1383450-02-9Relevant academic research and scientific papers
Synthesis and anti-influenza a virus activity of 6′-amino-6′-deoxy-glucoglycerolipids analogs
Ren, Li,Zhang, Jun,Ma, Haizhen,Sun, Linlin,Zhang, Xiaoshuang,Yu, Guangli,Guan, Huashi,Wang, Wei,Li, Chunxia
, (2016/07/06)
A series of aminoglucoglycerolipids derivatives had been synthesized, including 6′-acylamido-glucoglycerolipids 1a-1f and corresponding 2′-acylamido-glucoglycerolipids 2a-2c bearing different fatty acids, glucosyl diglycerides 3a-3e bearing different func
A hydrophobic disordered peptide spontaneously anchors a covalently bound RNA hairpin to giant lipidic vesicles
Isaad, Alexandra Le Chevalier,Carrara, Paolo,Stano, Pasquale,Krishnakumar, Kollappillil S.,Lafont, Dominique,Zamboulis, Alexandra,Buchet, Rene,Bouchu, Denis,Albrieux, Florian,Strazewski, Peter
, p. 6363 - 6373 (2014/08/18)
The attraction of nucleic acids to lipidic compartments is the first step for carriers of potentially inheritable information to self-organise in functionalised synthetic cells. Confocal fluorescence imaging shows that a synthetic amphiphilic peptidyl RNA molecule spontaneously accumulates at the outer bilayer membranes of phospho- and glycolipidic giant vesicles. Cooperatively attractive interactions of -3.4 to -4.0 kcal mol-1 between a random coil hydrophobic peptide and lipid membranes can thus pilot lipophobic RNA to its compartmentation. The separation of mixed lipid phases in the membranes further enhances the local concentration of anchored RNA. the Partner Organisations 2014.
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.
Synthesis of glycoglycerolipid of 1,2-dipalmitoyl-3-(N-palmitoyl-6′- amino-6′-deoxy-α-D-glucosyl)-sn-glycerol and its analogues, inhibitors of human Myt1-kinase
Sun, Yihua,Zhang, Jun,Li, Chunxia,Guan, Huashi,Yu, Guangli
, p. 6 - 12 (2012/08/08)
A glycoglycerolipid 1a isolated from a marine alga showed inhibition to Myt1 kinase with IC50 of 0.12 μg/mL. We synthesized 1a and its seven analogues (1b-h) in an efficient method with high stereoselectivity. The process employed trichloroacetimidate donor 4b at low substrate concentration to achieve high α-selectivity (α/β = 33:1) in glycosylation reaction. The present synthesis provided various acyl derivatives required for the study on the structure-activity relationship later.
