Ligand based approach: pharmacophore searches, bioisosteric replacement, 3D shape-based screening.Also, the library can be delivered in any other custom formats within a week only. The library is available in convenient and ready to ship pre-plated formats. In addition, the library was enriched with bioisosteric replacement and compounds bearing new chemotypes predominantly with polar scaffolds and cores to increase novelty of the targeted sets. The emphasis has been made on most promising and studied targets: Heat shock proteins (Hsp90, Hsp82, Hsp27), Chaperone activity of bc1 complex-like and histone-chaperone ASF1a complex (ASF1-histone interaction). Meanwhile, targeting molecular chaperones is proven to be crucial for the prevention of the many deleterious effects of protein misfolding and aggregation, which might lead in the end in cell death, in neurodegeneration and in other protein misfolding diseases.Įnamine has been following investigation on molecular chaperones for years and developed a library of 2 468 synthetic compounds potentially targeted molecular chaperones. In spite of intensive studies, the spectrum of cellular substrates and functions mediated by these different chaperones remains largely undefined. This set of diverse protein families assists a large variety of processes involving folding, translocation, unfolding, disaggregation and homeostasis of proteins within the cellular environment. Control of these processes in the cell achieves through action of assembly of enzymes known as molecular chaperones. Protein folding is very important as attractive field in new drug development paradigm.
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