|
|||||
|
|
RGD mimetics containing phthalimidine fragment as novel ligands of fibrinogen receptor |
|
| Authors: | Krysko Andrei A Samoylenko Georgiy V Polishchuk Pavel G Andronati Sergei A Kabanova Tatyana A Khristova Tetiana M Kuz'min Victor E Kabanov Vladimir M Krysko Olga L Varnek Alexandre A Grygorash Ruslan Ya |
| Institution: | A.V. Bogatsky Physico-Chemical Institute of the National Academy of Sciences of Ukraine, Lustdorfskaya doroga 86, Odessa 65080, Ukraine. peptides@paco.net |
| Abstract: | The novel RGD mimetics with phthalimidine central fragment were synthesized with the use of 4-piperidine-4-yl-butyric, 4-piperidine-4-yl-benzoic, 4-piperazine-4-yl-benzoic and 1,2,3,4-tetrahydroisoquinoline-7-carboxylic acids as surrogates of Arg motif. The synthesized compounds potently inhibited platelet aggregation in vitro and blocked FITC-Fg binding to α(IIb)β(3) integrin in a suspension of washed human platelets. The key α(IIb)β(3) protein-ligand interactions were determined in docking experiments. |
| Keywords: | Fibrinogen receptor antagonists αIIbβ3 RGD mimetics Phthalimidine Platelet aggregation |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |