IMR Press / FBL / Volume 17 / Issue 1 / DOI: 10.2741/3924

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 as a courtesy and upon agreement with Frontiers in Bioscience.

Open Access Review
Computerized modeling techniques predict the 3D structure of H₄R: facts and fiction
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1 Drug Discovery Informatics Lab, QRC-Qasemi Research Center,Al-Qasemi Academic College, P.O.B. 124, Baka El-Garbiah 30100, Israel
2 Center for Bioinformatics, Saarland University, D-66041 Saarbrücken, Germany
3 Faculty of Arts and Sciences, Arab American University Jenin, P.O. Box 240, Jenin, Palestine
Academic Editor:Ekaterini Tiligada
Front. Biosci. (Landmark Ed) 2012, 17(1), 232–247;
Published: 1 January 2012
(This article belongs to the Special Issue Histamine revisited: the H4 receptor in health and disease)

The functional characterization of proteins presents a daily challenge for biochemical, medical and computational sciences, especially when the structures are undetermined empirically, as in the case of the Histamine H4 Receptor (H₄R). H₄R is a member of the GPCR superfamily that plays a vital role in immune and inflammatory responses. To date, the concept of GPCRs modeling is highlighted in textbooks and pharmaceutical pamphlets, and this group of proteins has been the subject of almost 3500 publications in the scientific literature. The dynamic nature of determining the GPCRs structure was elucidated through elegant and creative modeling methodologies, implemented by many groups around the world. H₄R which belongs to the GPCR family was cloned in 2000; understandably, its biological activity was reported only 65 times in pubmed. Here we attempt to cover the fundamental concepts of H₄R structure modeling and its implementation in drug discovery, especially those that have been experimentally tested and to highlight some ideas that are currently being discussed on the dynamic nature of H₄R and GPCRs computerized techniques for 3D structure modeling.

H4R - H4 receptor
homology modeling
3Dstructure prediction
G-protein coupled receptors (GPCRs)
Drug Discovery
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