Thursday, January 10, 2013

SciBX: Science-Business eXchange Contents: January 10 2013, Volume 6 / Issue 1

SciBX: Science-Business eXchange

TABLE OF CONTENTS

January 10 2013, Volume 6 / Issue 1

Analysis

Cover Story
Translational Notes
Targets and Mechanisms
Tools

The Distillery: Therapeutics

Cancer
Cardiovascular disease
Endocrine/metabolic disease
Infectious disease
Musculoskeletal disease
Neurology

The Distillery: Techniques

Assays and screens
Chemistry
Drug delivery
Imaging
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Analysis

Cover Story

Top

mAb about FGF21
Chris Cain
doi:10.1038/scibx.2013.1
Amgen researchers have developed an antibody that mimics fibroblast growth factor 21 and has antidiabetic effects in monkeys. The findings cap a year of advances that have greatly increased understanding of the protein's tissue-specific actions and are informing drug development by at least six companies.
Full Text | PDF

Translational Notes

Top

DUX4 partnership
Lauren Martz
doi:10.1038/scibx.2013.2
Fred Hutchinson Cancer Research Center researchers have identified a mutation of double homeobox 4 that could be targeted in facioscapulohumeral muscular dystrophy. The team has partnered with GlaxoSmithKline to develop small molecule inhibitors against DUX4 or its downstream effectors.
Full Text | PDF

Targets and Mechanisms

Top

Targeting inflammation in AD
Lev Osherovich
doi:10.1038/scibx.2013.3
German researchers have implicated the inflammasome as a key player in Alzheimer's disease. The findings provide additional evidence that AD could be treated with anti-inflammatory agents that act upstream of β-amyloid deposition.
Full Text | PDF

Tools

Top

Scaling up iPS cells
Joanne Kotz
doi:10.1038/scibx.2013.4
A Memorial Sloan-Kettering team has conducted one of the first large-scale screens of a small molecule library in neuronal cells obtained by differentiating patient-derived iPS cells. Separately, a partnership led by Roche and the University of Oxford is aiming to establish a repository of iPS cells from 500 patients with diabetes or various neurological diseases.
Full Text | PDF

Distillery: Therapeutics

Cancer

Top

Sirtuin 6 (SIRT6)
doi:10.1038/scibx.2013.5
Patient tissue and mouse studies suggest activating SIRT6 could help modulate tumor metabolism to treat cancer.
Full Text | PDF

β-Catenin (CTNNB1); yes-associated protein 1 (YAP1); v-yes-1 Yamaguchi sarcoma viral oncogene homolog 1 (YES1; Yes)
doi:10.1038/scibx.2013.6
Studies in cancer cell lines suggest inhibiting YES1 could help treat CTNNB1-driven colon cancers.
Full Text | PDF

Enhancer of zeste homolog 2 (EZH2)
doi:10.1038/scibx.2013.7
In vitro studies identified an EZH2 inhibitor that could help treat DLBCL.
Full Text | PDF

Myeloid-lymphoid or mixed-lineage leukemia (MLL; HRX); WD repeat domain 5 (WDR5)
doi:10.1038/scibx.2013.8
In vitro studies identified inhibitors of the protein-protein interaction between WDR5 and MLL protein-protein interactions that could help treat leukemias.
Full Text | PDF

Neurofibromin 1 (NF1); MEK
doi:10.1038/scibx.2013.9
Two studies in mice suggest MEK inhibitors could help treat cancers with mutations in NF1.
Full Text | PDF

DNA methyltransferase
doi:10.1038/scibx.2013.10
In vitro and mouse studies suggest hypomethylating agents could help treat pancreatic ductal adenocarcinoma (PDAC).
Full Text | PDF

Enhancer of zeste homolog 2 (EZH2); protein kinase B (PKB; PKBA; AKT; AKT1)
doi:10.1038/scibx.2013.11
Cell culture studies suggest inhibiting the histone methyltransferase EZH2 could help treat prostate cancer.
Full Text | PDF

Cardiovascular disease

Top

Sirtuin 2 (SIRT2)
doi:10.1038/scibx.2013.12
Mouse studies suggest inhibiting SIRT2 could help treat ischemia/reperfusion injury.
Full Text | PDF

Endocrine/metabolic disease

Top

G protein–coupled receptor 119 (GPR119)
doi:10.1038/scibx.2013.13
Mouse studies identified a series of indolines that act as selective GPR119 agonists and could help treat type 2 diabetes.
Full Text | PDF

Infectious disease

Top

Protozoan signal peptide peptidase (SPP)
doi:10.1038/scibx.2013.14
Cell culture studies suggest inhibiting protozoan SPP could help treat parasitic infections.
Full Text | PDF

CC chemokine receptor 5 (CCR5; CD195)
doi:10.1038/scibx.2013.15
Cell culture and mouse studies suggest inhibiting CCR5 could help treat Staphylococcus aureus infections.
Full Text | PDF

Musculoskeletal disease

Top

Dystrophin (DMD)
doi:10.1038/scibx.2013.16
In vitro and mouse studies suggest the ryanodine receptor (RyR) inhibitor dantrolene could enhance the effects of antisense oligonucleotides to treat Duchenne muscular dystrophy.
Full Text | PDF

Transient receptor potential vanilloid 1 (TRPV1; VR1)
doi:10.1038/scibx.2013.17
In vitro and mouse studies suggest activating TRPV1 in skeletal muscle could help treat or prevent muscular atrophy.
Full Text | PDF

MicroRNA-214 (miR-214)
doi:10.1038/scibx.2013.18
In vitro and mouse studies suggest inhibiting miR-214 could help treat osteoporosis.
Full Text | PDF

Neurology

Top

GABAA receptor
doi:10.1038/scibx.2013.19
In vitro and mouse studies suggest GABAA receptor agonists could help treat motor dysfunctions associated with Angelman syndrome, a neurogenetic disorder caused by deletion or inactivation of genes on chromosome 15.
Full Text | PDF

Inhibitor of κ-light polypeptide gene enhancer in B cells kinase complex–associated protein (IKBKAP); adrenergic receptor α2 (ADRA2)
doi:10.1038/scibx.2013.20
A study in neural cells derived from patients with familial dysautonomia (FD) suggests antagonizing ADRA2 could help treat the disease.
Full Text | PDF

Unknown
doi:10.1038/scibx.2013.21
Mouse studies suggest lithium could help treat Down syndrome.
Full Text | PDF

Distillery: Techniques

Assays and screens

Top

Assays to monitor leucine-rich repeat kinase 2 (LRRK2) activity
doi:10.1038/scibx.2013.22
Cell-based and pharmacodynamic assays for monitoring LRRK2 activity could help identify compounds to treat Parkinson's disease (PD).
Full Text | PDF

Chemistry

Top

Natural product–based fragment libraries for ligand discovery
doi:10.1038/scibx.2013.23
Natural product–based fragment libraries could be used to identify ligands against targets that are difficult to drug.
Full Text | PDF

Drug delivery

Top

Glycosylated triterpene–mediated transdermal delivery of macromolecules
doi:10.1038/scibx.2013.24
Ex vivo studies suggest glycosylated triterpenes are capable of transdermal transport and could help mediate therapeutic macromolecule delivery.
Full Text | PDF

Imaging

Top

Probe for functional imaging of legumain (LGMN)
doi:10.1038/scibx.2013.25
An activity-based fluorescent probe could be used to study the activity of LGMN, a protein associated with cancer and inflammation.
Full Text | PDF

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