 是同类首创、强效且选择性的异双功能STAT3降解剂,可募集VHL E3连接酶进行泛素-蛋白酶体介导的降解。它在ALK⁺间变性大细胞淋巴瘤 (ALCL) 的临床前模型中诱导出强大的抗肿瘤活性。
MoreRalometostat (TNG908) is a potent, selective, and brain-penetrant PRMT5 inhibitor with an IC50 of 4 μM, exerting its effect through an MTA synergistic mechanism. It also demonstrates antitumor activity in xenograft models.
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