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.
TNF-α inhibitor Lenalidomide (CC-5013, LEN) is an immunomodulatory drug currently approved for the treatment of multiple myeloma (MM), 5q- myelodysplasia and mantle cell lymphoma. Lenalidomide (CC-5013)是Thalidomide的衍生物,是一种TNF-α分泌抑制剂,IC50为13 nM。
MoreLapatinib (GW572016) is a small-molecule dual inhibitor of EGFR and ErbB2 receptor kinase activities. Lapatinib可形成Lapatinib的二甲苯磺酸盐,是一种有效的EGFR和ErbB2抑制剂,IC50分别为10.2和9.8 nM。
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