Lee Yuan Liu-Chen

Summary

Affiliation: Temple University
Country: USA

Publications

  1. ncbi request reprint Agonist-induced regulation and trafficking of kappa opioid receptors
    Lee Yuan Liu-Chen
    Department of Pharmacology and Center for Substance Abuse Research, Temple University, School of Medicine, Philadelphia, PA 19140, USA
    Life Sci 75:511-36. 2004
  2. ncbi request reprint Detecting the mu opioid receptor in brain following SDS-PAGE with multiple approaches
    Peng Huang
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, PA 19140, USA
    Front Biosci (Elite Ed) 1:220-7. 2009
  3. ncbi request reprint GEC1 interacts with the kappa opioid receptor and enhances expression of the receptor
    Chongguang Chen
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    J Biol Chem 281:7983-93. 2006
  4. ncbi request reprint Localization of the kappa opioid receptor in lipid rafts
    Wei Xu
    Department of Pharmacology, Center for Substance Abuse Research, Temple University School of Medicine, 3420 N Broad St, Philadelphia, PA 19140, USA
    J Pharmacol Exp Ther 317:1295-306. 2006
  5. ncbi request reprint Molecular basis of differences in (-)(trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidiny)-cyclohexyl]benzeneacetamide-induced desensitization and phosphorylation between human and rat kappa-opioid receptors expressed in Chinese hamster ovary cells
    Jin Li
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    Mol Pharmacol 61:73-84. 2002
  6. ncbi request reprint Ezrin-radixin-moesin-binding phosphoprotein-50/Na+/H+ exchanger regulatory factor (EBP50/NHERF) blocks U50,488H-induced down-regulation of the human kappa opioid receptor by enhancing its recycling rate
    Jian Guo Li
    Department of Pharmacology, Center for Substance Abuse Research, Temple University School of Medicine, 3420 N Broad Street, Philadelphia, PA 19140, USA
    J Biol Chem 277:27545-52. 2002
  7. ncbi request reprint N-Glycosylation of the human kappa opioid receptor enhances its stability but slows its trafficking along the biosynthesis pathway
    Jian Guo Li
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    Biochemistry 46:10960-70. 2007
  8. pmc Agonist treatment did not affect association of mu opioid receptors with lipid rafts and cholesterol reduction had opposite effects on the receptor-mediated signaling in rat brain and CHO cells
    Peng Huang
    Department of Pharmacology, Temple University School of Medicine, Philadelphia, PA 19140, USA
    Brain Res 1184:46-56. 2007
  9. ncbi request reprint Comparison of pharmacological activities of three distinct kappa ligands (Salvinorin A, TRK-820 and 3FLB) on kappa opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo
    Yulin Wang
    Department of Pharmacology, Temple University School of Medicine, 3420 North Broad Street, Philadelphia, PA 19140, USA
    J Pharmacol Exp Ther 312:220-30. 2005
  10. pmc Cholesterol reduction by methyl-beta-cyclodextrin attenuates the delta opioid receptor-mediated signaling in neuronal cells but enhances it in non-neuronal cells
    Peng Huang
    Department of Pharmacology, Center for Substance Abuse Research, Temple University School of Medicine, 3420 N Broad Street, Philadelphia, PA 19140, United States
    Biochem Pharmacol 73:534-49. 2007

Research Grants

  1. MOLECULAR CHARACTERIZATION OF OPIOID RECEPTORS
    Lee Yuan Liu Chen; Fiscal Year: 2004
  2. Cellular Pharmacology of Kappa Opioid Receptor
    Lee Yuan Liu Chen; Fiscal Year: 2007
  3. Cellular Pharmacology of Kappa Opiod Receptor
    Lee Yuan Liu Chen; Fiscal Year: 2009
  4. REGULATION OF KAPPA OPIOID RECEPTORS
    Lee Yuan Liu Chen; Fiscal Year: 2002
  5. MOLECULAR CHARACTERIZATION OF THE MU OPIOID RECEPTOR
    Lee Yuan Liu Chen; Fiscal Year: 1999
  6. MOLECULAR CHARACTERIZATION OF MU OPIOID RECEPTORS
    Lee Yuan Liu Chen; Fiscal Year: 1993
  7. Cellular Pharmacology of Kappa Opiod Receptor
    Lee Yuan Liu Chen; Fiscal Year: 2010

Collaborators

Detail Information

Publications52

  1. ncbi request reprint Agonist-induced regulation and trafficking of kappa opioid receptors
    Lee Yuan Liu-Chen
    Department of Pharmacology and Center for Substance Abuse Research, Temple University, School of Medicine, Philadelphia, PA 19140, USA
    Life Sci 75:511-36. 2004
    ....
  2. ncbi request reprint Detecting the mu opioid receptor in brain following SDS-PAGE with multiple approaches
    Peng Huang
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, PA 19140, USA
    Front Biosci (Elite Ed) 1:220-7. 2009
    ..The distinct relative molecular masses (Mr's) and band patterns are largely due to variations in the extent of N-glycosylation in different cell lines, brain regions and species...
  3. ncbi request reprint GEC1 interacts with the kappa opioid receptor and enhances expression of the receptor
    Chongguang Chen
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    J Biol Chem 281:7983-93. 2006
    ..This is the first report on biological functions of GEC1 and the first demonstration that a GPCR interacts with a protein of the MAP family. The interaction is important for trafficking of the receptor in the biosynthesis pathway...
  4. ncbi request reprint Localization of the kappa opioid receptor in lipid rafts
    Wei Xu
    Department of Pharmacology, Center for Substance Abuse Research, Temple University School of Medicine, 3420 N Broad St, Philadelphia, PA 19140, USA
    J Pharmacol Exp Ther 317:1295-306. 2006
    ..Caveolin-1 also immunoprecipitated with FLAG-hKOR, but MCD treatment had no effect on the association. Thus, the KOR is located in lipid rafts and its localization in the microdomains greatly affects coupling to G proteins...
  5. ncbi request reprint Molecular basis of differences in (-)(trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidiny)-cyclohexyl]benzeneacetamide-induced desensitization and phosphorylation between human and rat kappa-opioid receptors expressed in Chinese hamster ovary cells
    Jin Li
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    Mol Pharmacol 61:73-84. 2002
    ..In addition, the C-terminal domain plays a crucial role in these differences and the 358 locus contributes to the differences. Our findings suggest caution in extrapolating studies on kappa-opioid receptor regulation from rats to humans...
  6. ncbi request reprint Ezrin-radixin-moesin-binding phosphoprotein-50/Na+/H+ exchanger regulatory factor (EBP50/NHERF) blocks U50,488H-induced down-regulation of the human kappa opioid receptor by enhancing its recycling rate
    Jian Guo Li
    Department of Pharmacology, Center for Substance Abuse Research, Temple University School of Medicine, 3420 N Broad Street, Philadelphia, PA 19140, USA
    J Biol Chem 277:27545-52. 2002
    ..EBP50/NHERF may have a broader binding specificity and may interact with a subset of G protein-coupled receptors to serve as a recycling signal for these receptors...
  7. ncbi request reprint N-Glycosylation of the human kappa opioid receptor enhances its stability but slows its trafficking along the biosynthesis pathway
    Jian Guo Li
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    Biochemistry 46:10960-70. 2007
    ..Thus, N-glycosylation of the hKOR plays important roles in stability and trafficking along the biosynthesis pathway of the receptor protein as well as agonist-induced receptor regulation...
  8. pmc Agonist treatment did not affect association of mu opioid receptors with lipid rafts and cholesterol reduction had opposite effects on the receptor-mediated signaling in rat brain and CHO cells
    Peng Huang
    Department of Pharmacology, Temple University School of Medicine, Philadelphia, PA 19140, USA
    Brain Res 1184:46-56. 2007
    ..However, MCD treatment had opposite impacts on MOR signaling in the two tissues: it attenuated MOR-mediated [(35)S]GTPgammaS binding in CPu but enhanced it in CHO-HA-rMOR...
  9. ncbi request reprint Comparison of pharmacological activities of three distinct kappa ligands (Salvinorin A, TRK-820 and 3FLB) on kappa opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo
    Yulin Wang
    Department of Pharmacology, Temple University School of Medicine, 3420 North Broad Street, Philadelphia, PA 19140, USA
    J Pharmacol Exp Ther 312:220-30. 2005
    ..The discrepancy between in vitro and in vivo results may be due to in vivo metabolism of salvinorin A and 3FLB and possibly to their effects on other pharmacological targets...
  10. pmc Cholesterol reduction by methyl-beta-cyclodextrin attenuates the delta opioid receptor-mediated signaling in neuronal cells but enhances it in non-neuronal cells
    Peng Huang
    Department of Pharmacology, Center for Substance Abuse Research, Temple University School of Medicine, 3420 N Broad Street, Philadelphia, PA 19140, United States
    Biochem Pharmacol 73:534-49. 2007
    ..Cholesterol-dependent association of caveolin-1 with and the resulting inhibition of G proteins may be a contributing factor...
  11. pmc Young and older good learners have higher levels of brain nicotinic receptor binding
    Diana S Woodruff-Pak
    Department of Psychology, Temple University, Philadelphia, PA 19122, USA
    Neurobiol Aging 31:1032-43. 2010
    ..However, individual differences in alphabeta heteromeric nAChRs also exist early in life, as better learning in 4-month rabbits was associated with significantly higher binding...
  12. ncbi request reprint Differential regulation of the human kappa opioid receptor by agonists: etorphine and levorphanol reduced dynorphin A- and U50,488H-induced internalization and phosphorylation
    Jian Guo Li
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    J Pharmacol Exp Ther 305:531-40. 2003
    ..Thus, the degree of superactivation caused by an agonist is unrelated to its ability to promote internalization of the hkor...
  13. ncbi request reprint Differential effects of agonists on adenylyl cyclase superactivation mediated by the kappa opioid receptors: adenylyl cyclase superactivation is independent of agonist-induced phosphorylation, desensitization, internalization, and down-regulation
    Yulin Wang
    Department of Pharmacology, Temple University School of Medicine, 3420 N Broad St, Philadelphia, PA 19140, USA
    J Pharmacol Exp Ther 307:1127-34. 2003
    ....
  14. ncbi request reprint (-)U50,488H [(trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamide] induces internalization and down-regulation of the human, but not the rat, kappa-opioid receptor: structural basis for the differential regulation
    Fengqin Zhang
    Department of Pharmacology, Center for Substance Abuse Research, Temple University School of Medicine, 3420 N Broad Street, Philadelphia, PA 19140, USA
    J Pharmacol Exp Ther 302:1184-92. 2002
    ..In addition, the trafficking of the FLAG-rkorN358S mutant seems to be more complex than the rkor and the hkor...
  15. ncbi request reprint Ligands regulate cell surface level of the human kappa opioid receptor by activation-induced down-regulation and pharmacological chaperone-mediated enhancement: differential effects of nonpeptide and peptide agonists
    Yong Chen
    Department of Pharmacology, Temple University School of Medicine, 3420 N Broad St, Philadelphia, PA 19140, USA
    J Pharmacol Exp Ther 319:765-75. 2006
    ..These results demonstrate that ligands have dual effects on receptor levels: enhancement by chaperone-like effects and agonist-promoted down-regulation, and the net effect reflects the algebraic sum of the two...
  16. pmc 14-3-3ζ Protein regulates anterograde transport of the human κ-opioid receptor (hKOPR)
    Jian Guo Li
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    J Biol Chem 287:37778-92. 2012
    ..14-3-3ζ knockdown increased association of COPI with the hKOPR. These results suggest that 14-3-3ζ promotes expression of the hKOPR by inhibiting COPI and RVR motif-mediated endoplasmic reticulum localization machinery...
  17. pmc Effects of C-terminal modifications of GEC1 protein and gamma-aminobutyric acid type A (GABA(A)) receptor-associated protein (GABARAP), two microtubule-associated proteins, on kappa opioid receptor expression
    Chongguang Chen
    Department of Pharmacology, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    J Biol Chem 286:15106-15. 2011
    ....
  18. doi request reprint L-isocorypalmine reduces behavioral sensitization and rewarding effects of cocaine in mice by acting on dopamine receptors
    Wei Xu
    Center for Substance Abuse Research and Department of Pharmacology, Temple University School of Medicine, 3500 North Broad Street, Philadelphia, PA 19140, USA
    Drug Alcohol Depend 133:693-703. 2013
    ..Here we characterized its in vitro pharmacological properties and examined its effects on cocaine-induced behaviors in mice...
  19. pmc PKA and ERK1/2 are involved in dopamine D₁ receptor-induced heterologous desensitization of the δ opioid receptor
    Wei Xu
    Department of Pharmacology and Center for Substance Abuse Research, School of Medicine, Temple University, Philadelphia, PA 19140, USA
    Life Sci 92:1101-9. 2013
    ..In addition, DOPR and D1R co-exist in some rat striatal neurons. In the present study, we examined the underlying mechanism of DOPR desensitization by D1R activation...
  20. doi request reprint A common single nucleotide polymorphism A118G of the μ opioid receptor alters its N-glycosylation and protein stability
    Peng Huang
    Department of Pharmacology, Temple University School of Medicine, Philadelphia, PA 19140, USA
    Biochem J 441:379-86. 2012
    ..Pulse-chase studies revealed that the half-life of the mature form of 118G/Asp40-hMOPR (~12 h) was shorter than that of 118A/Asn40-hMOPR (~28 h). Thus the A118G SNP reduces MOPR N-glycosylation and protein stability...
  21. pmc Agonist-promoted Lys63-linked polyubiquitination of the human kappa-opioid receptor is involved in receptor down-regulation
    Jian Guo Li
    Department of Pharmacology, Temple University School of Medicine, 3420 N Broad St, Philadelphia, PA 19140
    Mol Pharmacol 73:1319-30. 2008
    ..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...
  22. pmc Sex difference in κ-opioid receptor (KOPR)-mediated behaviors, brain region KOPR level and KOPR-mediated guanosine 5'-O-(3-[35S]thiotriphosphate) binding in the guinea pig
    Yu Jun Wang
    Department of Pharmacology, Temple University School of Medicine, 3420 N Broad Street, Philadelphia, PA 19140, USA
    J Pharmacol Exp Ther 339:438-50. 2011
    ..These data demonstrate that males and females differ in KOPR expression and KOPR-mediated G protein activation in distinct brain regions, which may contribute to the observed sex differences in KOPR-mediated pharmacology...
  23. pmc Brain region-specific N-glycosylation and lipid rafts association of the rat mu opioid receptor
    Peng Huang
    Department of Pharmacology, Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, PA 19140, USA
    Biochem Biophys Res Commun 365:82-8. 2008
    ..Cholesterol reduction by methyl-beta-cyclodextrin decreased DAGMO-induced [35S]GTPgammaS binding in rat CPu membranes to a greater extent than in the thalamus membranes...
  24. doi request reprint Anxiety-like effects of SR141716-precipitated delta9-tetrahydrocannabinol withdrawal in mice in the elevated plus-maze
    Peng Huang
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, 3420 N Broad St, Philadelphia, PA 19140, USA
    Neurosci Lett 475:165-8. 2010
    ..This animal model may help to identify the mechanisms that contribute to adaptations in the neuronal circuitry of the brain that are expressed as emotional symptoms of cannabinoid withdrawal...
  25. ncbi request reprint kappa Opioid receptor interacts with Na(+)/H(+)-exchanger regulatory factor-1/Ezrin-radixin-moesin-binding phosphoprotein-50 (NHERF-1/EBP50) to stimulate Na(+)/H(+) exchange independent of G(i)/G(o) proteins
    Peng Huang
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    J Biol Chem 279:25002-9. 2004
    ..This study provides the first direct evidence that a G protein-coupled receptor through association with NHERF-1/EBP-50 stimulates NHE3...
  26. ncbi request reprint The local environment at the cytoplasmic end of TM6 of the mu opioid receptor differs from those of rhodopsin and monoamine receptors: introduction of an ionic lock between the cytoplasmic ends of helices 3 and 6 by a L6.30(275)E mutation inactivates the
    Peng Huang
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, 3420 N Broad Street, Philadelphia, PA 19140, USA
    Biochemistry 41:11972-80. 2002
    ..Our molecular modeling results suggest that some specific differences in local geometry at the cytoplasmic ends of TM5 and TM6 may account in part for the observed differences in the molecular mechanisms of receptor activation...
  27. pmc 2-Methoxymethyl-salvinorin B is a potent kappa opioid receptor agonist with longer lasting action in vivo than salvinorin A
    Yulin Wang
    Department of Pharmacology, Temple University School of Medicine, 3420 North Broad Street, Philadelphia, PA 19140, USA
    J Pharmacol Exp Ther 324:1073-83. 2008
    ..Sal A at 10 mg/kg elicited neither antinociception nor hypothermia 30 min after administration to rats. In summary, MOM-Sal B is a potent and efficacious KOPR agonist with longer lasting in vivo effects than Sal A...
  28. pmc GEC1-kappa opioid receptor binding involves hydrophobic interactions: GEC1 has chaperone-like effect
    Yong Chen
    Department of Pharmacology, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    J Biol Chem 284:1673-85. 2009
    ..With its widespread distribution in the nervous system and its predominantly hydrophobic interactions, GEC1 may have chaperone-like effects for many cell surface proteins along the biosynthesis pathway...
  29. ncbi request reprint Effects of mu, kappa or delta opioids administered by pellet or pump on oral Salmonella infection and gastrointestinal transit
    Pu Feng
    Department of Microbiology and Immunology, Temple University School of Medicine, 3400 North Broad Street, Philadelphia, PA 19140, USA
    Eur J Pharmacol 534:250-7. 2006
    ..A delta1 opioid receptor agonist did not sensitize to infection, and a delta2 and a kappa opioid receptor agonist had minimal effects on either parameter...
  30. doi request reprint Hyperlocomotion and paw tremors are two highly quantifiable signs of SR141716-precipitated withdrawal from delta9-tetrahydrocannabinol in C57BL/6 mice
    Peng Huang
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, 3420N Broad St, OMS333, Philadelphia, PA 19140, USA
    Neurosci Lett 465:66-70. 2009
    ....
  31. ncbi request reprint Heterodimerization and cross-desensitization between the mu-opioid receptor and the chemokine CCR5 receptor
    Chongguang Chen
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, 3420 North Broad Street, Philadelphia, PA 19140, USA
    Eur J Pharmacol 483:175-86. 2004
    ..Heterodimerization between the two receptors may contribute to the observed cross-desensitization...
  32. doi request reprint A G protein-coupled receptor (GPCR) in red: live cell imaging of the kappa opioid receptor-tdTomato fusion protein (KOPR-tdT) in neuronal cells
    Peng Huang
    Center for Substance Abuse Research and Department of Pharmacology, Temple University School of Medicine, Philadelphia, PA 19140, United States
    J Pharmacol Toxicol Methods 68:340-5. 2013
    ..Among all the RFPs, tdTomato (tdT), one of the non-aggregating RFP, has the highest brightness score (about 3 times that of eGFP) and unsurpassed photostability...
  33. ncbi request reprint Selective inactivation of CCR5 and decreased infectivity of R5 HIV-1 strains mediated by opioid-induced heterologous desensitization
    Imre Szabo
    Department of Microbiology and Immunology, Temple University School of Medicine, 3400 N Broad Street, Philadelphia, PA 19140, USA
    J Leukoc Biol 74:1074-82. 2003
    ..The interference with HIV-1 uptake by heterologous desensitization of CCR5 suggests that HIV-1 interaction with this receptor is not passive but involves a signal transduction process...
  34. pmc Dynorphin peptides differentially regulate the human kappa opioid receptor
    Yong Chen
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, 3420 North Broad Street, Philadelphia, PA 19140, U S A
    Life Sci 80:1439-48. 2007
    ..Both stability in the presence of serum and intrinsic capacity to promote receptor adaptation play roles in the observed discrepancy among the dynorphin peptides...
  35. pmc Mephedrone ('bath salt') elicits conditioned place preference and dopamine-sensitive motor activation
    Renata Lisek
    Department of Pharmacology, Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, PA 19140, USA
    Drug Alcohol Depend 126:257-62. 2012
    ..The CPP and dopamine-sensitive motor activation produced by mephedrone is suggestive of abuse liability and indicates commonalities between the neuropharmacological profiles of mephedrone and established drugs of abuse...
  36. doi request reprint Activation of the mu opioid receptor involves conformational rearrangements of multiple transmembrane domains
    Wei Xu
    Department of Pharmacology, Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    Biochemistry 47:10576-86. 2008
    ....
  37. ncbi request reprint Insulin-like peptide 5: expression in the mouse brain and mobilization of calcium
    Siok L Dun
    Department of Pharmacology, Temple University School of Medicine, 3420 North Broad Street, Philadelphia, Pennsylvania 19140, USA
    Endocrinology 147:3243-8. 2006
    ..The concentration of irINSL5 in the hypothalamic-pituitary axis suggests a neuroendocrine function of this insulin superfamily member...
  38. ncbi request reprint Chaperone-like effects of cell-permeant ligands on opioid receptors
    Yong Chen
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, 3420 North Broad Street, Philadelphia, PA 19140, USA
    Front Biosci (Landmark Ed) 14:634-43. 2009
    ..Potential therapeutic applications of the chaperone-like function of opioid ligands are discussed...
  39. pmc Sex differences in kappa opioid pharmacology
    Khampaseuth Rasakham
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, PA 19140, United States
    Life Sci 88:2-16. 2011
    ..In light of the diverse pharmacology of KOPR we discuss the need for future studies characterizing the sexual dimorphism of KOPR neural circuitry and in examining other behaviors and processes that are modulated by the KOPR...
  40. pmc Mouse model of OPRM1 (A118G) polymorphism has sex-specific effects on drug-mediated behavior
    Stephen D Mague
    Department of Pharmacology, Abramson Cancer Center, University of Pennsylvania School of Medicine, Philadelphia, PA 19104, USA
    Proc Natl Acad Sci U S A 106:10847-52. 2009
    ..Further cross-species analysis will allow us to investigate mechanisms and adaptations present in humans carrying this SNP...
  41. pmc The seventh transmembrane domains of the delta and kappa opioid receptors have different accessibility patterns and interhelical interactions
    Wei Xu
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, PA 19140, USA
    Biochemistry 44:16014-25. 2005
    ..iv) The NPxxY motif in TM7 interacts with TM2, TM6, and helix 8 to maintain receptors in inactive states. To the best of our knowledge, this represents the first such comparison of the structures of two highly homologous GPCRs...
  42. pmc In vivo trafficking of endogenous opioid receptors
    Yulin Wang
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, 3420 North Broad Street, Philadelphia, PA 19140, USA
    Life Sci 83:693-9. 2008
    ..In vivo studies, therefore, are essential to provide insight into the mechanisms underlying opioid receptor regulation...
  43. doi request reprint Nicotinic acetylcholine receptors and modulation of learning in 4- and 27-month-old rabbits
    Jian Guo Li
    Department of Pharmacology, Temple University School of Medicine, Philadelphia, PA 19122, USA
    Neuropsychopharmacology 33:2820-30. 2008
    ..Results provide evidence for cortical as well as hippocampal nAChR modulation of delay eyeblink conditioning and demonstrate that more sensitive binding assays are required to assess nAChR effects in cerebellum...
  44. pmc Differential modulation of mu- and delta-opioid receptor agonists by endogenous RGS4 protein in SH-SY5Y cells
    Qin Wang
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan 48109, USA
    J Biol Chem 284:18357-67. 2009
    ..The findings demonstrate a role for endogenous RGS4 protein in modulating delta-opioid receptor signaling in SH-SY5Y cells and provide evidence for a receptor-specific effect of RGS4...
  45. pmc Effects of acute agonist treatment on subcellular distribution of kappa opioid receptor in rat spinal cord
    Yulin Wang
    Department of Pharmacology, School of Medicine, Temple University, Philadelphia, Pennsylvania 19140, USA
    J Neurosci Res 87:1695-702. 2009
    ..t., significantly decreased cell surface KOPR to approximately 19%. In summary, these data indicate that U50,488H and dynorphin A differentially regulate the subcellular distribution of endogenous KOPR...
  46. ncbi request reprint Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues
    David Y W Lee
    Bioorganic and Natural Products Laboratory, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 15:4169-73. 2005
    ..These C(4)-modified salvinorin A analogues were screened for binding and functional activities at the human kappa-opioid receptor and several potent new agonists have been identified...
  47. ncbi request reprint Pharmacokinetics and pharmacodynamics of oral oxycodone in healthy human subjects: role of circulating active metabolites
    Bojan Lalovic
    Department of Pharmaceutics, University of Washington, Seattle 98195, USA
    Clin Pharmacol Ther 79:461-79. 2006
    ....
  48. ncbi request reprint Butorphanol dependence increases hippocampal kappa-opioid receptor gene expression
    Sachiko Tanaka
    Department of Biochemical Toxicology, School of Pharmaceutical Science, Showa University, Tokyo, Japan
    J Neurosci Res 82:255-63. 2005
    ....
  49. ncbi request reprint Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18)
    Cecile Beguin
    Molecular Pharmacology Laboratory, McLean Hospital, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 16:4679-85. 2006
    ..Our preliminary SAR study at C(18) suggested that this part of the molecule interacts with a tight lipophilic pocket of the kappa-receptor...
  50. ncbi request reprint N-methylacetamide analog of salvinorin A: a highly potent and selective kappa-opioid receptor agonist with oral efficacy
    Cecile Beguin
    Department of Psychiatry, McLean Hospital, MRC 322A, 115 Mill Street, Belmont, MA 02478, USA
    J Pharmacol Exp Ther 324:188-95. 2008
    ....
  51. ncbi request reprint Synthesis and in vitro pharmacological studies of new C(4)-modified salvinorin A analogues
    David Y W Lee
    Bioorganic and Natural Products Laboratory, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 16:5498-502. 2006
    ..These C(4)-modified salvinorin A analogues were screened for binding and functional activities at the human kappa-opioid receptor and several new full agonists have been identified...
  52. ncbi request reprint Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2)
    Cecile Beguin
    Molecular Pharmacology Laboratory, McLean Hospital, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 15:2761-5. 2005
    ..Compound 10, containing an N-methyl carbamate at C(2), showed partial agonist activity with 81% efficacy when compared with the full agonist U50,488H. No antagonist ligands were observed...

Research Grants25

  1. MOLECULAR CHARACTERIZATION OF OPIOID RECEPTORS
    Lee Yuan Liu Chen; Fiscal Year: 2004
    ..The information will provide insights into the structures of the binding-site crevices of opioid receptors, which will aid in the design of selective agonists and antagonists for prevention and treatment of drug abuse. ..
  2. Cellular Pharmacology of Kappa Opioid Receptor
    Lee Yuan Liu Chen; Fiscal Year: 2007
    ..In addition, such understanding will have important ramifications for other G protein coupled receptors since these molecules may play similar roles for other receptors. ..
  3. Cellular Pharmacology of Kappa Opiod Receptor
    Lee Yuan Liu Chen; Fiscal Year: 2009
    ..PUBLIC HEALTH RELEVANCE: The proposed research will provide better understanding on how cell surface receptor numbers are regulated, which play important roles in response to external stimuli, including drugs and neurotransmitters. ..
  4. REGULATION OF KAPPA OPIOID RECEPTORS
    Lee Yuan Liu Chen; Fiscal Year: 2002
    ..Elucidation of the mechanisms involved in agonist-induced regulation of the KOR will lead to a better understanding of tolerance to kappa agonist, which will help in the development of better kappa agonists as useful drugs. ..
  5. MOLECULAR CHARACTERIZATION OF THE MU OPIOID RECEPTOR
    Lee Yuan Liu Chen; Fiscal Year: 1999
    ....
  6. MOLECULAR CHARACTERIZATION OF MU OPIOID RECEPTORS
    Lee Yuan Liu Chen; Fiscal Year: 1993
    ..The proposed research will lead to studies on regulation of expression of the mu receptor at the molecular level, which will shed light on the mechanism of development of opioid tolerance and dependence...
  7. Cellular Pharmacology of Kappa Opiod Receptor
    Lee Yuan Liu Chen; Fiscal Year: 2010
    ..PUBLIC HEALTH RELEVANCE: The proposed research will provide better understanding on how cell surface receptor numbers are regulated, which play important roles in response to external stimuli, including drugs and neurotransmitters. ..