scholarly journals Novel agonist‐ and antagonist‐based radioligands for the GLP‐2 receptor ‐ useful tools for studies of basic GLP‐2R pharmacology

2021 ◽  
Author(s):  
Sarina Gadgaard ◽  
Wijnand J. C. Velden ◽  
Sine P. Schiellerup ◽  
Jenna Elizabeth Hunt ◽  
Maria B. N. Gabe ◽  
...  
Keyword(s):  
Agonist And Antagonist

Recent Advances on QSAR-Based Profiling of Agonist and Antagonist A3 Adenosine Receptor Ligands

2013 ◽  
Vol 13 (9) ◽  
pp. 1048-1068 ◽  
Author(s):  
Changliang Deng ◽  
Feng Luan ◽  
Maykel Cruz- Monteagudo ◽  
Fernanda Borges ◽  
M. Natalia D. S. Cordeiro
Keyword(s):  
Adenosine Receptor ◽  
Receptor Ligands ◽  
Recent Advances ◽  
A3 Adenosine Receptor ◽  
Agonist And Antagonist ◽  
Adenosine Receptor Ligands

The Expression of Dopamine Receptors Gene and their Potential Role in Targeting Breast Cancer Cells with Selective Agonist and Antagonist Drugs. Could it be the Novel Insight to Therapy?

2019 ◽  
Vol 16 (2) ◽  
pp. 184-197 ◽  
Author(s):  
Hossein Bakhtou ◽  
Asiie Olfatbakhsh ◽  
Abdolkhaegh Deezagi ◽  
Ghasem Ahangari
Keyword(s):  
Breast Cancer ◽  
Gene Expression ◽  
Cancer Cells ◽  
Dopamine Receptors ◽  
Breast Cancer Cells ◽  
D2 Receptors ◽  
Healthy Individuals ◽  
Agonist And Antagonist ◽  
The Mean ◽  
Mcf 7

Background:Breast cancer is one of the common causes of mortality for women in Iran and other parts of the world. The substantial increasing rate of breast cancer in both developed and developing countries warns the scientists to provide more preventive steps and therapeutic measures. This study is conducted to investigate the impact of neurotransmitters (e.g., Dopamine) through their receptors and the importance of cancers via damaging immune system. It also evaluates dopamine receptors gene expression in the women with breast cancer at stages II or III and dopamine receptor D2 (DRD2) related agonist and antagonist drug effects on human breast cancer cells, including MCF-7 and SKBR-3.Methods:The patients were categorized into two groups: 30 native patients who were diagnosed with breast cancer at stages II and III, with the mean age of 44.6 years and they were reported to have the experience of a chronic stress or unpleasant life event. The second group included 30 individuals with the mean age of 39 years as the control group. In order to determine the RNA concentration in all samples, the RNA samples were extracted and cDNA was synthesized. The MCF-7 cells and SKBR-3 cells were treated with dopamine receptors agonists and antagonists. The MTT test was conducted to identify oxidative and reductive enzymes and to specify appropriate dosage at four concentrations of dopamine and Cabergoline on MCF-7 and SKBR-3 cells. Immunofluorescence staining was done by the use of a mixed dye containing acridine orange and ethidiume bromide on account of differentiating between apoptotic and necrotic cells. Flow cytometry assay was an applied method to differentiate necrotic from apoptotic cells.Results:Sixty seven and thirty three percent of the patients were related to stages II and III, respectively. About sixty three percent of the patients expressed ER, while fifty seven percent expressed PR. Thirty seven percent of the patients were identified as HER-2 positive. All types of D2-receptors were expressed in PBMC of patients with breast cancer and healthy individuals. The expression of the whole dopamine receptor subtypes (DRD2-DRD4) was carried out on MCF-7 cell line. The results of RT-PCR confirmed the expression of DRD2 on SKBR-3 cells, whereas the other types of D2- receptors did not have an expression. The remarkable differences in gene expression rates between patients and healthy individuals were revealed in the result of the Real-time PCR analysis. The over expression in DRD2 and DRD4 genes of PBMCs was observed in the patients with breast cancer at stages II and III. The great amount of apoptosis and necrosis occurred after the treatment of MCF-7 cells by Cabergoline from 25 to 100 µmolL-1 concentrations.Conclusion:This study revealed the features of dopamine receptors associated with apoptosis induction in breast cancer cells. Moreover, the use of D2-agonist based on dopamine receptors expression in various breast tumoral cells could be promising as a new insight of complementary therapy in breast cancer.

A Molecular Basis for Agonist and Antagonist Actions at GABACReceptors

2008 ◽  
Vol 71 (4) ◽  
pp. 306-327 ◽  
Author(s):  
Heba Abdel-Halim ◽  
Jane R. Hanrahan ◽  
David E. Hibbs ◽  
Graham A. R. Johnston ◽  
Mary Chebib
Keyword(s):  
Molecular Basis ◽  
Agonist And Antagonist

scholarly journals Agonist and antagonist properties of calmodulin fragments.

1984 ◽  
Vol 259 (7) ◽  
pp. 4419-4426 ◽  
Author(s):  
D L Newton ◽  
M D Oldewurtel ◽  
M H Krinks ◽  
J Shiloach ◽  
C B Klee
Keyword(s):  
Agonist And Antagonist

scholarly journals In Silico Screening of Agonist and Antagonist Natural Compounds from Reported Essential Oils against Bursaphelenchus xylophilus

2020 ◽  
Vol 3 (1) ◽  
pp. 31
Author(s):  
Jorge M. S. Faria ◽  
Ana Margarida Rodrigues ◽  
Pedro Barbosa ◽  
Manuel Mota
Keyword(s):  
Essential Oils ◽  
Pine Wilt Disease ◽  
Natural Compounds ◽  
Bursaphelenchus Xylophilus ◽  
Pinewood Nematode ◽  
Highly Active ◽  
Bibliographic Data ◽  
Agonist And Antagonist ◽  
Containment Strategy ◽  
Detailed Chemical

Chemical control has been the most effective and reliable containment strategy in integrated pest management of pine wilt disease (PWD), caused by the pinewood nematode (PWN), Bursaphelenchus xylophilus. Yet, large spectrum nematicides can be dangerous to human health and the environment. Essential oils (EOs) are safer sustainable alternatives, being composed of highly active natural compounds. A survey of bibliographic data on the detailed chemical composition and activity of the EOs used against the PWN allowed pinpointing monoterpenes as the main source of structures with agonist or antagonist properties. Transversal EO data treatment can identify potential highly active anti-PWN compounds.

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