Experts and Doctors on g protein coupled receptors in Philadelphia, Pennsylvania, United States


Locale: Philadelphia, Pennsylvania, United States
Topic: g protein coupled receptors

Top Publications

  1. Luo J, Benovic J. G protein-coupled receptor kinase interaction with Hsp90 mediates kinase maturation. J Biol Chem. 2003;278:50908-14 pubmed
    ..These studies demonstrate that GRK3, GRK5, and GRK6 are also stabilized by interaction with Hsp90. Taken together, our work revealed that GRK interaction with heat shock proteins plays an important role in regulating GRK maturation. ..
  2. Mennella J, Pepino M, Duke F, Reed D. Age modifies the genotype-phenotype relationship for the bitter receptor TAS2R38. BMC Genet. 2010;11:60 pubmed publisher
    ..These data imply that the change in PROP bitter sensitivity which occurs over the lifespan (from bitter sensitive to less so) is more common in people with a particular haplotype combination, i.e., AVI/PAV heterozygotes. ..
  3. Kapur A, Zhao P, Sharir H, Bai Y, Caron M, Barak L, et al. Atypical responsiveness of the orphan receptor GPR55 to cannabinoid ligands. J Biol Chem. 2009;284:29817-27 pubmed publisher
    ..The activation of GPR55 by rimonabant may be responsible for some of the off-target effects that led to its removal as a potential obesity therapy. ..
  4. Volgin D, Saghir M, Kubin L. Developmental changes in the orexin 2 receptor mRNA in hypoglossal motoneurons. Neuroreport. 2002;13:433-6 pubmed
    ..Thus, ORX may postsynaptically excite XII motoneurons, with the ORX2r mRNA production increased during the critical period for development of the rapid eye movement sleep and its disorder narcolepsy/cataplexy. ..
  5. Gompf H, Aston Jones G. Role of orexin input in the diurnal rhythm of locus coeruleus impulse activity. Brain Res. 2008;1224:43-52 pubmed publisher
    ..Therefore, we propose that DMH orexin neurons play a role in modulating the day-night differences of LC impulse activity. ..
  6. Zhang Y, Goss A, Cohen E, Kadzik R, Lepore J, Muthukumaraswamy K, et al. A Gata6-Wnt pathway required for epithelial stem cell development and airway regeneration. Nat Genet. 2008;40:862-70 pubmed publisher
    ..Together, these data demonstrate that Gata6-regulated Wnt signaling controls the balance between progenitor expansion and epithelial differentiation required for both lung development and regeneration. ..
  7. Mennella J, Pepino M, Reed D. Genetic and environmental determinants of bitter perception and sweet preferences. Pediatrics. 2005;115:e216-22 pubmed
    ..New knowledge about the molecular basis of food likes and dislikes in children, a generation that will struggle with obesity and diabetes, may suggest strategies to overcome diet-induced diseases. ..
  8. Li X, Inoue M, Reed D, Huque T, Puchalski R, Tordoff M, et al. High-resolution genetic mapping of the saccharin preference locus (Sac) and the putative sweet taste receptor (T1R1) gene (Gpr70) to mouse distal Chromosome 4. Mamm Genome. 2001;12:13-6 pubmed
    ..B6-Sac partially congenic mice originating from these two strains. The Gpr70 gene maps proximal to Sac, which demonstrates that they are different loci. ..
  9. Huang H, Klein P. The Frizzled family: receptors for multiple signal transduction pathways. Genome Biol. 2004;5:234 pubmed
    ..It is not yet clear how Frizzleds couple to downstream effectors, and this is a focus of intense study. ..

More Information


  1. Ahamed J, Ali H. Distinct roles of receptor phosphorylation, G protein usage, and mitogen-activated protein kinase activation on platelet activating factor-induced leukotriene C(4) generation and chemokine production. J Biol Chem. 2002;277:22685-91 pubmed
  2. Rives A, Rochlin K, Wehrli M, Schwartz S, Dinardo S. Endocytic trafficking of Wingless and its receptors, Arrow and DFrizzled-2, in the Drosophila wing. Dev Biol. 2006;293:268-83 pubmed
    ..Thus, signal modulation by endocytic routing will depend on the tissue to be patterned and the goals during that patterning event. ..
  3. Tan C, Deardorff M, Saint Jeannet J, Yang J, Arzoumanian A, Klein P. Kermit, a frizzled interacting protein, regulates frizzled 3 signaling in neural crest development. Development. 2001;128:3665-74 pubmed
    ..To the best of our knowledge, Kermit is the first protein identified that interacts directly with the cytoplasmic portion of frizzleds to modulate their signaling activity. ..
  4. Shankar H, Michal A, Kern R, Kang D, Gurevich V, Benovic J. Non-visual arrestins are constitutively associated with the centrosome and regulate centrosome function. J Biol Chem. 2010;285:8316-29 pubmed publisher
    ..Taken together, our data reveal that non-visual arrestins are novel centrosomal components and regulate normal centrosome function. ..
  5. Chen Q, Alarcon S, Tharp A, Ahmed O, Estrella N, Greene T, et al. Perceptual variation in umami taste and polymorphisms in TAS1R taste receptor genes. Am J Clin Nutr. 2009;90:770S-779S pubmed publisher
    ..The putative human taste receptor TAS1R1-TAS1R3 responds specifically to l-glutamate mixed with the ribonucleotide IMP. Thus, this receptor likely contributes to human umami taste perception. ..
  6. Lu B, Zhang Q, Wang H, Wang Y, Nakayama M, Ren D. Extracellular calcium controls background current and neuronal excitability via an UNC79-UNC80-NALCN cation channel complex. Neuron. 2010;68:488-99 pubmed publisher
    ..Therefore, extracellular Ca(2+) influences neuronal excitability through the UNC79-UNC80-NALCN complex in a G protein-dependent fashion. ..
  7. Jacobson S, Cideciyan A, Aleman T, Sumaroka A, Roman A, Gardner L, et al. Usher syndromes due to MYO7A, PCDH15, USH2A or GPR98 mutations share retinal disease mechanism. Hum Mol Genet. 2008;17:2405-15 pubmed publisher
    ..The results point to the photoreceptor cell as the therapeutic target for USH treatment trials, such as MYO7A somatic gene replacement therapy. ..
  8. Volgin D, Malinowska M, Kubin L. Dorsomedial pontine neurons with descending projections to the medullary reticular formation express orexin-1 and adrenergic alpha2A receptor mRNA. Neurosci Lett. 2009;459:115-8 pubmed publisher
    ..Our data suggest that ORX and adrenergic pathways converge on a subpopulation of cells of the pontine REM sleep-triggering region that have descending projections to the medullary region important for the motor control during REM sleep. ..
  9. Wallenfang M, Nayak R, Dinardo S. Dynamics of the male germline stem cell population during aging of Drosophila melanogaster. Aging Cell. 2006;5:297-304 pubmed
    ..Second, at any given time not all stem cells actively cycle, leading to 'clonal succession' from the reserve pool of initially quiescent stem cells. We find that neither of these mechanisms is used in Drosophila male GSCs. ..
  10. Paaby A, Schmidt P. Functional significance of allelic variation at methuselah, an aging gene in Drosophila. PLoS ONE. 2008;3:e1987 pubmed publisher
  11. Koh K, Zheng X, Sehgal A. JETLAG resets the Drosophila circadian clock by promoting light-induced degradation of TIMELESS. Science. 2006;312:1809-12 pubmed
    ..Our results suggest that JET is essential for resetting the clock by transmitting light signals from CRY to TIM. ..
  12. Li X, Li W, Wang H, Bayley D, Cao J, Reed D, et al. Cats lack a sweet taste receptor. J Nutr. 2006;136:1932S-1934S pubmed publisher
  13. Lin C, Ahmad M, Cashmore A. Arabidopsis cryptochrome 1 is a soluble protein mediating blue light-dependent regulation of plant growth and development. Plant J. 1996;10:893-902 pubmed
    ..It is concluded that CRY1 is a photoreceptor mediating blue light-dependent regulation of gene expression in addition to its affect on plant growth. ..
  14. Jarillo J, Capel J, Tang R, Yang H, Alonso J, Ecker J, et al. An Arabidopsis circadian clock component interacts with both CRY1 and phyB. Nature. 2001;410:487-90 pubmed
    ..Both yeast two-hybrid and in vitro binding studies show that there is a physical interaction between ADO1 and the photoreceptors CRY1 and phyB. We propose that ADO1 is an important component of the Arabidopsis circadian system. ..
  15. Zhou N, Fan X, Mukhtar M, Fang J, Patel C, DuBois G, et al. Cell-cell fusion and internalization of the CNS-based, HIV-1 co-receptor, APJ. Virology. 2003;307:22-36 pubmed
    ..The CNS represents a unique reservoir site for HIV-1. As such, molecular therapeutics and small molecular inhibitors of HIV-1 entry via this unique CNS receptor are now able to be rationally designed. ..
  16. Huque T, Cowart B, Dankulich Nagrudny L, Pribitkin E, Bayley D, Spielman A, et al. Sour ageusia in two individuals implicates ion channels of the ASIC and PKD families in human sour taste perception at the anterior tongue. PLoS ONE. 2009;4:e7347 pubmed publisher
    ..This is the first report of sour ageusia in humans, and the very existence of such individuals ("natural knockouts") suggests a cell lineage for sour that is independent of the other taste modalities. ..
  17. Brailoiu G, Dun S, Brailoiu E, Inan S, Yang J, Chang J, et al. Nesfatin-1: distribution and interaction with a G protein-coupled receptor in the rat brain. Endocrinology. 2007;148:5088-94 pubmed
  18. Reddy S, Andl T, Lu M, Morrisey E, Millar S. Expression of Frizzled genes in developing and postnatal hair follicles. J Invest Dermatol. 2004;123:275-82 pubmed
  19. Ariazi E, Brailoiu E, Yerrum S, Shupp H, Slifker M, Cunliffe H, et al. The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells. Cancer Res. 2010;70:1184-94 pubmed publisher
    ..Further, flow cytometry showed that G-1 blocked MCF-7 cell cycle progression at the G(1) phase. Thus, GPR30 antagonizes growth of ERalpha-positive breast cancer and may represent a new target to combat this disease. ..
  20. Brinks H, Eckhart A. Regulation of GPCR signaling in hypertension. Biochim Biophys Acta. 2010;1802:1268-75 pubmed publisher
    ..Therefore, therapeutic approaches using the inhibition of GRKs to regulate GPCRs are intriguing novel targets for treatment of hypertension and heart failure. ..
  21. McGarvey T, Maruta Y, Tomaszewski J, Linnenbach A, Malkowicz S. PTCH gene mutations in invasive transitional cell carcinoma of the bladder. Oncogene. 1998;17:1167-72 pubmed
  22. Schwartz S, Aleman T, Cideciyan A, Windsor E, Sumaroka A, Roman A, et al. Disease expression in Usher syndrome caused by VLGR1 gene mutation (USH2C) and comparison with USH2A phenotype. Invest Ophthalmol Vis Sci. 2005;46:734-43 pubmed
    ..Intrafamilial and interfamilial variation in retinal severity in USH2A, however, suggests that genetic or nongenetic modifiers may be involved in the disease expression. ..
  23. O Donnell L, Agrawal A, Sabnekar P, Dichter M, Lynch D, Kolson D. Apelin, an endogenous neuronal peptide, protects hippocampal neurons against excitotoxic injury. J Neurochem. 2007;102:1905-1917 pubmed publisher
    ..Thus, apelin/APJ signaling likely represents an endogenous hippocampal neuronal survival response, and therefore apelin should be further investigated as a potential neuroprotectant against hippocampal injury. ..
  24. Deardorff M, Klein P. Xenopus frizzled-2 is expressed highly in the developing eye, otic vesicle and somites. Mech Dev. 1999;87:229-33 pubmed
    ..It is expressed in the developing embryo from late gastrula stages onward. Xfz2 has a wide domain of expression but is concentrated in the eye anlage, otic vesicle, and developing somites. ..
  25. Chen H, Tliba O, Van Besien C, Panettieri R, Amrani Y. TNF-[alpha] modulates murine tracheal rings responsiveness to G-protein-coupled receptor agonists and KCl. J Appl Physiol (1985). 2003;95:864-72; discussion 863 pubmed
    ..Taken together, these data suggest that TNF-alpha may participate in the development of airway hyperresponsiveness in asthma via the modulation of ASM responsiveness to both contractile and beta-adrenoceptor GPCR agonists. ..
  26. Ahmad M, Cashmore A. The blue-light receptor cryptochrome 1 shows functional dependence on phytochrome A or phytochrome B in Arabidopsis thaliana. Plant J. 1997;11:421-7 pubmed
    ..It was concluded that CRY1-mediated inhibition of hypocotyl elongation and anthocyanin production requires active phytochrome for full expression, and that this requirement can be supplied by low levels of either phyA or phyB. ..
  27. Li X, Glaser D, Li W, Johnson W, O Brien S, Beauchamp G, et al. Analyses of sweet receptor gene (Tas1r2) and preference for sweet stimuli in species of Carnivora. J Hered. 2009;100 Suppl 1:S90-100 pubmed publisher
    ..The observation that the lesser panda highly preferred aspartame could be an example of evolutionary convergence in the identification of sweet stimuli...
  28. Tordoff M, Shao H, Alarcon L, Margolskee R, Mosinger B, Bachmanov A, et al. Involvement of T1R3 in calcium-magnesium taste. Physiol Genomics. 2008;34:338-48 pubmed publisher
    ..Our results imply that, in addition to its established roles in the detection of sweet and umami compounds, T1R3 functions as a gustatory calcium-magnesium receptor. ..
  29. Li J, Haines D, Liu Chen L. Agonist-promoted Lys63-linked polyubiquitination of the human kappa-opioid receptor is involved in receptor down-regulation. Mol Pharmacol. 2008;73:1319-30 pubmed publisher
    ..These results indicate that ubiquitinated hKOR after agonist treatment contains predominantly Lys63-linked polyubiquitin chains and ubiquitination of the hKOR involved in agonist-induced down-regulation. ..
  30. Galindo Cuspinera V, Breslin P. The liaison of sweet and savory. Chem Senses. 2006;31:221-5 pubmed
  31. Galindo Cuspinera V, Breslin P. Taste after-images: the science of "water-tastes". Cell Mol Life Sci. 2007;64:2049-52 pubmed
  32. Reed D, Li S, Li X, Huang L, Tordoff M, Starling Roney R, et al. Polymorphisms in the taste receptor gene (Tas1r3) region are associated with saccharin preference in 30 mouse strains. J Neurosci. 2004;24:938-46 pubmed
    ..Here, we present data for future studies directed to experimentally confirm the function of these polymorphisms and highlight some of the difficulties of identifying specific DNA sequence variants that underlie quantitative trait loci. ..
  33. Hoffman T, Stephens E, Narayan O, Doms R. HIV type I envelope determinants for use of the CCR2b, CCR3, STRL33, and APJ coreceptors. Proc Natl Acad Sci U S A. 1998;95:11360-5 pubmed
  34. Karasawa A, Rochester J, Lefer A. Beneficial actions of BN 50739, a new PAF receptor antagonist, in murine traumatic shock. Methods Find Exp Clin Pharmacol. 1990;12:231-7 pubmed
    ..The beneficial effects of PAF antagonism on traumatic shock are significant in the present study, and are consistent with the concept that PAF is involved in the pathogenesis of traumatic shock. ..
  35. Janson K, Cohen E, Wilder E. Expression of DWnt6, DWnt10, and DFz4 during Drosophila development. Mech Dev. 2001;103:117-20 pubmed
    ..We find that DFz4 is also expressed in a dynamic pattern in the mesoderm, gut, and central nervous system. ..
  36. Kishore R, Sundaram M. ced-10 Rac and mig-2 function redundantly and act with unc-73 trio to control the orientation of vulval cell divisions and migrations in Caenorhabditis elegans. Dev Biol. 2002;241:339-48 pubmed
    ..We discuss the similarities and differences between the cellular defects seen in Rac mutants and let-60 Ras or lin-17 Frizzled mutants. ..
  37. Chinchilla P, Xiao L, Kazanietz M, Riobo N. Hedgehog proteins activate pro-angiogenic responses in endothelial cells through non-canonical signaling pathways. Cell Cycle. 2010;9:570-79 pubmed
    ..of novel non-canonical responses elicited by Hh proteins in endothelial cells highlights the complexity of the Hh signaling pathway and reveals striking differences in ligand strength for transcriptional and non-transcriptional responses ..
  38. Ahmad M, Jarillo J, Smirnova O, Cashmore A. The CRY1 blue light photoreceptor of Arabidopsis interacts with phytochrome A in vitro. Mol Cell. 1998;1:939-48 pubmed
    ..In vivo labeling studies and specific mutant alleles of CRY1, which interfere with the function of phytochrome, suggest the possible relevance of these findings in vivo. ..
  39. Dun S, Brailoiu G, Gao X, Brailoiu E, Arterburn J, Prossnitz E, et al. Expression of estrogen receptor GPR30 in the rat spinal cord and in autonomic and sensory ganglia. J Neurosci Res. 2009;87:1610-9 pubmed publisher
  40. Cashmore A, Jarillo J, Wu Y, Liu D. Cryptochromes: blue light receptors for plants and animals. Science. 1999;284:760-5 pubmed
    ..This process of repeated evolution may have coincided with the origin in animals of a modified circadian clock based on the PERIOD, TIMELESS, CLOCK, and CYCLE proteins. ..
  41. Lin F, Song W, Meyer Bernstein E, Naidoo N, Sehgal A. Photic signaling by cryptochrome in the Drosophila circadian system. Mol Cell Biol. 2001;21:7287-94 pubmed
    ..High levels of CRY block TIM ubiquitination, suggesting a mechanism by which light-driven changes in CRY could control TIM ubiquitination. ..
  42. Windh R, Lee M, Hla T, An S, Barr A, Manning D. Differential coupling of the sphingosine 1-phosphate receptors Edg-1, Edg-3, and H218/Edg-5 to the G(i), G(q), and G(12) families of heterotrimeric G proteins. J Biol Chem. 1999;274:27351-8 pubmed
    ..These studies represent the first characterization of S1P receptor activity through G proteins directly and establish fundamental differences in coupling. ..
  43. Song W, Ranjan R, Dawson Scully K, Bronk P, Marin L, Seroude L, et al. Presynaptic regulation of neurotransmission in Drosophila by the g protein-coupled receptor methuselah. Neuron. 2002;36:105-19 pubmed
    ..Conditional expression of Mth restored normal release and normal vesicle docking and clustering but not the reduced size of synaptic sites, suggesting that Mth acutely adjusts vesicle trafficking to synaptic sites. ..
  44. Ahmad M, Jarillo J, Smirnova O, Cashmore A. Cryptochrome blue-light photoreceptors of Arabidopsis implicated in phototropism. Nature. 1998;392:720-3 pubmed
    ..Transgenic Arabidopsis plants overexpressing CRY1 or CRY2 show enhanced phototropic curvature. We conclude that cryptochrome is one of the photoreceptors mediating phototropism in plants. ..
  45. Radhika V, Proikas Cezanne T, Jayaraman M, Onesime D, Ha J, Dhanasekaran D. Chemical sensing of DNT by engineered olfactory yeast strain. Nat Chem Biol. 2007;3:325-30 pubmed
    ..With this approach, we have identified the novel rat olfactory receptor Olfr226, which is closely related to the mouse olfactory receptors Olfr2 and MOR226-1, as a 2,4-dinitrotoluene-responsive receptor. ..
  46. Lu J, Fenik V, Branconi J, Mann G, Rukhadze I, Kubin L. Disinhibition of perifornical hypothalamic neurones activates noradrenergic neurones and blocks pontine carbachol-induced REM sleep-like episodes in rats. J Physiol. 2007;582:553-67 pubmed
    ..A malfunction of the pathway that originates in GABA(A) receptor-expressing PF neurones may cause narcolepsy/cataplexy...
  47. Wang Z, Shu W, Lu M, Morrisey E. Wnt7b activates canonical signaling in epithelial and vascular smooth muscle cells through interactions with Fzd1, Fzd10, and LRP5. Mol Cell Biol. 2005;25:5022-30 pubmed
    ..Together, these data demonstrate that Wnt7b signals through Fzd1 and -10 and LRP5 and implicate these Wnt coreceptors in the regulation of lung airway and vascular development. ..
  48. Wang H, Ren D. UNC80 functions as a scaffold for Src kinases in NALCN channel function. Channels (Austin). 2009;3:161-3 pubmed
    ..This finding is consistent with the known requirement for Src kinases in the activation of NALCN, and may lead to new insights into the molecular mechanisms underlying G-protein-independent activation of the channel. ..
  49. DeGeorge B, Gao E, Boucher M, Vinge L, Martini J, Raake P, et al. Targeted inhibition of cardiomyocyte Gi signaling enhances susceptibility to apoptotic cell death in response to ischemic stress. Circulation. 2008;117:1378-87 pubmed publisher
    ..Our results with GiCT indicate that upregulation of G alpha(i2) is an adaptive protective response after ischemia to shield myocytes from apoptosis. ..
  50. Yang H, Tang R, Cashmore A. The signaling mechanism of Arabidopsis CRY1 involves direct interaction with COP1. Plant Cell. 2001;13:2573-87 pubmed
    ..These findings give new insight into the initial step in light signaling in Arabidopsis, providing a molecular link between the blue light receptor, CRY1, and COP1, a negative regulator of photomorphogenesis. ..
  51. Zhao P, Sharir H, Kapur A, Cowan A, Geller E, Adler M, et al. Targeting of the orphan receptor GPR35 by pamoic acid: a potent activator of extracellular signal-regulated kinase and ?-arrestin2 with antinociceptive activity. Mol Pharmacol. 2010;78:560-8 pubmed publisher
    ..Our results indicate that the unexpected biological functions of pamoic acid may yield potential new uses for a common drug constituent...
  52. Hawkins B, Solt L, Chowdhury I, Kazi A, Abid M, Aird W, et al. G protein-coupled receptor Ca2+-linked mitochondrial reactive oxygen species are essential for endothelial/leukocyte adherence. Mol Cell Biol. 2007;27:7582-93 pubmed
    ..These results demonstrate that mROS is the downstream effector molecule that translates receptor-mediated Ca(2+) signals into proinflammatory signaling and leukocyte/EC firm adhesion. ..
  53. Atluri P, Morine K, Liao G, Panlilio C, Berry M, Hsu V, et al. Ischemic heart failure enhances endogenous myocardial apelin and APJ receptor expression. Cell Mol Biol Lett. 2007;12:127-38 pubmed
    ..008). Infusion of apelin-13 significantly enhanced myocardial function in sham and failing hearts. We conclude that total myocardial apelin and APJ receptor levels increase in compensation for ischemic cardiomyopathy. ..