High Throughput Screening of Focused Virtual Library and Synthetic Protocols of Marine Sponge Derived Hymenialdisine Analogs as Potential Abnormal Signal Transduction Inhibitors

2021 ◽  
Vol 16 (3) ◽  
pp. 194-196
Author(s):  
Ankita Sharma Sharma ◽  
Sisir Nandi
2020 ◽  
Vol 15 (1) ◽  
pp. 3-11
Author(s):  
Ankita Sharma ◽  
Sisir Nandi

Background: Existing cancer chemotherapeutics can kill normal as well as malignant cells. To solve these issues, scientists are now more concerned about the design and discovery of potential anticancer, least toxic leads, which can promote apoptosis process and inhibition of abnormal signal transduction via hyperactivation of protein kinases such as Pim-1 due to overexpression or mutation of proto-oncogenes and tumor suppressor genes related to molecular mechanisms of senescence, cell cycle, apoptosis and metastatic invasion, thus leading to anticancer activities. Natural scaffolds play a great role in this aspect. Objective: Sea is full of biodiverse natural resources of medicinal compounds derived from marine plants, sponges, actinomycetes, cynobacteria, fungi, corals and animals. Many anticancer compounds were successfully discovered. But there are few potent compounds developed against abnormal signal transduction mechanism. Materials and Methods: Therefore, an attempt has been made in the present review to focus on molecular mechanisms of various targets in connection with the over-expression of Pim-1 mediated senescence, cell cycle, apoptosis and metastatic invasion and their potent inhibitors. Results: Biochemical mechanisms of the potent marine sourced inhibitors keeping activities against abnormal signal transduction were discussed in this study. It gives great attention to expand the capabilities in these upcoming areas to remain globally relevant. Conclusion: Existed marine sourced anticancer compounds tabulated in this study could be used as a template for further design and synthesis of promising congeneric synthetic compounds against another disease by the application of in silico high throughput screening through drug repositioning.


1997 ◽  
Vol 2 (2) ◽  
pp. 91-97 ◽  
Author(s):  
Ye Tian ◽  
Lan-Hsin Wu ◽  
Fu-Zon Chung

The G-protein coupled receptor family represents a large number of neurotransmitter receptors. Among the diverse signal transduction pathways mediated via G-proteins, phospholipase C mediated phosphatidylinositol hydrolysis represents one of the best characterized signal transduction mechanisms. Accordingly, the measurement of agonist-induced phosphatidylinositol turnover has been used as a convenient functional assay for receptor activation. Assays currently used for this purpose, however, are not suitable for high throughput screening. In this article, an improved technique using 96-well microtiter plate format for measuring phosphatidylinositol turnover is introduced. Anion exchange columns were prepared on fiber glass 96-well multiscreen filter plate. Separation and detection of released inositol phosphates were conducted in a 96-well format. Cells expressing certain neurotransmitter receptors were challenged with agonists and the receptor-mediated PI turnover was measured by the new technique and the results obtained were compared to that obtained from traditional assays. The results indicate that the 96-well assay is 10 to 20 times more efficient than the traditional method and is, furthermore, suitable for high throughput drug screening. Our data also indicate that this method is particularly useful for characterizing multiple antagonists by Schild analysis.


Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
L Hingorani ◽  
NP Seeram ◽  
B Ebersole

Planta Medica ◽  
2015 ◽  
Vol 81 (16) ◽  
Author(s):  
K Georgousaki ◽  
N DePedro ◽  
AM Chinchilla ◽  
N Aliagiannis ◽  
F Vicente ◽  
...  

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
LS Espindola ◽  
RG Dusi ◽  
KR Gustafson ◽  
J McMahon ◽  
JA Beutler

2014 ◽  
Author(s):  
Clair Cochrane ◽  
Halil Ruso ◽  
Anthony Hope ◽  
Rosemary G Clarke ◽  
Christopher Barratt ◽  
...  

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