Inhibitor-induced conformational change in cytochrome P-450CAM.

Inhibitor-induced conformational change in cytochrome P-450CAM.
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细胞色素 P-450CAM 抑制剂诱导的构象变化。

DOI:
10.1021/bi00068a013
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发表时间:
1993
期刊:
影响因子:
2.9
通讯作者:
Poulos,TL
Poulos,TL
中科院分区:
生物学3区
文献类型:
--
作者:
Raag,R;Li,H;Jones,BC;Poulos,TL

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材料和方法重组P-450 cam按照公开的方法纯化和结晶(Poulos等,1982; Unger等人,1986;阿特金斯和Sligar,1988)。首先将无底物的晶体浸泡在抑制剂(Pfizer化合物UK-39671)的对映体混合物中,该混合物由Pfizer Central Research,Sandwich,肯特,英格兰提供。该化合物已在Pfizer合成,作为寻找新型抗真菌剂的一部分(Richardson等人,1990),但也被发现是细菌酶细胞色素P-450 cam的抑制剂。然而,即使在对映体混合物中浸泡过夜后,P-450 cam的晶体也会破裂或产生质量差的衍射数据。随后,Pfizer Central Research提供了10 mg各抑制剂对映异构体UK-67254-13(+)和UK-67255-13(-)的单草酸盐。两种结构描述
MATERIALS AND METHODSRecombinant P-450cam was purified and crystallized according to published procedures (Poulos et al., 1982; Unger et al., 1986; Atkins & Sligar, 1988). Substrate-free crystals were initially soaked in ah enantiomeric mixture of the inhibitor (Pfizer compound UK-39671), provided by Pfizer Central Research, Sandwich, Kent, England. This compound had been synthesized at Pfizer as part of a search for novel antifungal agents (Richardson et al., 1990) but had also been found to be an inhibitor of the bacterial enzyme cytochrome P-450cam-However, following even an overnight soak in the enantiomeric mixture, crystals of P-450cam were either cracked or yielded diffraction data of poor quality. Subse-quently, Pfizer Central Research provided 10 mg of the monooxalate salt of each individual inhibitor enantiomer, UK-67254-13 (+) and UK-67255-13 (-). Both structures described
控制多底物单加氧酶 (P-450) 活性诱导的遗传机制。
DOI: 10.1146/annurev.pa.21.040181.002243
发表时间: 1981
影响因子: 12.5
作者:
D. Nebert;H. Eisen;M. Negishi;M. Lang;L. Hjelmeland;A. Okey
通讯作者: A. Okey
恶臭假单胞菌细胞色素P-450cam基因的核苷酸序列及其在大肠杆菌中的表达。
DOI: --
发表时间: 1986
期刊: The Journal of biological chemistry
影响因子: --
作者:
Unger,BP;Gunsalus,IC;Sligar,SG
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DOI: 10.1016/0022-2836(87)90190-2
发表时间: 1987-06-05
影响因子: 5.6
作者:
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DOI: 10.1021/bi00366a049
发表时间: 1986-09-09
期刊: BIOCHEMISTRY
影响因子: 2.9
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细胞色素 P450 和生物羟基化反应。
DOI: 10.1007/bfb0019663
发表时间: 1979
影响因子: 8.6
作者:
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通讯作者: V. Ullrich