【佳学基因靶向药物基因检测】一种从骨碎补中捕获潜在生物活性化合物的快速方法，利用钙敏感受体中的疾病相关突变来改变激动剂的结合亲和力

基因检测价格关注的原因

比较基因实验室人员知识更新明白《J Pharm Biomed Anal》在 2023 Jan 14;226:115253.发表了一篇题目为《》肿瘤靶向药物治疗基因检测临床研究文章。该研究由Kai-Li Meng, Mei-Zhi Jiao, Xian-Gang Shi, Ru Xu, Pei-Xuan Cheng, Hui-Ting Lv, Xiao-Hui Zheng, Chao-Ni Xiao等完成。促进了肿瘤的精准治疗与个性化用药的发展，进一步强调了基因信息检测与分析的重要性。

肿瘤基因检测及靶向药物治疗研究关键词：

钙敏感受体 (CaSR),细胞外结构域 (ECD),卤化烷烃脱卤酶（Halo）,骨质疏松症,骨碎补 (RD)。

肿瘤治疗检测基因临床应用结果

骨碎补(RD)因刺激骨形成和抑制骨吸收而被临床用于治疗骨质疏松症，但对骨具有双重作用的生物活性成分尚不清楚。钙敏感受体 (CaSR) 中的致病突变可以改变甲状旁腺激素的分泌，影响骨骼中 Ca2+ 的释放和肾脏对 Ca2+ 的重吸收，这表明 CaSR 是开发治疗骨质疏松症的潜在靶点。在此，建立了一种色谱方法，通过一步法将突变体 CaSR 固定到硅胶表面作为固定相，然后将不同的氨基酸作为竞争剂添加到流动相中，以探索已知激动剂的结合特征进一步筛选来自RD的配体。突变体CaSR包被柱无需复杂的受体纯化和分离即可快速制备，具有13.1 mg CaSR /g硅胶的大容量，至少35天保持良好的稳定性和特异性。 CaSR突变可减弱三种激动剂的结合亲和力，新霉素突变位点Thr151Met、庆大霉素-C突变位点Asn118Lys和Glu191Lys、卡那霉素突变位点Phe612Ser突变位点下降幅度最大，获得了新的认识进入它们的结构-功能关系。使用突变体 CaSR 涂层柱筛选 RD 中潜在的生物活性化合物，并使用 UPLC-MS 将其识别为香豆酸 4-O-β-D-吡喃葡萄糖苷、咖啡酸和柚皮苷。其中，靶向 CaSR 的柚皮苷可能解释了 RD 可以控制骨质疏松症。这些结果表明，这种利用 CaSR 中的疾病相关突变来改变激动剂结合亲和力的快速、简单的方法可用于从草药等复杂基质中有效捕获潜在的生物活性化合物。关键词：钙敏感受体(CaSR);细胞外结构域 (ECD)；卤化烷烃脱卤酶（Halo）；骨质疏松症；骨碎补 (RD)。

肿瘤发生与革命国际数据库描述：

Rhizoma Drynariae (RD) was used clinically to treat osteoporosis in China due to stimulating bone formation and inhibiting bone resorption, however, the bioactive constituents with the dual effect on bone are still unknown exactly. Disease-causing mutations in calcium sensing receptor (CaSR) can alter parathyroid hormone secretion and affect Ca2+ release from bone and Ca2+ reabsorption from kidney, which gives an indication that CaSR is a potential target for developing therapeutics to manage osteoporosis. Herein, a chromatographic approach was established, by immobilizing the mutant CaSR onto the surface of silica gels as stationary phase in a one-step procedure and then adding the different amino acids into mobile phase as competitors, for exploring the binding features of the known agonists and further screening ligands from RD. The mutant CaSR-coated column was prepared rapidly without the complicated purification and separation of the receptor, which had the large capacity of 13.1 mg CaSR /g silica gels and kept a good stability and specificity for at least 35 days. The CaSR mutation can weaken the binding affinities for three agonists, and the largest decreases occurred on the mutational site Thr151Met for neomycin, on the two sites of Asn118Lys and Glu191Lys for gentamicin-C, and on the site Phe612Ser for kanamycin, which gained new insights into their structure-function relationship. The potential bioactive compounds from RD were screened using the mutant CaSR-coated column and were recognized as coumaric acid 4-O-β-D-glucopyranoside, caffeic acid, and naringin using UPLC-MS. Among them, naringin targeting CaSR gives a possible explanation that RD could manage osteoporosis. These results indicated that, such a rapid and simple method, utilizing disease-associated mutation in CaSR to alter the binding affinity for agonists, can be applied in capturing the potential bioactive compounds efficiently from complex matrices like herb medicines.Keywords: Calcium-Sensing Receptor (CaSR); Extracellular domain (ECD); Halogenated alkane dehalogenase (Halo); Osteoporosis; Rhizoma Drynariae (RD).