L J Miller

Summary

Affiliation: Mayo Clinic
Country: USA

Publications

  1. pmc Sensitivity of cholecystokinin receptors to membrane cholesterol content
    Aditya J Desai
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic Scottsdale, AZ, USA
    Front Endocrinol (Lausanne) 3:123. 2012
  2. doi request reprint The orthosteric agonist-binding pocket in the prototypic class B G-protein-coupled secretin receptor
    Laurence J Miller
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, 13400 East Shea Boulevard, Scottsdale, AZ 85259, USA
    Biochem Soc Trans 41:154-8. 2013
  3. pmc Mapping spatial approximations between the amino terminus of secretin and each of the extracellular loops of its receptor using cysteine trapping
    Maoqing Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    FASEB J 26:5092-105. 2012
  4. pmc Ligand binding and activation of the secretin receptor, a prototypic family B G protein-coupled receptor
    Laurence J Miller
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ, USA
    Br J Pharmacol 166:18-26. 2012
  5. pmc Differential determinants for coupling of distinct G proteins with the class B secretin receptor
    Gene L Garcia
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ 85259, USA
    Am J Physiol Cell Physiol 302:C1202-12. 2012
  6. ncbi request reprint Molecular basis of agonist binding to the type A cholecystokinin receptor
    Laurence J Miller
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic and Foundation, Rochester, MN 55905, USA
    Pharmacol Toxicol 91:282-5. 2002
  7. pmc Ligand-induced internalization of the type 1 cholecystokinin receptor independent of recognized signaling activity
    Erin E Cawston
    Mayo Clinic, Scottsdale, AZ 85259, USA
    Am J Physiol Cell Physiol 302:C615-27. 2012
  8. ncbi request reprint Biochemical and cell biological mechanisms of cholecystokinin receptor regulation
    Laurence J Miller
    Mayo Clinic, Department of Molecular Pharmacology and Experimental Therapeutics, Scottsdale, Arizona 85259, USA
    Curr Top Med Chem 7:1166-72. 2007
  9. pmc Refinement of glucagon-like peptide 1 docking to its intact receptor using mid-region photolabile probes and molecular modeling
    Laurence J Miller
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    J Biol Chem 286:15895-907. 2011
  10. ncbi request reprint Insights into the molecular basis of ligand binding by the cholecystokinin receptor
    L J Miller
    Center for Basic Research in Digestive Diseases, Mayo Clinic and Foundation, Rochester, Minn, USA
    Pancreatology 1:336-42. 2001

Collaborators

Detail Information

Publications104 found, 100 shown here

  1. pmc Sensitivity of cholecystokinin receptors to membrane cholesterol content
    Aditya J Desai
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic Scottsdale, AZ, USA
    Front Endocrinol (Lausanne) 3:123. 2012
    ..This is believed to have substantial potential importance for the development of drugs targeting the CCK receptor...
  2. doi request reprint The orthosteric agonist-binding pocket in the prototypic class B G-protein-coupled secretin receptor
    Laurence J Miller
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, 13400 East Shea Boulevard, Scottsdale, AZ 85259, USA
    Biochem Soc Trans 41:154-8. 2013
    ..Such insights will be useful in the rational development of drugs acting at this important group of targets...
  3. pmc Mapping spatial approximations between the amino terminus of secretin and each of the extracellular loops of its receptor using cysteine trapping
    Maoqing Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    FASEB J 26:5092-105. 2012
    ..Key spatial approximations between peptide and receptor predicted by this model (H(1)-W(274), D(3)-N(268), G(4)-F(258)) were supported by mutagenesis and residue-residue complementation studies...
  4. pmc Ligand binding and activation of the secretin receptor, a prototypic family B G protein-coupled receptor
    Laurence J Miller
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ, USA
    Br J Pharmacol 166:18-26. 2012
    ..This complex is important for facilitating G protein association and achieving the high affinity state of this receptor...
  5. pmc Differential determinants for coupling of distinct G proteins with the class B secretin receptor
    Gene L Garcia
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ 85259, USA
    Am J Physiol Cell Physiol 302:C1202-12. 2012
    ..These data suggest that, while some receptor determinants are clearly shared, there are also distinct determinants for coupling with each of these G proteins...
  6. ncbi request reprint Molecular basis of agonist binding to the type A cholecystokinin receptor
    Laurence J Miller
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic and Foundation, Rochester, MN 55905, USA
    Pharmacol Toxicol 91:282-5. 2002
    ....
  7. pmc Ligand-induced internalization of the type 1 cholecystokinin receptor independent of recognized signaling activity
    Erin E Cawston
    Mayo Clinic, Scottsdale, AZ 85259, USA
    Am J Physiol Cell Physiol 302:C615-27. 2012
    ..Thus the 309-323 region of the type 1 CCK receptor affects antagonist-stimulated internalization of this receptor, although its mechanism and interacting partner are not yet clear...
  8. ncbi request reprint Biochemical and cell biological mechanisms of cholecystokinin receptor regulation
    Laurence J Miller
    Mayo Clinic, Department of Molecular Pharmacology and Experimental Therapeutics, Scottsdale, Arizona 85259, USA
    Curr Top Med Chem 7:1166-72. 2007
    ..Agonist occupation results in oligomer dissociation, but the functional significance of this observation has yet to be defined...
  9. pmc Refinement of glucagon-like peptide 1 docking to its intact receptor using mid-region photolabile probes and molecular modeling
    Laurence J Miller
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    J Biol Chem 286:15895-907. 2011
    ..Establishing ligand residue approximation with this loop region is unique among family members and may help to orient the receptor amino-terminal domain relative to its helical bundle region...
  10. ncbi request reprint Insights into the molecular basis of ligand binding by the cholecystokinin receptor
    L J Miller
    Center for Basic Research in Digestive Diseases, Mayo Clinic and Foundation, Rochester, Minn, USA
    Pancreatology 1:336-42. 2001
    ..In this work, we review the contributions of each of these complementary approaches and provide a current integrated view of the active complex of cholecystokinin bound to its receptor...
  11. ncbi request reprint Structural basis of natural ligand binding and activation of the Class II G-protein-coupled secretin receptor
    L J Miller
    Mayo Clinic, 13400 East Shea Boulevard, Scottsdale, AZ 85259, USA
    Biochem Soc Trans 35:709-12. 2007
    ..The site of action of this endogenous agonist could also provide a possible target for small molecule agonists to act...
  12. ncbi request reprint Informed development of drugs acting at family B G protein-coupled receptors
    Laurence J Miller
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ 85259, USA
    Ann N Y Acad Sci 1144:203-9. 2008
    ..Endogenous agonist activity within the amino terminus of these receptors could be key for the development of such drugs...
  13. pmc Structural basis of cholecystokinin receptor binding and regulation
    Laurence J Miller
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ 85259, USA
    Pharmacol Ther 119:83-95. 2008
    ..This degree of specialization is instructive and provides an encouraging basis for the diversity of potential drugs targeting these receptors and their actions that can be developed...
  14. ncbi request reprint G protein-coupled receptor structures, molecular associations, and modes of regulation
    Laurence J Miller
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ 85259, USA
    Ann N Y Acad Sci 1144:1-5. 2008
    ..In this report, key past accomplishments and possible future directions for this field of research are reviewed...
  15. ncbi request reprint Spatial approximation between two residues in the mid-region of secretin and the amino terminus of its receptor. Incorporation of seven sets of such constraints into a three-dimensional model of the agonist-bound secretin receptor
    Maoqing Dong
    Cancer Center and the Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic Scottsdale, Scottsdale, Arizona 85259, USA
    J Biol Chem 278:48300-12. 2003
    ..This provides clear insights into the molecular basis of natural ligand binding and supplies testable hypotheses regarding the molecular basis of activation of this receptor...
  16. ncbi request reprint Transmembrane segment IV contributes a functionally important interface for oligomerization of the Class II G protein-coupled secretin receptor
    Kaleeckal G Harikumar
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    J Biol Chem 282:30363-72. 2007
    ..This supports a clear functional effect of oligomerization of this receptor. Such an effect might be particularly relevant to clinical situations in which this receptor is overexpressed, such as in certain neoplasms...
  17. pmc Spatial approximation between secretin residue five and the third extracellular loop of its receptor provides new insight into the molecular basis of natural agonist binding
    Maoqing Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, 13400 East Shea Blvd, Scottsdale, AZ 85259, USA
    Mol Pharmacol 74:413-22. 2008
    ....
  18. ncbi request reprint Characterization of the type A cholecystokinin receptor hormone-binding domain: use of contrasting and complementary methodologies
    X Q Ding
    Center for Basic Research in Digestive Diseases, Mayo Clinic and Foundation, Rochester, MN 55905, USA
    Peptides 22:1223-8. 2001
    ..These support the key roles played by extracellular loop and tail regions of this receptor for binding its natural peptide ligand...
  19. ncbi request reprint Refinement of the structure of the ligand-occupied cholecystokinin receptor using a photolabile amino-terminal probe
    X Q Ding
    Center for Basic Research in Digestive Diseases, Mayo Clinic and Foundation, Rochester, Minnesota 55905, USA
    J Biol Chem 276:4236-44. 2001
    ..Use of these additional insights into molecular approximations provided key constraints for molecular modeling of the peptide-receptor complex, supporting the counterclockwise organization of the transmembrane helical domains...
  20. pmc Functional importance of a structurally distinct homodimeric complex of the family B G protein-coupled secretin receptor
    Fan Gao
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ 85259, USA
    Mol Pharmacol 76:264-74. 2009
    ..We propose the existence of a functionally important, structurally specific high-affinity dimeric state of the secretin receptor, which may be typical of family B G protein-coupled receptors...
  21. ncbi request reprint Molecular characterization and organ distribution of type A and B cholecystokinin receptors in cynomolgus monkey
    E L Holicky
    Departments of Internal Medicine and Biochemistry/Molecular Biology, Center for Basic Research in Digestive Diseases, Mayo Clinic and Foundation, Rochester, Minnesota 55905, USA
    Am J Physiol Gastrointest Liver Physiol 281:G507-14. 2001
    ..This work confirms the relevance of the cynomolgus species for preclinical testing of drugs acting on the type A CCK receptor...
  22. pmc Secretin occupies a single protomer of the homodimeric secretin receptor complex: insights from photoaffinity labeling studies using dual sites of covalent attachment
    Maoqing Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    J Biol Chem 285:9919-31. 2010
    ..These data are consistent with a model of secretin occupying a single secretin receptor protomer within the homodimeric receptor complex. A new molecular model accommodating all constraints is now proposed...
  23. pmc Role of lysine187 within the second extracellular loop of the type A cholecystokinin receptor in agonist-induced activation. Use of complementary charge-reversal mutagenesis to define a functionally important interdomain interaction
    Maoqing Dong
    Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    Biochemistry 46:4522-31. 2007
    ..This residue-residue interaction is nicely accommodated within a new molecular model of the agonist-occupied cholecystokinin receptor...
  24. ncbi request reprint Silencing of secretin receptor function by dimerization with a misspliced variant secretin receptor in ductal pancreatic adenocarcinoma
    Wei Qun Ding
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Rochester, MN 55905, USA
    Cancer Res 62:5223-9. 2002
    ..Suppression of this activity in pancreatic carcinoma might, therefore, facilitate tumor growth and progression of this aggressive neoplasm...
  25. pmc Molecular basis of association of receptor activity-modifying protein 3 with the family B G protein-coupled secretin receptor
    Kaleeckal G Harikumar
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    Biochemistry 48:11773-85. 2009
    ..This may be representative of similar interactions between other members of this receptor family and RAMP proteins...
  26. ncbi request reprint Spatial approximation between the amino terminus of a peptide agonist and the top of the sixth transmembrane segment of the secretin receptor
    Maoqing Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic Scottsdale, Scottsdale, Arizona 85259, USA
    J Biol Chem 279:2894-903. 2004
    ..This suggests that secretin binding may exert tension between the receptor amino terminus and the transmembrane domain to elicit a conformational change effecting receptor activation...
  27. ncbi request reprint Paired cysteine mutagenesis to establish the pattern of disulfide bonds in the functional intact secretin receptor
    Cayle S Lisenbee
    Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    J Biol Chem 280:12330-8. 2005
    ..In conclusion, these data suggest the same pattern of disulfide bonding as that predicted previously by NMR and thus support a consistent pattern of amino-terminal disulfide bonds in class B G protein-coupled receptors...
  28. ncbi request reprint Identification of peptide ligand-binding domains within the human motilin receptor using photoaffinity labeling
    B Coulie
    Center for Basic Research in Digestive Diseases, Departments of Internal Medicine and Biochemistry Molecular Biology, Mayo Clinic and Foundation, Rochester, Minnesota 55905, USA
    J Biol Chem 276:35518-22. 2001
    ..The spatial approximation of the pharmacophoric domain of motilin with these receptor domains support their functional importance as well...
  29. ncbi request reprint DNA binding of TEA/ATTS domain factors is regulated by protein kinase C phosphorylation in human choriocarcinoma cells
    S W Jiang
    Department of Medicine, Mayo Clinic, Rochester, Minnesota 55905, USA
    J Biol Chem 276:23464-70. 2001
    ..These data strongly suggest that PKC-mediated phosphorylation is a key factor controlling TEF function...
  30. pmc Elucidation of the molecular basis of cholecystokinin Peptide docking to its receptor using site-specific intrinsic photoaffinity labeling and molecular modeling
    Maoqing Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    Biochemistry 48:5303-12. 2009
    ..The resultant agonist ligand-occupied receptor models fully accommodate all existing experimental data and represent the best refined models of a peptide hormone receptor in this important family...
  31. pmc Molecular basis of glucagon-like peptide 1 docking to its intact receptor studied with carboxyl-terminal photolabile probes
    Quan Chen
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    J Biol Chem 284:34135-44. 2009
    ..This should expand our understanding of the molecular basis of natural agonist ligand binding to the GLP1 receptor and may be relevant to other family members...
  32. pmc Spatial approximations between residues 6 and 12 in the amino-terminal region of glucagon-like peptide 1 and its receptor: a region critical for biological activity
    Quan Chen
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    J Biol Chem 285:24508-18. 2010
    ..This region of interaction of peptide amino-terminal domains with the receptor may provide a pocket that can be targeted by small molecule agonists...
  33. ncbi request reprint Development of a biologically active secretin analogue incorporating a radioiodinatable photolabile p-(4-hydroxybenzoyl)phenylalanine in position 10
    Maoqing Dong
    Center for Basic Research in Digestive Diseases, Department of Internal Medicine, Mayo Clinic and Foundation, Rochester, MN 55905, USA
    Regul Pept 109:181-7. 2002
    ....
  34. ncbi request reprint Secretin and vasoactive intestinal peptide receptors: members of a unique family of G protein-coupled receptors
    C D Ulrich
    Center for Basic Research in Digestive Diseases, Department of Molecular Biology Biochemistry, Mayo Medical School, Rochester, Minnesota 55905, USA
    Gastroenterology 114:382-97. 1998
  35. ncbi request reprint Differences in partial agonist action at cholecystokinin receptors of mouse and rat are dependent on parameters extrinsic to receptor structure: molecular cloning, expression and functional characterization of the mouse type A cholecystokinin receptor
    D Ghanekar
    Center for Basic Research in Digestive Diseases, Mayo Clinic and Foundation, Rochester, Minnesota 55905, USA
    J Pharmacol Exp Ther 282:1206-12. 1997
    ..Receptor microenvironment makes an important, yet often ignored, contribution to receptor function...
  36. pmc Effects of cholecystokinin-58 on type 1 cholecystokinin receptor function and regulation
    S Vincent Wu
    Mayo Clinic, Department of Molecular Pharmacology and Experimental Therapeutics, 13400 East Shea Blvd, Scottsdale, AZ 85259, USA
    Am J Physiol Gastrointest Liver Physiol 295:G641-7. 2008
    ....
  37. ncbi request reprint Differential docking of high-affinity peptide ligands to type A and B cholecystokinin receptors demonstrated by photoaffinity labeling
    Maoqing Dong
    Mayo Clinic Scottsdale, Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, Scottsdale, Arizona 85259, USA
    Biochemistry 44:6693-700. 2005
    ..This provides a direct demonstration of distinct modes of docking the same high-affinity ligand to highly homologous receptors...
  38. ncbi request reprint Insights into the structure and molecular basis of ligand docking to the G protein-coupled secretin receptor using charge-modified amino-terminal agonist probes
    Maoqing Dong
    M D Director, Cancer Center Mayo Clinic in Scottsdale, 13400 East Shea Boulevard, Johnson Research Building, Scottsdale AZ 85259, USA
    Mol Endocrinol 19:1821-36. 2005
    ..This supports the possibility that there is a charge-charge interaction between this residue and the amino terminus of secretin that is critical to its normal docking...
  39. ncbi request reprint Functional characterization and purification of the secretin receptor expressed in baculovirus-infected insect cells
    Yan W Asmann
    Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic Scottsdale, Johnson Research Building, Scottsdale, AZ 85259, USA
    Regul Pept 123:217-23. 2004
    ..This expression system should facilitate the structural characterization of this receptor and its important amino-terminal domain...
  40. pmc Role of N-linked glycosylation in biosynthesis, trafficking, and function of the human glucagon-like peptide 1 receptor
    Quan Chen
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, 13400 East Shea Blvd, Scottsdale, AZ 85259, USA
    Am J Physiol Endocrinol Metab 299:E62-8. 2010
    ..These data suggest that N-linked glycosylation of the GLP-1 receptor is important for its normal folding and trafficking to the cell surface...
  41. ncbi request reprint Use of probes with fluorescence indicator distributed throughout the pharmacophore to examine the peptide agonist-binding environment of the family B G protein-coupled secretin receptor
    Kaleeckal G Harikumar
    Cancer Center and the Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    J Biol Chem 281:2543-50. 2006
    ..Combining the fluorescence data with photoaffinity labeling data provides insights into the conformation and dynamics of a natural peptide ligand docked to a Family B G protein-coupled receptor...
  42. pmc Novel benzodiazepine photoaffinity probe stereoselectively labels a site deep within the membrane-spanning domain of the cholecystokinin receptor
    Elizabeth M Hadac
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ 85259, USA
    J Med Chem 49:850-63. 2006
    ....
  43. ncbi request reprint Mapping the architecture of secretin receptors with intramolecular fluorescence resonance energy transfer using acousto-optic tunable filter-based spectral imaging
    Cayle S Lisenbee
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    Mol Endocrinol 21:1997-2008. 2007
    ..These data demonstrate changes in the relative positions of intracellular structures that support a model for secretin receptor activation...
  44. pmc Refinement of the pharmacophore of an agonist ligand of the secretin receptor using conformationally constrained cyclic hexapeptides
    Maoqing Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ 85259, United States
    Peptides 31:1094-8. 2010
    ..Molecular modeling supported the presence of a unique WD backbone conformation shared only by these active peptides, and provided a more constrained template for future receptor-active agonist drug development...
  45. ncbi request reprint Fluorescence resonance energy transfer analysis of secretin docking to its receptor: mapping distances between residues distributed throughout the ligand pharmacophore and distinct receptor residues
    Kaleeckal G Harikumar
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, 13400 E Shea Boulevard, Scottsdale, AZ 85259, USA
    J Biol Chem 282:32834-43. 2007
    ..This provides strong evidence for the orientation of peptide-binding and signaling domains of a prototypic Class II G protein-coupled receptor...
  46. ncbi request reprint Upregulation of secretin receptors on cholangiocytes after bile duct ligation
    P S Tietz
    Center for Basic Research in Digestive Diseases, Mayo Medical School, Clinic and Foundation, Rochester, MN 55905, USA
    Regul Pept 97:1-6. 2001
    ....
  47. ncbi request reprint Use of photoaffinity labeling to understand the molecular basis of ligand binding to the secretin receptor
    Maoqing Dong
    Mayo Clinic, 13400 East Shea Blvd, Scottsdale, AZ 85259, USA
    Ann N Y Acad Sci 1070:248-64. 2006
    ..Each of the themes discussed are also relevant to other members of this physiologically and pharmacologically important receptor family...
  48. ncbi request reprint Possible endogenous agonist mechanism for the activation of secretin family G protein-coupled receptors
    Maoqing Dong
    Mayo Clinic, 13400 E Shea Boulevard, Scottsdale, AZ 85259, USA
    Mol Pharmacol 70:206-13. 2006
    ..These data may provide a unique molecular mechanism and novel leads for the development of small-molecule agonists acting at potential drug targets within this physiologically important receptor family...
  49. ncbi request reprint Molecular approximations between residues 21 and 23 of secretin and its receptor: development of a model for peptide docking with the amino terminus of the secretin receptor
    Maoqing Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic Scottsdale, Scottsdale, Arizona, USA
    Mol Pharmacol 72:280-90. 2007
    ..This model was found to fully accommodate all existing constraints, as well as the two new approximations identified in this work...
  50. pmc Use of multidimensional fluorescence resonance energy transfer to establish the orientation of cholecystokinin docked at the type A cholecystokinin receptor
    Kaleeckal G Harikumar
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, 13400 East Shea Boulevard, Scottsdale, Arizona 85259, USA
    Biochemistry 47:9574-81. 2008
    ..Multidimensional FRET provides a new independent method to establish and refine structural insights into ligand-receptor complexes...
  51. ncbi request reprint Key differences in molecular complexes of the cholecystokinin receptor with structurally related peptide agonist, partial agonist, and antagonist
    Sonnet J H Arlander
    Cancer Center, Mayo Clinic in Scottsdale, 13400 East Shea Boulevard, Johnson Research Building, Scottsdale AZ 85259, USA
    Mol Pharmacol 66:545-52. 2004
    ..Of note, the analogous antagonist probe labeled a distinct region within the receptor amino terminus, confirming a key structural difference in active and inactive complexes...
  52. ncbi request reprint Dominant negative action of an abnormal secretin receptor arising from mRNA missplicing in a gastrinoma
    Wei Qun Ding
    Center for Basic Research in Digestive Diseases, Mayo Clinic and Foundation, Rochester, Minnesota 55905, USA
    Gastroenterology 122:500-11. 2002
    ..The aim of the present study was to explore the molecular basis for positive and false-negative secretin-stimulation test results in patients with these tumors...
  53. ncbi request reprint Interaction among four residues distributed through the secretin pharmacophore and a focused region of the secretin receptor amino terminus
    Maoqing Dong
    Center for Basic Research in Digestive Diseases, Department of Internal Medicine, Mayo Clinic and Foundation, Rochester, Minnesota 55905, USA
    Mol Endocrinol 16:2490-501. 2002
    ..Additional experimentally derived constraints will be necessary to determine the spatial positioning of this complex with the remainder of the SecR...
  54. pmc Modulation of cell surface expression of nonactivated cholecystokinin receptors using bivalent ligand-induced internalization
    Kaleeckal G Harikumar
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, 13400 East Shea Boulevard, Scottsdale, Arizona 85259, USA
    J Med Chem 53:2836-42. 2010
    ..Receptor tethering with appropriate bivalent ligands can down-regulate signaling by moving a nonactivated receptor into the endocytic pathway...
  55. ncbi request reprint Spatial approximation between a photolabile residue in position 13 of secretin and the amino terminus of the secretin receptor
    Mengwei Zang
    Cancer Center and the Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic Scottsdale, Scottsdale, Arizona 85259, USA
    Mol Pharmacol 63:993-1001. 2003
    ..Together, these five pairs of residue-residue approximations provide important constraints to better understand the molecular conformation of the agonist-bound receptor...
  56. ncbi request reprint Differential determinants for peptide and non-peptidyl ligand binding to the motilin receptor. Critical role of second extracellular loop for peptide binding and action
    Bunzo Matsuura
    Center for Basic Research in Digestive Diseases, Department of Internal Medicine, Mayo Clinic and Foundation, Rochester, Minnesota 55905, USA
    J Biol Chem 277:9834-9. 2002
    ....
  57. ncbi request reprint Heterodimerization of type A and B cholecystokinin receptors enhance signaling and promote cell growth
    Zhi jie Cheng
    Mayo Clinic Scottsdale, Cancer Center and, Department of Molecular Pharmacology and Experimental Therapeutics, Scottsdale, Arizona 85259, USA
    J Biol Chem 278:52972-9. 2003
    ..Our results provide the first evidence that heterodimerization of G protein-coupled receptors can form a more "powerful" signaling unit, which has potential clinical significance in promoting cell growth...
  58. pmc Monitoring the state of cholecystokinin receptor oligomerization after ligand binding using decay of time-resolved fluorescence anisotropy
    Kaleeckal G Harikumar
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ 85259, USA
    Ann N Y Acad Sci 1144:21-7. 2008
    ..This dynamic technique complements the other biochemical and steady-state fluorescence techniques to establish the presence of oligomeric receptor complexes in living cells...
  59. pmc The biochemical characterization of the native pancreatic cholecystokinin receptor using affinity labeling approaches
    L J Miller
    Center for Basic Research in Digestive Diseases, Mayo Clinic, Rochester, Minnesota 55905
    Yale J Biol Med 65:441-8; discussion 465-9. 1992
    ..This procedure confirmed that these two minor membrane proteins are spatially associated with each other.(ABSTRACT TRUNCATED AT 250 WORDS)..
  60. ncbi request reprint Control of cholecystokinin receptor dephosphorylation in pancreatic acinar cells
    M P Lutz
    Center for Basic Research in Digestive Diseases, Mayo Clinic and Foundation, Rochester, Minnesota 55905
    J Biol Chem 268:12136-42. 1993
    ..These data suggest that CCK coordinates the activity of both protein kinases and phosphatases acting on the CCK receptor to control the extent and duration of receptor phosphorylation in the pancreatic acinar cell...
  61. pmc Insights into the structural basis of endogenous agonist activation of family B G protein-coupled receptors
    Maoqing Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    Mol Endocrinol 22:1489-99. 2008
    ..This directly supports the relevance of the endogenous agonist concept to the GLP1 receptor and provides new insights into the rational development and refinement of new types of drugs activating this important receptor...
  62. pmc Pattern of intra-family hetero-oligomerization involving the G-protein-coupled secretin receptor
    Kaleeckal G Harikumar
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, 13400 East Shea Blvd, Scottsdale, AZ 85259, USA
    J Mol Neurosci 36:279-85. 2008
    ..Thus, Family B GPCR oligomerization occurs, with many structurally related members associating with each other. The specific functional implications of this need to be further evaluated...
  63. pmc Exploration of the endogenous agonist mechanism for activation of secretin and VPAC1 receptors using synthetic glycosylated peptides
    Maoqing Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, 13400 East Shea Boulevard, Scottsdale, AZ 85259, USA
    J Mol Neurosci 36:254-9. 2008
    ..These data provide further evidence for this proposed mechanism for the activation of this family of receptors...
  64. pmc Juxtamembranous region of the amino terminus of the family B G protein-coupled calcitonin receptor plays a critical role in small-molecule agonist action
    Maoqing Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    J Biol Chem 284:21839-47. 2009
    ..These findings focus attention on the potential importance of the juxtamembranous region of the amino terminus of the Family B calcitonin receptor for agonist drug action...
  65. pmc Dimerization in the absence of higher-order oligomerization of the G protein-coupled secretin receptor
    Kaleeckal G Harikumar
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ 85259, USA
    Biochim Biophys Acta 1778:2555-63. 2008
    ..These results suggest that the secretin receptor can exist only as a structurally-specific homo-dimer, without being present as higher-order oligomers...
  66. ncbi request reprint Distinct molecular mechanisms for agonist peptide binding to types A and B cholecystokinin receptors demonstrated using fluorescence spectroscopy
    Kaleeckal G Harikumar
    Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic Scottsdale, Scottsdale, Arizona 85259, USA
    J Biol Chem 280:1044-50. 2005
    ..Of interest, despite this difference in binding, activation of both receptors results in analogous direction of movement of the fluorescent indicator probes...
  67. ncbi request reprint Constitutive formation of oligomeric complexes between family B G protein-coupled vasoactive intestinal polypeptide and secretin receptors
    Kaleeckal G Harikumar
    Mayo Clinic, Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, Scottsdale, Arizona, USA
    Mol Pharmacol 69:363-73. 2006
    ..These studies provide new insight into the ability of family B G protein-coupled receptors to associate with each other in cells...
  68. ncbi request reprint Study of recurrence after surgical resection of intraductal papillary mucinous neoplasm of the pancreas
    Suresh T Chari
    Division of Gastroenterology and Hepatology, Mayo Clinic, Rochester, Minnesota 55905, USA
    Gastroenterology 123:1500-7. 2002
    ....
  69. ncbi request reprint Analysis of the cellular and molecular mechanisms of trophic action of a misspliced form of the type B cholecystokinin receptor present in colon and pancreatic cancer
    Zhi jie Cheng
    Mayo Clinic Cancer Center, Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic in Scottsdale, 13400 East Shea Boulevard, Scottsdale, AZ 85259, USA
    Cancer Lett 222:95-105. 2005
    ..Thus, this variant receptor can potentiate peptide-stimulated signaling and trophic action and may contribute to the proliferation of neoplasms expressing it...
  70. ncbi request reprint Fluorescence resonance energy transfer analysis of the antagonist- and partial agonist-occupied states of the cholecystokinin receptor
    Kaleeckal G Harikumar
    Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    J Biol Chem 280:18631-5. 2005
    ..This supports the possibilities of changes in the conformation of the probe and/or the receptor induced by structurally similar ligands having distinct intrinsic biological activities...
  71. ncbi request reprint Demonstration of a specific site of covalent labeling of the human motilin receptor using a biologically active photolabile motilin analog
    Bunzo Matsuura
    Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic in Scottsdale, AZ 85259, USA
    J Pharmacol Exp Ther 313:1101-8. 2005
    ....
  72. ncbi request reprint Molecular approximation between a residue in the amino-terminal region of calcitonin and the third extracellular loop of the class B G protein-coupled calcitonin receptor
    Maoqing Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic Scottsdale, Scottsdale, Arizona 85259, USA
    J Biol Chem 279:31177-82. 2004
    ..These data are consistent with a common ligand binding mechanism for receptors in this important family...
  73. ncbi request reprint Measurement of intermolecular distances for the natural agonist Peptide docked at the cholecystokinin receptor expressed in situ using fluorescence resonance energy transfer
    Kaleeckal G Harikumar
    Department of Molecular Pharmacology and Experimental Therapeutics, Cancer Center, Mayo Clinic Scottsdale, Scottsdale, AZ 85259, USA
    Mol Pharmacol 65:28-35. 2004
    ..This approach provides the initial insights into the conformation of extracellular loop regions of this receptor and establishes clear differences from analogous loops in the rhodopsin crystal structure...
  74. ncbi request reprint Importance of the amino terminus in secretin family G protein-coupled receptors. Intrinsic photoaffinity labeling establishes initial docking constraints for the calcitonin receptor
    Maoqing Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic Scottsdale, Scottsdale, Arizona 85259, USA
    J Biol Chem 279:1167-75. 2004
    ..These data are consistent with affinity labeling of other members of the class B G protein-coupled receptors using analogous probes and may suggest a common ligand binding mechanism for this family...
  75. ncbi request reprint Molecular pharmacology of the secretin receptor
    Maoqing Dong
    Center for Basic Research in Digestive Diseases, Departments of Internal Medicine and Biochemistry Molecular Biology, Mayo Clinic and Foundation, Guggenheim 17, Mayo Clinic, Rochester, MN 55905, USA
    Receptors Channels 8:189-200. 2002
    ..This receptor is regulated by agonist-stimulated phosphorylation and internalization, with details dependent on the cellular environment...
  76. ncbi request reprint Differential spatial approximation between secretin and its receptor residues in active and inactive conformations demonstrated by photoaffinity labeling
    Maoqing Dong
    Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    Mol Endocrinol 20:1688-98. 2006
    ....
  77. ncbi request reprint Molecular approximation between residue 10 of secretin and its receptor demonstrated by photoaffinity labeling
    Maoqing Dong
    Mayo Clinic Scottsdale, 13400 East Shea Blvd, Scottsdale, AZ 85259, USA
    Ann N Y Acad Sci 1070:243-7. 2006
    ..These data provide an important constraint for modeling the agonist-bound G protein-coupled secretin receptor and should add substantially to our current understanding of the molecular basis of ligand binding of this important receptor...
  78. ncbi request reprint Fluorescent indicators distributed throughout the pharmacophore of cholecystokinin provide insights into distinct modes of binding and activation of type A and B cholecystokinin receptors
    Kaleeckal G Harikumar
    Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    J Biol Chem 281:27072-80. 2006
    ..Although both type A and B cholecystokinin receptors bind cholecystokinin with high affinity, resulting in fully efficacious biological responses, these receptors utilize distinct molecular modes of binding...
  79. ncbi request reprint Critical contributions of amino-terminal extracellular domains in agonist binding and activation of secretin and vasoactive intestinal polypeptide receptors. Studies of chimeric receptors
    M H Holtmann
    Center for Basic Research in Digestive Diseases, Mayo Clinic and Foundation, Rochester, Minnesota 55905, USA
    J Biol Chem 270:14394-8. 1995
    ..Thus, the amino terminus of secretin and VIP receptors plays a key role in agonist recognition and responsiveness, with the first loop playing a critical complementary role for the secretin receptor...
  80. ncbi request reprint Environment and mobility of a series of fluorescent reporters at the amino terminus of structurally related peptide agonists and antagonists bound to the cholecystokinin receptor
    Kaleeckal G Harikumar
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic and Foundation, Rochester, Minnesota 55905, USA
    J Biol Chem 277:18552-60. 2002
    ....
  81. pmc Secretin receptor oligomers form intracellularly during maturation through receptor core domains
    Cayle S Lisenbee
    Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    Biochemistry 45:8216-26. 2006
    ..We conclude that secretin receptor oligomerization occurs through -GxxxG- motif-independent interactions of transmembrane segments during the maturation of nascent molecules...
  82. ncbi request reprint Refinement of the conformation of a critical region of charge-charge interaction between cholecystokinin and its receptor
    Xi Qin Ding
    Center for Basic Research in Digestive Diseases, Department of Internal Medicine, Mayo Clinic and Foundation, Rochester, Minnesota 55905, USA
    Mol Pharmacol 61:1041-52. 2002
    ..The strong correlation between predicted and experimental results support the reported refinement in the three-dimensional structure of the CCK-occupied receptor...
  83. ncbi request reprint Islet amyloid polypeptide is not a satisfactory marker for detecting pancreatic cancer
    S T Chari
    Division of Gastroenterology and Hepatology, Mayo Clinic, Rochester, Minnesota 55905, USA
    Gastroenterology 121:640-5. 2001
    ....
  84. pmc Structural and functional insights into the juxtamembranous amino-terminal tail and extracellular loop regions of class B GPCRs
    M Dong
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ, USA
    Br J Pharmacol 171:1085-101. 2014
    ....
  85. ncbi request reprint Molecular cloning and functional expression of the human gallbladder cholecystokinin A receptor
    C D Ulrich
    Center for Basic Research in Digestive Diseases, Mayo Clinic, Rochester, MN 55905
    Biochem Biophys Res Commun 193:204-11. 1993
    ..This should provide an important resource for the analysis of the role of this receptor in human physiology and pathophysiology...
  86. ncbi request reprint Glucose and forskolin regulate IAPP gene expression through different signal transduction pathways
    W Q Ding
    Department of Medicine, Mayo Clinic and Foundation, Rochester, Minnesota 55905, USA
    Am J Physiol Endocrinol Metab 281:E938-45. 2001
    ..These results demonstrate parallel and distinct regulatory pathways involved in glucose- and forskolin-induced IAPP gene expression in this model beta-cell system...
  87. ncbi request reprint Agonist-dependent dissociation of oligomeric complexes of G protein-coupled cholecystokinin receptors demonstrated in living cells using bioluminescence resonance energy transfer
    Z J Cheng
    Center for Basic Research in Digestive Diseases, Department of Medicine, Mayo Clinic and Foundation, Rochester, Minnesota 55905, USA
    J Biol Chem 276:48040-7. 2001
    ..This provides the first evidence for CCK receptor oligomerization in living cells, with insights that the active conformation of this receptor dissociates these complexes in a phosphorylation-independent manner...
  88. ncbi request reprint Abnormal processing of the human cholecystokinin receptor gene in association with gallstones and obesity
    L J Miller
    Center for Basic Research in Digestive Diseases, Mayo Clinic, Rochester, Minnesota, USA
    Gastroenterology 109:1375-80. 1995
    ..The aim of this study was to determine the abundance, functional significance, and mechanism for generating this gene product...
  89. ncbi request reprint International Union of Pharmacology. XXXV. The glucagon receptor family
    Kelly E Mayo
    Department of Biochemistry, Molecular Biology and Cell Biology, Northwestern University, Evanston, Illinois, USA
    Pharmacol Rev 55:167-94. 2003
    ....
  90. ncbi request reprint Signaling from novel splice variants of hormone receptors in cancer
    Wei Qun Ding
    Center for Basic Research in Digestive Diseases, Mayo Clinic and Foundation, Rochester, MN 55905, USA
    Int J Gastrointest Cancer 31:31-9. 2002
    ..This review summarizes recent findings on the signaling of novel variants of hormone receptors, including human HER-2/neu, the secretin receptor, the CCK-B/gastrin receptor and fibroblast growth factor receptor-2...
  91. ncbi request reprint Moleular models for cholecystokinin-A receptor
    Eric S Dawson
    Department of Chemistry, Vanderbilt University, Center for Structural Biology, Nashville, TN 37235 1822, USA
    Pharmacol Toxicol 91:290-6. 2002
    ..2002; Escrieut et al. 2002). Here, we review details of the various models and evaluate the impact of selected experimental data sets on model development...
  92. ncbi request reprint Fluorescence characteristics of hydrophobic partial agonist probes of the cholecystokinin receptor
    Kaleeckal G Harikumar
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic Cancer Center, Mayo Clinic, 13400 E Shea Blvd, Scottsdale, AZ 85259, USA
    Biosci Rep 26:89-100. 2006
    ..These data suggest that the partially activated conformational state of this receptor is more closely related to its fully active state than to its inactive state...
  93. ncbi request reprint Mutational analysis of predicted intracellular loop domains of human motilin receptor
    Hitoo Tokunaga
    Department of Gastroenterology and Metabology, Ehime University Graduate School of Medicine, Shitsukawa 454, Tohon, Ehime 791 0295, Japan
    Am J Physiol Gastrointest Liver Physiol 294:G460-6. 2008
    ..The identification of functionally important residues in the predicted cytosolic face provides strong candidates for playing roles in receptor-G protein interaction...
  94. ncbi request reprint Targeting the RNA splicing machinery as a novel treatment strategy for pancreatic carcinoma
    Gregory M Hayes
    Mayo Clinic Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, 13400 East Shea Boulevard, Scottsdale, AZ 85259, USA
    Cancer Res 66:3819-27. 2006
    ....
  95. ncbi request reprint Secretin receptors in the human liver: expression in biliary tract and cholangiocarcinoma, but not in hepatocytes or hepatocellular carcinoma
    Meike Korner
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Bern, Murtenstrasse 31, P O Box 62, CH 3010 Bern, Switzerland
    J Hepatol 45:825-35. 2006
    ..The secretin receptor expression was investigated in the human liver because the liver is a physiological secretin target and because novel diagnostic and treatment modalities are needed for liver cancer...
  96. ncbi request reprint Differential contributions of motilin receptor extracellular domains for peptide and non-peptidyl agonist binding and activity
    Bunzo Matsuura
    Third Department of Internal Medicine, Ehime University School of Medicine, Shitsukawa 454, Tohon, Ehime 791 0295, Japan
    J Biol Chem 281:12390-6. 2006
    ....
  97. pmc Secretin receptors in normal and diseased human pancreas: marked reduction of receptor binding in ductal neoplasia
    Meike Korner
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology of the University of Bern, Murtenstrasse 31, PO Box 62, CH 3010 Bern, Switzerland
    Am J Pathol 167:959-68. 2005
    ..Reduced secretin binding in pancreatic ductal tumors may relate to (alternatively spliced) secretin receptor isoforms. Thus, secretin receptors in pancreatic tumors may represent potential clinical targets...
  98. pmc Benzodiazepine ligands can act as allosteric modulators of the Type 1 cholecystokinin receptor
    Fan Gao
    Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, 13400 East Shea Boulevard, Scottsdale, AZ 85259, USA
    Bioorg Med Chem Lett 18:4401-4. 2008
    ..The allosteric nature of benzodiazepine binding to the CCK(1) receptor provides new opportunities for small molecule drug development...
  99. ncbi request reprint Insights into interactions between the alpha-helical region of the salmon calcitonin antagonists and the human calcitonin receptor using photoaffinity labeling
    Vi Pham
    Howard Florey Institute, The University of Melbourne, Victoria 3010, Australia
    J Biol Chem 280:28610-22. 2005
    ..The model was also consistent with cooperative interaction between the receptor amino terminus and the receptor core...
  100. pmc Transmembrane segment peptides can disrupt cholecystokinin receptor oligomerization without affecting receptor function
    Kaleeckal G Harikumar
    Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona 85259, USA
    Biochemistry 45:14706-16. 2006
    ....
  101. ncbi request reprint Disulfide bond structure and accessibility of cysteines in the ectodomain of the cholecystokinin receptor: specific mono-reactive receptor constructs examine charge-sensitivity of loop regions
    Xi Qin Ding
    Department of Molecular Pharmacology and Experimental Therapeutics, Cancer Center, Mayo Clinic Scottsdale, 13400 East Shea Boulevard, Scottsdale, AZ 85259, USA
    Receptors Channels 9:83-91. 2003
    ..This pattern was repeated in mutants having the same residue directly replaced with a charged residue...