Minimalist linkers suitable for irreversible inhibitors in simultaneous proteome profiling, live-cell imaging and drug screening

2019 ◽  
Vol 55 (6) ◽  
pp. 834-837 ◽  
Author(s):  
Cuiping Guo ◽  
Yu Chang ◽  
Xin Wang ◽  
Chengqian Zhang ◽  
Piliang Hao ◽  
...  
Keyword(s):  
Anticancer Drugs ◽  
Drug Screening ◽  
Live Cell Imaging ◽  
Cell Imaging ◽  
Live Cell ◽  
Proteome Profiling ◽  
Irreversible Inhibitors

A series of minimalist linkers were developed and have been demonstrated to be suitable for irreversible inhibitors in simultaneous proteome profiling, live-cell imaging and drug screening, thus facilitating the discovery of first-in-class anticancer drugs.

Hypoxia efficient and glutathione-resistant cytoselective ruthenium(ii)-p-cymene-arylimidazophenanthroline complexes: biomolecular interaction and live cell imaging

2020 ◽  
Vol 49 (36) ◽  
pp. 12865-12878 ◽  
Author(s):  
Ashaparna Mondal ◽  
Priyankar Paira
Keyword(s):  
Hela Cell ◽  
Anticancer Drugs ◽  
Live Cell Imaging ◽  
Cell Imaging ◽  
Live Cell ◽  
Biomolecular Interaction ◽  
Dna Targeting ◽  
Imaging Probes

A series of ruthenium(ii)–arene-2-arylimidazophenanthroline based DNA targeting, cytoselective, hypoxia efficient and glutathione-resistant luminescent anticancer drugs have been developed which are also represented as HeLa cell imaging probes.

scholarly journals Comparison of Calcium Dynamics and Specific Features for G Protein–Coupled Receptor–Targeting Drugs Using Live Cell Imaging and Automated Analysis

2017 ◽  
Vol 22 (7) ◽  
pp. 848-858 ◽  
Author(s):  
Rishikesh Kumar Gupta ◽  
Sarpras Swain ◽  
Dinesh Kankanamge ◽  
Pantula Devi Priyanka ◽  
Ranjana Singh ◽  
...  
Keyword(s):  
Feature Extraction ◽  
G Protein ◽  
Drug Screening ◽  
Live Cell Imaging ◽  
Cell Imaging ◽  
Live Cell ◽  
Calcium Dynamics ◽  
A Cell ◽  
G Protein Coupled

G protein–coupled receptors (GPCRs) are targets for designing a large fraction of the drugs in the pharmaceutical industry. For GPCR-targeting drug screening using cell-based assays, measurement of cytosolic calcium has been widely used to obtain dose–response profiles. However, it remains challenging to obtain drug-specific features due to cell-to-cell heterogeneity in drug–cell responses obtained from live cell imaging. Here, we present a framework combining live cell imaging of a cell population and a feature extraction method for classification of responses of drugs targeting GPCRs CXCR4 and α2AR. We measured the calcium dynamics using confocal microscopy and compared the responses for SDF-1α and norepinephrine. The results clearly show that the clustering patterns of responses for the two GPCRs are significantly different. Additionally, we show that different drugs targeting the same GPCR induce different calcium response signatures. We also implemented principal component analysis and k means for feature extraction and used nondominated (ND) sorting for ranking a group of drugs at various doses. The presented approach can be used to model a cell population as a mixture of subpopulations. It also offers specific advantages, such as higher spatial resolution, classification of responses, and ranking of drugs, potentially providing a platform for high-content drug screening.

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