Innovations In Clinical Neuroscience

Hot Topics in Drug Development Apr 2016

A peer-reviewed, evidence-based journal for clinicians in the field of neuroscience

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Hot Topics in Drug Development [April 2016] 13 JOURNAL WATCH future of PPI data analysis. The a uthors present the constraints that they believe have delayed the transition from the current methodologies to a holistic bioinformatics approach for linking biological and clinical data. They propose specific solutions for all these constraints in order to achieve the optimal exploitation of PPI bioinformatics' approaches. * PMID: PMC4584938 DREADDs: novel tools for drug discovery and development. Lee HM, Giguere PM, Roth BL. Drug Discov Today. 2014 Apr;19(4):469–73. doi: 10.1016/j.drudis.2013.10.018. Epub 2013 Nov 1. Summary: Here, the authors discuss how designer receptors exclusively activated by designer drugs (DREADDs) can be used as novel tools for drug discovery and development. The authors proposed that DREADDs can facilitate the identification of druggable targets and enable researchers to explore the activities of novel drugs against both known and orphan GPCRs * PMID: 24184433 Using quantitative systems pharmacology for novel drug discovery. Pérez-Nueno VI. Expert Opin Drug Discov. 2015 Dec;10(12):1315–31. doi: 10.1517/17460441.2015.1082543. Epub 2015 Aug 25. Summary: In this review article, the authors define quantitative and systems pharmacology (QSP), a new paradigm that aims to understand how drugs modulate cellular networks in space and time in order to predict drug targets and their role in human pathophysiology. The authors discuss existing computational and experimental QSP approaches, such as polypharmacology techniques combined with systems biology i nformation, and consider the use of new tools and ideas in a wider "systems-level" context in order to design new drugs with improved efficacy and fewer unwanted off-target effects. * PMID: 26328768 Single-cell analysis tools for drug discovery and development. Heath JR1, Ribas A2, Mischel PS3.Nat Rev Drug Discov. 2016 Mar;15(3):204-16. doi: 10.1038/nrd.2015.16. Epub 2015 Dec 16. Summary: Here, researchers review tools for single-cell genomic, transcriptomic, and multiplex proteomic analyses and assess their advantages and limitations. Emerging applications of single cell analysis tools in drug discovery and development, particularly in the field of oncology, are discussed. * PMID: 26669673 Application of chemical biology in target identification and drug discovery. Zhu Y, Xiao T, Lei S, et al. Arch Pharm Res. 2015 Sep;38(9):1642–50. doi: 10.1007/s12272-015-0643-2. Epub 2015 Aug 5. Summary: In this review, the authors highlight some applications of chemical biology in the context of target identification. The authors explain how chemical biology solves biological problems through searching previously unknown targets for pharmacologically active small molecules or finding ligands for well-defined drug targets. They describe how chemical biology allows the study of how these small molecules interact with their respective targets, as well as their roles in signal transduction, molecular recognition and cell functions. The authors describe therapeutic targets that are being identified and validated as a result of advances in functional genomics. * PMID: 26242900 The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs. Chen X, Choo H, Huang XP, et al. ACS Chem Neurosci. 2015 Mar 18;6(3):476–84. doi: 10.1021/cn500325v. Epub 2015 Jan 27. Summary: Here researchers explored multiple regions of the scaffold represented by clozapine N- oxide (CNO), a pharmacologically inert ligand, identified interesting structure-activity relationships (SARs) trends, and discovered several compounds that are very potent hM3Dq agonists but do not activate the native human M3 receptor (hM3). The authors reveal that the approved drug perlapine is a novel hM3Dq agonist with >10,000- fold selectivity for hM3Dq over hM3. * PMID: 25587888

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