TABLE OF CONTENTS |
February 21 2013, Volume 6 / Issue 7 |
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The Distillery: Therapeutics Cancer Dermatology Endocrine/metabolic disease Infectious disease Musculoskeletal disease Neurology Other Renal disease
The Distillery: Techniques Assays and screens Disease models Drug delivery Drug platforms
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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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SciBX: Science-Business eXchange Recommend SciBX to your library today
SciBx is a weekly publication that identifies and analyzes the most important translational research articles from over 40 journals. Find out which papers have real scientific and commercial potential, and why. Subscribe to SciBX and you won't miss the next big thing.
For more information visit: www.nature.com/scibx. | |
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Analysis |
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Cover Story | Top |
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NRG1 meets resistance Lev Osherovich doi:10.1038/scibx.2013.155
Researchers at Roche's Genentech unit have shown that neuregulin 1 can drive resistance to chemotherapy in non–small cell lung cancers. The team suggests countering resistance by hitting the kinase ligand and a pair of kinases in conjunction with conventional chemotherapy.
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Targets and Mechanisms | Top |
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Huperzine A in SCI Tim Fulmer doi:10.1038/scibx.2013.156
Harvard Medical School researchers have shown that the plant-derived small molecule huperzine A can reduce neuropathic pain in mice with spinal cord injury. Insero Health has licensed IP covering epilepsy and neuropathic pain and plans to report Phase Ib data this year in treatment-resistant epilepsy.
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Promoting telomerase Chris Cain doi:10.1038/scibx.2013.157
Two independent teams have identified activating mutations in the promoter of TERT that occur in more than 70% of melanoma cases. The functional role of these mutations still needs further exploration before their therapeutic relevance can be assessed.
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Tools | Top |
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Small molecules vs. teratomas Kai-Jye Lou doi:10.1038/scibx.2013.158
Researchers at The Hebrew University of Jerusalem and Roche have identified small molecules that prevented human pluripotent stem cells from forming teratomas in mice following transplantation. The molecules could be useful for reducing the tumorigenicity risk of cell therapies derived from stem cells.
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Distillery: Therapeutics |
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Cancer | Top |
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Stem cell factor receptor tyrosine kinase (c-Kit; KIT; CD117) doi:10.1038/scibx.2013.159
In vitro and mouse studies suggest an anti-KIT mAb could help treat gastrointestinal stromal tumors (GISTs).
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Neuregulin 1 (NRG1); epidermal growth factor receptor 3 (EGFR3; HER3; ErbB3); HER4 (EGFR4; ErbB4) doi:10.1038/scibx.2013.160
Cell culture and mouse studies suggest antagonizing NRG1, HER3 or HER4 could be useful for preventing chemotherapy resistance in NSCLC.
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BRAF; epidermal growth factor receptor 3 (EGFR3; HER3; ErbB3) doi:10.1038/scibx.2013.161
Cell culture and mouse studies suggest Zelboraf vemurafenib plus Tykerb lapatinib could be used to treat BRAF-mutant thyroid cancer.
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Dermatology | Top |
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Erythropoietin (EPO); colony stimulating factor 2 receptor-β low-affinity (CSF2RB; CD131) doi:10.1038/scibx.2013.162
Mouse studies suggest an EPO mimetic could help treat burns. EPO signaling through a heteromeric receptor that combines the EPO receptor and CD131 has been shown to decrease tissue damage.
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Endocrine/metabolic disease | Top |
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Receptor activator of NF-κB ligand (RANKL; TNFSF11) doi:10.1038/scibx.2013.163
Patient and mouse studies suggest RANKL antagonists could help treat type 2 diabetes.
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Infectious disease | Top |
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ATG6 autophagy related 6 homolog (BECN1; ATG6); GLI pathogenesis-related 2 (GLIPR2; GAPR-1) doi:10.1038/scibx.2013.164
Mouse and cell culture studies suggest blocking the interaction between BECN1 and GAPR-1 could help treat viral infections.
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Musculoskeletal disease | Top |
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Free fatty acid receptor 1 (FFAR1; GPR40) doi:10.1038/scibx.2013.165
Studies in mice suggest GPR40 agonists could help prevent bone loss.
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Neurology | Top |
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Metabotropic glutamate receptor subtype 2 (mGluR2; GRM2) doi:10.1038/scibx.2013.166
Patient sample and rat studies suggest normalizing mGluR2 expression could help treat alcoholism.
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CD36 (GPIV) doi:10.1038/scibx.2013.167
Mouse studies suggest antagonizing CD36 could help treat cerebral amyloid angiopathy.
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Glucocorticoid receptor (GCCR) doi:10.1038/scibx.2013.168
Mouse studies suggest targeting glucocorticoid-mediated modulation of neurogenesis could help prevent or treat stress-induced depression.
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Prostaglandin E2 receptor EP2 subtype (prostanoid EP1 receptor; PTGER2) doi:10.1038/scibx.2013.169
Mouse studies suggest PTGER2 antagonism could help treat status epilepticus, which is characterized by persistent seizures.
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Not applicable doi:10.1038/scibx.2013.170
Studies in rats suggest the small molecule natural product huperzine A could help treat neuropathic pain associated with spinal cord injury (SCI).
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Other | Top |
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Usher syndrome 1C (USH1C) doi:10.1038/scibx.2013.171
Mouse studies suggest using antisense oligonucleotides (ASOs) that correct splicing of mutant USH1C transcripts could help prevent Usher syndrome–associated hearing loss.
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Renal disease | Top |
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WAP four-disulfide core domain 2 (WFDC2; HE4) doi:10.1038/scibx.2013.172
Studies in patient tissue and in mice suggest antagonizing HE4 could help treat renal fibrosis.
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Distillery: Techniques |
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Assays and screens | Top |
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Cell-free protein synthesis (CFPS), whole-pathway screen to identify druggable host-virus protein-protein interactions doi:10.1038/scibx.2013.173
A CFPS, whole-pathway screen could help identify druggable host-virus protein-protein interactions.
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Disease models | Top |
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Engineered, functional bone organ as a model to study bone development and regeneration doi:10.1038/scibx.2013.174
An engineered, functional bone organ could be useful for studying bone development and regeneration.
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Mouse model for proteolytic clearance of plasma β-amyloid (Aβ) doi:10.1038/scibx.2013.175
Mouse studies suggest reducing plasma Aβ levels may not be sufficient to decrease Aβ in the CNS.
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Drug delivery | Top |
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Dendritic cell (DC)-mediated delivery of tacrolimus to autoreactive T cells doi:10.1038/scibx.2013.176
In vitro and mouse studies suggest DCs could be useful for delivering Prograf to treat autoimmune diseases.
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Injectable, protease-activated depots of glucagon-like peptide-1 (GLP-1) doi:10.1038/scibx.2013.177
Injectable, protease-activated depots of GLP-1 could enable sustained delivery of the peptide to treat diabetes.
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Drug platforms | Top |
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Epigenetic, methyllysine-binding protein inhibitors doi:10.1038/scibx.2013.178
Identification of the first potent and selective inhibitor of a methyllysine-binding domain suggests this class of epigenetic proteins could be targeted with small molecules.
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Human induced pluripotent stem (iPS) cell–derived oligodendrocyte progenitor cells for treating demyelinating diseases doi:10.1038/scibx.2013.179
Mouse studies suggest iPS cell–derived oligodendrocyte progenitors could help treat demyelinating diseases.
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