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Small-Molecule Inhibitors Targeting Receptor Tyrosine Kinases in Cancer
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2020
Mohammad Hojjat-Farsangi, Gholamreza Khamisipour
The MET oncogene is an α and β heterodimer RTK (Love et al., 2003) and is necessary for the normal development (Birchmeier and Gherardi, 1998) and the expression (low) in restricted to cells of epithelial or mesenchymal origin adult tissues (Sonnenberg et al., 1993). MET ligand, hepatocyte growth factor (HGF), and its binding to MET is associated with various roles such as cell proliferation, survival, differentiation, embryogenesis, tissue repair, and invasion (Birchmeier et al., 2003).
Metal-free domino amination-Knoevenagel condensation approach to access new coumarins as potent nanomolar inhibitors of VEGFR-2 and EGFR
Published in Green Chemistry Letters and Reviews, 2021
Essam M. Eliwa, Marcel Frese, Ahmed H. Halawa, Maha M. Soltan, Larissa V. Ponomareva, Jon S. Thorson, Khaled A. Shaaban, Mohamed Shaaban, Ahmed M. El-Agrody, Norbert Sewald
The most potent one against KB-3-1 and A549 cell lines (Table 2), 4e showed 1.2 and 2.5-fold inactivation toward VEGFR-2 and EGFR, respectively. Moderate activities were also obtained by 5e against the examined kinases. Regarding COVID-19, in silico studies have predicted higher affinity between the viral spike glycoprotein (S) and the inhibitors of the hepatocyte growth factor receptor (HGFR/c-MET), VEGFR and EGFR [56]. Consequently, exploring more agents against the above receptors is more than welcome.
A concise review on drug-loaded electrospun nanofibres as promising wound dressings
Published in Journal of Medical Engineering & Technology, 2019
Farzaneh Aavani, Sajedeh Khorshidi, Akbar Karkhaneh
Vitamins play specific roles in wound-healing stages. For instance, vitamins A and E promote wound-healing process. They both can increase collagen deposition in the repair zone of a wound. Enhancement of acid mucopolysaccharide synthesis in granulation tissue is the result of presence of vitamin A in wound site. In addition, vitamin C is a powerful water-soluble antioxidant and has the potential to cooperatively increase Hepatocyte Growth Factor secretion by fibroblasts, when vitamin C derivative is applied together with growth factors such as endothelial Growth Factor, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF). In 2013, Niiyama et al. investigated the potential of a wound dressing composed of hyaluronic acid (HA) and collagen (Col) spongy sheet containing epidermal growth factor (EGF) and vitamin C derivative (VC). They found that this wound dressing has potency to facilitate production of VEGF and HGF in vitro. In addition, it could enhance granulation tissue formation associated with angiogenesis and collagen deposition in vivo [50]. Li et al. fabricated gelatine nanofibres loaded with vitamin A palmitate and vitamin E TPGS (as stable forms of vitamin A & vitamin E, respectively). As a result, when cells were exposed to these meshes, the expression of collagen-specific genes was increased. In many cases, the special derivative of vitamin C could be used. For instance, one of the important derivative of vitamin C is magnesium ascorbyl phosphate. This molecule is a non-irritating, water-soluble and stable derivative of vitamin C. This molecule has the potential to promotion of collagen synthetic and it is effective in significantly lower concentrations compared to vitamin C [51]. Magnesium ascorbyl phosphate plays very important role in accelerating the deposition of several basement membrane proteins such as type IV and VII collagens, procollagens I and III and tenascin C at the dermal–epidermal junction [52].