Human endothelial cells (ECs) have been employed to monitor the protein changes induced by [3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one] (3PO), a compound able to inhibit the glycolytic flux partially and transiently and to reduce pathological angiogenesis in a variety of disease models. Normal and TNFα induced inflamed ECs were incubated with and without 3PO at a concentration (20 μM) able to inhibit cell proliferation without cell death. At the end of the incubation period, samples were submitted to the following steps: (a) whole protein extraction, reduction, alkylation, and digestion by trypsin; (b) peptide separation by nano-LC-MS/MS analysis using a high-resolution mass spectrometer; (c) data analysis including protein identification, quantification, and statistical analysis. An altered protein expression profiling in combination with protein network analysis was employed by using a mass spectrometry-based label-free quantification approach to explore the underlying mechanisms of 3PO at cellular level.
Mass Spectrometry-based Label-free Quantitative Proteomics to Study the Effect of 3PO Drug at Cellular Level / S.B. Nukala, G. Baron, G. Aldini, M. Carini, A. D'Amato. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - 10:4 (special issue)(2019 Apr), pp. 577-583.
|Titolo:||Mass Spectrometry-based Label-free Quantitative Proteomics to Study the Effect of 3PO Drug at Cellular Level|
NUKALA, SARATH BABU (Primo) (Corresponding)
BARON, GIOVANNA (Secondo)
CARINI, MARINA (Penultimo)
D'AMATO, ALFONSINA (Ultimo) (Corresponding)
|Parole Chiave:||3PO; cell pathway modulation; inflammation; mass spectrometry; PFKFB3 inhibitor; Quantitative proteomics; Biochemistry; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry|
|Settore Scientifico Disciplinare:||Settore CHIM/01 - Chimica Analitica|
Settore BIO/10 - Biochimica
Settore CHIM/08 - Chimica Farmaceutica
|Progetto:||Modulation of glycolytic flux as a new approach for treatment of atherosclerosis and plaque stabilization: a multidisciplinary study (MOGLYNET)|
|Data di pubblicazione:||apr-2019|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1021/acsmedchemlett.8b00593|
|Appare nelle tipologie:||01 - Articolo su periodico|