57 research outputs found

    Small molecules, big targets: drug discovery faces the protein-protein interaction challenge.

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    Protein-protein interactions (PPIs) are of pivotal importance in the regulation of biological systems and are consequently implicated in the development of disease states. Recent work has begun to show that, with the right tools, certain classes of PPI can yield to the efforts of medicinal chemists to develop inhibitors, and the first PPI inhibitors have reached clinical development. In this Review, we describe the research leading to these breakthroughs and highlight the existence of groups of structurally related PPIs within the PPI target class. For each of these groups, we use examples of successful discovery efforts to illustrate the research strategies that have proved most useful.JS, DES and ARB thank the Wellcome Trust for funding.This is the author accepted manuscript. The final version is available from Nature Publishing Group via http://dx.doi.org/10.1038/nrd.2016.2

    Epigenetic assays for chemical biology and drug discovery

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    Blends of synthetic plastic-derived polypeptide with Hydroxypropylmethylcellulose and polyvinyl alcohol: unraveling the specific interaction parameters, morphology and thermal stability of the polymers couple

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    The medleys of the plastic-derived polypeptide with commercially available polymers believably the suitable candidate for pharmaceutical and biomedical importance. The current research is focussed on the synthesis of a novel plastic-mimetic polypeptide (PLP), poly(IPAVG) by the solution phase method (where I, P, A, V, and G represent Isoleucine, Proline, Alanine, Valine, and Glycine, respectively). The miscibility attributes of PLP/polyvinyl alcohol (PVA) and PLP/hydroxypropylmethylcellulose (HPMC) blends were examined by viscometry and by other advanced analytical tools for different weight proportions. It is shown by the viscometry that the PLP/HPMC and PLP/PVA form an immiscible blend system at 10(omicron)C and further, the FTIR spectra of poly (IPAVG) /HPMC and poly (IPAVG) /PVA blend membranes manifest the lack of intermolecular interactions. DSC results proved the dual Tg for one blend proportion and lower Tg values for all other blend systems. The thermal property of the blends with different compositions was evaluated by thermogravimetric analysis (TGA). The TGA results showed that the blends possess inferior thermal stability to the native ones. The surface morphology was analyzed by SEM indicated the heterogeneity and X-ray diffraction (XRD) revealed the absence of any change in crystallinity advocated the immiscibility of the blends. Further, we ventured to prepare the non-woven fabrics from the solutions of 1-10 wt% concentrations at the voltages within 20-30 kV by electrospinning. The droplet formed at the spinneret failed to reach the collector plate, and consequently, no films developed for the collector device
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