Sulsky Richard, Magnin David R, Huang Yanting, Simpkins Ligaya, Taunk Prakash, Patel Manorama, Zhu Yeheng, Stouch Terry R, Bassolino-Klimas Donna, Parker Rex, Harrity Thomas, Stoffel Robert, Taylor David S, Lavoie Thomas B, Kish Kevin, Jacobson Bruce L, Sheriff Steven, Adam Leonard P, Ewing William R, Robl Jeffrey A
Department of Metabolic Disease Chemistry, Bristol Myers-Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA.
Bioorg Med Chem Lett. 2007 Jun 15;17(12):3511-5. doi: 10.1016/j.bmcl.2006.12.044. Epub 2006 Dec 21.
Herein we report the first disclosure of biphenyl azoles that are nanomolar binders of adipocyte fatty acid binding protein (aFABP or aP2) with up to thousand-fold selectivity against muscle fatty acid binding protein and epidermal fatty acid binding protein. In addition a new radio-ligand to determine binding against the three fatty acid binding proteins was also synthesized.
在此，我们首次披露了联苯唑类化合物，它们是脂肪细胞脂肪酸结合蛋白（aFABP或aP2）的纳摩尔级结合剂，对肌肉脂肪酸结合蛋白和表皮脂肪酸结合蛋白具有高达千倍的选择性。此外，还合成了一种用于测定与这三种脂肪酸结合蛋白结合情况的新型放射性配体。
