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Tytuł pozycji:

Development of MALDI MS peptide array for thrombin inhibitor screening.

Tytuł :
Development of MALDI MS peptide array for thrombin inhibitor screening.
Autorzy :
Tang W; State Key Laboratory of Natural Medicines and School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
Gordon A; State Key Laboratory of Natural Medicines and School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
Wang HY; State Key Laboratory of Natural Medicines and School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
Li P; State Key Laboratory of Natural Medicines and School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
Chen J; State Key Laboratory of Natural Medicines and School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, China. Electronic address: .
Li B; State Key Laboratory of Natural Medicines and School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, China. Electronic address: .
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Źródło :
Talanta [Talanta] 2021 May 01; Vol. 226, pp. 122129. Date of Electronic Publication: 2021 Jan 22.
Typ publikacji :
Journal Article
Język :
English
Imprint Name(s) :
Publication: Amsterdam : Elsevier
Original Publication: Oxford : Pergamon Press
MeSH Terms :
Peptides*
Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization*
Thrombin/*antagonists & inhibitors
Phospholipids
Contributed Indexing :
Keywords: Enzyme assay; Inhibitor screening; Mass spectrometry imaging; Proanthocyanidins; Surface-based MS
Substance Nomenclature :
0 (Peptides)
0 (Phospholipids)
EC 3.4.21.5 (Thrombin)
Entry Date(s) :
Date Created: 20210307 Date Completed: 20210514 Latest Revision: 20210621
Update Code :
20210628
DOI :
10.1016/j.talanta.2021.122129
PMID :
33676683
Czasopismo naukowe
The development of in situ methods for the analysis and visualization of enzyme activity is of paramount importance in drug discovery, research, and development. In this work, the functionalized and array patterned indium tin oxide (ITO) glass slides were fabricated by non-covalent immobilization of amphipathic phospholipid-tagged peptides encompassing the thrombin cleavage site on steric acid-modified ITO slides. The fabricated peptide arrays provide 60 spots per slide, and are compatible with matrix-assisted laser desorption/ionization mass spectrometry (MALDI MS) measurement, free matrix peak interference, and tolerance to repeated aqueous washing. The peptide arrays were used for the investigation of thrombin activity and screening for its potential inhibitors. The thrombin activity and its Michaelis-Menten constant (K m ) for immobilized peptide substrate was determined using developed MALDI MS peptide array. To investigate the applicability and effectiveness of peptide arrays, the anti-thrombin activity of grape seed proanthocyanidins with different degrees of polymerization (DP) was monitored and visualized. MALDI MS imaging results showed that the fractions of proanthocyanidins with the mean DP of 4.61-6.82 had good thrombin inhibitory activity and their half-maximal inhibitory concentration (IC 50 ) were below 10 μg/mL. Therefore, the developed peptide array is a reliable platform for the discovery of natural thrombin inhibitors.
(Copyright © 2021 Elsevier B.V. All rights reserved.)

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