22 research outputs found
TRY plant trait database â enhanced coverage and open access
Plant traits - the morphological, anatomical, physiological, biochemical and phenological characteristics of plants - determine how plants respond to environmental factors, affect other trophic levels, and influence ecosystem properties and their benefits and detriments to people. Plant trait data thus represent the basis for a vast area of research spanning from evolutionary biology, community and functional ecology, to biodiversity conservation, ecosystem and landscape management, restoration, biogeography and earth system modelling. Since its foundation in 2007, the TRY database of plant traits has grown continuously. It now provides unprecedented data coverage under an open access data policy and is the main plant trait database used by the research community worldwide. Increasingly, the TRY database also supports new frontiers of traitâbased plant research, including the identification of data gaps and the subsequent mobilization or measurement of new data. To support this development, in this article we evaluate the extent of the trait data compiled in TRY and analyse emerging patterns of data coverage and representativeness. Best species coverage is achieved for categorical traits - almost complete coverage for âplant growth formâ. However, most traits relevant for ecology and vegetation modelling are characterized by continuous intraspecific variation and traitâenvironmental relationships. These traits have to be measured on individual plants in their respective environment. Despite unprecedented data coverage, we observe a humbling lack of completeness and representativeness of these continuous traits in many aspects. We, therefore, conclude that reducing data gaps and biases in the TRY database remains a key challenge and requires a coordinated approach to data mobilization and trait measurements. This can only be achieved in collaboration with other initiatives
Discovery and Optimization of Potent, Selective, and <i>in Vivo</i> Efficacious 2âAryl Benzimidazole BCATm Inhibitors
To
identify BCATm inhibitors suitable for <i>in vivo</i> study,
Encoded Library Technology (ELT) was used to affinity screen
a 117 million member benzimidazole based DNA encoded library, which
identified an inhibitor series with both biochemical and cellular
activities. Subsequent SAR studies led to the discovery of a highly
potent and selective compound, 1-(3-(5-bromothiophene-2-carboxamido)Âcyclohexyl)-<i>N</i>-methyl-2-(pyridin-2-yl)-1<i>H</i>-benzoÂ[d]Âimidazole-5-carboxamide
(<b>8b</b>) with much improved PK properties. X-ray structure
revealed that <b>8b</b> binds to the active site of BACTm in
a unique mode via multiple H-bond and van der Waals interactions.
After oral administration, <b>8b</b> raised mouse blood levels
of all three branched chain amino acids as a consequence of BCATm
inhibition