SciBX: Science-Business eXchange Contents: August 22 2013, Volume 6 / Issue 32

TABLE OF CONTENTS August 22 2013, Volume 6 / Issue 32 Analysis Cover Story Translational Notes Targets and Mechanisms The Distillery: Therapeutics Autoimmune disease Cancer Cardiovascular disease Endocrine/metabolic disease Infectious disease Inflammation Musculoskeletal disease Neurology The Distillery: Techniques Assays and screens Computational models Disease models Drug platforms Imaging Advertisement Biopharma Dealmakers A supplement to Nature Biotechnology and Nature Reviews Drug Discovery  The June 2013 issue of Biopharma Dealmakers showcases companies with partnering opportunities. This week, find out about how you can collaborate with PolyPeptide Group.   Analysis Cover Story Top Deep pockets Amy Donner doi:10.1038/scibx.2013.846 The B class of GPCRs is brimming with therapeutic targets, but thus far, development of small molecule drugs has been stymied. New studies reporting the first-ever crystal structures of members of the family could change that and open up new therapeutic real estate. Full Text | PDF Translational Notes Top Found in translation: Institute Pasteur Korea Lev Osherovich doi:10.1038/scibx.2013.847 Institute Pasteur Korea is starting to see translatable results from its deal-making and drug screening efforts. After signing a pair of infectious disease discovery deals with Sanofi and Roche this year, the institute now has revealed details about a tuberculosis candidate licensed to Qurient. Full Text | PDF Targets and Mechanisms Top Tamping down TAU Lauren Martz doi:10.1038/scibx.2013.848 Despite evidence that pathologic TAU spreads through the brain in tauopathies and frontotemporal dementia, the actual mechanism is murky. According to new findings from the Washington University in St. Louis School of Medicine, heparan sulfate proteoglycans are key players. Full Text | PDF Subverting Treg-mediated protection for tumors Kai-Jye Lou doi:10.1038/scibx.2013.849 Treg cells present a conundrum for cancer researchers—the cells attenuate the effect of immunotherapies but their depletion can trigger inflammation and autoimmunity. Now, a team of researchers at St. Jude Children's Research Hospital has uncoupled these effects. Full Text | PDF Distillery: Therapeutics Autoimmune disease Top Activin A doi:10.1038/scibx.2013.850 Mouse and in vitro studies suggest activin A could help promote remyelination in MS. Full Text | PDF Cancer Top c-Mer proto-oncogene tyrosine kinase (MERTK) doi:10.1038/scibx.2013.851 In vitro and mouse studies suggest inhibiting MERTK could help treat ALL. Full Text | PDF EGF latrophilin and seven transmembrane domain containing 1 (ELTD1) doi:10.1038/scibx.2013.852 Studies in mice and in patient samples suggest inhibiting ELTD1 could help treat cancer. Full Text | PDF Lysyl oxidase (LOX) doi:10.1038/scibx.2013.853 Mouse studies suggest inhibiting LOX in the tumor stroma could help prevent metastasis. Full Text | PDF Neuropilin 1 (NRP1); semaphorin 4A (SEMA4A) doi:10.1038/scibx.2013.854 Mouse studies suggest blocking SEMA4A-NRP1 signaling could increase an antitumor immune response without causing pathogenic autoimmunity. Full Text | PDF Polypeptide N-acetylgalactosaminyltransferase (GALNT; GalNac-T) doi:10.1038/scibx.2013.855 Patient sample, cell culture and mouse studies suggest inhibiting GALNT could help treat cancer. Full Text | PDF Smoothened (SMO) doi:10.1038/scibx.2013.856 Cell culture studies suggest a small molecule antagonist of oxysterol binding to SMO could help treat cancer. Full Text | PDF Survivin (BIRC5) doi:10.1038/scibx.2013.857 In vitro and mouse studies suggest inhibiting a BIRC5 splicing isoform could help treat cancer. Full Text | PDF Tankyrase TRF1-interacting ankyrin-related ADP-ribose polymerase (TNKS); TNKS2 doi:10.1038/scibx.2013.858 In vitro and mouse studies suggest dual inhibitors of TNKS and TNKS2 could help treat cancer. Full Text | PDF Vasolin containing protein (VCP; p97) doi:10.1038/scibx.2013.859 In vitro studies identified two new classes of VCP inhibitors that could help treat cancer. Full Text | PDF Aldosterone synthase (ALDOS; CYP11B2); cytochrome P450 17 α-hydroxylase/C17, 20 lyase (CYP17) doi:10.1038/scibx.2013.860 In vitro studies identified dual CYP17 and CYP11B2 inhibitors that could help treat prostate cancer. Full Text | PDF Cyclin dependent kinase 4 (CDK4); CDK6 doi:10.1038/scibx.2013.861 In vitro and mouse studies suggest castration-resistant prostate cancers expressing the F876L androgen receptor (AR) mutation could be treated with CDK4 inhibitors. Full Text | PDF Cardiovascular disease Top Not applicable doi:10.1038/scibx.2013.862 Cell culture and mouse studies suggest a high-protein diet could improve bioavailability of the atrial fibrillation and CHF drug digoxin in patients. Full Text | PDF Endocrine/metabolic disease Top Stimulated by retinoic acid 6 (STRA6) doi:10.1038/scibx.2013.863 Mouse studies suggest antagonizing STRA6 could help treat metabolic syndrome and type 2 diabetes. Full Text | PDF Melanocortin 2 receptor accessory protein 2 (MRAP2) doi:10.1038/scibx.2013.864 Studies in human samples and in mice suggest activating MRAP2 could help treat obesity. Full Text | PDF Infectious disease Top Mycobacterium tuberculosis cytochrome bc1 doi:10.1038/scibx.2013.865 Cell culture and mouse studies identified an inhibitor of M. tuberculosis cytochrome bc1 that could be useful for treating multidrug-resistant (MDR) TB. Full Text | PDF Inflammation Top Thymic stromal lymphopoietin (TSLP) doi:10.1038/scibx.2013.866 Mouse and human biopsy studies suggest targeting TSLP could help treat eosinophilic esophagitis. Full Text | PDF Musculoskeletal disease Top Transmembrane protein 8c (TMEM8C; myomaker) doi:10.1038/scibx.2013.867 In vitro and mouse studies suggest TMEM8C could enhance muscle repair. Full Text | PDF Neurology Top Heparin sulfate proteoglycan (HSPG) doi:10.1038/scibx.2013.868 In vitro and mouse studies suggest inhibiting the interaction between microtubule-associated protein-τ (MAPT; TAU; FTDP-17) fibrils and HSPG could help treat AD. Full Text | PDF Lipocalin (LCN2; NGAL) doi:10.1038/scibx.2013.869 In vitro and mouse studies suggest inhibiting LCN2 could help treat neuropathic pain. Full Text | PDF HMG-CoA reductase; methyl CpG binding protein 2 (MECP2; RTT); squalene epoxidase (SQLE) doi:10.1038/scibx.2013.870 Mouse studies suggest inhibiting cholesterol synthesis could help treat Rett syndrome, which is caused by mutations in MECP2. Full Text | PDF Distillery: Techniques Assays and screens Top Sulfatase activity–based profiling for rapid identification of Mycobacterium species and strains doi:10.1038/scibx.2013.871 An assay for detecting bacterial sulfatase activity could enable rapid diagnosis of specific Mycobacterium infections. Full Text | PDF Computational models Top Computational prediction of clustered, regularly interspaced short palindromic repeats (CRISPR)-associated protein 9 (Cas9) target sites doi:10.1038/scibx.2013.872 A computational method to predict CRISPR-Cas9 target cleavage could help guide the design of new disease models. Full Text | PDF Disease models Top Neurobeachin-like 2 (Nbeal2) knockout mouse model of gray platelet syndrome doi:10.1038/scibx.2013.873 Mice lacking Nbeal2 could be used as models of gray platelet syndrome and could help develop new treatments for the condition. Full Text | PDF Scavenger receptor class F member 1 (SCARF1)-deficient mouse model of systemic lupus erythematosus (SLE) doi:10.1038/scibx.2013.874 In vitro and mouse studies suggest Scarf1−/− mice could model SLE and aid the development of therapeutics for the disease. Full Text | PDF Drug platforms Top Crystal structure of corticotropin-releasing factor receptor 1 (CRHR1; CRFR1) bound to a small molecule antagonist doi:10.1038/scibx.2013.875 A crystal structure of an antagonist-bound CRHR1 could help inform the development of compounds targeting class B G protein–coupled receptors (GPCRs). Full Text | PDF Crystal structure of inhibitor-bound resistance-nodulation-division multidrug efflux transporters AcrB and MexB, and a homology model of MexY doi:10.1038/scibx.2013.876 Structural studies identified binding sites on AcrB, MexB and MexY that could help design inhibitors to circumvent drug resistance in bacteria. Full Text | PDF Small molecule cocktail for generating pluripotent stem cells from somatic cells doi:10.1038/scibx.2013.877 A cocktail of small molecules could be used to reprogram fibroblasts into pluripotent stem cells. Full Text | PDF Imaging Top Genetically encoded fluorescent calcium sensors for neuronal activity imaging doi:10.1038/scibx.2013.878 In vitro and mouse studies identified fluorescent calcium sensors that could improve the sensitivity of neuronal imaging. Full Text | PDF Top Advertisement Nature Publishing Group and Relay Technology Management present: The Epigenetics Target Explorer  Click here to access this free online tool and the accompanying article in Nature Reviews Drug Discovery.

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