Advances in Cellular Target Engagement and Target Deconvolution

affinity based target deconvolution of safranal

High content cellular microarray for automated drug target deconvolution

Despite the promising paradigm offered by high-content screening, the concrete execution of hundred of thousands of visual cell-based experiments has remained highly challenging in terms of both statistical robustness and speed. An efficient computational method for cellular microarrays was developed at Institut Pasteur-Korea that allow for high speed, high content genome-wide siRNA screening. ...

Target deconvolution techniques in modern phenotypic profiling.

The past decade has seen rapid growth in the use of diverse compound libraries in classical phenotypic screens to identify modulators of a given process. The subsequent process of identifying the molecular targets of active hits, also called 'target deconvolution', is an essential step for understanding compound mechanism of action and for using the identified hits as tools for further dissecti...

Exploiting polypharmacology for drug target deconvolution.

Polypharmacology (action of drugs against multiple targets) represents a tempting avenue for new drug development; unfortunately, methods capable of exploiting the known polypharmacology of drugs for target deconvolution are lacking. Here, we present an ensemble approach using elastic net regularization combined with mRNA expression profiling and previously characterized data on a large set of ...

Advances in target therapy in lung cancer.

Herein, we have reviewed and analysed recent literature, published in 2013 and early 2014, in the context of pre-existing data. Considered target therapies were tyrosine kinase inhibitors of active epidermal growth factor receptor mutations (e.g. erlotinib, gefinitib and afatinib), anaplastic lymphoma kinase rearrangements (e.g. crizotinib) or angiogenesis (drugs under development), or monoclon...