Thursday, November 15, 2012

SciBX: Science-Business eXchange Contents: November 15 2012, Volume 5 / Issue 45

SciBX: Science-Business eXchange

TABLE OF CONTENTS

November 15 2012, Volume 5 / Issue 45

Analysis

Cover Story

The Distillery: Therapeutics

Autoimmune disease
Cancer
Infectious disease
Neurology
Pulmonary disease
Various

The Distillery: Techniques

Disease models
Drug platforms
Imaging
Markers
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Analysis

Cover Story

Top

Bringing macrocycles full circle
Joanne Kotz
doi:10.1038/scibx.2012.1176
At the recently held SciBX Innovation in Drug Discovery and Development Summit on macrocycles and constrained peptides, participants identified four areas of science in which work is needed to enable innovation in the field. Three of them—pharmacokinetics, cell permeability and oral bioavailability—aim to create an understanding of the rules that govern the behavior of macrocycles and thus enable developers to better identify drug-like compounds. The fourth one tackles the issue of targeting. Summit participants laid out a roadmap for progress across the various macrocycle platforms and concluded that much of the research should be done in the precompetitive setting.
Full Text | PDF

Distillery: Therapeutics

Autoimmune disease

Top

Transmembrane protein 173 (STING; TMEM173)
doi:10.1038/scibx.2012.1177
Mouse studies suggest inhibiting STING could help treat autoimmune disease triggered by extracellular host DNA.
Full Text | PDF

Cancer

Top

Jumonji domain containing 2C (JMJD2C; KDM4C)
doi:10.1038/scibx.2012.1178
Cell culture, mouse and patient sample studies suggest inhibiting JMJD2C could help treat breast cancer.
Full Text | PDF

SET domain and mariner transposase fusion gene (SETMAR; METNASE)
doi:10.1038/scibx.2012.1179
In vitro and mouse studies suggest ciprofloxacin could help sensitize tumors to chemotherapy.
Full Text | PDF

Epidermal growth factor receptor (EGFR)
doi:10.1038/scibx.2012.1180
In vitro and mouse studies identified 2,8-dianilino-purine compounds that could help treat EGFR-mutant lung cancer.
Full Text | PDF

MicroRNA-29 (miR-29); c-Myc (MYC); histone deacetylase 3 (HDAC3); enhancer of zeste homolog 2 (EZH2)
doi:10.1038/scibx.2012.1181
In vitro and mouse studies suggest increasing miR-29 expression by combined inhibition of HDAC3 and EZH2 could help treat MYC-overexpressing cancers.
Full Text | PDF

Indoleamine 2,3-dioxygenase (INDO; IDO)
doi:10.1038/scibx.2012.1182
Mouse studies suggest Salmonella typhimurium engineered to express IDO small hairpin RNA could help treat melanoma.
Full Text | PDF

Not applicable
doi:10.1038/scibx.2012.1183
Mouse studies identified a UV-radiation–independent mechanism contributing to melanoma development in fair-skinned patients that could be blocked to prevent the disease.
Full Text | PDF

Infectious disease

Top

Not applicable
doi:10.1038/scibx.2012.1184
Mouse studies suggest a combination of neutralizing antibodies could help treat HIV.
Full Text | PDF

Neurology

Top

Not applicable
doi:10.1038/scibx.2012.1185
Rat studies suggest blocking thalamocortical neuronal activity could help treat and prevent seizures.
Full Text | PDF

Pulmonary disease

Top

Poly(ADP-ribose) polymerase-3 (PARP-3)
doi:10.1038/scibx.2012.1186
Cell culture and mouse studies suggest antagonizing PARP-3 could be useful for treating CF.
Full Text | PDF

Transient receptor potential vanilloid 4 (TRPV4; VRL2)
doi:10.1038/scibx.2012.1187
Animal studies suggest inhibiting TRPV4 could help treat pulmonary edema.
Full Text | PDF

Various

Top

σ1 Receptor; σ2 receptor
doi:10.1038/scibx.2012.1188
In vitro and mouse studies suggest adamantine phenylalkylamines could help treat cancer and reduce neuropathic pain induced by cancer drugs.
Full Text | PDF

Distillery: Techniques

Disease models

Top

Crystal structures that model T cell receptor (TCR)-mediated nickel allergy
doi:10.1038/scibx.2012.1189
Crystal structures that model TCR-mediated nickel allergy could help identify new strategies to treat or prevent the condition.
Full Text | PDF

Microfluidic device to model IL-2–induced pulmonary edema
doi:10.1038/scibx.2012.1190
In vitro studies suggest a microfluidic device could be used to model pulmonary edema and identify molecules to prevent the disease.
Full Text | PDF

Drug platforms

Top

Bicyclic peptides conjugated to an albumin-binding peptide to extend serum half-life
doi:10.1038/scibx.2012.1191
A study in mice suggests conjugating bicyclic peptides to an albumin-binding peptide could increase therapeutic duration.
Full Text | PDF

Sinefungin derivatives as small molecule chemical probes of SET domain–containing histone methyltransferase function
doi:10.1038/scibx.2012.1192
Sinefungin derivatives could be used to probe the therapeutic potential of inhibiting SET domain–containing histone methyltransferases.
Full Text | PDF

Imaging

Top

Imaging cancer metastasis using aptamer-functionalized silica nanoparticles
doi:10.1038/scibx.2012.1193
Aptamer-functionalized silica nanoparticles could be used to image tumor metastasis.
Full Text | PDF

Noninvasive, laser-based imaging through opaque scattering
doi:10.1038/scibx.2012.1194
A noninvasive, laser-based approach to image through opaque scattering layers could be useful for imaging biological structures.
Full Text | PDF

Toll-like receptor 2 (TLR2) agonist–based fluorescent imaging of pancreatic tumors
doi:10.1038/scibx.2012.1195
A TLR2 agonist–based imaging agent could aid surgical resection of pancreatic tumors.
Full Text | PDF

Markers

Top

Bcl2 homology domain 3 (BH3)-derived peptides to predict patient outcome in acute myelogenous leukemia (AML)
doi:10.1038/scibx.2012.1196
A BH3 peptide–based assay could be used to predict outcomes for patients with AML in response to chemotherapy.
Full Text | PDF

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