Progress in the Research of GPIIb/IIIa Antagonists

Xie, Zhouling; Cao, Chen; Feng, Sen; Huang, Jing; Li, Zhiyu

doi:10.4155/fmc.15.53

Cited by 10 publications

(5 citation statements)

References 77 publications

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“…Unfortunately, RGD binds to most integrins precluding selective cell adhesion. Surfaces modified with this peptide attract apparently all cell types including thrombocytes via the platelet integrin glycoprotein IIb/IIIa . Additional sequences were discovered which interact preferentially with certain cell types, e.g., the motifs Arg-Glu-Asp-Val (REDV) and Tyr-Ile-Gly-Ser-Arg (YIGSR) which recognize ECs in a specific manner .…”

Section: Introductionmentioning

confidence: 51%

“…Surfaces modified with this peptide attract apparently all cell types including thrombocytes via the platelet integrin glycoprotein IIb/IIIa. 5 Additional sequences were discovered which interact preferentially with certain cell types, e.g., the motifs Arg-Glu-Asp-Val (REDV) and Tyr-Ile-Gly-Ser-Arg (YIGSR) which recognize ECs in a specific manner. 6 As a result, materials conjugated with these peptides are excellent substrates for endothelial adhesion and proliferation avoiding overgrowth with unwanted and in many cases faster-growing connective tissue cells, such as the ubiquitous fibroblasts.…”

Section: ■ Introductionmentioning

confidence: 99%

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Combined Endothelialization Promoting and Surface Binding Chimeric Conjugate with Low Thrombogenicity

2021

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Endothelialization of blood contacting implants, e.g., vascular stents, is regarded as a prerequisite for an improved performance in terms of minimizing thrombogenicity and the inhibition of restenosis. Commonly used materials, such as Ti-based alloys, can be surface-modified in order to improve endothelial cell (EC) colonization as well as to reduce platelet adhesion. Standard modification techniques involve silanization and are laborious and time-consuming. We propose a novel single-step procedure based on a surface-recognizing peptide generated by phage display methodology. Combining this with a polyethylene glycol (PEG) spacer and an EC-specific sequence yielded a conjugate applicable for the modification of Ti surfaces.

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Section: Introductionmentioning

confidence: 51%

Section: ■ Introductionmentioning

confidence: 99%

Combined Endothelialization Promoting and Surface Binding Chimeric Conjugate with Low Thrombogenicity

2021

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“…Однако в перечисленных случаях высокого риска тромботических осложнений обычной антиагрегантной терапии (ацетилсалициловой кислоты (АСК) и блокаторов P2Y 12 рецепторов) оказывается недостаточно [11]. Таким больным дополнительно назначают ингибиторы IIb/IIIa гликопротеиновых рецепторов (ГПР), которые являются наиболее мощными антиагрегантами [12]. Они способствуют быстрому восстановлению проходимости эпикардиальной артерии и улучшению перфузии миокарда на уровне микроциркуляторного русла с уменьшением размера инфаркта [13][14][15][16].…”

Section: Introductionunclassified

Results of a pilot clinical trial of the safety and efficacy of an original glycoprotein IIb/IIIa receptor inhibitor in acute coronary syndrome

Lukyanov,

Glukhov,

et al. 2023

Cardiovasc Ther Prev

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Aim. To study the safety and efficacy of Angipure in acute ST-segment elevation coronary syndrome (STE-ACS) and high-risk percutaneous transluminal coronary angioplasty (PTCA) compared with eptifibatide.Material and methods. The study included 157 patients with STE-ACS. High-risk PTCA included massive or total coronary artery thrombosis, noreflow/slow-reflow phenomenon, and acute stent thrombosis. Fifty-five people received Angipure at a dose of 0,72 mg/kg, 52 — at a dose of 0,40 mg/kg, while 50 patients received eptifibatide (Integrilin). We conducted clinical and laboratory studies, electrocardiography (ECG), coronary angiography.Results. According to the criteria "Frequency and severity of hemorrhagic events, including hemorrhagic stroke", "Frequency, severity of other adverse events", there were no differences in safety between Angipure at doses of 0,40 and 0,72 mg/kg and eptifibatide. Complaints, clinical symptoms, vital signs, complete blood count, biochemical and coagulation tests, ECG in patients of different groups were similar and had unidirectional dynamics. The use of Angipure or eptifibatide was considered effective if no adverse outcomes (death, recurrent acute ischemic event, need for urgent revascularization) were observed within 30 days. There were no lethal outcomes. One repeated acute ischemic event was registered in each group. In groups of patients receiving Angipure 0,40 mg/kg and eptifibatide, urgent revascularization was required once each.Conclusion. Angipure and eptifibatide have similar safety and efficacy.

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“…Integrin α IIb β 3 , which is the most abundant adhesion receptor on the surface of platelets with numbers as high as 60,000–80,000 per platelet, has been revealed to have a pivotal role in the process of platelet aggregation. α IIb β 3 is a transmembrane glycoprotein, composed of α IIb and β 3 subunit [5]. It has two states: resting and active state.…”

Section: Introductionmentioning

confidence: 99%

A Short Half-Life αIIbβ3 Antagonist ANTP266 Reduces Thrombus Formation

Liu

Ren

Ding

et al. 2018

IJMS

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Integrin αIIbβ3 plays a pivotal role in platelet aggregation. Three αIIbβ3 antagonists have been approved by the Food and Drug Administration (FDA) for the treatment of cardiovascular diseases. Unfortunately, all of these three drugs can cause the side effect of severe bleeding. Therefore, developing a new αIIbβ3 antagonist with low bleeding was needed. In the present study, we screened compounds by using a fibrinogen/integrin αIIbβ3 enzyme-linked immunosorbent assay (ELISA), and a novel αIIbβ3 antagonist ANTP266 was attained. The antithrombotic effects of ANTP266 were estimated by using two animal models, the bleeding risk was estimated by using a mice tail cutting assay, and the plasma half-life time was tested by LC-MS/MS. The results showed that ANTP266 potently decreased thrombosis formation, while not prolonging bleeding time at its effective dosage. The bleeding of ANTP266 reduced rapidly as time went on from 5 to 60 min, but tirofiban produced high bleeding continuously. The plasma half-life of ANTP266 in rats was 10.8 min. Taken together, ANTP266 is an effective antithrombotic agent with a low bleeding risk. The shorter bleeding time benefits from its short plasma half-life. ANTP266 could be a candidate for developing the αIIbβ3 antagonist of rapid elimination for a patient undergoing percutaneous coronary intervention.

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Progress in the Research of GPIIb/IIIa Antagonists

Cited by 10 publications

References 77 publications

Combined Endothelialization Promoting and Surface Binding Chimeric Conjugate with Low Thrombogenicity

Combined Endothelialization Promoting and Surface Binding Chimeric Conjugate with Low Thrombogenicity

Results of a pilot clinical trial of the safety and efficacy of an original glycoprotein IIb/IIIa receptor inhibitor in acute coronary syndrome

A Short Half-Life αIIbβ3 Antagonist ANTP266 Reduces Thrombus Formation

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