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Force spectroscopy between acetylcholine and single acetylcholinesterase molecules and the effects of inhibitors and reactivators studied by atomic force microscopy
Yingge, Z; Chunli, B; Chen, W; Delu, Z
2001-05-01
Source PublicationJOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
ISSN0022-3565
Volume297Issue:2Pages:798-803
AbstractForce spectroscopy between a single acetylcholinesterase (AChE) molecule and its natural substrates was performed, and the effects of inhibitors and reactivators on the force spectrum were studied with atomic force microscopy (AFM). The force spectrum between normal AChE and its substrates had its special shape. Inhibitors, which inhibit AChE by occupying the active center of the enzyme, could change the force spectrum shape noticeably. Reactivators, which reactivate the inhibited AChE by pulling the inhibitor off the active center of the enzyme, could make the normal shape of force spectrum reappear. This meant the shape features of the force spectrum could be used as a good index to observe the time course of the interactions between a single AChE molecule and its special inhibitors and reactivators in real time. The results of the real-time observation demonstrated that the inhibition times of soman and sarin on AChE were longer than 2 h and that of eserine, a reversible inhibitor of AChE, was 34 +/- 3 min. The reactivation time of HI-6 on soman-inhibited AChE was 6 +/- 2 min. These results indicated that AFM was a useful tool in pharmacology and toxicology, and could reveal time information of the interactions between AChE and its ligands.
Indexed BySCI
Language英语
WOS IDWOS:000168107900042
PublisherAMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS
Citation statistics
Document Type期刊论文
Identifierhttp://ir.iccas.ac.cn/handle/121111/77350
Collection中国科学院化学研究所
Corresponding AuthorYingge, Z
Affiliation1.Acad Sinica, Inst Pharmacol & Toxicol, Beijing 100850, Peoples R China
2.Acad Sinica, Inst Chem, Beijing 100850, Peoples R China
Recommended Citation
GB/T 7714
Yingge, Z,Chunli, B,Chen, W,et al. Force spectroscopy between acetylcholine and single acetylcholinesterase molecules and the effects of inhibitors and reactivators studied by atomic force microscopy[J]. JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS,2001,297(2):798-803.
APA Yingge, Z,Chunli, B,Chen, W,&Delu, Z.(2001).Force spectroscopy between acetylcholine and single acetylcholinesterase molecules and the effects of inhibitors and reactivators studied by atomic force microscopy.JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS,297(2),798-803.
MLA Yingge, Z,et al."Force spectroscopy between acetylcholine and single acetylcholinesterase molecules and the effects of inhibitors and reactivators studied by atomic force microscopy".JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS 297.2(2001):798-803.
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