A Naphthalenic Derivative ND-1 Inhibits Thrombus Formation by Interfering the Binding of Fibrinogen to Integrin αIIbβ3 Article Swipe
YOU?
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· 2016
· Open Access
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· DOI: https://doi.org/10.1155/2016/8587164
Integrin α IIb β 3 plays a crucial role in the process of platelet aggregation. Three integrin α IIb β 3 antagonists (abciximab, eptifibatide, and tirofiban) have been approved by FDA for clinical use. Unfortunately, they all showed severe side effects such as thrombocytopenia and bleeding risk. Thus, researches on the development of more effective and safer antiplatelet agents are needed. In this manuscript we reported a novel naphthalenic derivative compound ND-1 with potent antithrombotic effect and lower bleeding risk. ND-1 inhibited ADP-, collagen-, thrombin-, and U46619-induced platelet aggregation with IC 50 values of 1.29, 14.46, 12.84, and 40.24 μ M, respectively. Mechanism studies indicated that ND-1 inhibited the binding of fibrinogen to integrin α IIb β 3 in a dose-dependent manner with an IC 50 value of 3.12 μ M. ND-1 inhibited P-selectin expression induced by ADP, collagen, thrombin, and U46619 on the surface of platelets. Additionally, this compound reduced platelets spreading to the immobilized fibrinogen. In vivo, ND-1 potently decreased thrombus formation in an arteriovenous shunt thrombosis model in rats and slightly prolonged bleeding time in a tail cutting model in mice. Taken together, our results reveal that ND-1 is a novel antagonist of α IIb β 3 with strong antithrombotic effect and lower bleeding risk.
Related Topics
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.1155/2016/8587164
- https://downloads.hindawi.com/journals/bmri/2016/8587164.pdf
- OA Status
- hybrid
- Cited By
- 4
- References
- 33
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W2566559571
Raw OpenAlex JSON
- OpenAlex ID
-
https://openalex.org/W2566559571Canonical identifier for this work in OpenAlex
- DOI
-
https://doi.org/10.1155/2016/8587164Digital Object Identifier
- Title
-
A Naphthalenic Derivative ND-1 Inhibits Thrombus Formation by Interfering the Binding of Fibrinogen to Integrin αIIbβ3Work title
- Type
-
articleOpenAlex work type
- Language
-
enPrimary language
- Publication year
-
2016Year of publication
- Publication date
-
2016-01-01Full publication date if available
- Authors
-
Xue Ding, Tongdan Liu, Zhouling Xie, Qi Zhao, Yuan Cao, Xiaodong Liu, Caihui Wang, Rwibasira Rudinga Gamariel, Xin Ming, Zhiyu Li, Yi KongList of authors in order
- Landing page
-
https://doi.org/10.1155/2016/8587164Publisher landing page
- PDF URL
-
https://downloads.hindawi.com/journals/bmri/2016/8587164.pdfDirect link to full text PDF
- Open access
-
YesWhether a free full text is available
- OA status
-
hybridOpen access status per OpenAlex
- OA URL
-
https://downloads.hindawi.com/journals/bmri/2016/8587164.pdfDirect OA link when available
- Concepts
-
Tirofiban, Antithrombotic, Fibrinogen, Platelet, Integrin, Pharmacology, Thrombin, Abciximab, Thrombus, Chemistry, Clot retraction, Eptifibatide, Medicine, Immunology, Biochemistry, Internal medicine, Receptor, Conventional PCI, Myocardial infarctionTop concepts (fields/topics) attached by OpenAlex
- Cited by
-
4Total citation count in OpenAlex
- Citations by year (recent)
-
2023: 1, 2021: 1, 2018: 2Per-year citation counts (last 5 years)
- References (count)
-
33Number of works referenced by this work
- Related works (count)
-
10Other works algorithmically related by OpenAlex
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