{"title":"Interfering with Receptors","authors":"","doi":"10.1126/scisignal.1472002tw316","DOIUrl":null,"url":null,"abstract":"The family of receptors for epidermal growth factor (EGF) transmits signals critical for growth and differentiation of cells in a wide variety of tissues during development. Inappropriate expression of these receptors occurs in many human cancers, and Herceptin, an antibody against one of these receptors (HER2), is used in the treatment of breast cancer. Cho and Leahy present the 2.6 angstrom crystal structure of the entire extracellular portion of one member of this receptor family, HER3. One of the L-shaped halves sits atop the other and assumes a toroidal shape with a protruding spur. Previously mapped regions of the EGF binding site, on the spur and the torus, must be brought together in order to interact productively with the ligand. Interference with this large-scale conformational change might offer a promising route to therapeutics. H.-S. Cho, D. J. Leahy, Structure of the extracellular region of HER3 reveals an interdomain tether, Science 297, 1330-1333 (2002). [Abstract] [Full Text]","PeriodicalId":21619,"journal":{"name":"Science's STKE","volume":"70 1","pages":"TW316 - tw316"},"PeriodicalIF":0.0000,"publicationDate":"2002-08-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Science's STKE","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1126/scisignal.1472002tw316","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
Abstract
The family of receptors for epidermal growth factor (EGF) transmits signals critical for growth and differentiation of cells in a wide variety of tissues during development. Inappropriate expression of these receptors occurs in many human cancers, and Herceptin, an antibody against one of these receptors (HER2), is used in the treatment of breast cancer. Cho and Leahy present the 2.6 angstrom crystal structure of the entire extracellular portion of one member of this receptor family, HER3. One of the L-shaped halves sits atop the other and assumes a toroidal shape with a protruding spur. Previously mapped regions of the EGF binding site, on the spur and the torus, must be brought together in order to interact productively with the ligand. Interference with this large-scale conformational change might offer a promising route to therapeutics. H.-S. Cho, D. J. Leahy, Structure of the extracellular region of HER3 reveals an interdomain tether, Science 297, 1330-1333 (2002). [Abstract] [Full Text]
表皮生长因子(EGF)受体家族在多种组织发育过程中传递对细胞生长和分化至关重要的信号。这些受体的不适当表达发生在许多人类癌症中，赫赛汀是一种针对这些受体之一(HER2)的抗体，用于治疗乳腺癌。Cho和Leahy展示了该受体家族成员HER3的整个细胞外部分的2.6埃晶体结构。其中一个l形的一半位于另一个的顶部，呈环形，有一个突出的马刺。先前绘制的EGF结合位点区域，在骨刺和环面上，必须聚集在一起，以便与配体有效地相互作用。干扰这种大规模的构象变化可能为治疗提供一条有希望的途径。H.-S。Cho, D. J. Leahy, HER3的胞外区结构揭示了一个域间链，科学297,1330-1333(2002)。【摘要】【全文】
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