Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
Histologic spectrum studies in patients revealed fatty acid binding proteins 1 (FABP1) as a potential new target for the treatment of metabolic associated fatty liver disease. However, there is no FABP1 inhibitor has been reported except the first-in-class FABP1 inhibitor bearing acid moiety reported by our laboratory. Herein, we firstly report the structure-activity relationship of novel non-carboxylic acid FABP1 inhibitors, which resulted in the identification of the potent and selective FABP1 inhibitor 30. The IC value of compound 30 for subtype FABP4 in the same family was greater than 80 μM. Moreover, compound 30 significantly alleviated the hepatic steatosis in DIO mice, which is equivalent to that of clinical drug obeticholic acid. This study might be provided a promising probe for the development of FABP1 inhibitors and thus can help to further elucidate the pharmacology of FABP1.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejmech.2024.116705 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Gastric cancer adapts high lipid microenvironment via suppressing PPARG-FABP1 axis after arriving in the lymph node.
Redox Biol
September 2025
Department of Gastrointestinal Surgery, The First Affiliated Hospital of Sun Yat-sen University, No. 58, Zhongshan 2 Road, Guangzhou, Guangdong, 510080, People's Republic of China. Electronic address:
Aim: Gastric cancer (GC) primarily metastasizes through lymphatic channels, although lymphatic metastasis remains relatively inefficient. Changes in cellular metabolism, known as metabolic reprogramming, plays a significant role in the adaptive survival of cells during the process. Therefore, understanding the mechanism underlying metabolic reprogramming in lymph node (LN) metastasis is crucial for the development of targeted therapies for advanced gastric cancer.
View Article and Find Full Text PDFBiomarkers and early-onset acute kidney injury in critically ill COVID-19 patients, a prospective monocentric observational study.
BMC Nephrol
July 2025
CHU Clermont-Ferrand, Service de Réanimation Médicale, Clermont- Ferrand, France.
Background: The present study evaluated the diagnostic and prognostic value of biomarkers, including soluble forms of the receptor for advanced glycation end-products (s-RAGE), soluble urokinase plasminogen activator receptor (SuPAR), and others, for the occurrence of early-onset acute kidney injury (EO-AKI), EO-AKI non-recovery, day-90 major adverse kidney events (MAKE-90), and day-90 mortality in critically ill patients with Coronavirus Disease-19 (Covid-19).
Methods: A single-center, prospective study was conducted at the University Hospital of Clermont-Ferrand, France, between March 2020 and February 2021. The study included adult patients suffering from severe pneumonia caused by the SARS-CoV-2 virus, who were admitted to the hospital's intensive care unit.
Single-cell multi-omics reveals that FABP1 + renal cell carcinoma drive tumor angiogenesis through the PLG-PLAT axis under fatty acid reprogramming.
Mol Cancer
June 2025
Department of Vascular Surgery, The First Affiliated Hospital, Fujian Medical University, Fuzhou, 350005, China.
Renal cell carcinoma is characterized by a poor prognosis. Recently, renal cell carcinoma has been recognized as a metabolic disease associated with fatty acid metabolic reprogramming, although in-depth studies on this topic are still lacking. We found that fatty acid metabolism reprogramming in renal cell carcinoma is primarily characterized by high expression of FABP1.
View Article and Find Full Text PDFNeurotensin inhibits AMPK activity and concurrently enhances FABP1 expression in small intestinal epithelial cells associated with obesity and aging.
Exp Mol Med
June 2025
University of Kentucky, Lexington, KY, USA.
We previously demonstrated that neurotensin, a 13-amino-acid gut hormone peptide, enhances small intestinal epithelial cell fatty acid uptake through inhibition of AMPK. Here, utilizing Drosophila and mouse models in vivo, as well as mouse and human small intestinal epithelial organoids or monolayers ex vivo, we determine the targets of neurotensin and AMPK associated with obesity and aging. High-fat diet and aging decreased AMPK and insulin signaling, which was prevented by neurotensin deficiency.
View Article and Find Full Text PDFDiscovery of the first-in-class FABP/PPAR multiple modulator for the treatment of metabolic dysfunction-associated steatohepatitis.
Eur J Med Chem
July 2025
School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, 510006, PR China. Electronic address:
Metabolic dysfunction-associated steatohepatitis (MASH) is a complex metabolic syndrome, and the development of new drugs is urgently needed. Fatty acid binding proteins (FABPs) and peroxisome proliferator-activated receptors (PPARs) play an important role in the regulation of lipid absorption, metabolism and inflammation. Considering the synergistic effect of FABP and PPAR in the regulation of MASH pathophysiology, the development of FABP/PPAR multiple modulators might be a promising anti-MASH strategy.
View Article and Find Full Text PDF