Development of L-3-aminotyrosine suitably protected for the synthesis of a novel nonphosphorylated hexapeptide with low-nanomolar Grb2-SH2 domain-binding affinity
文献类型：期刊论文
| 作者 | Song, YL; Roller, PP; Long, YQ |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2004-06-21 |
| 卷号 | 14期号:12页码:3205-3208 |
| 关键词 | aminotyrosine Grb2-SH2 domain nonphosphorylated ligand cyclic peptide sulfoxide SPR assay |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2004.03.103 |
| 文献子类 | Article |
| 英文摘要 | Synthesis of orthogonally protected (2S)-2-amino-3-(3 -amino-4-hydroxy-phenyl)-propionic acid (10) suitable for solid phase peptide synthesis and its first use for the preparation of nonphosphorylated Grb2-SH2 domain antagonists (4a-c) are reported. The 3-aminotyrosine containing sulfoxide-cyclized hexapeptide (4b) exhibited potent Grb2-SH2 domain binding affinity with IC50 = 50 nM which represents the highest affinity yet reported for a peptide inhibitor against Grb2-SH2 domain with only six residues free of phosphotyrosine or phosphotyrosine mimics. This potent small peptidomimetic 4b may be representative of a new class of therapeutically relevant Grb2-SH2 domain-directed agents, and acts as a chemotherapeutic lead for the treatment of erbB2-related cancers. (C) 2004 Elsevier Ltd. All rights reserved. |
| WOS关键词 | CYCLIC PEPTIDE ANTAGONISTS ; STRUCTURE-BASED DESIGN ; SH2 DOMAIN ; SIGNAL-TRANSDUCTION ; STRUCTURAL BASIS ; INHIBITOR ; RECOGNITION ; AGENTS ; AMIDES |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000221776800041 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274060]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Long, YQ |
| 作者单位 | 1.CAS, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.NCI, Med Chem Lab, NIH, Frederick, MD 21702 USA |
| 推荐引用方式 GB/T 7714 | Song, YL,Roller, PP,Long, YQ. Development of L-3-aminotyrosine suitably protected for the synthesis of a novel nonphosphorylated hexapeptide with low-nanomolar Grb2-SH2 domain-binding affinity[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2004,14(12):3205-3208. |
| APA | Song, YL,Roller, PP,&Long, YQ.(2004).Development of L-3-aminotyrosine suitably protected for the synthesis of a novel nonphosphorylated hexapeptide with low-nanomolar Grb2-SH2 domain-binding affinity.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,14(12),3205-3208. |
| MLA | Song, YL,et al."Development of L-3-aminotyrosine suitably protected for the synthesis of a novel nonphosphorylated hexapeptide with low-nanomolar Grb2-SH2 domain-binding affinity".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 14.12(2004):3205-3208. |
入库方式： OAI收割
来源：上海药物研究所
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