73111-56-5Relevant 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.
A focused sulfated glycoconjugate Ugi library for probing heparan sulfate-binding angiogenic growth factors
Liu, Ligong,Li, Caiping,Cochran, Siska,Feder, Daniel,Guddat, Luke W.,Ferro, Vito
supporting information, p. 6190 - 6194 (2012/10/29)
A library of small molecule heparan sulfate (HS) mimetics was synthesized by employing the Ugi four-component condensation of d-mannopyranoside-derived isocyanides with formaldehyde as the carbonyl component and a selection of carboxylic acids and amines,
Synthesis of non-glycosidically linked selenoether pseudodisaccharides
Fournière, Viviane,Cumpstey, Ian
supporting information; experimental part, p. 2127 - 2129 (2010/06/14)
Non-glycosidically linked disaccharide mimetics with a selenoether functionality linking the two monosaccharide residues have been synthesised. Protected Glc(Se3-3)Glc, Glc(Se3-6)Glc and Glc(Se3-6)Man structures were obtained. Selenium was introduced by d
Non-glycosidically linked pseudodisaccharides: Thioethers, sulfoxides, sulfones, ethers, selenoethers, and their binding to lectins
Cumpstey, Ian,Ramstadius, Clinton,Akhtar, Tashfeen,Goldstein, Irwin J.,Winter, Harry C.
experimental part, p. 1951 - 1970 (2010/06/13)
Hydrolytically stable non-glycosidically linked tail-to-tail pseudodisaccharides are linked by a single bridging atom remote from the anomeric centre of the constituent monosaccharides. Some such pseudodisaccharides with sulfur or oxy gen bridges were found to act as disaccharide mimetics in their binding to the Banana Lectin and to Concanavalin A. A versatile synthetic route to a small library of such compounds is described.
New oligosaccharide analogues: Non-glycosidically linked thioether-bridged pseudodisaccharides
Cumpstey, Ian
, p. 1711 - 1714 (2008/02/03)
The synthesis of six disaccharide analogues is reported. The pseudodisaccharides each consist of two monosaccharide residues linked non-glycosidically via a thioether functionality; both C2-symmetric and unsymmetrically substituted examples are
