食管癌是常见的消化道恶性肿瘤之一,其发病率逐年提高,确诊即是进展期,预后差[1-3].在我国,每年约有15万人死于食管癌,病死率仅次于肺癌、胃癌、肝癌,居第4位.食管癌的发生、发展过程涉及大量基因表达水平的改变,包括细胞周期调控发生改...食管癌是常见的消化道恶性肿瘤之一,其发病率逐年提高,确诊即是进展期,预后差[1-3].在我国,每年约有15万人死于食管癌,病死率仅次于肺癌、胃癌、肝癌,居第4位.食管癌的发生、发展过程涉及大量基因表达水平的改变,包括细胞周期调控发生改变,DNA修复,核受体改变等.其中核受体改变就有维甲酸类受体（retinoic aid receptors, RARs）,RARs与食管癌的发生、发展关系密切.1999年Xu等[4]首次研究了RARs与食管癌的关系,指出食管癌的发生可能与维甲酸（retinoicoid, RA）β受体表达缺失有关.近年来已受到国内外学者重视,陆续有文献报道RARs在食管癌的发生、发展中的作用,本文就此进行综述.展开更多
维甲类X受体(Retinoid X Receptor,RXR)是继维甲酸受体(RAR)之后发现的又一类核受体,它的配体9-顺式维甲酸也是新发现的又一种维甲类生理活性物质。本文就维甲类X受体及其配体的最新研究进展作一综述,并就其在血液学中的研究前景作一简...维甲类X受体(Retinoid X Receptor,RXR)是继维甲酸受体(RAR)之后发现的又一类核受体,它的配体9-顺式维甲酸也是新发现的又一种维甲类生理活性物质。本文就维甲类X受体及其配体的最新研究进展作一综述,并就其在血液学中的研究前景作一简要展望,以推动血液学在这一新领域的深入研究。展开更多
Fast and precise prediction of the receptor-ligand binding constant is an important aspect of structure-based drug design. Almost all de novo design methods or 3D database search methods tend to structure generation i...Fast and precise prediction of the receptor-ligand binding constant is an important aspect of structure-based drug design. Almost all de novo design methods or 3D database search methods tend to structure generation instead of structure evaluation. In this article, epididymal retinoic acid binding protein (ERABP) was used as a template to simulate the interaction between retinoids and their receptor. We deduced an equation predicting the drug-receptor binding constant. Furthermore, the conformers after docking were used in CoMFA analysis to get a pharmacophore model of this series of compounds.展开更多
文摘食管癌是常见的消化道恶性肿瘤之一,其发病率逐年提高,确诊即是进展期,预后差[1-3].在我国,每年约有15万人死于食管癌,病死率仅次于肺癌、胃癌、肝癌,居第4位.食管癌的发生、发展过程涉及大量基因表达水平的改变,包括细胞周期调控发生改变,DNA修复,核受体改变等.其中核受体改变就有维甲酸类受体（retinoic aid receptors, RARs）,RARs与食管癌的发生、发展关系密切.1999年Xu等[4]首次研究了RARs与食管癌的关系,指出食管癌的发生可能与维甲酸（retinoicoid, RA）β受体表达缺失有关.近年来已受到国内外学者重视,陆续有文献报道RARs在食管癌的发生、发展中的作用,本文就此进行综述.
文摘Fast and precise prediction of the receptor-ligand binding constant is an important aspect of structure-based drug design. Almost all de novo design methods or 3D database search methods tend to structure generation instead of structure evaluation. In this article, epididymal retinoic acid binding protein (ERABP) was used as a template to simulate the interaction between retinoids and their receptor. We deduced an equation predicting the drug-receptor binding constant. Furthermore, the conformers after docking were used in CoMFA analysis to get a pharmacophore model of this series of compounds.
