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Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP) |
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| Authors: | 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 |
| Institution: | Department of Metabolic Disease Chemistry, Bristol Myers-Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. sulskyr@bms.com |
| Abstract: | 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. |
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