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Receptors coupling to G proteins: Is there a signal behind the sequence?
(Wiley-Blackwell, 2000-12-01)
Upon the binding of their ligands, G protein-coupled receptors couple to the heterotrimeric G proteins to transduce a signal. One receptor family may couple to a single G protein subtype and another family to several ones. ...
Expanding the horizons of G protein-coupled receptor structure-based ligand discovery and optimization using homology models
(Royal Society of Chemistry, 2015-07)
With >800 members in humans, the G protein-coupled receptor (GPCR) super-family is the target for more than 30% of the marketed drugs. The recent boom in GPCR crystallography has enabled the solution of ∼30 different GPCR ...
A low resolution model for the interaction of G proteins with G protein-coupled receptors
(Oxford Univ Press, 1999-12-01)
A model is presented for the interaction between G proteins and G protein-coupled receptors, the model is based on the fact that this interaction shows Little specificity and thus conserved parts of the G proteins have to ...
Expression of a G protein-coupled receptor (GPCR) leads to attenuation of signaling by other GPCRs: experimental evidence for a spontaneous GPCR constitutive inactive form
(American Society For Biochemistry And Molecular Biology, 2010-05-14)
The idea of G protein-coupled receptors (GPCRs) coupling to G protein solely in their active form was abolished when it was found that certain ligands induce a G protein-coupled but inactive receptor form. This receptor ...
Antineoplastic effect of 1α,25(OH)2D3 in spheroids from endothelial cells transformed by Kaposi’s sarcoma-associated herpesvirus G protein coupled receptor
(Elsevier Science, 2019-02)
The Kaposi´s sarcoma-associated herpesvirus G protein-coupled receptor (KSHV/vGPCR) is a key molecule in the pathogenesis of Kaposi´s sarcoma. In endothelial cells, tumor maintenance and NF-κB activation depends on vGPCR ...
Ligand and decoy sets for docking to G protein-coupled receptors
(American Chemical Society, 2012-01)
We compiled a G protein-coupled receptor (GPCR) ligand library (GLL) for 147 targets, selecting for each ligand 39 decoy molecules, collected in the GPCR Decoy Database (GDD). Decoys were chosen ensuring a ligand-decoy ...
Recent updates on GPCR biased agonism
(Elsevier B.V., 2016-10-01)
G protein-coupled receptors (GPCRs) are the most important targets for drug discovery and not surprisingly similar to 40% of all drugs currently in the market act on these receptors. Currently, one of the most active areas ...
KSHV G-protein coupled receptor vGPCR oncogenic signaling upregulation of Cyclooxygenase-2 expression mediates angiogenesis and tumorigenesis in Kaposi's sarcoma
(Public Library of Science, 2020-10)
Kaposi's sarcoma-associated herpesvirus (KSHV) vGPCR is a constitutively active G protein-coupled receptor that subverts proliferative and inflammatory signaling pathways to induce cell transformation in Kaposi's sarcoma. ...
GPCR mediated control of calcium dynamics: A systems perspective
G-protein coupled receptor (GPCR) mediated calcium (Ca2+)-signaling transduction remains
crucial in designing drugs for various complex diseases including neurodegeneration, chronic
heart failure as well as respiratory ...
Antiproliferative effects of Bortezomib in endothelial cells transformed by viral G protein-coupled receptor associated to Kaposi's sarcoma
(Elsevier Science Inc, 2017-04)
The Kaposi's Sarcoma-associated Herpes virus G Protein-Coupled Receptor (vGPCR) is a key molecule in the pathogenesis of Kaposi Sarcoma. We have previously demonstrated that the proteasome inhibitor Bortezomib inhibits ...