Common coupling map advances GPCR-G protein selectivity
Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
Standard
Common coupling map advances GPCR-G protein selectivity. / Hauser, Alexander S.; Avet, Charlotte; Normand, Claire; Mancini, Arturo; Inoue, Asuka; Bouvier, Michel; Gloriam, David E.
I: eLife, Bind 11, e74107, 2022.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
Harvard
APA
Vancouver
Author
Bibtex
}
RIS
TY - JOUR
T1 - Common coupling map advances GPCR-G protein selectivity
AU - Hauser, Alexander S.
AU - Avet, Charlotte
AU - Normand, Claire
AU - Mancini, Arturo
AU - Inoue, Asuka
AU - Bouvier, Michel
AU - Gloriam, David E.
N1 - Publisher Copyright: © 2022, Hauser et al.
PY - 2022
Y1 - 2022
N2 - Two-thirds of human hormones and one-third of clinical drugs act on membrane receptors that couple to G proteins to achieve appropriate functional responses. While G protein transducers from literature are annotated in the Guide to Pharmacology database, two recent large-scale datasets now expand the receptor-G protein 'couplome'. However, these three datasets differ in scope and reported G protein couplings giving different coverage and conclusions on G protein-coupled receptor (GPCR)-G protein signaling. Here, we report a common coupling map uncovering novel couplings supported by both large-scale studies, the selectivity/promiscuity of GPCRs and G proteins, and how the co-coupling and co-expression of G proteins compare to the families from phylogenetic relationships. The coupling map and insights on GPCR-G protein selectivity will catalyze advances in receptor research and cellular signaling toward the exploitation of G protein signaling bias in design of safer drugs.
AB - Two-thirds of human hormones and one-third of clinical drugs act on membrane receptors that couple to G proteins to achieve appropriate functional responses. While G protein transducers from literature are annotated in the Guide to Pharmacology database, two recent large-scale datasets now expand the receptor-G protein 'couplome'. However, these three datasets differ in scope and reported G protein couplings giving different coverage and conclusions on G protein-coupled receptor (GPCR)-G protein signaling. Here, we report a common coupling map uncovering novel couplings supported by both large-scale studies, the selectivity/promiscuity of GPCRs and G proteins, and how the co-coupling and co-expression of G proteins compare to the families from phylogenetic relationships. The coupling map and insights on GPCR-G protein selectivity will catalyze advances in receptor research and cellular signaling toward the exploitation of G protein signaling bias in design of safer drugs.
KW - computational biology
KW - G protein
KW - GPCR
KW - human
KW - pharmacology
KW - signal transduction
KW - systems biology
U2 - 10.7554/eLife.74107
DO - 10.7554/eLife.74107
M3 - Journal article
C2 - 35302494
AN - SCOPUS:85128489166
VL - 11
JO - eLife
JF - eLife
SN - 2050-084X
M1 - e74107
ER -
ID: 304783674