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首页> 外文期刊>Proceedings of the National Academy of Sciences of the United States of America >A substance P (neurokinin-1) receptor mutant carboxyl-terminally truncated to resemble a naturally occurring receptor isoform displays enhanced responsiveness and resistance to desensitization
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A substance P (neurokinin-1) receptor mutant carboxyl-terminally truncated to resemble a naturally occurring receptor isoform displays enhanced responsiveness and resistance to desensitization

机译:羧基末端被截短以类似于天然受体同工型的P(神经激肽-1)受体突变体表现出增强的响应能力和对脱敏的抵抗力

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摘要

Two isoforms of the substance P (SP) recep- tor, differing in the length of the cytoplasmic carboxyl- terminus by ≈8 kDa, have been detected previously in rat salivary glands and other tissues. The binding and functional properties of these two isoforms have been investigated using full-length (407 amino acids) and carboxyl-terminally trun- cated (324 amino acids) rat SP receptors transfected stably into Chinese hamster ovary cells. Both the full-length and the truncated receptor bound radiolabeled SP with a similar Kd (≈0.1 nM). The average number of high affinity SP binding sites per cell was 1.0 * 10~5 and 0.3 * 10~5 for the full-length and the truncated SP receptor, respectively.
机译:先前已在大鼠唾液腺和其他组织中检测到了两种物质P(SP)受体的同工型,其胞质羧基末端的长度相差≈8kDa。已经使用稳定转染到中国仓鼠卵巢细胞中的全长(407个氨基酸)和羧基末端截短的(324个氨基酸)大鼠SP受体研究了这两种同工型的结合和功能特性。全长和截短的受体都以相似的Kd(≈0.1nM)结合放射性标记的SP。对于全长和截短的SP受体,每个细胞的高亲和力SP结合位点的平均数分别为1.0 * 10〜5和0.3 * 10〜5。

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