TABLE OF CONTENTS |
May 17 2012, Volume 5 / Issue 20 |
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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