We describe the development of quinolylnitrones(QNs)as multifunctional ligands inhibiting cholinesterases(ChEs:acetylcholinesterase and butyrylcholinesterase—h BChE)and monoamine oxidases(hMAO-A/B)for the therapy of ...
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We describe the development of quinolylnitrones(QNs)as multifunctional ligands inhibiting cholinesterases(ChEs:acetylcholinesterase and butyrylcholinesterase—h BChE)and monoamine oxidases(hMAO-A/B)for the therapy of neurodegenerative *** identified QN 19,a simple,low molecular weight nitrone,that is readily synthesized from commercially available *** 19 has no typical pharmacophoric element to suggest ChE or MAO inhibition,yet unexpectedly showed potent inhibition of h BChE(IC50=1.06±0.31 nmol/L)and h MAO-B(IC_(50)=4.46±0.18μmol/L).The crystal structures of 19 with hBChE and hMAO-B provided the structural basis for potent binding,which was further studied by enzyme *** 19 acted as a free radical scavenger and biometal chelator,crossed the blood—brain barrier,was not cytotoxic,and showed neuroprotective properties in a 6-hydroxydopamine cell model of Parkinson's *** addition,in vivo studies showed the anti-amnesic effect of 19 in the scopolamine-induced mouse model of AD without adverse effects on motoric function and ***,chronic treatment of double transgenic APPswe-PS1δE9 mice with 19 reduced amyloid plaque load in the hippocampus and cortex of female mice,underscoring the disease-modifying effect of QN 19.
Members of the ERF Family of Transcription Factors play an important role in plant development and gene expression that regulates responses to biotic and abiotic *** work identified 36 ERF family genes in Coffea arabi...
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Members of the ERF Family of Transcription Factors play an important role in plant development and gene expression that regulates responses to biotic and abiotic *** work identified 36 ERF family genes in Coffea arabica within the AP2/ERF full domain,using the EST-based genomic resource of the Brazilian Coffee Genome *** ERF family genes were classified into nine of the ten existing groups through phylogenetic analysis of the deduced amino acid sequences and comparison with the sequences of the ERF family genes in *** addition to the AP2 domain,other conserved domains were identified,typical of members of each *** in silico analysis and expression profiling showed high levels of expression for libraries derived from tissues of fruits,leaves and flowers as well as for libraries subjected to water *** results suggest the participation of the ERF family genes of *** in distinct biological functions,such as control of development,maturation,and responses to water *** results of this work imply in the selection of promising genes for further functional characterizations that will provide a better understanding of the complex regulatory networks related to plant development and responses to stress,opening up opportunities for coffee breeding programs.
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