Dysregulated GPCR Signaling and Therapeutic Options in Uveal Melanoma. [PDF]
Uveal melanoma is the most common primary intraocular malignant tumor in adults and arises from the transformation of melanocytes in the uveal tract. Even after treatment of the primary tumor, up to 50% of patients succumb to metastatic disease.
Aplin, Andrew E. +5 more
core +1 more source
Computational Modeling for the Activation Cycle of G-proteins by G-protein-coupled Receptors
In this paper, we survey five different computational modeling methods. For comparison, we use the activation cycle of G-proteins that regulate cellular signaling events downstream of G-protein-coupled receptors (GPCRs) as a driving example.
Adriana Compagnoni +33 more
core +2 more sources
The GAPs, GEFs, and GDIs of heterotrimeric G-protein alpha subunits
The heterotrimeric G-protein alpha subunit has long been considered a bimodal, GTP-hydrolyzing switch controlling the duration of signal transduction by seven-transmembrane domain (7TM) cell-surface receptors.
doaj
Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor. [PDF]
The intrinsic efficacy of orthosteric ligands acting at G-protein-coupled receptors (GPCRs) reflects their ability to stabilize active receptor states (R*) and is a major determinant of their physiological effects.
Livingston, Kathryn E +4 more
core
D₂ Dopamine Receptors Colocalize Regulator of G-Protein Signaling 9-2 (RGS9-2) via the RGS9 DEP Domain, and RGS9 Knock-Out Mice Develop Dyskinesias Associated with Dopamine Pathways [PDF]
Regulator of G-protein signaling 9-2 (RGS9-2), a member of the RGS family of Gα GTPase accelerating proteins, is expressed specifically in the striatum, which participates in antipsychotic-induced tardive dyskinesia and in levodopa-induced dyskinesia. We
Axelrod, Jeffrey D. +10 more
core
Simulation of spontaneous G protein activation reveals a new intermediate driving GDP unbinding [PDF]
Activation of heterotrimeric G proteins is a key step in many signaling cascades. However, a complete mechanism for this process, which requires allosteric communication between binding sites that are ~30 Å apart, remains elusive.
Blumer, Kendall J +3 more
core +1 more source
Enhanced expression of heterotrimeric GTP-binding protein subunits in Zajdela ascitic hepatoma.
G protein beta subunit (Gbeta2) is over-expressed in Zajdela ascitic hepatoma (ZAH), a rat ascitic tumour, at mRNA as well as protein levels. Nuclear run-off transcription analysis suggests that the expression of Gbeta2 in ZAH is regulated mainly at transcriptional as well as post-transcriptional levels. Galphai3 is also over-expressed in ZAH.
S K, Sharma, M R, Das
openaire +1 more source
Gz, a guanine nucleotide-binding protein with unique biochemical properties [PDF]
Cloning of a complementary DNA (cDNA) for Gz alpha, a newly appreciated member of the family of guanine nucleotide-binding regulatory proteins (G proteins), has allowed preparation of specific antisera to identify the protein in tissues and to assay it ...
Casey, Patrick J. +3 more
core
The beta subunit of the signal recognition particle receptor is a transmembrane GTPase that anchors the alpha subunit, a peripheral membrane GTPase, to the endoplasmic reticulum membrane. [PDF]
The signal recognition particle receptor (SR) is required for the cotranslational targeting of both secretory and membrane proteins to the endoplasmic reticulum (ER) membrane.
Lauffer, L +3 more
core
Random Mutagenesis of G protein ɑ Subunit G_oɑ. Mutations altering nucleotide binding [PDF]
Nucleotide binding properties of the G protein ɑ subunit G_oɑ were probed by mutational analysis in recombinant Escherichia coli. Thousands of random mutations generated by polymerase chain reaction were screened by in situ [^(35)S]GTPyS (guanosine 5'-(3-
Aragay, Anna M. +5 more
core

