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Activity-Dependent Proteolytic Cleavage of Neuroligin-1
It is reported that neuroligin-1 (NLG1) undergoes ectodomain shedding at the juxtamembrane stalk region to generate a secreted form of NLG1 and a membrane-tethered C-terminal fragment (CTF) in adult rat brains in vivo as well as in neuronal cultures. Expand
BACE1 Activity Is Modulated by Cell-Associated Sphingosine-1-Phosphate
It is shown that the activity of β-site APP cleaving enzyme-1 (BACE1), the rate-limiting enzyme for amyloid-β peptide production, is modulated by S1P in mouse neurons, suggesting that cellular S1p directly modulates BACE1 activity. Expand
BIN1 regulates BACE1 intracellular trafficking and amyloid-β production.
It is reported that the depletion of BIN1 increases cellular BACE1 levels through impaired endosomal trafficking and reduces Bace1 lysosomal degradation, resulting in increased Aβ production. Expand
BACE1 activity is modulated by cell-associated sphingosine-1-phosphate
heimer’s disease since it participates in the generation of the toxic amyloid ß-peptide (Aß) from the amyloid precursor protein (APP). g-Secretase is a membrane bound protein complex consisting ofExpand
Allosteric regulation of γ-secretase activity by a phenylimidazole-type γ-secretase modulator
A model for the mechanism of action of the phenylimidazole-type GSM in which binding at the luminal side of PS induces a conformational change in the catalytic center of γ-secretase to modulate Aβ production is provided. Expand
Phenylpiperidine‐type γ‐secretase modulators target the transmembrane domain 1 of presenilin 1
It is shown that a phenylpiperidine‐type compound GSM‐1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1) by photoaffinity labelling experiments combined with limited digestion, indicating an allosteric action of G SM‐1 by directly binding to the TMD1 of PS1, pinpointing the target structure of the phenylmethine‐type GSMs. Expand
Identification of novel deoxyribofuranosyl indole antimicrobial agents
Three novel deoxyribofuranosyl indole derivatives, FG050227 (1), FG050223 (2) and FG050204 (3), were identified as antimicrobial agents effective against Gram-positive bacterial strains and someExpand
Total synthesis of (-)-lepenine.
The first asymmetric total synthesis of lepenine has been accomplished, resulting in stereoselective construction of the unique hexacyclic system. Expand
Total synthesis of (-)-morphine.
An efficient total synthesis of (-)-morphine in 5% overall yield with the longest linear sequence consisting of 17 steps from 2-cyclohexen-1-one with an N-methyl-DNs-amide moiety is developed. Expand
Facile Palladium-Mediated Conversion of Ethanethiol Esters to Aldehydes and Ketones
Treatment of ethanethiol esters with triethylsilane and palladium on carbon at ambient temperature furnished aldehydes. In addition, a variety of ketones have been prepared by a palladium-catalyzedExpand