2788-84-3Relevant articles and documents
Synthesis and conformational analysis of poly(phenylacetylene)s with serinol-tethered carbohydrate appendages
Masubuchi, Kana,Maehata, Masakiyo,Suzuki, Chieko,Matsuoka, Ryoji,Sekiguchi, Maki,Chigira, Naoto,Amano, Yoshitsugu,Inokuchi, Mayu,Li, Qintong,Hasegawa, Teruaki
, p. 23 - 30 (2019)
We synthesized phenylacetylenes containing β-lactoside, β-cellobioside, or β-maltoside, and polymerized them to produce the corresponding poly (phenylacetylene)s. In these poly (phenylacetylene)s, the pendent carbohydrates were tethered to the mainchains
Alcohol functionality in the fatty acid backbone of sphingomyelin guides the inhibition of blood coagulation
Mallik,Prasad,Das,Sen
, p. 3390 - 3398 (2021/02/03)
Cell-surface sphingomyelin (SM) inhibits binary and ternary complex activity of blood coagulation by an unknown mechanism. Here we show the OH functionality of SM contributes in forming the close assembly through intermolecular H-bond and through Ca2+ chelation, which restricts the protein-lipid/protein-protein interactions and thus inhibits the coagulation procedure.
Liposomal FRET Assay Identifies Potent Drug-Like Inhibitors of the Ceramide Transport Protein (CERT)
Aglar, ?znur,Arenz, Christoph,Banhart, Sebastian,Cong, Xiaojing,Hamdo, Housam H.,Heuer, Dagmar,Kleuser, Burkhard,M?ller, Heiko M.,Saied, Essa M.,Samaha, Doaa,Schumacher, Fabian
supporting information, p. 16616 - 16621 (2020/11/30)
Ceramide transfer protein (CERT) mediates non-vesicular transfer of ceramide from endoplasmic reticulum to Golgi apparatus and thus catalyzes the rate-limiting step of sphingomyelin biosynthesis. Usually, CERT ligands are evaluated in tedious binding assays or non-homogenous transfer assays using radiolabeled ceramides. Herein, a facile and sensitive assay for CERT, based on F?rster resonance energy transfer (FRET), is presented. To this end, we mixed donor and acceptor vesicles, each containing a different fluorescent ceramide species. By CERT-mediated transfer of fluorescent ceramide, a FRET system was established, which allows readout in 96-well plate format, despite the high hydrophobicity of the components. Screening of a 2 000 compound library resulted in two new potent CERT inhibitors. One is approved for use in humans and one is approved for use in animals. Evaluation of cellular activity by quantitative mass spectrometry and confocal microscopy showed inhibition of ceramide trafficking and sphingomyelin biosynthesis.
Glycosylated tris-bipyridine ferrous complexes as molecular mimics of densely packed glycoclusters on cell surfaces: spatial carbohydrate packing of glycoclusters changes on additions of salts
Chigira, Naoto,Maeda, Nao,Tachikawa, Kanako,Sekiguchi, Maki,Amano, Yoshitsugu,Inokuchi, Mayu,Li, Qintong,Hasegawa, Teruaki
, p. 246 - 267 (2019/06/25)
Tris-bipyridine ferrous complexes having β-lactosides, β-maltosides or α-mannosides with serinol spacers were prepared as molecular mimics of densely packed carbohydrate clusters on cell surfaces. Conformational analysis on these glycosylated complexes we