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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Marshall F H, Patel K, Lundstrom K, Camacho J, Foord S M, Lee M G

Receptor Systems Unit, Glaxo Wellcome Medicines Research Centre, Hertfordshire.

Br J Pharmacol. 1997 Aug;121(8):1673-8. doi: 10.1038/sj.bjp.0701332.

The human prostaglandin EP4 receptor has been expressed by use of the Semliki Forest virus system. 2. In cell membranes [3H]-prostaglandin E2 ([3H]-PGE2) bound to a high affinity site with a Kd of 1.12 +/- 0.3 nM and a Bmax of 3.1 +/- 0.3 pmol mg-1 protein. 3. In competition studies the rank order of potency for prostaglandins was PGE2 = PGE1 > > PGE2 alpha = PGI2. 4. The binding of [3H]-PGE2 to cell membranes was inhibited by approximately 60% by the addition of guanylnucleotides, suggesting that this proportion of the receptors was G-protein coupled. 5. [3H]-PGE2 binding was increased by greater than 200% by the addition of divalent cations, with little change in the IC50 of PGE2. 6. In saturation studies removal of divalent cations and addition of GTP gamma S resulted in a 65% reduction in the Bmax with no change in the Kd. These results are consistent with the ligand labelling two states of the receptor R*, a high affinity state and R*G, a high affinity G protein coupled state.

人类前列腺素EP4受体已通过塞姆利基森林病毒系统表达。2. 在细胞膜中，[3H] - 前列腺素E2（[3H] - PGE2）与一个高亲和力位点结合，解离常数（Kd）为1.12±0.3 nM，最大结合量（Bmax）为3.1±0.3 pmol mg-1蛋白。3. 在竞争研究中，前列腺素的效力排序为PGE2 = PGE1 >> PGE2α = PGI2。4. 添加鸟苷酸后，[3H] - PGE2与细胞膜的结合被抑制约60%，这表明该比例的受体是与G蛋白偶联的。5. 添加二价阳离子后，[3H] - PGE2的结合增加超过200%，而PGE2的半数抑制浓度（IC50）变化不大。6. 在饱和研究中，去除二价阳离子并添加GTPγS导致最大结合量降低65%，而解离常数不变。这些结果与配体标记受体的两种状态R*（高亲和力状态）和R*G（高亲和力G蛋白偶联状态）一致。

Marshall F H, Patel K, Lundstrom K, Camacho J, Foord S M, Lee M G

Receptor Systems Unit, Glaxo Wellcome Medicines Research Centre, Hertfordshire.

Br J Pharmacol. 1997 Aug;121(8):1673-8. doi: 10.1038/sj.bjp.0701332.

The human prostaglandin EP4 receptor has been expressed by use of the Semliki Forest virus system. 2. In cell membranes [3H]-prostaglandin E2 ([3H]-PGE2) bound to a high affinity site with a Kd of 1.12 +/- 0.3 nM and a Bmax of 3.1 +/- 0.3 pmol mg-1 protein. 3. In competition studies the rank order of potency for prostaglandins was PGE2 = PGE1 > > PGE2 alpha = PGI2. 4. The binding of [3H]-PGE2 to cell membranes was inhibited by approximately 60% by the addition of guanylnucleotides, suggesting that this proportion of the receptors was G-protein coupled. 5. [3H]-PGE2 binding was increased by greater than 200% by the addition of divalent cations, with little change in the IC50 of PGE2. 6. In saturation studies removal of divalent cations and addition of GTP gamma S resulted in a 65% reduction in the Bmax with no change in the Kd. These results are consistent with the ligand labelling two states of the receptor R*, a high affinity state and R*G, a high affinity G protein coupled state.

人类前列腺素EP4受体已通过塞姆利基森林病毒系统表达。2. 在细胞膜中，[3H] - 前列腺素E2（[3H] - PGE2）与一个高亲和力位点结合，解离常数（Kd）为1.12±0.3 nM，最大结合量（Bmax）为3.1±0.3 pmol mg-1蛋白。3. 在竞争研究中，前列腺素的效力排序为PGE2 = PGE1 >> PGE2α = PGI2。4. 添加鸟苷酸后，[3H] - PGE2与细胞膜的结合被抑制约60%，这表明该比例的受体是与G蛋白偶联的。5. 添加二价阳离子后，[3H] - PGE2的结合增加超过200%，而PGE2的半数抑制浓度（IC50）变化不大。6. 在饱和研究中，去除二价阳离子并添加GTPγS导致最大结合量降低65%，而解离常数不变。这些结果与配体标记受体的两种状态R*（高亲和力状态）和R*G（高亲和力G蛋白偶联状态）一致。