The non-signalling agonist, non-transported competitive inhibitor

The non-signalling agonist, non-transported competitive inhibitor of Gap1 transport, L-Asp-gamma-L-Phe, induces oligo-ubiquitination but

no discernible endocytosis. The Km of L-citrulline transport is much lower than the threshold concentration for signalling and endocytosis. These Combretastatin A4 clinical trial results show that molecules can be transported without triggering signalling or substantial endocytosis, and that oligo-ubiquitination and endocytosis do not require signalling nor metabolism. Oligo-ubiquitination is required, but apparently not sufficient to trigger endocytosis. In addition, we demonstrate intracellular cross-induction of endocytosis of transport-defective Gap1(Y395C) by ubiquitination- and endocytosis-deficient Gap1(K9R,K16R). Our results support the concept that different substrates bind to partially overlapping binding sites in the same general substrate-binding pocket of Gap1, triggering divergent conformations, resulting in different conformation-induced downstream processes.”
“The synthesis of diesel or jet fuels intermediates from furfural high throughput screening or 5-hydroxymethylfurfural (HMF) via aqueous aldol-condensation with cyclopentanone was studied. Cyclopentanone is the product of furfural rearrangement

in an aqueous system. Since the aldol-condensation reaction is conducted in an aqueous solution all these biomass-derived reactants can be applied as water solutions formed in the processes of their preparation. The aldol condensation of furfural with cyclopentanone is at low concentration of base and molar ratio of reactants 2:1 highly selective and after 40-80 mm of reaction at

a temperature of 40-100 C more than 95 mol% yield of 2,5-bis (2-furylmethylidene) cyclopentan-1-one (F2C) was obtained. When instead of furfural as a reactant HMF was used higher than 98 mol% yield of 2,5-bis (5-hydroxymethy1-2-furylmethylidene) cyclopentan-1-one was achieved. The final products of aldol CYT387 condensation of furfural and HMF are exclusively corresponding dimers, what enables to obtain after subsequent hydrogenation/hydrodeoxygenation step dialkylcyclopentane type of diesel or jet fuels having C-15 or C-17 molecules. (C) 2014 Elsevier Ltd. All rights reserved.”
“Identifying key mediators of cancer cell invasion and metastasis is critical to the development of more effective cancer therapies. We previously identified Filamin A interacting protein 1-like (FILIP1L) as an important inhibitor of cell migration and invasion in ovarian cancer. FILIP1L expression was inversely correlated with the invasive potential of ovarian cancer cell lines and ovarian cancer specimens. We also demonstrated that DNA methylation in the FILIP1L promoter was a mechanism by which FILIP1L was down-regulated in ovarian cancer. In our present study, we tested this observation in other cancer histologies: breast, colon, lung and pancreatic cancers.

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