Inhibitory Activities of Novel Pyrimidine Derivatives on the Contact Hypersensitivity Reaction.

ChemInform ◽  
2003 ◽  
Vol 34 (33) ◽  
Author(s):  
Yoshiaki Isobe ◽  
Masanori Tobe ◽  
Yoshifumi Inoue ◽  
Yuso Goto ◽  
Fumihiro Obara ◽  
...  
Keyword(s):  
Hypersensitivity Reaction ◽  
Contact Hypersensitivity ◽  
Pyrimidine Derivatives ◽  
Inhibitory Activities

scholarly journals Inhibitory Activities of Novel Pyrimidine Derivatives on the Contact Hypersensitivity Reaction

2003 ◽  
Vol 51 (3) ◽  
pp. 309-312 ◽  
Author(s):  
Yoshiaki Isobe ◽  
Masanori Tobe ◽  
Yoshifumi Inoue ◽  
Yuso Goto ◽  
Fumihiro Obara ◽  
...  
Keyword(s):  
Hypersensitivity Reaction ◽  
Contact Hypersensitivity ◽  
Pyrimidine Derivatives ◽  
Inhibitory Activities

3D-QSAR and Docking Studies on Pyrimidine Derivatives as CSF-1R Inhibitors

2020 ◽  
Vol 17 (3) ◽  
pp. 341-355
Author(s):  
Ya-ting Deng ◽  
Jun-wei Wang ◽  
Han Chu ◽  
Juan Wang ◽  
Yong Hu ◽  
...  
Keyword(s):  
Poor Prognosis ◽  
3D Qsar ◽  
Docking Studies ◽  
Colony Stimulating Factor ◽  
Training Set ◽  
Pyrimidine Derivatives ◽  
Comfa Model ◽  
Inhibitory Activities ◽  
The Relationship ◽  
Stimulating Factor

Background: Colony Stimulating Factor-1 Receptor (CSF-1R) is associated with malignancy, invasiveness and poor prognosis of tumors, and pyrimidine derivatives are considered as a novel class of CSF-1R inhibitor. Methods: To explore the relationship between the structures of substituted pyrimidine derivatives and their inhibitory activities against CSF-1R, CoMFA and CoMSIA analyses, and molecular docking studies were performed on a dataset of forty-four compounds. Results: We found in CoMFA model including steric and electrostatic fields for the training set, the cross-validated q2 value was 0.617 and the non-cross-validated r2 value was 0.983. While, the crossvalidated q2 value was 0.637 and the non-cross-validated r2 value was 0.984 in CoMSIA Model which include steric, electrostatic and hydrophobic fields. 3D equipotential maps generated from CoMFA and CoMSIA along with the docking binding structures provided enough information about the structural requirements for better activity. Conclusion: The data generated from the present study helped us to predict the activity of new inhibitors and further design some novel and potent CSF-1R inhibitors.

scholarly journals Itraconazole Suppresses an Elicitation Phase of a Contact Hypersensitivity Reaction

2006 ◽  
Vol 126 (5) ◽  
pp. 1028-1035 ◽  
Author(s):  
Urupongsa Ausaneya ◽  
Akira Kawada ◽  
Yoshinori Aragane
Keyword(s):  
Hypersensitivity Reaction ◽  
Contact Hypersensitivity

Modification of LC Phenotype and Suppression of Contact Hypersensitivity Response by Stress

1998 ◽  
Vol 3 (2) ◽  
pp. 79-84 ◽  
Author(s):  
Junichi Hosoi ◽  
Toru Tsuchiya ◽  
Mitsuhiro Denda ◽  
Yutaka Ashida ◽  
Akira Takashima ◽  
...  
Keyword(s):  
Immune System ◽  
Hypersensitivity Reaction ◽  
Laser Scanning ◽  
Immobilization Stress ◽  
Confocal Laser Scanning Microscope ◽  
Contact Hypersensitivity ◽  
Confocal Laser ◽  
Scanning Microscope ◽  
Histocompatibility Complex ◽  
Epidermal Langerhans Cells

Background: Stress is thought to exacerbate a number of diseases, some of which are skin disorders. Epidermal Langerhans' cells play a major role in cutaneous immune reactions. Objective: The effects of two types of stress on the cutaneous immune system were to be assessed in mice. Methods: Mice received stress by immobilization or housing at various population densities. Epidermal sheets were stained for I-A molecules (a member of class II major histocompatibility complex) and analyzed with a confocal-laser-scanning microscope. Contact hypersensitivity reaction to 2,4,6-trinitrochlorobenzene was elicited in mouse ears. Results: The cell density, intensity of I-A expression, and number of dendrites were decreased as the population density increased. Elicitation of contact hypersensitivity was suppressed in mice that received either population or immobilization stress. Increased I-A expression and number of dendrites were observed in adrenalectomized compared to sham-operated mice. The population-dependent suppression of contact hypersensitivity reaction was not observed in adrenalectomized mice. After incubation with serum from mice that received either immobilization stress or population stress, the expression of I-A molecules on a XS52 Langerhans' cell-like cell line was reduced. Conclusion: Stress affected the cutaneous immune system. There were indications that adrenergic hormones played a role in the regulation of the system.

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