Bioorganic & medicinal chemistry letters, 2007-06, Vol.17 (12), p.3511-3515
- 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.
2007
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- Autor(en) / Beteiligte
- 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.
- Titel
- Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP)
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2007-06, Vol.17 (12), p.3511-3515
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2007
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- X-ray crystal structure of an FABP inhibitor bound to the active site of aFABP. 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2006.12.044Titel-ID: cdi_proquest_miscellaneous_70563847
- Format
- –
- Schlagworte
- Adipocytes - drug effects, Adipocytes - metabolism, aFABP, Animals, aP2, Azoles - antagonists & inhibitors, Binding Sites, Biological and medical sciences, Biphenyl azoles, Biphenyl Compounds - antagonists & inhibitors, Contrast media. Radiopharmaceuticals, Disease Models, Animal, Epidermis - metabolism, Fatty acid binding protein, Fatty Acid-Binding Proteins - antagonists & inhibitors, Hypoglycemic Agents - chemical synthesis, Hypoglycemic Agents - pharmacology, Hypolipidemic Agents - chemical synthesis, Hypolipidemic Agents - pharmacology, Medical sciences, Mice, Miscellaneous, Models, Chemical, Pharmacology. Drug treatments, Radioligand Assay