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3fr2
From Proteopedia
| 3fr2, resolution 2.20Å () | |||||||||
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| Sites: | |||||||||
| Ligands: | |||||||||
| Gene: | FABP4 (Homo sapiens) | ||||||||
| Related: | 3fr4, 3fr5 | ||||||||
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||
N-Benzyl-indolo carboxylic acids: Design and synthesis of potent and selective adipocyte Fatty-Acid Binding Protein (A-FABP) inhibitors
Small molecule inhibitors of adipocyte fatty-acid binding protein (A-FABP) have gained renewed interest following the recent publication of pharmacologically beneficial effects of such inhibitors. Despite the potential utility of selective A-FABP inhibitors within the fields of metabolic disease, inflammation and atherosclerosis, there are few examples of useful A-FABP inhibitors in the public domain. Herein, we describe the optimization of N-benzyl-tetrahydrocarbazole derivatives through the use of co-crystal structure guided medicinal chemistry efforts. This led to the identification of a potent and selective class of A-FABP inhibitors as illustrated by N-benzyl-hexahydrocyclohepta[b]indole 30.
N-Benzyl-indolo carboxylic acids: Design and synthesis of potent and selective adipocyte fatty-acid binding protein (A-FABP) inhibitors., Barf T, Lehmann F, Hammer K, Haile S, Axen E, Medina C, Uppenberg J, Svensson S, Rondahl L, Lundback T, Bioorg Med Chem Lett. 2009 Mar 15;19(6):1745-8. Epub 2009 Jan 30. PMID:19217286
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
3FR2 is a 1 chain structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
- Barf T, Lehmann F, Hammer K, Haile S, Axen E, Medina C, Uppenberg J, Svensson S, Rondahl L, Lundback T. N-Benzyl-indolo carboxylic acids: Design and synthesis of potent and selective adipocyte fatty-acid binding protein (A-FABP) inhibitors. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1745-8. Epub 2009 Jan 30. PMID:19217286 doi:10.1016/j.bmcl.2009.01.084
Page seeded by OCA on Thu Apr 2 16:22:59 2009
Categories: Homo sapiens | Axen, E. | Barf, T | Haile, S. | Hammer, K. | Lehmann, F. | Medina, C. | Rondahl, L. | Svensson, S. | Uppenberg, J. | Ck, T Lundb. | Cytoplasm | Lipid binding protein | Lipid-binding | Nucleus | Phosphoprotein | Polymorphism | Transport
