HENRY MOSBERG

Summary

Affiliation: University of Michigan
Country: USA

Publications

  1. pmc Opioid Peptidomimetics: Leads for the Design of Bioavailable Mixed Efficacy μ Opioid Receptor (MOR) Agonist/δ Opioid Receptor (DOR) Antagonist Ligands
    Henry I Mosberg
    Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109, United States
    J Med Chem 56:2139-49. 2013
  2. pmc The role of hydrophobic interactions in positioning of peripheral proteins in membranes
    Andrei L Lomize
    Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, MI 48109 1065, USA
    BMC Struct Biol 7:44. 2007
  3. pmc A covalent peptide inhibitor of RGS4 identified in a focused one-bead, one compound library screen
    Rebecca A Roof
    Department of Pharmacology, University of Michigan, 1301 MSRB III SPC 5632, 1150 W, Medical Center Dr, Ann Arbor, MI 48109, USA
    BMC Pharmacol 9:9. 2009
  4. ncbi request reprint Development and validation of opioid ligand-receptor interaction models: the structural basis of mu vs delta selectivity
    H I Mosberg
    Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor 48109 1065, USA
    J Pept Res 60:329-35. 2002
  5. ncbi request reprint Roles of residues 3 and 4 in cyclic tetrapeptide ligand recognition by the kappa-opioid receptor
    M J Przydzial
    Department of Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109, USA
    J Pept Res 65:333-42. 2005
  6. ncbi request reprint Design of high affinity cyclic pentapeptide ligands for kappa-opioid receptors
    M J Przydzial
    Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, MI 48109, USA
    J Pept Res 66:255-62. 2005
  7. pmc Intracisternal nor-binaltorphimine distinguishes central and peripheral kappa-opioid antinociception in rhesus monkeys
    M C Ko
    Department of Pharmacology, Medical School, The University of Michigan, Ann Arbor, Michigan 48109 0632, USA
    J Pharmacol Exp Ther 291:1113-20. 1999
  8. ncbi request reprint Prediction of protein structure: the problem of fold multiplicity
    A L Lomize
    College of Pharmacy, University of Michigan, Ann Arbor 48109, USA
    Proteins . 1999
  9. pmc Quantification of helix-helix binding affinities in micelles and lipid bilayers
    Andrei L Lomize
    College of Pharmacy, University of Michigan, 428 Church St, Ann Arbor, MI 48109 1065, USA
    Protein Sci 13:2600-12. 2004
  10. ncbi request reprint Key residues defining the mu-opioid receptor binding pocket: a site-directed mutagenesis study
    A Mansour
    Mental Health Research Institute, University of Michigan, Ann Arbor 48109 0720, USA
    J Neurochem 68:344-53. 1997

Research Grants

Collaborators

Detail Information

Publications33

  1. pmc Opioid Peptidomimetics: Leads for the Design of Bioavailable Mixed Efficacy μ Opioid Receptor (MOR) Agonist/δ Opioid Receptor (DOR) Antagonist Ligands
    Henry I Mosberg
    Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109, United States
    J Med Chem 56:2139-49. 2013
    ....
  2. pmc The role of hydrophobic interactions in positioning of peripheral proteins in membranes
    Andrei L Lomize
    Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, MI 48109 1065, USA
    BMC Struct Biol 7:44. 2007
    ..Biological activity, stability, and conformations of these proteins depend on their spatial positions with respect to the lipid bilayer. However, these positions are usually undetermined...
  3. pmc A covalent peptide inhibitor of RGS4 identified in a focused one-bead, one compound library screen
    Rebecca A Roof
    Department of Pharmacology, University of Michigan, 1301 MSRB III SPC 5632, 1150 W, Medical Center Dr, Ann Arbor, MI 48109, USA
    BMC Pharmacol 9:9. 2009
    ..We recently described a focused one-bead, one-compound (OBOC) library screen to identify peptide inhibitors of RGS4. Here we extend our observations to include another peptide with a different mechanism of action...
  4. ncbi request reprint Development and validation of opioid ligand-receptor interaction models: the structural basis of mu vs delta selectivity
    H I Mosberg
    Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor 48109 1065, USA
    J Pept Res 60:329-35. 2002
    ..Testing this hypothesis by examining the binding of JOM-6 and several of its key analogs with specific micro receptor mutants is described. Our initial results are consistent with the proposed ligand-receptor interaction models...
  5. ncbi request reprint Roles of residues 3 and 4 in cyclic tetrapeptide ligand recognition by the kappa-opioid receptor
    M J Przydzial
    Department of Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109, USA
    J Pept Res 65:333-42. 2005
    ..The magnitude of this energy penalty depends on the nature of the fourth residue of the peptide (d-Pen or d-Cys) and correlates well with the observed kappa-receptor binding affinity...
  6. ncbi request reprint Design of high affinity cyclic pentapeptide ligands for kappa-opioid receptors
    M J Przydzial
    Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, MI 48109, USA
    J Pept Res 66:255-62. 2005
    ..Nonetheless, the high affinity KOR peptides in this series represent excellent leads for the development of structurally related, selective KOR ligands designed to exploit structurally specific features of KOR, MOR, and DOR...
  7. pmc Intracisternal nor-binaltorphimine distinguishes central and peripheral kappa-opioid antinociception in rhesus monkeys
    M C Ko
    Department of Pharmacology, Medical School, The University of Michigan, Ann Arbor, Michigan 48109 0632, USA
    J Pharmacol Exp Ther 291:1113-20. 1999
    ..Moreover, it provides a valuable pharmacological basis for further characterizing different sources of kappaOR-mediated effects, namely, from central or peripheral nervous system receptors...
  8. ncbi request reprint Prediction of protein structure: the problem of fold multiplicity
    A L Lomize
    College of Pharmacy, University of Michigan, Ann Arbor 48109, USA
    Proteins . 1999
    ....
  9. pmc Quantification of helix-helix binding affinities in micelles and lipid bilayers
    Andrei L Lomize
    College of Pharmacy, University of Michigan, 428 Church St, Ann Arbor, MI 48109 1065, USA
    Protein Sci 13:2600-12. 2004
    ..The energetics of amino acid substitutions in bacteriorhodopsin was complicated by specific binding of lipid and water molecules to cavities created in certain mutants...
  10. ncbi request reprint Key residues defining the mu-opioid receptor binding pocket: a site-directed mutagenesis study
    A Mansour
    Mental Health Research Institute, University of Michigan, Ann Arbor 48109 0720, USA
    J Neurochem 68:344-53. 1997
    ....
  11. pmc The transmembrane 7-alpha-bundle of rhodopsin: distance geometry calculations with hydrogen bonding constraints
    I D Pogozheva
    College of Pharmacy, University of Michigan, Ann Arbor 48109, USA
    Biophys J 72:1963-85. 1997
    ..The rhodopsin model and the published structure of bacteriorhodopsin have very similar retinal-binding pockets...
  12. ncbi request reprint kappa-Opioid receptor binding populations in rhesus monkey brain: relationship to an assay of thermal antinociception
    E R Butelman
    Department of Pharmacology, College of Pharmacy, University of Michigan, Ann Arbor, USA
    J Pharmacol Exp Ther 285:595-601. 1998
    ..Overall, the present results suggest that at least two functional kappa receptor populations may be present in rhesus monkey brain...
  13. ncbi request reprint Structure-based design, synthesis, and pharmacologic evaluation of peptide RGS4 inhibitors
    Y Jin
    Department of Medicinal Chemistry, The University of Michigan, Ann Arbor, MI 48109, USA
    J Pept Res 63:141-6. 2004
    ..These compounds should prove useful for elucidating RGS-mediated activity and serve as a starting point for the development of a novel class of therapeutic agent...
  14. ncbi request reprint Receptor-antagonist interactions in the complexes of agouti and agouti-related protein with human melanocortin 1 and 4 receptors
    Biao Xin Chai
    Department of Surgery, School of Medicine, University of Michigan, Ann Arbor, Michigan 48109, USA
    Biochemistry 44:3418-31. 2005
    ....
  15. ncbi request reprint OPM: orientations of proteins in membranes database
    Mikhail A Lomize
    College of Literature, Science and the Arts, University of Michigan, Ann Arbor, MI 48109 1065, USA
    Bioinformatics 22:623-5. 2006
    ..All coordinate files with the calculated membrane boundaries are available for downloading...
  16. pmc Behavioral and neurobiological effects of the enkephalinase inhibitor RB101 relative to its antidepressant effects
    Emily M Jutkiewicz
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, MI 48109 0632, USA
    Eur J Pharmacol 531:151-9. 2006
    ..v.) in rats. RB101 did not produce convulsions or seizures and did not alter BDNF mRNA expression. In conclusion, RB101 has the potential to produce antidepressant effects without convulsions...
  17. ncbi request reprint Molecular mechanism of the constitutive activation of the L250Q human melanocortin-4 receptor polymorphism
    Bettina Proneth
    Department of Medicinal Chemistry, University of Florida, PO Box 100485, Gainesville, FL 32610 0485, USA
    Chem Biol Drug Des 67:215-29. 2006
    ....
  18. pmc Positioning of proteins in membranes: a computational approach
    Andrei L Lomize
    College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109 1065, USA
    Protein Sci 15:1318-33. 2006
    ..Coordinates of all studied proteins with their membrane boundaries can be found in the Orientations of Proteins in Membranes (OPM) database:http://opm.phar.umich.edu/...
  19. ncbi request reprint Synthesis of novel peptide inhibitors of thrombin-induced platelet activation
    Fernanda M Burke
    Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, 428 Church Street, Ann Arbor, MI 48109 1065, USA
    Chem Biol Drug Des 68:235-8. 2006
    ....
  20. ncbi request reprint Peptide and small molecules rescue the functional activity and agonist potency of dysfunctional human melanocortin-4 receptor polymorphisms
    Zhimin Xiang
    Department of Medicinal Chemistry, University of Florida, Gainesville, Florida 32610, USA
    Biochemistry 46:8273-87. 2007
    ..Thus, these ligands could generically rescue the potency and stimulatory response of the abnormally functioning hMC4Rs studied and may provide tools to further clarify the molecular mechanism(s) involving these receptor modifications...
  21. pmc Peptidic delta opioid receptor agonists produce antidepressant-like effects in the forced swim test and regulate BDNF mRNA expression in rats
    Mary M Torregrossa
    Neuroscience Program, University of Michigan, Ann Arbor, MI 48109, USA
    Brain Res 1069:172-81. 2006
    ....
  22. ncbi request reprint Complex of an active mu-opioid receptor with a cyclic peptide agonist modeled from experimental constraints
    Carol B Fowler
    Department of Medicinal Chemistry, University of Michigan, 428 Church Street, Ann Arbor, Michigan 48109 1065, USA
    Biochemistry 43:15796-810. 2004
    ..In the active state, the binding pocket of the mu-receptor is complementary to the previously proposed receptor-bound conformation of JOM6...
  23. ncbi request reprint Refinement of a homology model of the mu-opioid receptor using distance constraints from intrinsic and engineered zinc-binding sites
    Carol B Fowler
    Department of Medicinal Chemistry, University of Michigan, 428 Church Street, Ann Arbor, Michigan 48109 1065, USA
    Biochemistry 43:8700-10. 2004
    ..Subsequent distance geometry refinement of the MOR model indicates that the rhodopsin-like alpha aneurism is likely absent in TM2 but present in TM5...
  24. pmc Interactions of human melanocortin 4 receptor with nonpeptide and peptide agonists
    Irina D Pogozheva
    Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109, USA
    Biochemistry 44:11329-41. 2005
    ....
  25. ncbi request reprint Mutagenesis and peptide analysis of the DRY motif in the alpha2A adrenergic receptor: evidence for alternate mechanisms in G protein-coupled receptors
    Duane A Chung
    Biophysics Research Division, The University of Michigan, Ann Arbor, MI 48109, USA
    Biochem Biophys Res Commun 293:1233-41. 2002
    ..These results indicate that the alpha2A AR does not follow the conventional GPCR mechanistic paradigm with respect to the function of the DRY motif...
  26. ncbi request reprint Structure-based design, synthesis, and activity of peptide inhibitors of RGS4 GAP activity
    Yafei Jin
    Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor 48109, USA
    Methods Enzymol 389:266-77. 2004
    ..These compounds should prove useful for elucidating RGS-mediated activity and serve as a starting point for the development of a novel class of therapeutic agent...
  27. pmc Activation of kappa-opioid receptors inhibits pruritus evoked by subcutaneous or intrathecal administration of morphine in monkeys
    M C Holden Ko
    Department of Pharmacology, Division of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109 0632, USA
    J Pharmacol Exp Ther 305:173-9. 2003
    ..This mechanism-based finding provides functional evidence in support of the clinical potential of KOR agonists as antipruritics in the presence of MOR agonist-induced pruritus...
  28. pmc Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity
    Bettina Proneth
    Department of Pharmacodynamics, University of Florida, Gainesville, Florida 32610, USA
    J Med Chem 51:5585-93. 2008
    ..These SAR studies provide experimental evidence that the molecular mechanism of antagonism at the mMC3R differentiates this subtype from the mMC4R...
  29. pmc Homology modeling of opioid receptor-ligand complexes using experimental constraints
    Irina D Pogozheva
    Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, MI 48109, USA
    AAPS J 7:E434-48. 2005
    ....
  30. pmc Membrane composition determines pardaxin's mechanism of lipid bilayer disruption
    Kevin J Hallock
    Department of Chemistry, University of Michigan, Ann Arbor, Michigan 48109, USA
    Biophys J 83:1004-13. 2002
    ..Considered together, these data demonstrate that the mechanism of P1a is dependent on membrane composition...
  31. ncbi request reprint Mechanism of action and structural requirements of constrained peptide inhibitors of RGS proteins
    Rebecca A Roof
    Department of Pharmacology, 1150 W Medical Center Dr, University of Michigan, Ann Arbor, MI 48109, USA
    Chem Biol Drug Des 67:266-74. 2006
    ..These data support the proposed mechanism of action of peptide RGS inhibitors, demonstrate their action in native cells, and provide a starting point for the design of RGS inhibitor drugs...
  32. ncbi request reprint NMR structure of the second intracellular loop of the alpha 2A adrenergic receptor: evidence for a novel cytoplasmic helix
    Duane A Chung
    Biophysics Research Division and Department of Pharmacology, The University of Michigan, Ann Arbor, Michigan 48109, USA
    Biochemistry 41:3596-604. 2002
    ..These data should lead to more accurate models of the intracellular surface of GPCRs and of receptor-mediated G protein activation...
  33. ncbi request reprint Amino acid ester prodrugs of floxuridine: synthesis and effects of structure, stereochemistry, and site of esterification on the rate of hydrolysis
    Balvinder S Vig
    Department of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109, USA
    Pharm Res 20:1381-8. 2003
    ..To synthesize amino acid ester prodrugs of floxuridine (FUdR) and to investigate the effects of structure, stereochemistry, and site of esterification of promoiety on the rates of hydrolysis of these prodrugs in Caco-2 cell homogenates...

Research Grants27

  1. CONFORMATION - SELECTIVITY RELATIONS OF OPIOID PEPTIDES
    HENRY MOSBERG; Fiscal Year: 2001
    ..These studies will be done in collaboration with Richard Houghten of Torrey Pines Institute for Molecular Studies. ..
  2. RESEARCH FACILITIES CONSTRUCTION
    HENRY MOSBERG; Fiscal Year: 2003
    ..The renovations proposed here will position to make important contributions in these areas by providing the infrastructure to support current funded research as well as exciting, new investigator initiated applications. ..
  3. CONFORMATION-SELECTIVITY RELATIONS OF OPIOID PEPTIDES
    HENRY MOSBERG; Fiscal Year: 2006
    ..abstract_text> ..
  4. CONFORMATION - SELECTIVITY RELATIONS OF OPIOID PEPTIDES
    HENRY ISAAC MOSBERG; Fiscal Year: 2010
    ....
  5. CONFORMATION- SELECTIVITY RELATIONS OF OPIOID PEPTIDES
    HENRY MOSBERG; Fiscal Year: 1993
    ..Our multidisciplinary, integrated approach provides us with all the tools necessary to pursue our goals in a reasonable and efficient manner...
  6. CONFORMATION-SELECTIVITY RELATIONS OF OPIOID PEPTIDES
    HENRY MOSBERG; Fiscal Year: 1991
    ..Comparison of the energies of these structures will address the reasonableness of the approach and may provide insight into binding energetics...
  7. CONFORMATION - SELECTIVITY RELATIONS OF OPIOID PEPTIDES
    HENRY MOSBERG; Fiscal Year: 2009
    ..Gaining a precise understanding of these interactions is the first step toward the design and development of opioid drugs with more tailored actions, especially opioids with reduced tolerance, dependence liability, and abuse potential. ..