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μM。",{"key":236,"value":237},"相关类别","信号通路\n>>\nMAPK\u002FERK信号通路\n>>\np38 MAPK\n信号通路\n>>\nMAPK\u002FERK信号通路\n>>\n拉夫\n研究领域\n>>\n炎症\u002F免疫",{"key":239,"value":240},"靶点","B-Raf:83.4 nM (IC50)\np38α:4 nM (IC50)\nAbl:14600 nM (IC50)",{"key":242,"value":243},"体外研究","Doramapimod(BIRB 796)是一种高效的p38α抑制剂,一种丝氨酸\u002F苏氨酸丝裂原活化蛋白激酶(MAPK),由于其在T细胞增殖和细胞因子产生中的作用,通常与炎症相关[1]。 Doramapimod(BIRB 796)是人p38 MAP激酶的皮摩尔抑制剂[2]。在用山梨糖醇刺激(渗透压休克)之前,将HEK293细胞与不同浓度的Doramapimod(BIRB 796)孵育30分钟或2小时,并通过测量其活性检查MAPKAP-K2的活化。 MAPKAP-K2活化在这些细胞中以时间依赖性方式被抑制,30分钟后表观IC50为30 nM或与Doramapimod预培养2小时后8 nM [3]。",{"key":245,"value":246},"体内研究","Doramapimod(BIRB 796)加紫杉醇组(1.14±0.48 g)的平均异种移植重量轻于对照,Doramapimod或紫杉醇组(1.84±0.61,1.80±0.62和1.65±0.29 g)(P \u003C0.05)在Athymic裸体中小鼠(BALB\u002Fc-nu\u002Fnu)。 Doramapimod,紫杉醇和Doramapimod加紫杉醇的抑制率分别为1.93％,9.93％和38％。重要的是,与对照组,紫杉醇或单独的Doramapimod相比,Doramapimod和紫杉醇的组合可显着抑制肿瘤生长[4]。 Doramapimod(BIRB 796)治疗略微降低血压(第7周166±7 mm Hg; P \u003C0.05),而SD大鼠血压正常(123±3 mm Hg)。尽管血压降低,未治疗和Doramapimod治疗的dTGR具有相似的心脏重量和心脏肥大指数(心脏-胫骨比),与非转基因SD大鼠相比显着更高(310±6对307±6对比206±分别为5 mg\u002Fcm; P \u003C0.05)[5]。",{"key":248,"value":249},"激酶实验","在含有20mM Bis-Tris丙烷，pH 7.0,2mM EDTA，0.01％（w \u002F v）NaN 3和0.15％（w \u002F v）正辛基葡糖苷的缓冲液中进行结合研究。在配备有停止流量控制器的Kintech荧光检测器系统上收集SK＆F 86002与p38 MAP激酶结合的动力学数据。数据同时适合描述动态结合的适当方程式，用于简单的一步结合机制。针对未结合配体的背景荧光校正BIRB 796的荧光类似物结合的数据。使用SLM Aminco Bowman Series 2 Model SQ-340荧光检测器将交换曲线测定作为两个半反应进行。在第一个半反应中，将p38 MAP激酶和SK＆F 86002预孵育3分钟。在第二个半反应中，将p38 MAP激酶与Doramapimod预孵育60分钟。对于第一次半反应，观察到荧光探针的净离解，并且观察到第二次半反应的净关联。来自两个半反应的原始数据同时适合描述简单竞争抑制的等式。通过用组成型活性重组MKK6（通过将两个活化残基Ser189和Thr193诱变为Glu残基制备）预处理p38。纯化活化的p38并用作标准激酶活性测定中的酶来源，监测放射性磷酸盐掺入重组人MAPKAP k2中。细胞试验遵循公开的程序。简言之，在存在或不存在化合物的情况下，用1μg\u002F mL LPS刺激人THP.1细胞，然后使用商业ELISA kitkinase测定释放的TNF [2]。",{"key":251,"value":252},"细胞实验","将人胚肾（HEK）293和HeLa细胞暴露于0.5M山梨糖醇30分钟或100ng \u002F mL EGF 10分钟，然后在缓冲液A（50mM Tris-HCl，pH7.5,1mM EGTA，1mM）中裂解。 EDTA，1 mM原钒酸钠，10 mM氟化钠，50 mMβ-甘油磷酸钠，5 mM焦磷酸盐，0.27 M蔗糖，0.1 mM苯甲基磺酰氟，1％（v \u002F v）Triton X-100）加0.1％（v \u002F v）2-巯基乙醇和完全蛋白酶抑制剂混合物。将裂解物在4℃下以18,000×g离心5分钟，除去上清液，在液氮中快速冷冻，并在-20℃下储存直至使用。需要时，将细胞在没有或不含10μMSB203580或10μMPD184352或不同浓度的Doramapimod的情况下预培养1小时，持续时间如图[3]所示。",{"key":254,"value":255},"动物实验","使用小鼠[4]无胸腺裸鼠（BALB \u002F c-nu \u002F nu），6至8周龄，体重18至24g。在该研究中使用KBV200接种的裸鼠异种移植模型。简而言之，将收获的KBV200细胞（2×10 7个细胞\u002F0.2mL \u002F小鼠）皮下植入裸鼠的肩部。当肿瘤达到平均直径0.5 cm3时，将小鼠随机分成4组，并用以下方案治疗：1）盐水溶液（每3天×5）; 2）紫杉醇（18mg \u002F kg ip，每3天×5）; 3）Doramapimod（10mg \u002F kg po，每3天×5）; 4）紫杉醇（18mg \u002F kg ip，每3天×5）加Doramapimod（10mg \u002F kg po，每3天×5，在注射紫杉醇前1小时给药）。每3天记录动物的体重和两个垂直肿瘤直径（A和B），并根据下式估算肿瘤体积（V）：V =（π\u002F 6）[（A + B） ）\u002F 2] 3。根据肿瘤体积和植入时间绘制肿瘤生长和体重的曲线。当对照组中的平均肿瘤重量超过1g时，将小鼠麻醉并杀死。从小鼠切下肿瘤组织，测量它们的重量。生长抑制率（IR）根据下式计算：IR = [1-（实验组的平均肿瘤重量\u002F对照组的平均肿瘤重量）]×100％。大鼠[5]使用雄性转基因dTGR（RCC Ltd）和年龄匹配的非转基因Sprague-Dawley（SD）大鼠（MDC）。执行2种不同的协议。在方案2中，分析未处理的dTGR（n = 15），dTGR + BIRB796（饮食中每天30mg \u002F kg，持续3周; n = 11）和SD（每组n = 8）。通过尾套每周测量收缩压。从第5周到第7周在代谢笼中收集二十四小时的尿样。在第7周收集血清。通过临床常规测定测量血清肌酸酐和胱抑素C.通过酶联免疫吸附测定法测定尿大鼠白蛋白。方案2的目的是关注电生理学改变和死亡率。研究未治疗的dTGR（n = 10），dTGR + BIRB796（n = 10）和SD（n = 10）大鼠至第8周。在异氟烷麻醉下在第7周进行心脏磁场作图（CMFM）。进行超声心动图检查。",{"key":257,"value":258},"参考文献","[1].\nDietrich J, et al. The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796. Bioorg Med Chem. 2010 Aug 1;18(15):5738-48\n[2].\nPargellis C, et al. Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat Struct Biol, 2002, 9(4), 268-272.\n[3].\nKuma Y, et al. BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo. J Biol Chem, 2005, 280(20), 19472-19479.\n[4].\nHe D, et al. BIRB796, the inhibitor of p38 mitogen-activated protein kinase, enhances the efficacy of chemotherapeutic agents in ABCB1 overexpression cells. PLoS One. 2013;8(1):e54181.\n[5].\nPark JK, et al. p38 mitogen-activated protein kinase inhibition ameliorates angiotensin II-induced target organ damage. 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