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Page 1
Pharmacological Inhibition of Lipid Import and Transport Proteins in Ovarian Cancer.
Lemberger L, Wagner R, Heller G, Pils D, Grunt TW. Lemberger L, et al. Cancers (Basel). 2022 Dec 5;14(23):6004. doi: 10.3390/cancers14236004. Cancers (Basel). 2022. PMID: 36497485 Free PMC article.
Overall, the small molecule inhibitors of lipid handling proteins BMS309403, HTS01037, NAV2729, SB-FI-26, and sulfosuccinimidyl oleate (SSO) caused a drug-specific, dose-/time-dependent inhibition of FA/LDL uptake, associated with reduced proliferation, cell cycle arrest, …
Overall, the small molecule inhibitors of lipid handling proteins BMS309403, HTS01037, NAV2729, SB-FI-26, and sulfosuccinimidyl oleat …
Identification of a fatty acid binding protein4-UCP2 axis regulating microglial mediated neuroinflammation.
Duffy CM, Xu H, Nixon JP, Bernlohr DA, Butterick TA. Duffy CM, et al. Mol Cell Neurosci. 2017 Apr;80:52-57. doi: 10.1016/j.mcn.2017.02.004. Epub 2017 Feb 16. Mol Cell Neurosci. 2017. PMID: 28214555 Free PMC article.
Gene expression confirmed expression of FABP4 in brain tissue lysate from C57Bl/6J mice and BV2 microglia. Treatment of microglial cells with an FABP inhibitor (HTS01037) increased expression of Ucp2 and arginase in the presence or absence of PA. Moreover, cells exposed to …
Gene expression confirmed expression of FABP4 in brain tissue lysate from C57Bl/6J mice and BV2 microglia. Treatment of microglial cells wit …
Uncoupling lipid metabolism from inflammation through fatty acid binding protein-dependent expression of UCP2.
Xu H, Hertzel AV, Steen KA, Wang Q, Suttles J, Bernlohr DA. Xu H, et al. Mol Cell Biol. 2015 Mar;35(6):1055-65. doi: 10.1128/MCB.01122-14. Epub 2015 Jan 12. Mol Cell Biol. 2015. PMID: 25582199 Free PMC article.
Pharmacologic inhibition of FABP4/aP2 with the FABP inhibitor HTS01037 also upregulated UCP2 and reduced expression of BiP, CHOP, and XBP-1s. ...
Pharmacologic inhibition of FABP4/aP2 with the FABP inhibitor HTS01037 also upregulated UCP2 and reduced expression of BiP, CHOP, and …
Identification and characterization of a small molecule inhibitor of Fatty Acid binding proteins.
Hertzel AV, Hellberg K, Reynolds JM, Kruse AC, Juhlmann BE, Smith AJ, Sanders MA, Ohlendorf DH, Suttles J, Bernlohr DA. Hertzel AV, et al. J Med Chem. 2009 Oct 8;52(19):6024-31. doi: 10.1021/jm900720m. J Med Chem. 2009. PMID: 19754198 Free PMC article.
Because small molecule inhibitors may be efficacious in defining the mechanism(s) of AFABP/aP2 action, a chemical library was screened and identified 1 (HTS01037) as a pharmacologic ligand capable of displacing the fluorophore 1-anilinonaphthalene 8-sulfonic acid from the …
Because small molecule inhibitors may be efficacious in defining the mechanism(s) of AFABP/aP2 action, a chemical library was screened and i …
FABP4 inhibition suppresses PPARγ activity and VLDL-induced foam cell formation in IL-4-polarized human macrophages.
Boss M, Kemmerer M, Brüne B, Namgaladze D. Boss M, et al. Atherosclerosis. 2015 Jun;240(2):424-30. doi: 10.1016/j.atherosclerosis.2015.03.042. Epub 2015 Apr 3. Atherosclerosis. 2015. PMID: 25897794
Inhibition of FABP4 during differentiation using chemical inhibitors BMS309403 and HTS01037 or FABP4 siRNA decreased the expression of FABP4 and LPL, and reduced lipid accumulation in macrophages treated with VLDL. ...
Inhibition of FABP4 during differentiation using chemical inhibitors BMS309403 and HTS01037 or FABP4 siRNA decreased the expression o …
Fatty acids induce leukotriene C4 synthesis in macrophages in a fatty acid binding protein-dependent manner.
Long EK, Hellberg K, Foncea R, Hertzel AV, Suttles J, Bernlohr DA. Long EK, et al. Biochim Biophys Acta. 2012 Jul;1831(7):1199-207. doi: 10.1016/j.bbalip.2013.04.004. Epub 2013 Apr 12. Biochim Biophys Acta. 2012. PMID: 23583845 Free PMC article.
Consistent with a role for FABPs in LTC4 synthesis, treatment of macrophages with HTS01037, a specific FABP inhibitor, resulted in a marked decrease in both basal and fatty acid-stimulated LTC4 secretion but no change in 5-HETE production or 5-lipoxygenase expression. ...
Consistent with a role for FABPs in LTC4 synthesis, treatment of macrophages with HTS01037, a specific FABP inhibitor, resulted in a …
Fatty acids induce leukotriene C4 synthesis in macrophages in a fatty acid binding protein-dependent manner.
Long EK, Hellberg K, Foncea R, Hertzel AV, Suttles J, Bernlohr DA. Long EK, et al. Biochim Biophys Acta. 2013 Jul;1831(7):1199-207. Biochim Biophys Acta. 2013. PMID: 24046860
Consistent with a role for FABPs in LTC4 synthesis, treatment of macrophages with HTS01037, a specific FABP inhibitor, resulted in a marked decrease in both basal and fatty acid-stimulated LTC4 secretion but no change in 5-HETE production or 5-lipoxygenase expression. ...
Consistent with a role for FABPs in LTC4 synthesis, treatment of macrophages with HTS01037, a specific FABP inhibitor, resulted in a …