1,3,4-Oxadiazoles as Potential Pharmacophore for Cytotoxic Potentiality: A Comprehensive Review

Author(s):  
Divya Sharma ◽  
Salahuddin ◽  
Vikas Sharma ◽  
Rajnish Kumar ◽  
Sagar Joshi ◽  
...  

: Cancer is a kind of disease that has scared many people for many years. Cancer is due to the excessive growth of cells in every particular part of the body. Oxadiazole 1,3,4 is a magical organic moiety that has anticancer potential. Various works on the 1,3,4-oxadiazoles moiety showing anticancer activity have been reported. The present analysis summarizes general synthetic methods for 1,3,4 oxadiazole. Different receptors on which these drug acts are discussed. Pharmacophore models are also presented in this review for topoisomerase-I, histone deacetylase, epidermal growth factor enzymes.

Antioxidants ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 1909
Author(s):  
Min Jeong Kim ◽  
Su Jeong Ha ◽  
Bo Ram So ◽  
Chang-Kil Kim ◽  
Kyung-Min Kim ◽  
...  

The skin acts as the primary defense organ that protects the body from the external environment. Skin cancer is one of the most common cancers in the world. Skin carcinogenesis is usually caused by cell degeneration due to exposure to ultraviolet (UV) radiation, which causes changes in various signaling networks, disrupting the homeostasis of single skin cells. In this review, we summarize the roles of nicotinamide adenine dinucleotide phosphate oxidase (NOX) and epidermal growth factor receptor (EGFR) in UV-induced skin carcinogenesis. Furthermore, we describe the crosstalk that exists between NOX, EGFR, and protein tyrosine phosphatase κ and its oncogenic downstream signaling pathways. Chemoprevention is the use of chemical compounds to recover the healthy status of the skin or delay cancer development. Current evidence from in vitro and in vivo studies on chemopreventive phytochemicals that target NOX, EGFR, or both, as major regulators of skin carcinogenesis will also be discussed.


Cancers ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 1588 ◽  
Author(s):  
Teresa Maria Elisa Modica ◽  
Francesco Dituri ◽  
Serena Mancarella ◽  
Claudio Pisano ◽  
Isabel Fabregat ◽  
...  

Calcium is the most abundant element in the human body. Its role is essential in physiological and biochemical processes such as signal transduction from outside to inside the cell between the cells of an organ, as well as the release of neurotransmitters from neurons, muscle contraction, fertilization, bone building, and blood clotting. As a result, intra- and extracellular calcium levels are tightly regulated by the body. The liver is the most specialized organ of the body, as its functions, carried out by hepatocytes, are strongly governed by calcium ions. In this work, we analyze the role of calcium in human hepatoma (HCC) cell lines harboring a wild type form of the Epidermal Growth Factor Receptor (EGFR), particularly its role in proliferation and in EGFR downmodulation. Our results highlight that calcium is involved in the proliferative capability of HCC cells, as its subtraction is responsible for EGFR degradation by proteasome machinery and, as a consequence, for EGFR intracellular signaling downregulation. However, calcium-regulated EGFR signaling is cell line-dependent. In cells responding weakly to the epidermal growth factor (EGF), calcium seems to have an opposite effect on EGFR internalization/degradation mechanisms. These results suggest that besides EGFR, calcium could be a new therapeutic target in HCC.


1993 ◽  
Vol 265 (2) ◽  
pp. E323-E331 ◽  
Author(s):  
H. Kurachi ◽  
H. Adachi ◽  
S. Ohtsuka ◽  
K. Morishige ◽  
K. Amemiya ◽  
...  

Ovariectomy (Ovx) of mice significantly increases the epidermal growth factor (EGF) concentration in the submandibular gland. To elucidate the role of this elevated EGF in obesity of Ovx mice, we examined the effects of sialoadenectomy (Sx) and anti-EGF rabbit antiserum administration on the body weight (BW) gain and carcass fat deposition in Ovx animals. Studies were performed in four groups of mice consisting of control, Ovx, Ovx+Sx, and Ovx+anti-EGF groups. Ovx increased the BW gain compared with the control animals, whereas Sx and anti-EGF significantly reduced it. Although the relative weights (weight ratio to BW) of the liver and kidney were not significantly changed by Ovx, Sx, or anti-EGF treatment of Ovx mice, the relative weights of mesenteric, parametrial, and subcutaneous fat tissues were increased in Ovx mice, and this increase was significantly reduced by Sx or anti-EGF administration. Ovx induced adipocyte hypertrophy, and this effect was eliminated by Sx and anti-EGF. Moreover, acyl-CoA synthetase mRNA level was increased by Ovx, and this increase was reduced by Sx and anti-EGF in mesenteric fat tissue. These findings suggest that elevation of EGF may play a role in the induction of obesity in Ovx mice.


1984 ◽  
Vol 100 (1) ◽  
pp. 25-31 ◽  
Author(s):  
B. A. Panaretto ◽  
Z. Leish ◽  
G. P. M. Moore ◽  
D. M. Robertson

ABSTRACT Two groups of three Merino wethers were infused intravenously with either 0·12 mg mouse epidermal growth factor (mEGF)/kg fleece-free body weight or 0·9% (w/v) NaCl over 24 h. Sheep treated with mEGF rejected food during treatment but feed intake was kept equal for both groups. Wool growth and plasma concentrations of mEGF were measured during the experiment. Pieces of skin taken from the wool-growing regions of the body were incubated with radioactive thymidine in order to measure its rate of incorporation into DNA. The skin was then divided at about the level of the sebaceous glands into sections that contained the upper dermis and epidermis (E sections) and those containing the generative wool-follicle bulbs (D sections). No mEGF was detected in the controls whereas mean levels of about 35 μg mEGF/l plasma were detected during the last 4 h of infusion in the protein-treated group. After infusion, wool growth was reduced by about 20% of the mean pretreatment level in the controls and no shedding of wool fibre was evident. In the mEGF-treated sheep, on the other hand, wool growth was depressed by 75–95% of the mean pretreatment level and the fleeces were almost completely cast in all three of the animals, leaving them nude on the wool-growing regions of the body. Wool growth was restored to its pretreatment level in this group about 1 month after infusion. The D sections of skin contributed 50–60% of skin wet weight in controls throughout the experiment. In the mEGF group, however, E sections increased in weight by about 25% and D sections decreased by 25%, relative to pretreatment values, during the 2 weeks after infusion. Both skin sections contributed equally to skin weight thereafter. Whereas the DNA content of E sections tended to increase after mEGF treatment there was a loss of 40%, relative to pretreatment values, in the DNA content of D sections. A significant decrease in thymidine incorporation into DNA in D sections was found, which lasted for at least 72 h after the start of infusion. Thymidine incorporation into E sections was raised during this period and again at about 10–14 days after infusion, when it was increased in both skin sections. We have concluded that the inhibition of wool growth in the mEGF-treated animals was associated with the inhibition of DNA synthesis in the dermal skin sections which contain proliferating cells of wool follicles. J. Endocr. (1984) 100, 25–31


2019 ◽  
Vol 4 (1) ◽  
Author(s):  
Nur Febrianti ◽  
Takdir Tahir ◽  
Saldy Yusuf

Background: Wounds occur when normal skin structures are damaged. Injury events in Indonesia have increased by 8.2% and the highest prevalence in South Sulawesi is 12.8%. One of the growth factors that play a role in the wound healing process is epidermal growth factor (EGF). EGF includes polypeptides that contain 53 amino acids, and EGF is present in all fluids in the body and platelets. This review aims to determine the role of EGF in the process of wound healing. Method: Data collected since 2017 using 8 databases (pubmed, science direct, google schollar) where the literature used is internationally published literature, additional references are taken from the bibliography of all relevant articles, all relevant articles are reviewed and analyzed. Results: EGF has a role in wound healing. EGF increases motility and epithelial cell migration. EGF can stimulate cell growth, proliferation and differentiation by binding to high affinity to the EGF receptor (EGFR) on the cell surface. The goal of EGF healing is most epithelial tissue, fibroblasts, and endothelial cells. EGF can call three important biological actions in tissue repair including cytoprotection, mitogenesis, and migration. Conclusion: EGF plays an important role in the wound healing process, especially in the re-epithelial process. Based on this review, it is suggested that the selection of dressings that are used should support EGF.


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