Structural dynamics bridge the gap between the genetic and functional levels of GPCRs
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Structural dynamics bridge the gap between the genetic and functional levels of GPCRs. / Torrens-Fontanals, Mariona; Stepniewski, Tomasz M.; Gloriam, David E.; Selent, Jana.
In: Current Opinion in Structural Biology, Vol. 69, 2021, p. 150-159.Research output: Contribution to journal › Review › Research › peer-review
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TY - JOUR
T1 - Structural dynamics bridge the gap between the genetic and functional levels of GPCRs
AU - Torrens-Fontanals, Mariona
AU - Stepniewski, Tomasz M.
AU - Gloriam, David E.
AU - Selent, Jana
N1 - Publisher Copyright: © 2021 Elsevier Ltd
PY - 2021
Y1 - 2021
N2 - G protein–coupled receptors (GPCRs) are implicated in nearly all physiological processes in the human body and represent an important drug targeting class. The genes encoding the different GPCR (sub)types determine their specific functionality, which can be altered by natural genetic variants and isoforms. Deciphering the molecular link between sequence diversity and its functional consequences is a current challenge and critical for the comprehension of the physiological response of GPCRs. It requires a global understanding of how protein sequence translates into protein structure, how this impacts the structural motions of the protein, and, finally, how all these factors determine the receptor functionality. Here, we discuss available resources and state-of-the-art computational approaches to address this question.
AB - G protein–coupled receptors (GPCRs) are implicated in nearly all physiological processes in the human body and represent an important drug targeting class. The genes encoding the different GPCR (sub)types determine their specific functionality, which can be altered by natural genetic variants and isoforms. Deciphering the molecular link between sequence diversity and its functional consequences is a current challenge and critical for the comprehension of the physiological response of GPCRs. It requires a global understanding of how protein sequence translates into protein structure, how this impacts the structural motions of the protein, and, finally, how all these factors determine the receptor functionality. Here, we discuss available resources and state-of-the-art computational approaches to address this question.
KW - Computational biology
KW - GPCRs
KW - Receptor signaling
KW - Structural dynamics
KW - Web resources
U2 - 10.1016/j.sbi.2021.04.005
DO - 10.1016/j.sbi.2021.04.005
M3 - Review
C2 - 34052782
AN - SCOPUS:85106901736
VL - 69
SP - 150
EP - 159
JO - Current Opinion in Structural Biology
JF - Current Opinion in Structural Biology
SN - 0959-440X
ER -
ID: 273636286