Journal Name:
Frontiers in Bioscience
Volume:
17
Issue:
1
Pages From:
232
To:
247
Date:
Sunday, January 1, 2012
Abstract:
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