A combinatorial in silico and cellular approach to identify a new class of compounds that target VEGFR2 receptor tyrosine kinase activity and angiogenesis
Jayakanth Kankanala,Antony M. Latham,A.P. Johnson,Shervanthi Homer-Vanniasinkam,Colin W. G. Fishwick,Sreenivasan Ponnambalam +5 more
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TLDR
The de novo design of a new generation pyrazole‐based molecule (JK‐P3) that targets VEGFR2 kinase activity and angiogenesis is described.Abstract:
BACKGROUND AND PURPOSE
Vascular endothelial growth factor receptor 2 (VEGFR2) is an attractive therapeutic target for the treatment of diseases such as cancer. Small-molecule VEGFR2 inhibitors of a variety of chemical classes are currently under development or in clinical use. In this study, we describe the de novo design of a new generation pyrazole-based molecule (JK-P3) that targets VEGFR2 kinase activity and angiogenesis.read more
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Cerium Oxide Nanoparticle Modified Scaffold Interface Enhances Vascularization of Bone Grafts by Activating Calcium Channel of Mesenchymal Stem Cells.
Junyu Xiang,Jianmei Li,Jian He,Xiangyu Tang,Ce Dou,Zhen Cao,Bo Yu,Chunrong Zhao,Fei Kang,Lu Yang,Shiwu Dong,Xiaochao Yang +11 more
TL;DR: In vivo ectopic bone formation experiment demonstrated this method could significantly improve the blood vessel distribution inside of TEB and promote the proliferation, differentiation, and tube formation ability of EPCs.
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Formononetin, a novel FGFR2 inhibitor, potently inhibits angiogenesis and tumor growth in preclinical models.
Xiao Yu Wu,Hao Xu,Zhen Feng Wu,Che Chen,Jia Yun Liu,Guan Nan Wu,Xue Quan Yao,Fu Kun Liu,Gang Li,Liang Shen +9 more
TL;DR: Results indicate that formononetin targets the FGFR2-mediated Akt signaling pathway, leading to the suppression of tumor growth and angiogenesis.
Journal ArticleDOI
Design, synthesis, molecular docking and anticancer evaluations of 5-benzylidenethiazolidine-2,4-dione derivatives targeting VEGFR-2 enzyme.
Khaled El-Adl,Khaled El-Adl,Abdel-Ghany A. El-Helby,Helmy Sakr,Ibrahim H. Eissa,Sanadelaslam S. A. El‐Hddad,Fatma M.I.A. Shoman +6 more
TL;DR: Novel series of 5-benzylidenethiazolidine-2,4-dione derivatives 4a-c-8a-f was designed, synthesized and evaluated for anticancer activity against HepG2, HCT-116 and MCF-7 cell lines, finding compounds 8f to be the most potent derivative that inhibited VEGFR-2 at IC50 value of 0.22 ± 0.02 µM.
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Endosome-to-plasma membrane recycling of VEGFR2 receptor tyrosine kinase regulates endothelial function and blood vessel formation.
Helen M. Jopling,Adam F. Odell,Caroline Pellet-Many,Antony M. Latham,Paul Frankel,Asipu Sivaprasadarao,John H. Walker,Ian Zachary,Sreenivasan Ponnambalam +8 more
TL;DR: Evaluation of a transgenic zebrafish model showed that both Rab4 and Rab11a are functionally required for blood vessel formation and animal viability and Interestingly, depletion of Rab4a levels stimulated VEGF-A-regulated endothelial cell proliferation, which was also both required for endothelial tubulogenesis.
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Design, Synthesis, Molecular Docking, and Anticancer Activity of Phthalazine Derivatives as VEGFR-2 Inhibitors.
Abdel-Ghany A. El-Helby,Rezk R. Ayyad,Helmy Sakr,Khaled El-Adl,Mamdouh M. Ali,Fathalla Khedr +5 more
TL;DR: Novel series of phthalazine derivatives 6–11 were designed, synthesized, and evaluated for their anticancer activity against two human tumor cell lines, HCT‐116 human colon adenocarcinoma and MCF‐7 breast cancer cells, targeting the VEGFR‐2 enzyme.
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