TABLE OF CONTENTS |
May 17 2012, Volume 5 / Issue 20 |
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| Analysis Cover Story Targets and Mechanisms Tools
The Distillery: Therapeutics Cancer Cardiovascular disease Endocrine/metabolic disease Infectious disease Inflammation Neurology Ophthalmic disease Pulmonary disease Renal disease Various
The Distillery: Techniques Drug platforms
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Analysis |
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Cover Story | Top |
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Eyeing the inflammasome Tim Fulmer doi:10.1038/scibx.2012.511 Two academic teams have independently shown that targeting the inflammasome reduces retinal damage in mouse models of age-related macular degeneration. One study favors inhibiting inflammasome activation to treat dry AMD, and those findings are licensed to iVeena Pharmaceuticals. The other approach suggests boosting the inflammasome to treat wet AMD. Full Text | PDF |
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Targets and Mechanisms | Top |
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Paradoxical P2X7 Tracey Baas doi:10.1038/scibx.2012.512 Italian researchers have shown that inhibiting the P2X7 receptor can treat cancer. The findings could open up a new disease area for companies developing P2X7 antagonists to treat pain, multiple sclerosis, inflammatory bowel disease and rheumatoid arthritis. Full Text | PDF |
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K-Ras in cancer metabolism Lauren Martz doi:10.1038/scibx.2012.513 Researchers from the Dana-Farber Cancer Institute have identified a glucose metabolism pathway that is activated by the K-Ras oncogene in pancreatic cancer. Based on the findings, it may be possible to target proteins in the pathway to block proliferation of K-Ras-driven cancers. Full Text | PDF |
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Tools | Top |
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PROTAC the protein Kai-Jye Lou doi:10.1038/scibx.2012.514 GSK and Yale researchers have announced a collaboration to develop a platform that selectively tags disease-associated proteins with an E3 ubiquitin ligase ligand, thus targeting them to a cell's protein degradation machinery. GSK hopes the platform could be a cornerstone for a new Discovery Performance Unit at the pharma, and the partners are aiming to have proof-of-principle results in cell culture by year end. Full Text | PDF |
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Distillery: Therapeutics |
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Cancer | Top |
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Neutrophil elastase (NE; ELA-2); cyclin E (CCNE) doi:10.1038/scibx.2012.515 In vitro studies suggest a vaccine based on a peptide that NE cleaves from CCNE could help treat breast cancer. Full Text | PDF |
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Phosphoinositide 3-kinase-β (PI3Kβ); PTEN (MMAC1; TEP1) doi:10.1038/scibx.2012.516 A study in mice identified PI3Kβ-selective inhibitors that could help treat PTEN-deficient cancers. Full Text | PDF |
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Glutamine–fructose-6-phosphate transaminase 1 (GFPT1); K-Ras; MEK; ribose 5-phosphate isomerase A (RPIA) doi:10.1038/scibx.2012.517 In vitro studies identified targets involved in pancreatic cancer metabolism that could help treat K-Ras-driven cancers. Full Text | PDF |
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Cardiovascular disease | Top |
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Phosphoinositide 3-kinase (PI3K) doi:10.1038/scibx.2012.518 In vitro and mouse studies suggest some doses of PI3K inhibitors may induce long QT syndrome when used to treat cancer. Full Text | PDF |
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VEGF receptor 1 (FLT1; VEGFR-1) doi:10.1038/scibx.2012.519 Human and mouse studies suggest inhibiting soluble FLT1 (sFLT1) could help prevent or treat peripartum cardiomyopathy (PPCM) in women with pre-eclampsia, a known risk factor for PPCM. Full Text | PDF |
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Perilipin 5 (PLIN5) doi:10.1038/scibx.2012.520 Mouse studies suggest PLIN5 could help protect against fatty acid–induced oxidative stress and cardiac toxicity. Full Text | PDF |
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Toll-like receptor 9 (TLR9) doi:10.1038/scibx.2012.521 Mouse studies suggest inhibiting TLR9 could help prevent heart failure caused by inflammation. Full Text | PDF |
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Endocrine/metabolic disease | Top |
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Not applicable doi:10.1038/scibx.2012.522 Rodent studies suggest hydroxyflavone analogs could help treat type 2 diabetes and dyslipidemia. Full Text | PDF |
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Infectious disease | Top |
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DNA repair doi:10.1038/scibx.2012.523 In vitro studies identified a common mechanism of antibiotic-induced cell death that could aid the design of antibiotic adjuvants. Full Text | PDF |
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Influenza A virus PB1-F2 protein (PB1-F2) doi:10.1038/scibx.2012.524 In vitro and mouse studies identified a PB1-F2 inhibitor that could help treat influenza. Full Text | PDF |
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Inflammation | Top |
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Phosphoinositide 3-kinase-γ (PI3Kγ) doi:10.1038/scibx.2012.525 In vitro and mouse studies identified a sulfamoylphenyl pyrazine PI3Kγ inhibitor that could help treat inflammatory diseases. Full Text | PDF |
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Neurology | Top |
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Diacylglycerol kinase-ε (DGKE) doi:10.1038/scibx.2012.526 Mouse, fly and cell culture studies suggest inhibiting DGKE could help treat HD. Full Text | PDF |
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Bradykinin B1 receptor (BDKRB1; B1R) doi:10.1038/scibx.2012.527 An in vitro and mouse study identified cyclic peptide–based B1R antagonists that could help treat pain. Full Text | PDF |
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Monoacylglycerol lipase (MAGL) doi:10.1038/scibx.2012.528 In vitro and rodent studies identified a class of O-hexafluoroisopropyl (HFIP) carbamates that selectively inhibited MAGL and could help treat pain. Full Text | PDF |
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Ophthalmic disease | Top |
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IL-18 doi:10.1038/scibx.2012.529 Mouse studies suggest local delivery of IL-18 to the retina could help treat wet AMD. Full Text | PDF |
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Myeloid differentiation primary response gene 88 (MYD88) doi:10.1038/scibx.2012.530 Mouse studies suggest inhibiting MYD88 in the retinal pigment epithelium (RPE) could help treat dry AMD. Full Text | PDF |
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Pulmonary disease | Top |
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Sirtuin 1 (SIRT1) doi:10.1038/scibx.2012.531 Mouse studies suggest activating SIRT1 could help treat emphysema. Full Text | PDF |
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Renal disease | Top |
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Uromodulin (UMOD; THP) doi:10.1038/scibx.2012.532 Rat studies suggest antagonizing UMOD binding to immunoglobulin light chain could be useful for treating nephropathy associated with multiple myeloma. Full Text | PDF |
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Various | Top |
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Phosphoinositide 3-kinase-γ (PI3Kγ) doi:10.1038/scibx.2012.533 In vitro, cell culture and mouse studies suggest highly selective inhibitors of PI3Kγ could help treat inflammation and autoimmune diseases. Full Text | PDF |
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Heat shock protein 90 (Hsp90); lipopolysaccharide (LPS) doi:10.1038/scibx.2012.534 Cell culture studies suggest inhibiting the Hsp90-LPS interaction could help treat cancer and LPS-mediated inflammatory responses like sepsis. Full Text | PDF |
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Distillery: Techniques |
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Drug platforms | Top |
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Antisense oligonucleotides composed of 2′-deoxy-2′-fluoro (2′-F) nucleotides to modulate splicing doi:10.1038/scibx.2012.535 Antisense oligonucleotides composed of 2′-F nucleotides could help modulate splicing for therapeutic applications. Full Text | PDF |
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