2009
DOI: 10.1016/j.bmcl.2009.01.084
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N-Benzyl-indolo carboxylic acids: Design and synthesis of potent and selective adipocyte fatty-acid binding protein (A-FABP) inhibitors

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Cited by 104 publications
(80 citation statements)
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“…Several other selective FABP4 inhibitors have also been reported with various degrees of in vitro (but not in vivo) characterizations ( 12,17,18 ). In this study, we present the recent report showed that >70% germline knockdown of FABP4 by RNA interference in mice did not improve insulin sensitivity in diet-induced obese mice ( 31 ).…”
Section: Discussionmentioning
confidence: 63%
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“…Several other selective FABP4 inhibitors have also been reported with various degrees of in vitro (but not in vivo) characterizations ( 12,17,18 ). In this study, we present the recent report showed that >70% germline knockdown of FABP4 by RNA interference in mice did not improve insulin sensitivity in diet-induced obese mice ( 31 ).…”
Section: Discussionmentioning
confidence: 63%
“…Indeed, a selective biphenyl azole inhibitor of FABP4, BMS309403, was identifi ed as binding FABP4 with nM affi nity and >100-fold selectivity against FABP5 as well as the heart isoform FABP3 ( 9 ). In a ligand displacement assay using 1,8-ANS (8-anilino-1-naphthalene-sulfonic acid) as the probe, the compound displays inhibition constant ( K i ) values of <2 nM, 250 nM, and 350 nM for FABP4, FABP5, and FABP3, respectively ( 10 ) (12)(13)(14), with one compound displaying an IC 50 value of 600 nM in a fl uorescence polarization (FP) assay ( 15 ), and another compound in the same series an IC 50 value of 49 nM in a scintillation proximity assay ( 16 ). However, no biological characterization in cell-based or in vivo assays has been reported.…”
Section: Ligand Displacement Fp Assay For Fabp4 and Fabp5mentioning
confidence: 99%
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“…Of a series of chemical inhibitors of FABP4 that was discovered over the last decade [12,[14][15][16][17] , the selective inhibitor BMS309403 was proven to be effective for improving insulin resistance in the ob/ob mouse model and can ameliorate the symptoms of atherosclerosis [7] . However, none of these compounds are in clinical development.…”
Section: Discussionmentioning
confidence: 99%
“…The binding mode demonstrated that the 3,5-dibromo-4-hydroxyphenyl moiety of BBR is nicely accommodated in a lipophilic pocket defined by Phe16, Tyr19, Met20, Val25, Thr29, Ala33, Phe57, Figure 3A). Moreover, the carbonyl group of BBR forms stable polar interaction with Arg126, a critical residue for the binding of inhibitors [12,[14][15][16][17] . In addition, the oxygen atom in the benzofuran of BBR forms a hydrogen bond with Ser55 ( Figure 3A).…”
Section: Interaction Mechanisms Between Fabp4 and Bbrmentioning
confidence: 99%