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.

Mass Spectrometry-based Label-free Quantitative Proteomics to Study the Effect of 3PO Drug at Cellular Level

S.B. Nukala
Primo
;
G. Baron
Secondo
;
G. Aldini;M. Carini
Penultimo
;
A. D'Amato
Ultimo
2019

Abstract

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.
3PO; cell pathway modulation; inflammation; mass spectrometry; PFKFB3 inhibitor; Quantitative proteomics; Biochemistry; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry
Settore CHIM/01 - Chimica Analitica
Settore BIO/10 - Biochimica
Settore CHIM/08 - Chimica Farmaceutica
   Modulation of glycolytic flux as a new approach for treatment of atherosclerosis and plaque stabilization: a multidisciplinary study (MOGLYNET)
   MOGLYNET
   EUROPEAN COMMISSION
   H2020
   675527
apr-2019
Article (author)
File in questo prodotto:
File Dimensione Formato  
acsmedchemlett.8b00593.pdf

accesso riservato

Tipologia: Publisher's version/PDF
Dimensione 4.56 MB
Formato Adobe PDF
4.56 MB Adobe PDF   Visualizza/Apri   Richiedi una copia
Nukalaetal_ACS_postprint.pdf

accesso aperto

Descrizione: 3PO_ACS_post_print
Tipologia: Post-print, accepted manuscript ecc. (versione accettata dall'editore)
Dimensione 1.23 MB
Formato Adobe PDF
1.23 MB Adobe PDF Visualizza/Apri
Pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/623360
Citazioni
  • ???jsp.display-item.citation.pmc??? 1
  • Scopus 4
  • ???jsp.display-item.citation.isi??? 4
social impact