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Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on imrpress.com as a courtesy and upon agreement with Frontiers in Bioscience.
In silico modeling techniques for predicting the tertiary structure of human H4 receptor
1 Drug Discovery Informatics Lab, QRC - Qasemi Research Center, Al-Qasemi Academic College, Baka EL-Garbiah 30100, Israel
2 Computer Science Department, Al-Qasemi Academic College, Baka EL-Garbiah 30100, Israel
3 Bone Regeneration Lab, Oral and Maxillofacial Surgery Department, Galilee Medical Center, Nahariya 22100, Israel
4 Science Education Department, Al-Qasemi Academic College, Baka EL-Garbiah 30100, Israel
Abstract
First cloned in 2000, the human Histamine H4 Receptor (hH4R) is the last member of the histamine receptors family discovered so far, it belongs to the GPCR super-family and is involved in a wide variety of immunological and inflammatory responses. Potential hH4R antagonists are proposed to have therapeutic potential for the treatment of allergies, inflammation, asthma and colitis. So far, no hH4R ligands have been successfully introduced to the pharmaceutical market, which creates a strong demand for new selective ligands to be developed. In silico techniques and structural based modeling are likely to facilitate the achievement of this goal. In this review paper we attempt to cover the fundamental concepts of hH4R structure modeling and its implementations in drug discovery and development, especially those that have been experimentally tested and to highlight some ideas that are currently being discussed on the dynamic nature of hH4R and GPCRs, in regards to computerized techniques for 3-D structure modeling.
Keywords
- H4R-H4 receptor
- homology modeling
- 3D-structure prediction
- G-protein coupled receptors (GPCRs)
- Drug Discovery
- Review
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