scholarly journals Measurement of AhR Ligands in the Tissues of Colon Cancer Patients with XRE Luciferase Reporter

2019 ◽  
Vol 1 (1) ◽  
Author(s):  
Margarita A Bystriakova ◽  
Sergei A Koshkin ◽  
Elena N Tolkunova
Keyword(s):  
Colon Cancer ◽  
Anticancer Agents ◽  
Tumor Tissue ◽  
Test System ◽  
Luciferase Reporter ◽  
Human Colon Cancer ◽  
Tissue Samples ◽  
High Affinity ◽  
Affinity Ligand ◽  
High Affinity Ligand

The Aryl hydrocarbon receptor (AhR) ligands exhibiting modulating activity represents a new class of anticancer agents that can be directed towards several tumors. We have examined AhR expression in human colon cancer and adjacent non-tumor tissue. AhR expression level was about 2-7 times higher in tumor tissue samples than in the adjacent non-tumor samples (in 82% of all the samples). We were unable to find any increase of ABCG2 expression on the level of the transcription, while the expression of MDR2 was increased in half of the tumors compared to the levels of expression in normal adjacent tissue. We have used FICZ as a potent high affinity ligand of the AhR to calibrate the reporter cell line HEK293T-AhR-luc as a potent high affinity ligand of the AhR. The concentration of xenobiotic response element (XRE) ligands is higher, than in the blood of healthy people in 86% of the patients. The proposed test system will allow the use of the AhR ligand level as an additional diagnostic marker in the treatment of colon cancer.

scholarly journals A novel radioiodinated high affinity ligand for the D2 -dopamine receptor

FEBS Letters ◽  
1984 ◽  
Vol 176 (2) ◽  
pp. 436-440 ◽  
Author(s):  
Nourdine Amlaiky ◽  
Brian F. Kilpatrick ◽  
Marc G. Caron
Keyword(s):  
Dopamine Receptor ◽  
D2 Dopamine Receptor ◽  
High Affinity ◽  
Affinity Ligand ◽  
High Affinity Ligand

scholarly journals High-Affinity Ligand Probes of CD22 Overcome the Threshold Set bycisLigands to Allow for Binding, Endocytosis, and Killing of B Cells

2006 ◽  
Vol 177 (5) ◽  
pp. 2994-3003 ◽  
Author(s):  
Brian E. Collins ◽  
Ola Blixt ◽  
Shoufa Han ◽  
Bao Duong ◽  
Hongyi Li ◽  
...  
Keyword(s):  
B Cells ◽  
High Affinity ◽  
Affinity Ligand ◽  
High Affinity Ligand

scholarly journals RS-45041-190: a selective, high-affinity ligand for I2 imidazoline receptors

1995 ◽  
Vol 116 (2) ◽  
pp. 1737-1744 ◽  
Author(s):  
C.M. Brown ◽  
A.C. MacKinnon ◽  
W.S. Redfern ◽  
A. Williams ◽  
C. Linton ◽  
...  
Keyword(s):  
Imidazoline Receptors ◽  
High Affinity ◽  
Affinity Ligand ◽  
High Affinity Ligand

Cortistatin A is a High-Affinity Ligand of Protein Kinases ROCK, CDK8, and CDK11

2009 ◽  
Vol 48 (47) ◽  
pp. 8952-8957 ◽  
Author(s):  
Victor J. Cee ◽  
David Y.-K. Chen ◽  
Matthew R. Lee ◽  
K. C. Nicolaou
Keyword(s):  
Protein Kinases ◽  
High Affinity ◽  
Affinity Ligand ◽  
High Affinity Ligand

scholarly journals Synthesis of Novel 1,2,4-Triazolyl Coumarin Derivatives as Potential Anticancer Agents

2018 ◽  
Vol 2018 ◽  
pp. 1-8 ◽  
Author(s):  
Lamya H. Al-Wahaibi ◽  
Hanaa M. Abu-Melha ◽  
Diaa A. Ibrahim
Keyword(s):  
Colon Cancer ◽  
Molecular Docking ◽  
Anticancer Agents ◽  
Tyrosine Kinases ◽  
Hct116 Cell ◽  
Human Colon ◽  
Docking Studies ◽  
Coumarin Derivatives ◽  
Human Colon Cancer

A series of novel coumarin derivatives carrying 1,2,4-triazole or 1,2,4-triazolo[3,4-b][1,3,4]thiadiazole moieties were prepared and evaluated in vitro as anticancer in the human colon cancer (HCT116) cell line. The derivatives 4c and 8c exhibited marked anticancer activity with IC50 values 4.363 and 2.656 µM, respectively. The molecular docking studies suggested possible interaction with tyrosine kinases (CDK2).

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