单胺转运体：脆弱而重要的守门员。
Monoamine transporters: vulnerable and vital doorkeepers.
机构信息
Department of Psychiatry, Harvard Medical School and Division of Alcohol and Drug Abuse, McLean Hospital, Belmont, Massachusetts, USA.
出版信息
Prog Mol Biol Transl Sci. 2011;98:1-46. doi: 10.1016/B978-0-12-385506-0.00001-6.
Abstract
Transporters of dopamine, serotonin, and norepinephrine have been empirically used as medication targets for several mental illnesses in the last decades. These protein-targeted medications are effective only for subpopulations of patients with transporter-related brain disorders. Since the cDNA clonings in early 1990s, molecular studies of these transporters have revealed a wealth of information about the transporters' structure-activity relationship (SAR), neuropharmacology, cell biology, biochemistry, pharmacogenetics, and the diseases related to the human genes encoding these transporters among related regulators. Such new information creates a unique opportunity to develop transporter-specific medications based on SAR, mRNA, DNA, and perhaps transporter trafficking regulation for a number of highly relevant diseases including substance abuse, depression, schizophrenia, and Parkinson's disease.
摘要
在过去几十年中，多巴胺、血清素和去甲肾上腺素的转运体已被经验性地用作几种精神疾病的药物靶点。这些靶向蛋白的药物仅对与转运体相关的脑疾病的亚群患者有效。自 20 世纪 90 年代初 cDNA 克隆以来，对这些转运体的分子研究揭示了大量关于转运体结构-活性关系（SAR）、神经药理学、细胞生物学、生物化学、药物遗传学以及与编码这些转运体的人类基因相关的调节剂的信息。这些新信息为开发基于 SAR、mRNA、DNA 的转运体特异性药物提供了独特的机会，也许还包括转运体运输调节，以治疗许多高度相关的疾病，包括物质滥用、抑郁、精神分裂症和帕金森病。
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