TY - JOUR
T1 - In silico modeling techniques for predicting the tertiary structure of human H4 receptor
AU - Zaid, Hilal
AU - Raiyn, Jamal
AU - Osman, Midhat
AU - Falah, Mizied
AU - Srouji, Samer
AU - Rayan, Anwar
PY - 2016/1/1
Y1 - 2016/1/1
N2 - 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.
AB - 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.
KW - 3D-structure prediction
KW - Drug Discovery
KW - G-protein coupled receptors (GPCRs)
KW - H4R - H4 receptor
KW - Homology modeling
KW - Review
UR - http://www.scopus.com/inward/record.url?scp=85016104757&partnerID=8YFLogxK
U2 - 10.2741/4409
DO - 10.2741/4409
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C2 - 26709794
AN - SCOPUS:85016104757
SN - 2768-6701
VL - 21
SP - 597
EP - 619
JO - Frontiers in Bioscience - Landmark
JF - Frontiers in Bioscience - Landmark
IS - 3
ER -