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No proteases have been identified to be oligodendrocyte-specific though there are phenomena in which proteases may be committed. We have cloned a cDNA for mouse homologue of protease M/neurosin, serine protease, and localized its mRNA in the mouse brain. The cDNA and the deduced amino acid sequences were 66% identical to those of human protease M/neurosin.… (More)
A cDNA for a putative novel serine protease, TLSP, was cloned from human hippocampus cDNA with polymerase chain reaction based strategies. The putative amino acid sequence of TLSP is similar to the trypsin-type serine proteases. TLSP mRNA is expressed in keratinocytes. Overexpressed TLSP protein in neuro2a cells was detected in culture medium.
By targeting dual active sites of AChE, a series of bis-huperzine B analogues with various lengths of the tether were designed, synthesized, and tested for their inhibition and selectivity. The most potent bis-huperzine B (5g) exhibited 3900-fold increase in AChE inhibition and 930-fold greater in selectivity for AChE vs BuChE than its parent huperzine B.
(-)-Huperzine A (5, HupA), an alkaloid isolated from the herb Huperzia serrata, is a potent, selective and reversible acetylcholinesterase (AchE) inhibitor. Based on the hypothesis with respect to two binding sites in the active gorge of AChE and the good example of bis-tacrine, it was predicted from the docking studies of alkylene-linked dimers of HupA… (More)
Proteases are involved in a variety of processes including demyelination after injury to the central nervous system. Neuropsin is a serine protease, which is constitutively expressed in the neurons of the limbic system. In the present study, intrahippocampal kainate injection and enucleation were performed on adult mice. Neuropsin mRNA and protein… (More)
By targeting dual active sites of AChE, a number of new derivatives of HupB have been synthesized and tested as acetylcholinesterase inhibitors. The most potent compound, bis-HupB 5b is 72-fold more potent in AChE inhibition and 79-fold more selective for AChE versus BChE than HupB.
The severe acute respiratory syndrome (SARS) coronavirus 3CL protease is an attractive target for the development of anti-SARS drugs. In this paper, cinanserin (1) analogs were synthesized and tested for the inhibitory activities against SARS-coronavirus (CoV) 3CL protease by fluorescence resonance energy transfer (FRET) assay. Four analogs show significant… (More)
We have shown that neuropsin is expressed in the neurons of the limbic system in the adult mouse. After the central nervous system was injured by incision or intraperitoneal kainate injection, neuropsin mRNA was induced in the peri-lesioned region. The cells in which neuropsin mRNA was induced were localized mainly in axon fiber pathways and closely… (More)
A number of aglycon analogues of sarmentosin were prepared and their bioactivities on the proliferation of T-lymphocytes and B-lymphocytes were assayed.
In search of small molecule compounds as the ligands of cyclophilin A, a series of quinoxalines were prepared, and their K(d) values of cyclophilin A and IC50 values for peptidyl-prolyl isomerase activity of cyclophilin A were tested. The results suggest that some quinoxalines are promising ligands of cyclophilin A.