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尿嘧啶置于硫酸,硝酸体系中,化学反应 3.0H,以92%的收率获得产物5-硝基尿嘧啶
参考文献:The P38-Mk2-Hur Pathway Potentiates Egfrviii-il-1β-Driven Il-6 Secretion In Glioblastoma Cells
标题:The P38-Mk2-Hur Pathway Potentiates Egfrviii-il-1β-Driven Il-6 Secretion In Glioblastoma Cells
摘要:胶质母细胞瘤(Gbm)的微环境中含有高水平的炎症细胞因子白细胞介素6(Il-6),这有助于促进肿瘤进展和侵袭.gbm中常见的表皮生长因子受体变异体iii(Egfrviii)突变与更高的il-6水平显著相关.此外,Gbm肿瘤中升高的il-1β水平也被认为能激活gbm细胞并增强il-6的产生.然而,导致il-6过度产生gbm中的致癌基因-微环境中的这些内在和外在因素之间的相互作用在很大程度上仍未得到理解.在这里,我们展示了egfrviii增强了il-1β诱导的gbm细胞中的il-6分泌.重要的是,在表达egfrviii的gbm细胞中,P38促分裂原活化蛋白激酶(P38 Mapk)和mapk活化蛋白激酶2(Mk2)的抑制剂最有效地减弱了il-6的产生.在表达egfrviii的gbm细胞中,增强的il-6产生和对药物p38 Mapk和mk2抑制剂的增加的敏感性与增加的依赖mk2的核质穿梭和il-6 Mrna稳定蛋白--人抗原r(Hur)在胞质的积累相关.il-1β刺激的p38 Mapk-Mk2-Hur途径的激活在携带egfrviii的gbm细胞中显著增强了il-6 Mrna的稳定性.进一步支持p38 Mapk-Mk2-Hur途径在gbm炎症环境发展中的作用,在超过50%的被调查的gbm组织中发现了激活的mk2,并且与较低级别和继发性gbm相关.总的来说,P38 Mapk-Mk2-Hur信号可能增强内在(Egfrviii)和外在(Il-1β)因素发展gbm炎症环境的潜力.因此,进一步改进针对p38 Mapk,Mk2和hur的脑渗透和抗炎抑制剂可能有助于阻止低级别胶质瘤进展为侵袭性gbm.
DOI:10.1038/onc.2014.225

专利信息

专利号:US-4849513-A
优先权日:1983-12-20
标 题 :Deoxyribonucleoside phosphoramidites in which an aliphatic amino group is attached to the sugar ring and their use for the preparation of oligonucleotides containing aliphatic amino groups
发明人：SMITH LLOYD M; FUNG STEVEN; KAISER ROBERT J
权利人:CALIFORNIA INST OF TECHN
摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.

专利号:US-5118802-A
优先权日:1983-12-20
标 题:DNA-reporter conjugates linked via the 2' or 5'-primary amino group of the 5'-terminal nucleoside
发明人：SMITH LLOYD M; FUNG STEVEN; KAISER JR ROBERT J
权利人:CALIFORNIA INST OF TECHN
摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.

专利号:US-5118800-A
优先权日:1983-12-20
标 题 :Oligonucleotides possessing a primary amino group in the terminal nucleotide
发明人：SMITH LLOYD M; FUNG STEVEN; KAISER JR ROBERT J
权利人:CALIFORNIA INST OF TECHN
摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.

专利号:US-8501941-B2
优先权日:2005-02-25
标题 :Methods for the synthesis of unsymmetrical cycloakyl substituted xanthines
发明人：WANG GUOQUAN; RIEGER JAYSON M; THOMPSON ROBERT D
权利人:WANG GUOQUAN; RIEGER JAYSON M; THOMPSON ROBERT D; DOGWOOD PHARMACEUTICALS INC
摘要:The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A 2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents. Also provided are processes for the preparation of the compounds and their intermediates.

专利号:WO-2022090101-A1
优先权日:2020-10-26
标题 :Process for synthesis of 2,4-dichloro-5-aminopyrimidine
发明人：GROLL KLAUS; PANGERL MICHAEL; WANG YANLING; XING LIDONG; XU JIANPING; ZHANG PINJIE; ZHANG YONGSHENG; ZHU ZHIBIN
权利人:BOEHRINGER INGELHEIM INT
摘要:The invention is directed to the commercially synthetic process of 2,4-Dichloro-5-amino- pyrimidine, starting from 5-nitrouracil.

专利号:US-5015733-A
优先权日:1983-12-20
标题 :Nucleosides possessing blocked aliphatic amino groups
发明人：SMITH LLOYD M; FUND STEVEN; KAISER JR ROBERT J
权利人:CALIFORNIA INST OF TECHN
摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieites may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.