该技术最初用于研究药物在哺乳动物细胞中的结合,但现在广泛用于验证和量化药物在不同物种的细胞和组织中的靶点接合。 具体而言,该方法通过将目标细胞和药物在不同温度下共培育一定时间后裂解,与药物结合的蛋白会因为热稳定性提高而更不容易发生变性而沉淀,随后通过离心把沉淀的未结合蛋白去除,最后通过蛋白免疫印迹法(We...
揭示生命机制的热力钥匙：Cellular Thermal Shift Assay（CETSA）的深度探索CETSA，这一生物物理技术的璀璨明珠，自2013年问世以来，以其独特的洞察力在细胞生物学领域崭露头角。它聚焦于药物与细胞内蛋白的互动，尤其在药物靶向性和脱靶效应的评估中发挥着关键作用。通过在不同温度下培育细胞与药物，CETSA揭...
但是现在还没有方法能够有效且直接的测量药物分子到达并结合靶蛋白的方法。卡罗林斯卡研究中心科学家开发出一种称之为细胞热转移(CETSA,Cellular Thermal Shift Assay)的方法(Monitoring drug target engagement in cells and tissues using the cellular thermal shift assay, D Martinez Molina, R Jafari, M Ignatushc...
in cells should be also assessed, especially for drugs aimed at modulating intracellular signaling pathways . as a result, the development of a cellular thermal shift assay (cetsa) has become an important tool for determining the binding affinity of drugs to their intracellular targets. cell lines...
Cellular thermal shift assay (CETSA) The ability of compounds to interact with, and thereby stabilize the target in intact cells, was analysed essentially as described by Molinaet al.21. Detailed protocol is provided in theSupplementary materials and methods. ...
from a CETSA experiment is a comparison between apparent melting curves (or, more accurately, tempera-ture-induced aggregation curves), in which the protein in the presence and absence of ligand is subjected to a panel of tempera-tures such that a potential thermal stabilization can be assessed....
The cellular thermal shift assay (CETSA), as a method to determine protein–ligand interaction and cellular protein modification, has rapidly become routine laboratory practice. However, current options to determine that (1) sample was loaded in each lane of the analysed western blot and (2) the...
They discuss molecular targets in cancer, cancer nanomedicine, T-cell chimeric antigen receptors, cancer drug resistance, RNA interference-based therapeutics, targeting RNA with small molecules, the cellular thermal shift assay, genome editing, 26S proteasome inhibitors, biobanking, mitochondrial biogenesis...
文档热度: 文档分类: 待分类 DOI:10.1126/science.1233606,84(2013);341Scienceetal.DanielMartinezMolinaCellularThermalShiftAssayMonitoringDrugTargetEngagementinCellsandTissuesUsingtheThiscopyisforyourpersonal,non-commercialuseonly.clickinghere.colleagues,clients,orcustomersby,youcanorderhigh-qualitycopiesforyourIfyou...
Recently, we published a proof-of-principle study describing the implementation of thermal shift assays in a cellular format, which we call the cellular thermal shift assay (CETSA). The method allows studies of target engagement of drug candidates in a cellular context, herein exemplified with ...