Biosensor Studies of Estrogenic Compounds with hER-A & B

描述(由申请人提供)：在第一阶段，IA Inc.和HRL开发 一种用于实时监测的新型、可再生的光纤生物传感器， 雌激素受体调节剂与HER-α的分子相互作用 而她--贝塔。这些生物传感器不需要受体的荧光团标记， 比监测传感器表面上的质量的传感器更具体，并且 每个样本仅使用10毫微米分子的受体。传感器提供了一种动力学 化合物的缔合和解离曲线在9-10分钟内。传感器数据 多种外源、植物和内源雌激素之间的相互作用 HER-α或HER-β与先前报道的结合情况基本一致 学习。还获得了令人振奋的新数据。特别重要的是 观察到染料木素，一种被认为具有保护作用的植物雌激素 某些癌症，会产生更多的稳定的复合体形成 在她和贝塔之间，而不是她的阿尔法之间。也叫邻苯二甲酸二乙酯，一种 广泛用于古龙水和化妆品中的化合物，选择性地激活形成 在ERE和HER-α之间的稳定复合体，但不是HER-β。第二阶段工程 将开发一台原型仪器，并进一步探索 区分有益和有害的雌激素受体调节剂 使用HER-α和HER-β进行动力学测量。 建议的商业应用： 不可用

DESCRIPTION (provided by applicant): During Phase I, IA Inc. and HRL developed a novel, regenerable, fiber optic biosensor for monitoring in real-time, molecular interactions between estrogen receptor modulators and both hER-alpha and hER-beta. These biosensors don't require fluorophore labeling of receptor, are more specific than sensors monitoring mass on the sensor surface, and utilize only 10 femtomoles of receptor per sample. Sensors provide a kinetic association and dissociation curve for a compound in 9-10 minutes. Sensor data on the interaction between a variety of xeno-, phyto- and endogenous estrogens and hER-alpha or hER-beta generally agrees with previously reported binding studies. Exciting new data was also obtained. Of particular significance is the observation that genistein, a phytoestrogen believed to be protective against certain cancers, produces a greater increase in stable complex formation between ERE and hER-beta than it does with hER-alpha. Also diethyl phthalate, a compound widely used in colognes and cosmetics, selectively activates formation of stable complex between ERE and hER-alpha but not hER-beta. Phase II work will develop a prototype instrument and further explore the possibility of distinguishing between beneficial and harmful estrogen receptor modulators by kinetic measurements using hER-alpha and hER-beta. PROPOSED COMMERCIAL APPLICATION: Not Available