Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).

No abstract is available for this paper.

• Publication year

  2007

• Venue

  Bioorganic & Medicinal Chemistry Letters

• Publication date

  2007-06-15

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1016/J.BMCL.2006.12.044PMID 17502136
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• NMR structure of a potent small molecule inhibitor bound to human keratinocyte fatty acid-binding protein.

  2006cited by this paper
• Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors.

  2004cited by this paper
• Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target.

  2004cited by this paper
• Assay of the binding of fatty acids by proteins: evaluation of the Lipidex 1000 procedure

  2004cited by this paper
• New insights into the structure and function of fatty acid-binding proteins

  2002cited by this paper
• Structure-based screening as applied to human FABP4: a highly efficient alternative to HTS for hit generation.

  2002cited by this paper
• Role of macrophage‐expressed adipocyte fatty acid binding protein in the development of accelerated atherosclerosis in hypercholesterolemic mice

  2001cited by this paper
• Lack of macrophage fatty-acid–binding protein aP2 protects mice deficient in apolipoprotein E against atherosclerosis

  2001cited by this paper
• The mammalian fatty acid-binding protein multigene family: molecular and genetic insights into function.

  2000cited by this paper
• Improved Glucose and Lipid Metabolism in Genetically Obese Mice Lacking aP2.

  2000cited by this paper
• Improved glucose and lipid metabolism in genetically obese mice lacking aP2.

  2000cited by this paper
• Altered insulin secretion associated with reduced lipolytic efficiency in aP2-/- mice.

  1999cited by this paper
• Intracellular transport of fatty acids in muscle. Role of cytoplasmic fatty acid-binding protein.

  1998cited by this paper
• Intracellular Transport of Fatty Acids in Muscle

  1998cited by this paper
• Critical evaluation of search algorithms for automated molecular docking and database screening

  1997cited by this paper
• Affinity of fatty acid for (r)rat intestinal fatty acid binding protein:further examination.

  1996cited by this paper
• Affinity of fatty acid for rRat intestinal fatty acid binding protein: further examination

  1996cited by this paper
• Lipid-binding proteins: a family of fatty acid and retinoid transport proteins.

  1994cited by this paper
• X-ray crystallographic structures of adipocyte lipid-binding protein complexed with palmitate and hexadecanesulfonic acid. Properties of cavity binding sites.

  1994cited by this paper
• Accurate modeling of protein conformation by automatic segment matching.

  1992cited by this paper
• Tissue specific expression of p422 protein, a putative lipid carrier, in mouse adipocytes.

  1985cited by this paper
• Addition von Aldehyden an aktivierte Doppelbindungen, XXXVI. Synthesen und Reaktionen von 3-Acyl-1,5-dicarbonyl-Verbindungen

  1985cited by this paper
• Protein folding by restrained energy minimization and molecular dynamics.

  1983cited by this paper

• Adipocyte fatty acid‐binding protein as a cerebrospinal fluid–accessible biomarker and druggable target in subarachnoid haemorrhage: Linking fatty acid dysregulation to microglial neuroinflammation

  2026cites this paper
• Novel Triazolopyrimidinone Compounds as Inhibitors of Adipocyte Fatty Acid–Binding Protein (FABP4)

  2025cites this paper
• Fatty acid binding protein 4 regulates doxorubicin-induced renal injury via mediating lipid metabolism and apoptosis.

  2025cites this paper
• Metabolic Roles of Fatty Acid Binding Protein 4 (FABP4) in Fetal and Maternal Health and Maintenance of Pregnancy in Women with Obesity: A Review

  2025cites this paper
• FABP4 inhibition protects renal tubular cells and ameliorates renal inflammation in diabetic kidney disease.

  2025cites this paper
• Evaluation of the Anti-Inflammatory Effects of Novel Fatty Acid-Binding Protein 4 Inhibitors in Microglia

  2025cites this paper
• Chemical Probes for Investigating the Endocannabinoid System.

  2025cites this paper
• Potential safety implications of fatty acid-binding protein inhibition.

  2024cites this paper
• FABP4 as a therapeutic host target controlling SARS-CoV-2 infection

  2024cites this paper
• Recent Advances on Small-Molecule Inhibitors of Lipocalin-like Proteins.

  2024cites this paper
• Targeting Dysregulated Lipid Metabolism in Cancer with Pharmacological Inhibitors

  2024cites this paper
• Diabetes and the fabkin complex: A dual-edged sword.

  2024cites this paper
• The Effects of FABP4 on Cardiovascular Disease in the Aging Population

  2024cites this paper
• Development of a humanized anti-FABP4 monoclonal antibody for potential treatment of breast cancer

  2024cites this paper
• Pathophysiological Insight into Fatty Acid-Binding Protein-4: Multifaced Roles in Reproduction, Pregnancy, and Offspring Health

  2023cites this paper
• Development of a therapeutic monoclonal antibody against circulating adipocyte fatty acid binding protein to treat ischaemic stroke

  2023cites this paper
• Naturally-occurring carboxylic acids from traditional antidiabetic plants as potential pancreatic islet FABP3 inhibitors. A molecular docking-aided study.

  2023cites this paper
• Four-component condesation of ethyl acetoacetate, phenylglyoxal hydrate, barbituric acid and primary amines

  2023cites this paper
• Targeting FABP4 in elderly mice rejuvenates liver metabolism and ameliorates aging-associated metabolic disorders.

  2023cites this paper
• Impact of Intracellular Lipid Binding Proteins on Endogenous and Xenobiotic Ligand Metabolism and Disposition

  2023cites this paper
• WaterKit: Thermodynamic Profiling of Protein Hydration Sites.

  2023cites this paper
• Goods and Bads of the Endocannabinoid System as a Therapeutic Target: Lessons Learned after 30 Years

  2023cites this paper
• Interleukin-10 increases macrophage-mediated chemotherapy resistance via FABP5 signaling in multiple myeloma.

  2023cites this paper
• Omentum provides a special cell microenvironment for ovarian cancer

  2023cites this paper
• Levofloxacin alleviates blood-brain barrier disruption following cerebral ischemia and reperfusion via directly inhibiting A-FABP.

  2023cites this paper
• Four-Component Condensation of Ethyl Acetoacetate, Phenylglyoxal Hydrate, Barbituric Acid, and Primary Amines

  2023cites this paper
• Targeting adipokines in polycystic ovary syndrome and related metabolic disorders: from experimental insights to clinical studies.

  2022cites this paper
• Discovery of Cobimetinib as a novel A-FABP inhibitor using machine learning and molecular docking-based virtual screening

  2022cites this paper
• Unveiling the Role of the Fatty Acid Binding Protein 4 in the Metabolic-Associated Fatty Liver Disease

  2022cites this paper
• Fatty acid-binding proteins and fatty acid synthase influence glial reactivity and promote the formation of Müller glia-derived progenitor cells in the chick retina.

  2022cites this paper
• Adipocyte fatty acid binding protein 4 (FABP4) inhibitors. An update from 2017 to early 2022.

  2022cites this paper
• Fatty acid-binding protein 4 in kidney diseases: From mechanisms to clinics.

  2022cites this paper
• Fatty acid binding protein 4 promotes autoimmune diabetes by recruitment and activation of pancreatic islet macrophages

  2021cites this paper
• Free fatty-acid transport via CD36 drives β-oxidation-mediated hematopoietic stem cell response to infection

  2021cites this paper
• Inhibition of FABP6 Reduces Tumor Cell Invasion and Angiogenesis through the Decrease in MMP-2 and VEGF in Human Glioblastoma Cells

  2021cites this paper
• A three-component condensation of cyclic enamino ketones, phenylglyoxal hydrate, and ethyl cyanoacetate

  2021cites this paper
• Adipose-Derived Lipid-Binding Proteins: The Good, the Bad and the Metabolic Diseases

  2021cites this paper
• Cooperative Study Combining X-ray Crystal Structure Analysis and FMO Calculation: Interaction Analysis of FABP4 Inhibitors

  2021cites this paper
• Molecular mechanisms of inhibitor bindings to A-FABP deciphered by using molecular dynamics simulations and calculations of MM-GBSA

  2021cites this paper
• Adipocyte Fatty Acid Binding Protein Promotes the Onset and Progression of Liver Fibrosis via Mediating the Crosstalk between Liver Sinusoidal Endothelial Cells and Hepatic Stellate Cells

  2021cites this paper
• Fatty acid-binding protein 7 triggers α-synuclein oligomerization in glial cells and oligodendrocytes associated with oxidative stress

  2021cites this paper
• Epidermal Fatty Acid-Binding Protein 5 (FABP5) Involvement in Alpha-Synuclein-Induced Mitochondrial Injury under Oxidative Stress

  2021cites this paper
• Regulative effect of maternal serum fatty acid-binding protein 4 on insulin resistance and the development of gestational diabetes mellitus.

  2020cites this paper
• Fatty acid binding protein-4 promotes alcohol-dependent hepatosteatosis and hepatocellular carcinoma progression

  2020cites this paper
• 3-Methyl-4,5-dihydro-1H-pyrazol-5-one Adduct with 1,4-Diphenylbut-2-ene-1,4-dione in Reactions with Primary Amines

  2020cites this paper
• Adipocyte-Induced FABP4 Expression in Ovarian Cancer Cells Promotes Metastasis and Mediates Carboplatin Resistance

  2020cites this paper
• Pemodelan Homologi Komparatif FABP Belalang Kembara (Locusta migratoria) Dengan PHYRE2 dan Skrining Virtual Inhibitor Potensial

  2020cites this paper
• Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.

  2020cites this paper
• Energy transfer from adipocytes to cancer cells in breast cancer.

  2020cites this paper
• Analysis of binding affinity and docking of novel fatty acid-binding protein (FABP) ligands.

  2020cites this paper
• Disruption of hypoxia-inducible fatty acid binding protein 7 induces beige fat-like differentiation and thermogenesis in breast cancer cells

  2020cites this paper
• Application of target repositioning and in silico screening to exploit fatty acid binding proteins (FABPs) from Echinococcus multilocularis as possible drug targets

  2020cites this paper
• Fatty Acid Binding Proteins Facilitate Reprogramming of Müller Glia into Progenitor Cells

  2020cites this paper
• The anti-inflammatory agent bindarit acts as a modulator of fatty acid-binding protein 4 in human monocytic cells

  2019cites this paper
• Mitochondrial Integrity Regulated by Lipid Metabolism Is a Cell-Intrinsic Checkpoint for Treg Suppressive Function

  2019cites this paper
• Computational Tools in the Discovery of FABP4 Ligands: A Statistical and Molecular Modeling Approach †

  2019cites this paper
• Fatty Acid-Binding Protein 4 in Cardiovascular and Metabolic Diseases

  2019cites this paper
• Identification of new dual FABP4/5 inhibitors based on a naphthalene-1-sulfonamide FABP4 inhibitor.

  2019cites this paper
• Development of FABP3 ligands that inhibit arachidonic acid-induced α-synuclein oligomerization.

  2019cites this paper
• Phyllanthus emblica fruit extract attenuates lipid metabolism in 3T3-L1 adipocytes via activating apoptosis mediated cell death.

  2019cites this paper
• Fatty Acid-Binding Proteins, a Family of Lipid Chaperones

  2019cites this paper
• Effects of host fatty acid–binding protein 4 on Eimeria tenella sporozoites invasion of cells

  2019cites this paper
• FABP4 inhibitors 3D-QSAR model and isosteric replacement of BMS309403 datasets

  2018cites this paper
• Crystal structure of human FABP4 complexed with ligand 4-Fluoro-3-((4-methoxynaphthalene)-1-sulfonamido) benzoic acid

  2018cites this paper
• Targeting the endocannabinoid system as a potential anticancer approach

  2018influential citation
• FABP4 inhibitor BMS309403 decreases saturated-fatty-acid-induced endoplasmic reticulum stress-associated inflammation in skeletal muscle by reducing p38 MAPK activation.

  2018cites this paper
• HDL-AuNPs-BMS nanoparticle conjugates as molecularly targeted therapy for leukemia

  2018cites this paper
• Molecular Dynamics Exploration of Selectivity of Dual Inhibitors 5M7, 65X, and 65Z toward Fatty Acid Binding Proteins 4 and 5

  2018cites this paper
• Electrostatic interaction-mediated conformational changes of adipocyte fatty acid binding protein probed by molecular dynamics simulation

  2018cites this paper
• From hit to lead: Structure-based discovery of naphthalene-1-sulfonamide derivatives as potent and selective inhibitors of fatty acid binding protein 4.

  2018cites this paper
• Adipocyte Fatty Acid Binding Protein Potentiates Toxic Lipids-Induced Endoplasmic Reticulum Stress in Macrophages via Inhibition of Janus Kinase 2-dependent Autophagy

  2017cites this paper
• Adipocyte fatty acid binding protein 4 (FABP4) inhibitors. A comprehensive systematic review.

  2017cites this paper
• Vasculo-protective effect of BMS-309403 is independent of its specific inhibition of fatty acid-binding protein 4

  2017cites this paper
• Role of the fatty acid-binding protein 4 in heart failure and cardiovascular disease.

  2017cites this paper
• A vicious loop of fatty acid-binding protein 4 and DNA methyltransferase 1 promotes acute myeloid leukemia and acts as a therapeutic target

  2017cites this paper
• Combined Virtual Screening and Substructure Search for Discovery of Novel FABP4 Inhibitors

  2017cites this paper
• Endothelial APLNR regulates tissue fatty acid uptake and is essential for apelin’s glucose-lowering effects

  2017cites this paper
• Knocking out or pharmaceutical inhibition of fatty acid binding protein 4 (FABP4) alleviates osteoarthritis induced by high-fat diet in mice.

  2017cites this paper
• Adipokines: Potential Therapeutic Targets for Vascular Dysfunction in Type II Diabetes Mellitus and Obesity

  2017cites this paper
• The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biological evaluation.

  2016cites this paper
• Herbalog: A tool for target-based identification of herbal drug efficacy through molecular docking.

  2016cites this paper
• Interaction Analysis of FABP4 Inhibitors by X-ray Crystallography and Fragment Molecular Orbital Analysis.

  2016cites this paper
• X-ray Crystallographic Structure of Ibuprofen Bound to Human Adipocyte Fatty Acid Binding Protein at 1.4 Å Resolution

  2016cites this paper
• Using molecular docking screening for identifying hyperoside as an inhibitor of fatty acid binding protein 4 from a natural product database

  2016cites this paper
• Design and synthesis of selective, dual fatty acid binding protein 4 and 5 inhibitors.

  2016cites this paper
• Chemical Genetic Approaches for the Investigation of Neutral Lipid Metabolism

  2016cites this paper
• Fatty acid binding protein-4 ( FABP 4 ) is a hypoxia inducible gene that sensitizes mice to liver ischemia / reperfusion injury

  2016cites this paper
• Structural analysis of ibuprofen binding to human adipocyte fatty-acid binding protein (FABP4).

  2015influential citation
• Inhibition of tumor growth by a newly-identified activator for epidermal fatty acid binding protein

  2015cites this paper
• The unusual lipid binding proteins of parasitic helminths and their potential roles in parasitism and as therapeutic targets.

  2015cites this paper
• Targeting epidermal fatty acid binding protein for treatment of experimental autoimmune encephalomyelitis

  2015cites this paper
• Endocannabinoid transport revisited.

  2015cites this paper
• Hydrogen‐Bonded His93 As a Sensitive Probe for Identifying Inhibitors of the Endocannabinoid Transport Protein FABP7

  2015cites this paper
• Pimozide, a novel fatty acid binding protein 4 inhibitor, promotes adipogenesis of 3T3-L1 cells by activating PPARγ.

  2015cites this paper
• Novel fatty acid binding protein 4 (FABP4) inhibitors: virtual screening, synthesis and crystal structure determination.

  2015cites this paper
• Fatty acid binding protein-4 (FABP4) is a hypoxia inducible gene that sensitizes mice to liver ischemia/reperfusion injury.

  2015cites this paper
• All-Purpose Containers? Lipid-Binding Protein – Drug Interactions

  2015cites this paper
• The mAb against adipocyte fatty acid-binding protein 2E4 attenuates the inflammation in the mouse model of high-fat diet-induced obesity via toll-like receptor 4 pathway.

  2015cites this paper
• Fatty Acid-binding Proteins Interact with Comparative Gene Identification-58 Linking Lipolysis with Lipid Ligand Shuttling

  2015cites this paper
• Inhibition of Fatty Acid Binding Proteins Elevates Brain Anandamide Levels and Produces Analgesia

  2014cites this paper