Discovery of novel inhibitor of human leukocyte common antigen-related phosphatase
文献类型：期刊论文
| 作者 | Yang, XN; Li, JY ; Zhou, YY; Shen, Q; Chen, JW; Li, J
|
| 刊名 | BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS
 |
| 出版日期 | 2005-10-30 |
| 卷号 | 1726期号:1页码:34-41 |
| 关键词 | LAR protein tyrosine phosphatase high-throughput screening competitive inhibitor meD peptide |
| ISSN号 | 0304-4165 |
| DOI | 10.1016/j.bbagen.2005.07.001 |
| 文献子类 | Article |
| 英文摘要 | Human leukocyte common antigen-related phosphatase (LAR) may play a role in type 2 diabetes and cancer, and in the development of the nervous system, and it may be an attractive target for the treatment of diabetes and cancer. We identified eight hits from the random screening of LAR D1 with a high-throughput screening assay. Further validation of the eight hits showed that the meD insertion was associated with inhibition of LAR D1D2 and LAR D1Q. These data suggest that the inserted meD peptide influences the interaction of the enzyme and inhibitor, which is consistent with the kinetic catalysis constants of the substrate pNPP. Our data showed that Hit 1, the first published novel inhibitor of LAR, is a competitive inhibitor with a K-i of 330 nM that displays obvious selectivity for LAR and mouse PTP sigma, but not for other protein tyrosine phosphatases. (c) 2005 Published by Elsevier B.V. |
| WOS关键词 | PROTEIN-TYROSINE-PHOSPHATASE ; INSULIN SIGNAL-TRANSDUCTION ; SKELETAL-MUSCLE ; INCREASED ABUNDANCE ; ADIPOSE-TISSUE ; PTP-SIGMA ; RECEPTOR ; LAR ; OVEREXPRESSION ; MODULATION |
| WOS研究方向 | Biochemistry & Molecular Biology ; Biophysics |
| 语种 | 英语 |
| WOS记录号 | WOS:000233156800005 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273788]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Li, J |
| 作者单位 | 1.E China Normal Univ, Acad Life Sci, Shanghai 200062, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Biol sci, Shanghai Inst Mat Med, Nalt Ctr Drug Screening, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, XN,Li, JY,Zhou, YY,et al. Discovery of novel inhibitor of human leukocyte common antigen-related phosphatase[J]. BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS,2005,1726(1):34-41. |
| APA | Yang, XN,Li, JY,Zhou, YY,Shen, Q,Chen, JW,&Li, J.(2005).Discovery of novel inhibitor of human leukocyte common antigen-related phosphatase.BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS,1726(1),34-41. |
| MLA | Yang, XN,et al."Discovery of novel inhibitor of human leukocyte common antigen-related phosphatase".BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS 1726.1(2005):34-41. |
入库方式： OAI收割
来源：上海药物研究所
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