Thursday, January 5, 2012

SciBX: Science-Business eXchange Contents: January 05 2012, Volume 5 / Issue 1

SciBX: Science-Business eXchange

TABLE OF CONTENTS

January 5 2012, Volume 5 / Issue 1

Analysis

Cover Story
Translational Notes
Targets and Mechanisms
Tools

The Distillery: Therapeutics

Cancer
Cardiovascular disease
Dermatology
Endocrine/metabolic disease
Infectious disease
Musculoskeletal disease
Neurology
Ophthalmic disease
Autoimmune disease

The Distillery: Techniques

Assays and screens
Chemistry
Drug platforms
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Analysis

Cover Story

Top

No place like inflammasome
Lauren Martz
doi:10.1038/scibx.2012.1
Researchers at Virginia Commonwealth University have found that inhibiting inflammasome formation with P2X7 antagonists could help prevent heart failure following acute myocardial infarction. The findings point to a repurposing opportunity for P2X7 antagonists that companies have in the clinic for inflammatory indications.
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Translational Notes

Top

AstraZeneca's compound interest
Lev Osherovich
doi:10.1038/scibx.2012.2
The U.K.'s Medical Research Council has partnered with AstraZeneca to make the pharma's shelved compounds available to academics investigating basic disease mechanisms. A first call for proposals is in progress.
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Targets and Mechanisms

Top

Fine-tuning mGluRs
Lev Osherovich
doi:10.1038/scibx.2012.3
UPenn and MIT teams have independently converged on mGluRs as players in ADHD and autism. The findings suggest agonizing mGluRs in patients with ADHD or certain forms of autism and antagonizing the targets in other forms of autism.
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Tools

Top

Eau de fluorescence
Joanne Kotz
doi:10.1038/scibx.2012.4
NCI and University of Tokyo researchers have developed a fluorescent probe that can be sprayed onto tissue during surgery to detect small metastases. The researchers plan to validate the method in fresh surgical tissue from ovarian cancer patients in preparation for an IND.
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Distillery: Therapeutics

Autoimmune disease

Top

DEAD box polypeptide 58 (DDX58; RIG-I); interferon induced with helicase C domain 1 (IFIH1; MDA5)
doi:10.1038/scibx.2012.5
Mouse studies suggest activating RIG-I or MDA5 could help treat MS.
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Sphingosine 1-phosphate receptor 1 (S1PR1; S1P1; EDG1)
doi:10.1038/scibx.2012.6
Mouse studies suggest an S1P1 antagonist might help treat RA and other autoimmune indications.
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Cancer

Top

Neuroblastoma Ras viral oncogene (NRAS); lysophospholipase I (LYPLA1; APT-1)
doi:10.1038/scibx.2012.7
Cell culture studies suggest inhibiting APT-1 could help treat mutant NRAS–driven leukemias.
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c-Myc (MYC); SUMO1 activating enzyme subunit 1 (SAE1); ubiquitin-like modifier activating enzyme 2 (UBA2; SAE2)
doi:10.1038/scibx.2012.8
Patient tissue and mouse studies suggest inhibiting SAE1 and/or SAE2 could help treat MYC-driven breast cancers.
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Vascular cell adhesion molecule-1 (VCAM-1); integrin α4 (VLA-4; CD49D)
doi:10.1038/scibx.2012.9
In vitro, mouse and human studies suggest inhibiting VCAM-1 or its receptor VLA-4 could help prevent bone metastases in breast cancer.
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Checkpoint kinase 1 (Chk1)
doi:10.1038/scibx.2012.10
Mouse and cell culture studies suggest Chk1 inhibitors should not be combined with histone deacetylase (HDAC) inhibitors to treat cancer.
Full Text | PDF

Thioredoxin; thioredoxin reductases
doi:10.1038/scibx.2012.11
Mouse studies identified peptidomimetic inhibitors of the thioredoxin reductase pathway that could help treat cancer.
Full Text | PDF

MEK; BCR-ABL tyrosine kinase
doi:10.1038/scibx.2012.12
Cell culture and mouse studies suggest combining Tasigna nilotinib with MEK inhibitors could help treat drug-resistant CML.
Full Text | PDF

Bone morphogenetic protein 7 (BMP7; OP-1)
doi:10.1038/scibx.2012.13
Mouse studies suggest BMP7 could help prevent bone metastasis in prostate cancer.
Full Text | PDF

Cardiovascular disease

Top

G protein–coupled bile acid receptor 1 (GPBAR1; TGR5)
doi:10.1038/scibx.2012.14
Mouse studies suggest agonizing TGR5 could help prevent atherosclerosis.
Full Text | PDF

Rho kinase
doi:10.1038/scibx.2012.15
In vitro and mouse studies suggest inhibiting rho kinase could help prevent atherosclerosis progression.
Full Text | PDF

Dermatology

Top

Focal adhesion kinase (FAK)
doi:10.1038/scibx.2012.16

Full Text | PDF

Endocrine/metabolic disease

Top

Histone deacetylase (HDAC); glucocerebrosidase (GBA; GCase)
doi:10.1038/scibx.2012.17
In vitro studies suggest HDAC inhibitors could help treat Gaucher's disease.
Full Text | PDF

Infectious disease

Top

PD-1 receptor (PDCD1; PD-1; CD279); programmed cell death 1 ligand 1 (CD274 molecule; PD-L1; B7-H1); lymphocyte-activation gene 3 (LAG3; CD223)
doi:10.1038/scibx.2012.18
Patient sample and mouse studies suggest inhibiting PD-L1 and LAG3 could help treat malaria.
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Heme oxygenase decycling 1 (HMOX1; HO-1; Hsp32)
doi:10.1038/scibx.2012.19
Mouse studies suggest inhibiting HO-1 could protect against Salmonella infection in patients exposed to malaria.
Full Text | PDF

Musculoskeletal disease

Top

Guanine nucleotide binding protein (G protein) α-inhibiting activity polypeptide 2 (GNAI2)
doi:10.1038/scibx.2012.20
Mouse and tissue culture studies suggest increasing GNAI2 signaling could help promote muscle repair and regeneration.
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Neurology

Top

β-Amyloid (Aβ)
doi:10.1038/scibx.2012.21
In vitro studies suggest grafted antibodies that recognize AD-associated Aβ fibrils could help treat AD.
Full Text | PDF

Metabotropic glutamate receptor subtype 5 (mGluR5; GRM5); mGluR7 (GRM7); mGluR8 (GRM8)
doi:10.1038/scibx.2012.22
A genomewide association study suggests agonizing mGluR5, mGluR7 or mGluR8 could be useful for treating ADHD.
Full Text | PDF

Metabotropic glutamate receptor subtype 5 (mGluR5; GRM5)
doi:10.1038/scibx.2012.23
Studies in mice suggest agonizing mGluR5 may help treat a hereditary form of ASD caused by tuberous sclerosis complex (TSC).
Full Text | PDF

Ophthalmic disease

Top

Vimentin (VIM)
doi:10.1038/scibx.2012.24
A study in mice suggests decreasing VIM expression could help reduce fibrosis resulting from corneal wounds.
Full Text | PDF

Distillery: Techniques

Assays and screens

Top

High throughput sequencing of tumor tissue to guide clinical trial enrollment
doi:10.1038/scibx.2012.25
High throughput sequencing of tumor tissue from patients with advanced cancer could help guide clinical trial enrollment.
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Quantification of minimal residual disease in chronic lymphocytic leukemia (CLL) following hematopoietic stem cell transplant
doi:10.1038/scibx.2012.26
High throughput measurement of minimal residual disease in CLL following hematopoietic stem cell transplant could improve early intervention to prevent disease relapse.
Full Text | PDF

Real-time classification of glioma tumors with mass spectrometry–based lipid profiling
doi:10.1038/scibx.2012.27
A mass spectrometry–based method for profiling lipids in glioma tissue samples could enable classification of brain tumors during surgery.
Full Text | PDF

Chemistry

Top

Selective arylation of imidazoles to synthesize Tasigna nilotinib and its analogs
doi:10.1038/scibx.2012.28
N1-selective palladium-catalyzed arylation of imidazoles could be used to synthesize Tasigna nilotinib and its analogs.
Full Text | PDF

Drug platforms

Top

Prophylactic vaccination with antibody-expressing adenoviral transgenes
doi:10.1038/scibx.2012.29
An adenoviral vector encoding pathogen-neutralizing antibodies could help prevent viral infections.
Full Text | PDF

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