GPCR LIGANDS IDENTIFIED BY COMPUTATIONAL MODELING

Disclosed are pharmacophores for developing and screening compounds having G-protein-coupled receptor antagonist activity, including LPA1, LPA2, LPA3 and S1P antagonists. These compositions have therapeutic benefit in the fields of cancer chemotherapy, cardiovascular disease prevention, and protecti...

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Bibliographic Details
Main Authors TIGYI, GABOR, PARRILL, ABBY, FELLS, JAMES, PERYGIN, DONNA
Format Patent
LanguageEnglish
French
Published 06.12.2007
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Summary:Disclosed are pharmacophores for developing and screening compounds having G-protein-coupled receptor antagonist activity, including LPA1, LPA2, LPA3 and S1P antagonists. These compositions have therapeutic benefit in the fields of cancer chemotherapy, cardiovascular disease prevention, and protective agents during radiation and chemotherapy. L'invention concerne des pharmacophores destinés à élaborer et cribler des composés présentant une activité antagoniste des récepteurs couplés aux protéines G, tels que des antagonistes de LPA1, LPA2, LPA3 et S1P. Ces compositions sont thérapeutiquement utiles dans la chimiothérapie anticancéreuse, dans la prévention des maladies cardiovasculaires et comme agents protecteurs pendant une radiothérapie et une chimiothérapie.
Bibliography:Application Number: WO2007US12514