Cloning and expression of cDNA for human diazepam binding inhibitor, a natural ligand of an allosteric regulatory site of the gamma-aminobutyric acid type A receptor.

Cloning and expression of cDNA for human diazepam binding inhibitor, a natural ligand of an allosteric regulatory site of the gamma-aminobutyric acid type A receptor.
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人地西泮结合抑制剂(γ-氨基丁酸 A 型受体变构调节位点的天然配体)的 cDNA 的克隆和表达。

DOI:
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发表时间:
1986
影响因子:
11.1
通讯作者:
E. Costa
E. Costa
中科院分区:
综合性期刊1区
文献类型:
--
作者:
P. Gray;D. Glaister;P. Seeburg;A. Guidotti;E. Costa

文献摘要

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安定结合抑制物(DBI)是一种蛋白质,它取代与β-卡莫林/苯二氮识别位点结合的配体,该位点是A型伽马-氨基丁酸受体复合体的变构调节位点。分离到一个编码DBI的不完整大鼠cDNA克隆。利用该大鼠序列鉴定了编码人DBI全部104个残基的cDNA克隆。重组DBI具有与天然人DBI相同的生化和抗原性。DBI由至少5个成员组成的多基因家族编码,但单个基因似乎占DBI表达的大部分。DBI以组织特异性的方式表达。在中枢神经系统组织中发现表达,并似乎延伸到富含外周型苯二氮卓类药物识别位点的外周组织。这些部位和DBI在肾上腺、睾丸和肾脏中的作用仍有待确定。
Diazepam binding inhibitor (DBI) is a protein that displaces ligands bound to the beta-carboline/benzodiazepine recognition site, an allosteric modulatory site of the type A gamma-aminobutyric acid receptor complex. An incomplete rat cDNA clone coding for DBI was isolated. This rat sequence was utilized to identify a cDNA clone that encoded the entire 104 residues of human DBI. This sequence was engineered for expression in E. coli, and recombinant DBI exhibits identical biochemical and antigenic characteristics of natural human DBI. DBI is encoded by a multigene family of at least five members, but a single gene appears to account for the majority of DBI expression. DBI is expressed in a tissue-specific manner. Expression is found in central nervous system tissues and appears to extend to peripheral tissues rich in the peripheral type of high-affinity benzodiazepine recognition sites. The role of these sites and DBI in adrenal gland, testis, and kidney remains to be determined.