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Signal Pathway


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.

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    KT-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。

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  • Ralometostat EY8034

    Ralometostat (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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  • Navlimetostat EY8033

    MRTX1719 is a potent and selective inhibitor of the protein arginine methyltransferase 5·methylthioadenosine phosphorylase complex (PRMT5·MTA), which serves as a potential selective therapeutic target for tumor intervention.

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  • Onametostat EY8032

    Onametostat (JNJ-64619178)是PRMT5抑制剂，具有较高的选择性和效力（PRMT5-MEP-50, IC50=0.14 nM）、良好的药代动力学特性以及安全性

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  • Copanlisib EY8031

    Copanlisib是一个高效的泛I型 PI3K抑制剂，其对PI3Kα/β/γ/δ抑制的IC50分别为0.5, 3.7, 6.4, and 0.7 nM。Phase 3.

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