scholarly journals Localization Mechanisms of Radiopharmaceuticals

2021 ◽  
Author(s):  
Sana Komal ◽  
Sana Nadeem ◽  
Zahra Faheem ◽  
Arouma Raza ◽  
Komal Sarwer ◽  
...  

Scintigraphic techniques have opened a new era of developments in the localization of infectious and cancerous foci. Diseases area targeting mechanisms of radiopharmaceuticals encompasses visualization, characterization, and measurement of physiological and biological functioning at targeted sites in addition to measure the area and density of the disease. The accumulation of a radiopharmaceutical at specific organ is based upon numerous processes such as enzymatic interactions, receptor binding site, transport of chemical species and elimination of damaged cells from circulation by a normal metabolic process. PET and SPECT are developing scanning techniques that provides effective diagnostic tool to identify pathophysiology of diseased cells. In this chapter, we are exploring and explaining different mechanisms of radiopharmaceutical localization for imaging and therapeutic processes. The knowledge of these mechanisms will help to develop target based new radiopharmaceuticals using variety of medically used radioisotopes either for imaging or therapy of diseased cells.




2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Yu-Jen Chang ◽  
Cheng-Yun Yeh ◽  
Ju-Chien Cheng ◽  
Yu-Qi Huang ◽  
Kai-Cheng Hsu ◽  
...  

AbstractEradicating influenza A virus (IAV) is difficult, due to its genetic drift and reassortment ability. As the infectious cycle is initiated by the influenza glycoprotein, hemagglutinin (HA), which mediates the binding of virions to terminal sialic acids moieties, HA is a tempting target of anti-influenza inhibitors. However, the complexity of the HA structure has prevented delineation of the structural characterization of the HA protein–ligand complex. Our computational strategy efficiently analyzed > 200,000 records of compounds held in the United States National Cancer Institute (NCI) database and identified potential HA inhibitors, by modeling the sialic acid (SA) receptor binding site (RBS) for the HA structure. Our modeling revealed that compound NSC85561 showed significant antiviral activity against the IAV H1N1 strain with EC50 values ranging from 2.31 to 2.53 µM and negligible cytotoxicity (CC50 > 700 µM). Using the NSC85561 compound as the template to generate 12 derivatives, robust bioassay results revealed the strongest antiviral efficacies with NSC47715 and NSC7223. Virtual screening clearly identified three SA receptor binding site inhibitors that were successfully validated in experimental data. Thus, our computational strategy has identified SA receptor binding site inhibitors against HA that show IAV-associated antiviral activity.



1993 ◽  
Vol 7 (7) ◽  
pp. 907-914
Author(s):  
E P Slater ◽  
H Hesse ◽  
J M Müller ◽  
M Beato


Science ◽  
1995 ◽  
Vol 268 (5209) ◽  
pp. 439-442 ◽  
Author(s):  
M. Nowak ◽  
P. Kearney ◽  
Sampson ◽  
M. Saks ◽  
C. Labarca ◽  
...  






2004 ◽  
Vol 241 (2) ◽  
pp. 185-191 ◽  
Author(s):  
Maria Helena Neves Lobo Silva-Filha ◽  
Cláudia Maria Fontes de Oliveira ◽  
Lêda Regis ◽  
Zhiming Yuan ◽  
Clara Martinez Rico ◽  
...  






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