Last update 01 Nov 2024

αIIbβ3

Last update 01 Nov 2024

Basic Info

Synonyms-

Introduction-

Drugs associated with αIIbβ3

ML165

Target

αIIbβ3

Mechanism

αIIbβ3 inhibitors

Active Org.

National Human Genome Research Institute

Originator Org.

National Human Genome Research Institute

Active Indication-

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with αIIbβ3

100 Translational Medicine associated with αIIbβ3

0 Patents (Medical) associated with αIIbβ3

124

Literatures (Medical) associated with αIIbβ3

31 Dec 2024·Animal Cells and Systems

Producing highly effective extracellular vesicles using IBAR and talin F3 domain fusion

Article

Author: Lee, MinHyeong ; Lee, Joonha ; Kim, Jiyoon ; Cho, Eun-Gyung ; Kim, Chungho

Extracellular vesicles (EVs), transporting diverse cellular components, play a crucial role in intercellular communication in numerous physiological and pathological processes. EVs have also been recognized as a drug delivery platform for therapeutic purposes and cell-free regenerative medicine. While various approaches have focused on increasing EV production for efficient use therapeutic use of EVs, enhancing the quality of EVs, such as ensuring efficient uptake by their target cells, has not been widely explored. In this study, we linked a negative membrane curvature-forming inverse BAR (IBAR) domain with an integrin β tail-binding talin F3 domain to create the IBAR-F3 fusion protein. We observed that IBAR-F3 can trigger filopodia-like membrane protrusions and attract integrins to those protrusion-rich regions, when expressed in Chinese hamster ovary cells expressing integrin αIIbβ3. Surprisingly, the expression of IBAR-F3 also induced a robust production of EVs, which were then efficiently taken up by nearby cells in an integrin-dependent manner. Moreover, IBAR triggered integrin activation, presumably by inducing negative membrane curvature that likely disrupts the interaction between the integrin α and β transmembrane domain. Therefore, we suggest that IBAR-F3 should be utilized to promote both EV production and efficient uptake mediated by integrins. Furthermore, the negative curvature-inducing integrin activation suggests that integrins on EVs can be activated by the nanoscale change in the curvature of the EV without the need for conventional machinery to activate integrin inside the EVs.

31 Dec 2024·Journal of Obstetrics and Gynaecology

Decoction of Yougui Wan combined with Wuzi Yanzong Wan ameliorates thin endometrium in a mouse model

Article

Author: Zhou, Xiaohong ; Su, Aifang ; Xiang, Jun

BACKGROUNDThis study aimed to determine the effect and mechanism of the Decoction of Yougui Wan combined with Wuzi Yanzong Wan (DYWWYW), a traditional Chinese herbal formula, in a mouse model with thin endometrium induced by 95% ethanol.METHODSThin endometrium mice were treated with progynova (0.002 mg) as well as a low and high dose of DYWWYW (0.05 and 0.5 mL DYWWYW, respectively, diluted in 2 mL normal saline). Western blotting and qRT-PCR analyses were performed to determine the protein and mRNA expression levels, respectively, of integrin αγβ3 and leukaemia inhibitor factor (LIF) in uterus tissues. Serum oestradiol and progesterone concentrations were determined via ELISA. The remaining thin endometrium mice were mated with male mice, and the number of embryos implanted in the different groups was calculated.RESULTSA high dose of DYWWYW effectively ameliorated the injury of endometrium caused by 95% ethanol. The levels of oestradiol, progesterone, αγβ3 and LIF in thin endometrium mice treated with a high dose of DYWWYW were also significantly elevated. Additionally, a high dose of DYWWYW remarkably increased the number of embryo implantations in mice with thin endometrium.CONCLUSIONDYWWYW has improvement effects on thin endometrium by elevating the levels of endogenous oestradiol, progesterone, αγβ3, and LIF in a mouse model.

01 Dec 2024·International Immunopharmacology

The natural flavonoid pinocembrin shows antithrombotic activity and suppresses septic thrombosis

Article

Author: Li, Zhaoyan ; Da, Xingwen ; Li, Gaoxiang ; Pu, Jun ; Liu, Wenhua

Sepsis, an extreme host response to systemic infection, remains one of the leading causes of mortality worldwide. Platelets, which are integral to both thrombosis and inflammation, play a crucial role in the pathophysiology of sepsis. Excessive platelet activation and aggregation significantly increase the risk of thrombosis, thereby elevating mortality in septic patients. However, the etiology and treatment of this condition have not been comprehensively studied. This study identifies pinocembrin, a natural flavonoid compound derived from propolis, as a potential therapeutic agent for mitigating platelet activation and treating sepsis. In vivo, pinocembrin effectively inhibited FeCl₃-induced carotid arterial occlusive thrombus formation and collagen/epinephrine-induced pulmonary thromboembolism in mouse models. In vitro, pinocembrin treatment suppressed multiple facets of platelet activation, including aggregation, secretion, and αIIbβ3-mediated signaling events. Mechanistically, pinocembrin repressed platelet functions by inhibiting Src/Syk/PLCγ2/MAPK signaling pathway. Using cecal ligation and puncture (CLP) mouse model to simulate human sepsis, pinocembrin reduced inflammatory cytokine release and septic thrombosis, thereby improving the survival rate of septic mice. Lipopolysaccharide (LPS)-induced model further substantiated these results. Overall, the inhibition of platelet activity by pinocembrin demonstrates significant therapeutic potential for managing life-threatening septic thrombosis.

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αIIbβ3

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