Protein Information

Name G protein coupled receptor
Synonyms ASRT 2; ASRT2; G protein coupled receptor 154; G protein coupled receptor for asthma susceptibility; G protein coupled receptor; G protein coupled receptor PGR14; GPR154; GPRA…

Compound Information

Name cycloheximide
CAS

Reference List

PubMed Abstract RScore(About this table)
16644694 Koehler JA, Drucker DJ: Activation of glucagon-like peptide-1 receptor signaling does not modify the growth or apoptosis of human pancreatic cancer cells. Diabetes. 2006 May;55(5):1369-79.

Glucagon-like peptide (GLP)-1 promotes beta-cell proliferation and survival through stimulation of its specific G-protein-coupled receptor; however, the potential for GLP-1 receptor (GLP-1R) agonists to promote growth and proliferation of human pancreatic-derived cells remains poorly understood.
Ex-4 did not modulate the proliferation of these cell lines in vitro and did not inhibit apoptosis after exposure of cells to cytotoxic agents such as cycloheximide, indomethacin, LY294002, or cyclopamine.
1(0,0,0,1) Details
17425429 Huang Y, Huang X, Zhang J, Gui J, Zhang Q: Subcellular localization and characterization of G protein-coupled receptor homolog from lymphocystis disease virus isolated in China. Viral Immunol. 2007 Spring;20(1):150-9.

Quantitative analysis of apoptotic cells indicated that a considerable decrease in the apoptotic fraction of cells expressing GPCR, compared with the control cells, was detected after exposure to ActD and cycloheximide.
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16739117 Martin-Negrier ML, Charron G, Bloch B: Receptor recycling mediates plasma membrane recovery of dopamine D1 receptors in dendrites and axons after agonist-induced endocytosis in primary cultures of striatal neurons. Synapse. 2006 Sep 1;60(3):194-204.

The pharmacological stimulation of G-protein-coupled receptor induces receptor internalization.
Recovery was unaffected by cycloheximide (70 microM) but was prevented by monensin (100 microM) that inhibits endosomal acidification and receptor recycling.
1(0,0,0,1) Details
17253962 Sainz E, Cavenagh MM, Gutierrez J, Battey JF, Northup JK, Sullivan SL: Functional characterization of human bitter taste receptors. . Biochem J. 2007 May 1;403(3):537-43.

The T2Rs belong to a multi-gene family of G-protein-coupled receptors responsible for the detection of ingested bitter-tasting compounds.
We confirm that the mT2R5, hT2R43 and hT2R47 receptors respond selectively to micromolar concentrations of cycloheximide, aristolochic acid and denatonium respectively.
1(0,0,0,1) Details
17178924 Moreau ME, Bawolak MT, Morissette G, Adam A, Marceau F: Role of nuclear factor-kappaB and protein kinase C signaling in the expression of the kinin B1 receptor in human vascular smooth muscle cells. Mol Pharmacol. 2007 Mar;71(3):949-56. Epub 2006 Dec 18.

Kinin B1 receptor expression was characterized in human umbilical artery smooth muscle cells to further elucidate the function and specificity of three previously proposed pathways [nuclear factor-kappaB (NF-kappaB), protein kinase C, and agonist autoregulation] that regulate this inducible G protein-coupled receptor.
Various stimulatory compounds that increase receptor mRNA stability only (human and bovine sera, cycloheximide) or that stimulate NF-kappaB nuclear translocation and both mRNA concentration and stability [interleukin (IL)-1beta, phorbol 12-myristate 13-acetate (PMA)] all increased the density of binding sites for the tritiated B1 receptor agonist [3H] Lys-des-Arg9-bradykinin (without change in receptor affinity) in cell-based assays.
1(0,0,0,1) Details
19126785 Conti F, Sertic S, Reversi A, Chini B: Intracellular trafficking of the human oxytocin receptor: evidence of receptor recycling via a Rab4/Rab5 "short cycle". Am J Physiol Endocrinol Metab. 2009 Mar;296(3):E532-42. Epub 2009 Jan 6.

As in the case of most G protein-coupled receptors, agonist stimulation of human oxytocin receptors (OTRs) leads to desensitization and internalization; however, little is known about the subsequent intracellular OTR trafficking, which is crucial for reestablishing agonist responsiveness.
Similar results were also obtained in the presence of cycloheximide, thus indicating that receptor recycling and not de novo receptor synthesis was responsible for the resensitization.
1(0,0,0,1) Details
17400304 Hettinger TP, Formaker BK, Frank ME: Cycloheximide: no ordinary bitter stimulus. Behav Brain Res. 2007 Jun 4;180(1):4-17. Epub 2007 Feb 23.

Rats and mice avoid it at concentrations well below the thresholds for most bitter stimuli and T2R G-protein-coupled receptors specific for CyX with appropriate sensitivity are identified for those species.
1(0,0,0,1) Details
16728719 Sun YH, Gao X, Tang YJ, Xu CL, Wang LH: Androgens induce increases in intracellular calcium via a G protein-coupled receptor in LNCaP prostate cancer cells. J Androl. 2006 Sep-Oct;27(5):671-8. Epub 2006 May 25.

Neither an antagonist of intracellular androgen receptors (cyproterone acetate) nor a protein synthesis inhibitor (cycloheximide) affected this fast Ca2+ influx.
1(0,0,0,1) Details
17405813 Neel NF, Lapierre LA, Goldenring JR, Richmond A: RhoB plays an essential role in CXCR2 sorting decisions. J Cell Sci. 2007 May 1;120(Pt 9):1559-71. Epub 2007 Apr 3.


The CXCR2 chemokine receptor is a G-protein-coupled receptor that undergoes clathrin-mediated endocytosis upon ligand binding.
1(0,0,0,1) Details
16914085 Sanchez-Laorden BL, Sanchez-Mas J, Turpin MC, Garcia-Borron JC, Jimenez-Cervantes C: Variant amino acids in different domains of the human melanocortin 1 receptor impair cell surface expression. Cell Mol Biol (Noisy-le-grand). 2006 May 30;52(2):39-46.


The alpha melanocyte-stimulating hormone receptor (MC1R) is a heptahelical G protein-coupled receptor (GPCR) found in the plasma membrane of melanocytes.
1(0,0,0,1) Details
15619605 Gravel SP, Servant MJ: Roles of an IkappaB kinase-related pathway in human cytomegalovirus-infected vascular smooth muscle cells: a molecular link in pathogen-induced proatherosclerotic conditions. J Biol Chem. 2005 Mar 4;280(9):7477-86. Epub 2004 Dec 24.


Activation of the TBK1/IRF-3 pathway was independent of epidermal growth factor receptor and pertussis toxin-sensitive G protein-coupled receptor activation.
1(0,0,0,1) Details
18617631 Fernandez N, Monczor F, Baldi A, Davio C, Shayo C: Histamine H2 receptor trafficking: role of arrestin, dynamin, and clathrin in histamine H2 receptor internalization. Mol Pharmacol. 2008 Oct;74(4):1109-18. Epub 2008 Jul 10.

Agonist-induced internalization of G protein-coupled receptors (GPCRs) has been implicated in receptor desensitization, resensitization, and down-regulation.
Similar results were obtained in the presence of cycloheximide, an inhibitor of protein synthesis.
1(0,0,0,1) Details
15886333 Wu SV, Chen MC, Rozengurt E: Genomic organization, expression, and function of bitter taste receptors (T2R) in mouse and rat. Physiol Genomics. 2005 Jul 14;22(2):139-49. Epub 2005 May 10.

Mammalian type 2 taste receptors (T2R) are a family of G protein-coupled receptors that mediate bitter signals in taste cells.
The addition of DB, PTC, or cycloheximide to AR42J cells induced a rapid increase in the intracellular Ca (2+) concentration.
1(0,0,0,1) Details
16849335 Cottrell GS, Padilla B, Pikios S, Roosterman D, Steinhoff M, Gehringer D, Grady EF, Bunnett NW: Ubiquitin-dependent down-regulation of the neurokinin-1 receptor. . J Biol Chem. 2006 Sep 22;281(38):27773-83. Epub 2006 Jul 17.

Resensitization occurred after 16 h, and cycloheximide prevented resensitization, implicating new receptor synthesis.
Lysine ubiquitination of G-protein-coupled receptors is a signal for their trafficking and degradation.
1(0,0,0,1) Details