88713-84-2Relevant academic research and scientific papers
Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay
Rohe, Alexander,Goellner, Christiane,Wichapong, Kanin,Erdmann, Frank,Al-Mazaideh, Ghassab M.A.,Sippl, Wolfgang,Schmidt, Matthias
, p. 41 - 48 (2013/04/23)
In the human cell cycle, the Myt1 kinase is a crucial regulator of the G2/M transition. Because this membrane-associated kinase is hard to obtain and assay, there is a distinct lack of data so far. Here we report the derivatization of a glycoglycerolipid which was shown previously to be active in a Myt1 activity assay. These compounds were tested in a binding assay together with a set of common kinase inhibitors against a full-length Myt1 expressed in a human cell line. Dasatinib exhibited nanomolar affinity whereas broad coverage inhibitors such as sunitinib and staurosporine derivatives did not show any effect. We also carried out docking studies for the most potent compounds allowing further insights into the inhibitor interaction of this kinase. The glycoglycerolipids showed no significant effects in the binding assay, endorsing the idea of a mechanism of action distant from the active site.
An improved synthesis of dansylated α-galactosylceramide and its use as a fluorescent probe for the monitoring of glycolipid uptake by cells
Cheng, Janice M.H.,Chee, Stephanie H.,Knight, Deborah A.,Acha-Orbea, Hans,Hermans, Ian F.,Timmer, Mattie S.M.,Stocker, Bridget L.
, p. 914 - 926 (2011/06/19)
A highly efficient synthesis of the biologically important fluorescent probe dansyl α-GalCer is presented. Key in our strategy is the incorporation of the fluorescent dansyl group at an early stage in the synthesis to facilitate in the monitoring and purification of intermediates via TLC and flash column chromatography, respectively, and the use of a high yielding α-selective glycosylation reaction between the phytosphingosine lipid and a galactosyl iodide donor. The ability of dansyl α-GalCer to activate iNKT cells and to serve as a fluorescent marker for the uptake of glycolipid by dendritic cells is also presented.
Optimized procedure for the synthesis of 6-azido-6-deoxy-galactopyranosides from 6-O-tosyl-galactopyranosides
Li, Shu-Chun,Meng, Xiang-Bao,Cai, Meng-Shen,Li, Zhong-Jun
, p. 637 - 643 (2007/10/03)
The reaction conditions for preparation of 6-azido-6-deoxy-glycoside remain elusive, although there are many successful cases in hand. After careful investigation of the reaction conditions, a practical procedure for the preparation of 6-azido-6-deoxy-gal
SYNTHESIS OF METHYL 2,3-O-D-GLYCOPYRANOSYLIDENE α-D-MANNOPYRANOSIDES HAVING VARIOUS SUBSTITUENTS
Yoshimura, Juji,Asano, Katsuji,Umemura, Kazuyuki,Horito, Shigeomi,Hashimoto, Hironobu
, p. 187 - 204 (2007/10/02)
The title compounds were obtained by condensation of D-glucono-, D-galactono-, or L-glycero-D-gluco-heptono-1,5-lactones with methyl 2,3-di-O-(trimethylsilyl)-α-D-mannopyranosides having various substituents on C-4 and C-6, in the presence of trimethylsil
