43 research outputs found
Protocol for a retrospective, controlled cohort study of the impact of a change in Nature journals' editorial policy for life sciences research on the completeness of reporting study design and execution
In recent years there has been increasing concern about the rigor of laboratory research. Here we present the protocol for a study comparing the completeness of reporting of in vivo and in vitro research carried in Nature Publication Group journals before and after the introduction of a change in editorial policy (the introduction of a set of guidelines for reporting); and in similar research published in other journals in the same periods. ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (doi:10.1007/s11192-016-1964-8) contains supplementary material, which is available to authorized users
Metabolism and signaling activities of nuclear lipids
Apart from the lipids present in the nuclear envelope,
the nucleus also contains lipids which are located
further inside and are resistant to treatment with nonionic
detergents. Evidence is being accumulated on the importance
of internal nuclear lipid metabolism. Nuclear lipid
metabolism gives rise to several lipid second messengers
that function within the nucleus. Moreover, it is beginning
to emerge that nuclear lipids not only act as precursors of
bioactive second messengers but may be directly involved
in regulation of nuclear structure and gene expression.
Over the last 10 years, especially the role of the inositol
lipid cycle in nuclear signal transduction has been extensively studied. This cycle is activated following a variety
of stimuli and is regulated independently from the inositide
cycle located at the plasma membrane. However, the
nucleus contain other lipids, such as phosphatidylcholine,
sphingomyelin, fatty acids and eicosanoids. There are numerous
reports which suggest that these classes of nuclear
lipids may play roles in the nucleus as important as those
of phosphoinositides. This review aims at highlighting the
most important aspects regarding the metabolism and signaling
activities of nuclear phosphatidylcholine, sphingomyelin,
fatty acids and eicosanoids
Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer
Kinases are signalling proteins which have proven to be successful targets for the treatment of a variety of diseases, predominantly in cancers. However, only a small proportion of kinases (<20%) have been investigated for their therapeutic viability, likely due to the lack of available chemical tools across the kinome. In this work we describe initial efforts in the development of a selective chemical tool for protein kinase N2 (PKN2), a relatively unexplored kinase of interest in several types of cancer. The most successful compound, 5, has a measured IC<sub>50</sub> of 0.064 μM against PKN2, with ca. 17-fold selectivity over close homologue, PKN1