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Protein kinases constitute a large family of proteins that is now firmly established as a major class of drug targets for the pharmaceutical industry. With so many inhibitors reported to be in clinical development and many more in preclinical development, kinase inhibitors now make up a significant fraction of most major pharmaceutical companies' pipelines, as well as an area of focus for many biotechnology companies. The increased interest in this class of targets reflects both advances in identifying selective protein kinase inhibitors and a growing perception that these drugs offer a novel, well-tolerated oral therapy in some of the most untreatable cancers.
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Proteases constitute one of the largest potential drug target enzyme families, with 647 human gene products incorporating protease sequences and mutated proteases having been identified. In addition, there are many more proteases found in viruses, bacteria, and parasites, which are also potential drug targets. The therapeutic promise of protease inhibitors has been most clearly demonstrated by angiotensin-converting enzyme (ACE) and HIV drugs. Inhibition of protease activity modulates physiological functions, either by reducing the formation of undesirable peptide mediators or by enhancing the beneficial effects of peptides by preventing their catabolism.
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Current advances in functional screening methodologies, medicinal chemistry, and structure-based drug design have generated large increases in the number and diversity of GPCR drug targets. Furthermore, basic research advances have opened the way for still further exploitation of this target class. G protein-coupled receptors (GPCRs) are popular drug targets, accounting for about one-third of approved drugs and many hundreds of drugs currently in development.
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To date, ion channel modulators have been identified by various means, relatively few of which have so far been focused on direct screening of compounds for their activity on the channel(s) of interest. The past few years have seen significant developments that facilitate the identification of novel ion channel modulators. These improvements in screening methods should lead to more selective agents being identified and progressing into clinical development.
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Otava offers 127 Focused Libraries designed not towards specific molecular target, but rather to show general biomedical activity. These libraries are proposed for screening in various research and drug development projects.
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101 uncategorized Focused Libraries designed with Ligand-based approach are listed below. These libraries are proposed for screening in various research and drug development projects.
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Full collection of 330 Otava's Focused Libraries designed with Receptor-based or Ligand-based approach is represented here.
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