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开发方便的结晶抑制试验,用于在发现结晶抑制剂的过程中进行结构-活性关系研究

Jeffrey Yang¹, Haifa Albanyan¹, Yiling Wang¹

¹Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, New Jersey 08854, United States.

Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents

|September 8, 2023

概括

一个新的,高效的测试平台有助于发现结石的小分子抑制剂. 这种方法成功地发现了强大的L-cystine二胺抑制剂,对于预防囊尿相关的结石至关重要.

科学领域:

生物化学生物化学
药用化学医学化学
腎臟病學 (nephrology) 是一種醫學.

背景情况:

结石疾病是一个日益严重的全球健康问题,患病率和复发率越来越高.
开发新的治疗方法来预防结石的形成是一个关键的医疗需求.
针对结晶过程的小分子抑制剂是一个有前途的治疗途径.

研究的目的:

开发和验证一个方便的,中高吞吐量测试平台,用于评估结晶抑制剂.
选和识别L-cystine结晶的抑制剂,用于预防cystinuria中的结石.
为了促进药物发现工作和结晶抑制剂的结构-活性关系研究.

主要方法:

制备L-cystine的超和溶液.
化超和溶液与测试抑制剂在小体积 (<1毫升) 72小时.
在离心后,通过色度或度方法量化超的剩余L-cystine度.

主要成果:

建立了一个小型化的多井测试平台,展示了简单性,成本效益和广泛适用性.
该试验成功选了L-cystine结晶的抑制剂.
发现L-cystine二化物是强大的抑制剂,LH708的EC50值为0.058μM,明显比L-CDME更强.

结论:

开发的测试平台是高通量评估结晶抑制剂的宝贵工具.
这个平台有助于发现用于预防结石的强效抑制剂,特别是用于囊性尿.
已识别的L-cystine二氧化物代表了未来治疗结石的有希望的候选人.

关键词:

结晶抑制试验试验结晶抑制试验结晶抑制剂结晶抑制剂囊尿症是什么意思囊尿患有结石疾病的患者.这是一种L-氨酸.乌罗石质病是一种质病.

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