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Transfer of Manipulated Tumor-associated Neutrophils into Tumor-Bearing Mice to Study their Angiogenic Potential In Vivo
Published on: July 20, 2019
Antiangiogenesis and anticancer efficacy of TA138, a novel alphavbeta3 antagonist
Shaker A Mousa1, Seema Mohamed, Eric J Wexler
1Pharmaceutical Research Institute, Albany College of Pharmacy, Albany, NY 12208, USA. mousas@acp.edu
Background:
Angiogenesis is a complex process involving endothelial cell migration, proliferation, invasion, and tube formation. Inhibition of these processes might have implications in various angiogenesis-mediated disorders.
Materials And Methods:
The antiangiogenic efficacy of the novel alphavbeta3 antagonist TA138 was examined using in vivo and in vitro model systems.
Results:
The in vitro studies demonstrated the ability of TA138 and RP747 (conjugated TA138) to inhibit endothelial cell migration toward vitronectin, with an IC50=0.04 and 0.045 microM, respectively. Furthermore, utilizing the chick chorioallantoic membrane models, TA138 inhibited basic fibroblast growth factor-induced neovascularization.
Conclusion:
TA138 might be a useful tool for the inhibition of angiogenesis associated with human tumor growth, or other pathological neovascularization processes. RP747 demonstrated antitumor efficacy in 1 spontaneous tumor model (c-neu oncomouse model, alphavbeta3 positive cells) and in 1 xenograft model (HCT116 human tumor colon carcinoma, alphavbeta3 negative cells) injected subcutaneously into nude mice.
Insights
The novel alphavbeta3 antagonist TA138 effectively inhibits angiogenesis by blocking endothelial cell migration and neovascularization. This compound shows promise for treating angiogenesis-related disorders and tumor growth.
Area of Science:
- Biochemistry
- Cell Biology
- Pharmacology
Background:
- Angiogenesis is crucial for development and disease, involving endothelial cell migration, proliferation, invasion, and tube formation.
- Inhibiting angiogenesis may offer therapeutic strategies for various angiogenesis-mediated disorders.
Purpose of the Study:
- To evaluate the antiangiogenic efficacy of the novel alphavbeta3 antagonist TA138.
- To assess the potential of TA138 and its conjugate RP747 in inhibiting angiogenesis and tumor growth.
Main Methods:
- In vitro studies assessed endothelial cell migration inhibition toward vitronectin.
- In vivo chick chorioallantoic membrane models were used to evaluate neovascularization inhibition.
- Antitumor efficacy was tested in spontaneous and xenograft tumor models.
Main Results:
- TA138 and RP747 inhibited endothelial cell migration with IC50 values of 0.04 and 0.045 microM, respectively.
- TA138 demonstrated inhibition of basic fibroblast growth factor-induced neovascularization in chick chorioallantoic membrane models.
- RP747 showed antitumor efficacy in both spontaneous and xenograft tumor models.
Conclusions:
- TA138 is a potential therapeutic agent for inhibiting angiogenesis in human tumor growth and other pathological neovascularization.
- RP747 exhibits antitumor efficacy, suggesting its utility in cancer treatment.
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