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A comprehensive review on the antidiabetic activity of flavonoids targeting PTP1B and DPP-4: a structure-activity relationship analysis

Title
A comprehensive review on the antidiabetic activity of flavonoids targeting PTP1B and DPP-4: a structure-activity relationship analysis
Type
Article in International Scientific Journal
Year
2022
Authors
Proença, C
(Author)
Other
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Ribeiro, D
(Author)
Other
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Freitas, M
(Author)
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Carvalho, F
(Author)
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Eduarda Fernandes
(Author)
FFUP
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Journal
Pages: 1-57
ISSN: 1040-8398
Publisher: Taylor & Francis
Indexing
Other information
Authenticus ID: P-00T-GFN
Abstract (EN): Type 2 diabetes (T2D) is an expanding global health problem, resulting from defects in insulin secretion and/or insulin resistance. In the past few years, both protein tyrosine phosphatase 1B (PTP1B) and dipeptidyl peptidase-4 (DPP-4), as well as their role in T2D, have attracted the attention of the scientific community. PTP1B plays an important role in insulin resistance and is currently one of the most promising targets for the treatment of T2D, since no available PTP1B inhibitors were still approved. DPP-4 inhibitors are among the most recent agents used in the treatment of T2D (although its use has been associated with possible cardiovascular adverse events). The antidiabetic properties of flavonoids are well-recognized, and include inhibitory effects on the above enzymes, although hitherto not therapeutically explored. In the present study, a comprehensive review of the literature of both synthetic and natural isolated flavonoids as inhibitors of PTP1B and DPP-4 activities is made, including their type of inhibition and experimental conditions, and structure-activity relationship, covering a total of 351 compounds. We intend to provide the most favorable chemical features of flavonoids for the inhibition of PTP1B and DPP-4, gathering information for the future development of compounds with improved potential as T2D therapeutic agents. © 2021 Taylor & Francis Group, LLC.
Language: English
Type (Professor's evaluation): Scientific
No. of pages: 57
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