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The novel benzimidazole derivative BRP-7 inhibits leukotriene biosynthesis in vitro and in vivo by targeting 5-lipoxygenase-activating protein (FLAP).
Pergola C, Gerstmeier J, Mönch B, Çalışkan B, Luderer S, Weinigel C, Barz D, Maczewsky J, Pace S, Rossi A, Sautebin L, Banoglu E, Werz O. Pergola C, et al. Among authors: gerstmeier j. Br J Pharmacol. 2014 Jun;171(12):3051-64. doi: 10.1111/bph.12625. Br J Pharmacol. 2014. PMID: 24641614 Free PMC article.
Identification of novel benzimidazole derivatives as inhibitors of leukotriene biosynthesis by virtual screening targeting 5-lipoxygenase-activating protein (FLAP).
Banoglu E, Çalişkan B, Luderer S, Eren G, Özkan Y, Altenhofen W, Weinigel C, Barz D, Gerstmeier J, Pergola C, Werz O. Banoglu E, et al. Among authors: gerstmeier j. Bioorg Med Chem. 2012 Jun 15;20(12):3728-41. doi: 10.1016/j.bmc.2012.04.048. Epub 2012 May 1. Bioorg Med Chem. 2012. PMID: 22607880
5-Lipoxygenase-activating protein rescues activity of 5-lipoxygenase mutations that delay nuclear membrane association and disrupt product formation.
Gerstmeier J, Newcomer ME, Dennhardt S, Romp E, Fischer J, Werz O, Garscha U. Gerstmeier J, et al. FASEB J. 2016 May;30(5):1892-900. doi: 10.1096/fj.201500210R. Epub 2016 Feb 3. FASEB J. 2016. PMID: 26842853 Free PMC article.
Together, the data suggest that the concealed FY cork impacts membrane association and that FLAP may help shield an uncapped active site.-Gerstmeier, J., Newcomer, M. E., Dennhardt, S., Romp, E., Fischer, J., Werz, O., Garscha, U. 5-Lipoxygenase-activating pr …
Together, the data suggest that the concealed FY cork impacts membrane association and that FLAP may help shield an uncapped active site.- …
4,5-Diarylisoxazol-3-carboxylic acids: A new class of leukotriene biosynthesis inhibitors potentially targeting 5-lipoxygenase-activating protein (FLAP).
Banoglu E, Çelikoğlu E, Völker S, Olgaç A, Gerstmeier J, Garscha U, Çalışkan B, Schubert US, Carotti A, Macchiarulo A, Werz O. Banoglu E, et al. Among authors: gerstmeier j. Eur J Med Chem. 2016 May 4;113:1-10. doi: 10.1016/j.ejmech.2016.02.027. Epub 2016 Feb 15. Eur J Med Chem. 2016. PMID: 26922224
54 results