Int J Mol Sci
June 2023
Huntington's disease (HD) is a disorder caused by an abnormal expansion of trinucleotide CAG repeats within the huntingtin (Htt) gene. Under normal conditions, the CREB Binding Protein interacts with CREB elements and acetylates Lysine 27 of Histone 3 to direct the expression of several genes. However, mutant Htt causes depletion of CBP, which in turn induces altered histone acetylation patterns and transcriptional deregulation.
View Article and Find Full Text PDFCucurbit[7]uril (CB7) catalyzes the hydrolysis reaction of bis(4-nitrophenyl)carbonate () but inhibits that of bis(4-nitrophenyl)thiocarbonate (). Two relevant CB7 effects are proposed, a base-catalyst mediated by the CB7 portal and an inhibitory role attributed to the lower interaction of the thiocarbonyl group with the solvent in the host cavity, respectively.
View Article and Find Full Text PDFThis work describes the microwave assisted synthesis of twelve novel histamine H receptor ligands. They display pyrrolo[2,3-d]pyrimidine derivatives with rigidized aliphatic amines as warheads. The compounds were screened for HR and HR binding affinities in radioligand displacement assays and the most potent compounds were evaluated for HR binding properties in vitro and in docking studies.
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