scholarly journals Preclinical Activities of Epigallocatechin Gallate in Signaling Pathways in Cancer

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 467 ◽  
Author(s):  
Mehdi Sharifi-Rad ◽  
Raffaele Pezzani ◽  
Marco Redaelli ◽  
Maira Zorzan ◽  
Muhammad Imran ◽  
...  
Keyword(s):  
Growth Factor ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Growth Factor Receptor ◽  
Epigallocatechin Gallate ◽  
Proteasome Inhibition ◽  
Cellular Processes ◽  
Bioactive Component ◽  
Cell Death Mechanisms ◽  
Endothelial Growth Factor

Epigallocatechin gallate (EGCG) is the main bioactive component of catechins predominantly present in various types of tea. EGCG is well known for a wide spectrum of biological activities as an anti-oxidative, anti-inflammatory, and anti-tumor agent. The effect of EGCG on cell death mechanisms via the induction of apoptosis, necrosis, and autophagy has been documented. Moreover, its anti-proliferative action has been demonstrated in many cancer cell lines. It was also involved in the modulation of cyclooxygenase-2, oxidative stress and inflammation of different cellular processes. EGCG has been reported as a promising agent target for plasma membrane proteins, such as epidermal growth factor receptor. In addition, it has been demonstrated a mechanism of action relying on the inhibition of ERK1/2, p38 MAPK, NF-κB, and vascular endothelial growth factor. Furthermore, EGCG and its derivatives were used in proteasome inhibition and they were involved in epigenetic mechanisms. In summary, EGCG is the most predominant and bioactive constituent of tea and may play a role in cancer prevention.

scholarly journals The Vascular Endothelial Growth Factor Receptor Flt-1 Mediates Biological Activities

1996 ◽  
Vol 271 (30) ◽  
pp. 17629-17634 ◽  
Author(s):  
Matthias Clauss ◽  
Herbert Weich ◽  
Georg Breier ◽  
Ulrike Knies ◽  
Wolfgang Röckl ◽  
...  
Keyword(s):  
Vascular Endothelial Growth Factor ◽  
Growth Factor ◽  
Biological Activities ◽  
Growth Factor Receptor ◽  
Vascular Endothelial ◽  
Endothelial Growth Factor

scholarly journals Alkaloid extract of Corydalis yanhusuo inhibits angiogenesis via targeting vascular endothelial growth factor receptor signaling

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Li Wan ◽  
Yang Zhao ◽  
Qun Zhang ◽  
Guangyi Gao ◽  
Shanlan Zhang ◽  
...  
Keyword(s):  
Vascular Endothelial Growth Factor ◽  
Growth Factor ◽  
Wide Spectrum ◽  
Growth Factor Receptor ◽  
Tube Formation ◽  
Drug Candidate ◽  
Vascular Endothelial ◽  
Migration Ability ◽  
Endothelial Growth Factor

Abstract Background Corydalis yanhusuo W.T. Wang (YHS) is a well-known Chinese flowering herbal plant commonly used for centuries in functional food and traditional Chinese medicine. In the present study, we have identified and characterized a novel inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2) with low toxicity, alkaloid extract of YHS, which suppressed angiogenesis that plays a fundamental role in a wide spectrum of physiological functions and pathological processes. Methods Proliferative ability of human umbilical vascular endothelial cells (HUVECs) was assessed using MTT assay and Ki67 immunofluorescence staining. Migration ability of HUVECs was evaluated by wound healing and transwell assays. In vitro angiogenesis was tested by spheroid sprouting and tube formation assays. In vivo vascularization was examined using Matrigel plug and chick chorioallantoic membrane (CAM) models. Protein expression and phosphorylation levels of VEGFR2, AKT, ERK and STAT3 were determined by Western blot assay. Results We demonstrated that alkaloid extract of YHS significantly inhibited a variety of VEGF-induced angiogenesis processes including proliferation, migration, sprouting, and tube formation of HUVECs. Moreover, alkaloid extract of YHS contributed to reduced in vivo neo-vessel formation in Matrigel plugs of mice and CAM models. Further mechanistic studies revealed that alkaloid extract of YHS suppressed VEGF-induced signaling pathway as evaluated by diminished phosphorylation of VEGFR2 and subsequently attenuated its downstream regulators including phospho-ERK1/2, phospho-AKT and phospho-STAT3 levels in HUVECs. Conclusion Collectively, these preclinical findings indicate that alkaloid extract of YHS remarkably limits angiogenesis and may serve as a promising anti-angiogenic drug candidate.

The Basis for the Distinct Biological Activities of Vascular Endothelial Growth Factor Receptor-1 Ligands

2013 ◽  
Vol 6 (282) ◽  
pp. ra52-ra52 ◽  
Author(s):  
A. Anisimov ◽  
V.-M. Leppanen ◽  
D. Tvorogov ◽  
G. Zarkada ◽  
M. Jeltsch ◽  
...  
Keyword(s):  
Vascular Endothelial Growth Factor ◽  
Growth Factor ◽  
Biological Activities ◽  
Growth Factor Receptor ◽  
Vascular Endothelial ◽  
Endothelial Growth Factor

scholarly journals Members of the Fibroblast Growth Factor Receptor Superfamily Are Proteolytically Cleaved by Two Differently Activated Metalloproteases

2021 ◽  
Vol 22 (6) ◽  
pp. 3165
Author(s):  
Garima Dixit ◽  
Willow Schanz ◽  
Benjamin A. Pappas ◽  
Thorsten Maretzky
Keyword(s):  
Growth Factor ◽  
Fibroblast Growth Factor ◽  
Tyrosine Kinases ◽  
Biological Activities ◽  
Growth Factor Receptor ◽  
Cell Movement ◽  
Calcium Ionophore ◽  
Fibroblast Growth ◽  
Fibroblast Growth Factor Receptors ◽  
Cellular Processes

Fibroblast growth factor receptors (FGFRs) are a family of receptor tyrosine kinases that have been associated not only with various cellular processes, such as embryonic development and adult wound healing but also enhanced tumor survival, angiogenesis, and metastatic spread. Proteolytic cleavage of these single-pass transmembrane receptors has been suggested to regulate biological activities of their ligands during growth and development, yet little is known about the proteases responsible for this process. In this study, we monitored the release of membrane-anchored FGFRs 1, 2, 3, and 4 in cell-based assays. We demonstrate here that metalloprotease-dependent metalloprotease family, ADAM10 and ADAM17. Loss- and gain-of-function studies in murine embryonic fibroblasts showed that constitutive shedding as well as phorbol-ester-induced processing of FGFRs 1, 3, and 4 is mediated by ADAM17. In contrast, treatment with the calcium ionophore ionomycin stimulated ADAM10-mediated FGFR2 shedding. Cell migration assays with keratinocytes in the presence or absence of soluble FGFRs suggest that ectodomain shedding can modulate the function of ligand-induced FGFR signaling during cell movement. Our data identify ADAM10 and ADAM17 as differentially regulated FGFR membrane sheddases and may therefore provide new insight into the regulation of FGFR functions.

Fortgeschrittenes medulläres Schilddrüsenkarzinom: Vandetanib verbessert das progressionsfreie Überleben

2012 ◽  
Vol 03 (02) ◽  
pp. 93-92
Author(s):  
Alexander Kretzschmar
Keyword(s):  
Vascular Endothelial Growth Factor ◽  
Epidermal Growth Factor Receptor ◽  
Growth Factor ◽  
Epidermal Growth Factor ◽  
Growth Factor Receptor ◽  
Phase Iii ◽  
Vascular Endothelial ◽  
Medulläres Schilddrüsenkarzinom ◽  
Epidermal Growth ◽  
Endothelial Growth Factor

Vandetanib ist ein oraler Hemmer des RET-Kinase-, VEGF (Vascular Endothelial Growth Factor Receptor)- und EGFR (Epidermal Growth Factor Receptor)-Signalwegs. In einer zulassungsrelevanten, randomisierten, doppelblinden, placebokontrollierten Phase- III-Studie verlängerte der Tyrosinkinasehemmer das progressionsfreie Überleben (PFS) signifikant länger als Placebo.

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