Differences in the elemental composition of plants, mainly C, N, and P, have been shown to be related to differences in their nutritional status, and their morphological and functional traits. The relationship between morphological traits and micronutrients and trace elements, however, has been much less studied. Additionally, in bryophytes, research devoted to investigating these relationships is still very scarce.
View Article and Find Full Text PDFEcological stoichiometry and studies of biogeochemical niches have mainly focused on plankton and vascular plants, but the phenotypically closest modern relatives of early plants, bryophytes, have been largely neglected. We analysed C:N:P stoichiometries and elemental compositions (K, Na, Mg, Ca, S, Fe) of 35 widely distributed bryophyte species inhabiting springs. We estimated bryophyte C:N:P ratios and their biogeochemical niches, investigated how elementomes respond to the environment and determined whether they tend to diverge more for coexisting than non-coexisting individuals and species.
View Article and Find Full Text PDFACS Med Chem Lett
November 2020
Protein arginine methyltransferase 5 (PRMT5) is an enzyme that can symmetrically dimethylate arginine residues in histones and nonhistone proteins by using -adenosyl methionine (SAM) as the methyl donating cofactor. We have designed a library of SAM analogues and discovered potent, cell-active, and selective spiro diamines as inhibitors of the enzymatic function of PRMT5. Crystallographic studies confirmed a very interesting binding mode, involving protein flexibility, where both the cofactor pocket and part of substrate binding site are occupied by these inhibitors.
View Article and Find Full Text PDFIn the search for novel influenza inhibitors we evaluated 7-fluoro-substituted indoles as bioisosteric replacements for the 7-azaindole scaffold of Pimodivir, a PB2 (polymerase basic protein 2) inhibitor currently in clinical development. Specifically, a 5,7-difluoroindole derivative was identified as a potent and metabolically stable influenza inhibitor. demonstrated a favorable oral pharmacokinetic profile and in vivo efficacy in mice.
View Article and Find Full Text PDFThe ³Cat-3/MOTS (3: Cube, Cat: Catalunya, 3: 3rd CubeSat mission/Missió Observació Terra Satèl·lit) mission is a joint initiative between the Institut Cartogràfic i Geològic de Catalunya (ICGC) and the Universitat Politècnica de Catalunya-BarcelonaTech (UPC) to foster innovative Earth Observation (EO) techniques based on data fusion of Global Navigation Satellite Systems Reflectometry (GNSS-R) and optical payloads. It is based on a 6U CubeSat platform, roughly a 10 cm × 20 cm × 30 cm parallelepiped. Since 2012, there has been a fast growing trend to use small satellites, especially nanosatellites, and in particular those following the CubeSat form factor.
View Article and Find Full Text PDFThe integration of rooftop greenhouses (RTGs) in urban buildings is a practice that is becoming increasingly important in the world for their contribution to food security and sustainable development. However, the supply of tools and procedures to facilitate their implementation at the city scale is limited and laborious. This work aims to develop a specific and automated methodology for identifying the feasibility of implementation of rooftop greenhouses in non-residential urban areas, using airborne sensors.
View Article and Find Full Text PDFThe replacement of acylamino by cyclic substituents in the position 4 of the pyrazolo[3,4-]pyrimidine scaffold, led to highly active sigma-1 receptor (σR) ligands. Phenyl or pyrazolyl groups were the best in terms of affinity for the σR and the 4-(1-methylpyrazol-5-yl) derivative, , was the most selective. Compound is also one of the best σR ligands ever described in terms of lipophilic ligand efficiency, which translates into a good physicochemical and ADMET profile.
View Article and Find Full Text PDFThe synthesis of a new series of 4-acylaminopyrazolo[3,4-]pyrimidines active on the sigma-1 receptor (σR) is reported. Compounds were efficiently prepared using a two to three step process starting from commercially available 1-pyrazolo[3,4-]pyrimidin-4-amine. A SAR study shows that the σR requires the presence of relatively highly lipophilic substituents at opposite sides of the central scaffold, while selectivity the σR can be improved by shortening the distance of the basic nitrogen to it.
View Article and Find Full Text PDFA new cumacean genus and species, Ithyleucon sorbeigen. et sp. n.
View Article and Find Full Text PDFTwo new 2-(2´-hydroxyaryl)benzotriazole derivatives were synthesized and studied by photophysical and photochemical techniques in order to assess their ability to act as UV-filters. The absorption and emission properties of both compounds were determined in solvents of different polarity. In non polar solvent, a photoinduced excited state intramolecular proton transfer was established leading to efficient non radiative dissipation of UV-energy.
View Article and Find Full Text PDFThe Mediterranean Sea is a marine biodiversity hot spot. Here we combined an extensive literature analysis with expert opinions to update publicly available estimates of major taxa in this marine ecosystem and to revise and update several species lists. We also assessed overall spatial and temporal patterns of species diversity and identified major changes and threats.
View Article and Find Full Text PDFCent Nerv Syst Agents Med Chem
September 2009
A large number of therapeutic roles have been proposed for sigma(1) receptors but the involvement of sigma(1) receptor in non-acute pain had not been well explored up to now. sigma(1) receptor knock-out mice became available offering us the possibility to study the role of sigma(1) receptor in nociception, particularly in models where central sensitization processes play a significant role. Given the attractive therapeutic potential, we have developed a chemical program aimed at the discovery of novel and selective sigma(1) ligands.
View Article and Find Full Text PDFBased on a medicinal-chemistry-guided approach, three novel series of druglike cycloalkyl-annelated pyrazoles were synthesized and display high affinity (pKi>8) for the sigma1 receptor. Structure-affinity relationships were established, and the different scaffolds were optimized with respect to sigma1 binding and selectivity versus the sigma2 receptor and the hERG channel, resulting in selective compounds that have Ki values (for sigma1) in the subnanomolar range. Selected compounds were screened for cytochrome P450 inhibition (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4), metabolic stability (rat and human liver microsomes), and cell-membrane permeability (Caco-2).
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