Category Ranking

98%

Total Visits

921

Avg Visit Duration

2 minutes

Citations

20

Article Abstract

A convergent synthesis to access hydrophobic tail analogs and head group modifications of AAL(S) is described. The analogs synthesised were evaluated for their ability to inhibit ceramide synthase 1 and for their cytotoxicity in K562 cells. Our results have identified inhibitors which are non-cytotoxic yet maintain CerS1 inhibition.

Download full-text PDF

Source
http://dx.doi.org/10.1039/c5ob01931aDOI Listing

Publication Analysis

Top Keywords

ceramide synthase
8
synthesis biological
4
biological evaluation
4
evaluation analogs
4
analogs aals
4
aals ceramide
4
synthase inhibitors
4
inhibitors convergent
4
convergent synthesis
4
synthesis access
4

Similar Publications

Leishmania donovani is an intracellular protozoan parasite that has successfully evolved to manipulate host macrophages. The exact mechanism by which Leishmania spp evades macrophage function is not fully understood. Recently, several studies have shown that pathogens target host-microRNA to alter cellular pathways for their persistence.

View Article and Find Full Text PDF

Unlabelled: Triple-negative breast cancer (TNBC) remains a significant clinical challenge due to its aggressive nature and lack of effective targeted therapies. The enzyme ceramide synthase 2 (CerS2), which synthesizes pro-apoptotic very long-chain ceramides (VLCCs), represents a promising therapeutic target. Here, we identify and characterize DH20931, a novel, first-in-class small-molecule agonist of CerS2.

View Article and Find Full Text PDF

KLF9 Inhibits Brain Metastasis of Non-Small Cell Lung Cancer by Regulating Ceramide Synthase 1 Synthesis.

FASEB J

September 2025

Fujian Provincial Key Laboratory of Medical Big Data Engineering, Fujian Provincial Hospital, Shengli Clinical College of Fujian Medical University, Fuzhou, Fujian Province, China.

The regulatory mechanisms driving brain metastasis (BM) in non-small cell lung cancer (NSCLC) are complex, with Ceramide synthase 1 (Cers1) playing a critical role. However, the upstream factors controlling Cers1 expression remain unclear. Additionally, Kruppel-like factor 9 (KLF9) has been implicated as a potential tumor suppressor transcription factor (TF) in lung cancer.

View Article and Find Full Text PDF

Porcine respiratory disease complex induces pulmonary fibrosis related to the aberrant sphingolipid metabolism.

Int J Exp Pathol

September 2025

Laboratory of Pharmacobiology, State Key Laboratory of Animal Nutrition and Feeding, Institute of Animal Science, Chinese Academy of Agricultural Sciences, Beijing, China.

Porcine respiratory disease complex (PRDC) is a common syndrome in the modern swine industry worldwide, and its pathogenesis remains unclear to date. Our study aimed to investigate PRDC-induced pulmonary fibrosis and sphingolipid metabolism, and their relationship. Mouse and cell line (A549 and 3D4/21) models exposed to bleomycin and/or transforming growth factor-β1 (TGF-β1) were developed.

View Article and Find Full Text PDF

The Emerging Mycotoxin 2-Amino-14, 16-Dimethyloctadecan-3-ol (AOD) Alters Transcriptional Regulation and Sphingolipid Metabolism and Undergoes -Acylation by HepG2 Cells.

Toxins (Basel)

August 2025

Jiangxi Key Laboratory of Aging and Disease, Sphingolipid Metabolism and Aging, Human Aging Research Institute (HARI) and School of Life Science, Nanchang University, Nanchang 330031, China.

2-Amino-14,16-dimethyloctadecan-3-ol (AOD) is commonly found in foods contaminated with , particularly cereals or fruits, and is structurally related to mycotoxins (fumonisins) and mammalian sphingoid bases, especially 1-deoxysphinganine (m18:0); therefore, it might enter systemic circulation and tissues upon dietary intake. Knowledge about what happens when cells are exposed to AOD is limited, but it has been reported to be cytotoxic and to induce vacuolization in HepG2 cells. We also found that AOD is cytotoxic for HepG2 cells, but even at a concentration where cell viability remained above 85% (5 μM), it altered 24 differentially expressed genes based on RNA sequencing-based transcriptomic profiling.

View Article and Find Full Text PDF