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A STRUCTURE BASED DRUG DESIGN STUDY ON VEGFR-2 INHIBITORS



Год выпуска: 2011
Автор: Ajay Babu P,Viswa Teja Colluru and Naishitha Anaparthy
Издательство: LAP Lambert Academic Publishing
Страниц: 72
ISBN: 9783844319897
Описание
VEGF (Vascular Endothelial Growth Factor) is a potent angiogenic signal implicated with a key role in several pathological processes, including tumour vascularization, angiogenesis, and endothelial cell growth. The members of VEGF family bind to tyrosine kinase receptors on the cell surface to initiate a signalling cascade. VEGFR-2 is one such Receptor Tyrosine Kinase(RTK) that is found to mediate a majority of the cellular responses to VEGF. A structure based drug design study was performed on VEGFR-2 inhibitors based on the article “Hetaryl imidazoles: A novel dual inhibitors of VEGF receptors 1 and 2”. The target protein was retrieved from the Protein Data Bank (I.D. 2OH4), based on the Ramachandran plot. The structures of reported inhibitors were obtained in 3-D format using standard software packages. These 3-D analogues were docked to the protein of choice using Molegro Virtual Docker. Based on a correlation between experimentally obtained log IC50 values and...


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