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Aromatic-Amine Pendants Produce Highly Potent and Efficacious Mixed Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Peptidomimetics with Enhanced Metabolic Stability.

Henry S, Anand JP, Twarozynski JJ, Brinkel AC, Pogozheva ID, Sears BF, Jutkiewicz EM, Traynor JR, Mosberg HI.

J Med Chem. 2020 Feb 27;63(4):1671-1683. doi: 10.1021/acs.jmedchem.9b01818. Epub 2020 Feb 10.


Structure-Activity Relationships of 7-Substituted Dimethyltyrosine-Tetrahydroisoquinoline Opioid Peptidomimetics.

Montgomery D, Anand JP, Baber MA, Twarozynski JJ, Hartman JG, Delong LJ, Traynor JR, Mosberg HI.

Molecules. 2019 Nov 26;24(23). pii: E4302. doi: 10.3390/molecules24234302.


Novel Dimethyltyrosine-Tetrahydroisoquinoline Peptidomimetics with Aromatic Tetrahydroisoquinoline Substitutions Show in Vitro Kappa and Mu Opioid Receptor Agonism.

Montgomery D, Anand JP, Griggs NW, Fernandez TJ, Hartman JG, Sánchez-Santiago AA, Pogozheva ID, Traynor JR, Mosberg HI.

ACS Chem Neurosci. 2019 Aug 21;10(8):3682-3689. doi: 10.1021/acschemneuro.9b00250. Epub 2019 Jul 1.


Structural Simplification of a Tetrahydroquinoline-Core Peptidomimetic μ-Opioid Receptor (MOR) Agonist/δ-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability.

Henry SP, Fernandez TJ, Anand JP, Griggs NW, Traynor JR, Mosberg HI.

J Med Chem. 2019 Apr 25;62(8):4142-4157. doi: 10.1021/acs.jmedchem.9b00219. Epub 2019 Apr 12.


Dual Pharmacophores Explored via Structure-Activity Relationship (SAR) Matrix: Insights into Potent, Bifunctional Opioid Ligand Design.

Nastase AF, Anand JP, Bender AM, Montgomery D, Griggs NW, Fernandez TJ, Jutkiewicz EM, Traynor JR, Mosberg HI.

J Med Chem. 2019 Apr 25;62(8):4193-4203. doi: 10.1021/acs.jmedchem.9b00378. Epub 2019 Apr 9.


Synthesis and Pharmacological Evaluation of Novel C-8 Substituted Tetrahydroquinolines as Balanced-Affinity Mu/Delta Opioid Ligands for the Treatment of Pain.

Nastase AF, Griggs NW, Anand JP, Fernandez TJ, Harland AA, Trask TJ, Jutkiewicz EM, Traynor JR, Mosberg HI.

ACS Chem Neurosci. 2018 Jul 18;9(7):1840-1848. doi: 10.1021/acschemneuro.8b00139. Epub 2018 May 2.


In vivo effects of μ-opioid receptor agonist/δ-opioid receptor antagonist peptidomimetics following acute and repeated administration.

Anand JP, Kochan KE, Nastase AF, Montgomery D, Griggs NW, Traynor JR, Mosberg HI, Jutkiewicz EM.

Br J Pharmacol. 2018 Jun;175(11):2013-2027. doi: 10.1111/bph.14148. Epub 2018 Apr 24.


Placement of Hydroxy Moiety on Pendant of Peptidomimetic Scaffold Modulates Mu and Kappa Opioid Receptor Efficacy.

Harland AA, Pogozheva ID, Griggs NW, Trask TJ, Traynor JR, Mosberg HI.

ACS Chem Neurosci. 2017 Nov 15;8(11):2549-2557. doi: 10.1021/acschemneuro.7b00284. Epub 2017 Aug 25.


Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Ligands.

Harland AA, Bender AM, Griggs NW, Gao C, Anand JP, Pogozheva ID, Traynor JR, Jutkiewicz EM, Mosberg HI.

J Med Chem. 2016 May 26;59(10):4985-98. doi: 10.1021/acs.jmedchem.6b00308. Epub 2016 May 16.


The behavioral effects of a mixed efficacy antinociceptive peptide, VRP26, following chronic administration in mice.

Anand JP, Boyer BT, Mosberg HI, Jutkiewicz EM.

Psychopharmacology (Berl). 2016 Jul;233(13):2479-87. doi: 10.1007/s00213-016-4296-8. Epub 2016 Apr 27.


Rapid Synthesis of Boc-2',6'-dimethyl-l-tyrosine and Derivatives and Incorporation into Opioid Peptidomimetics.

Bender AM, Griggs NW, Gao C, Trask TJ, Traynor JR, Mosberg HI.

ACS Med Chem Lett. 2015 Oct 19;6(12):1199-203. doi: 10.1021/acsmedchemlett.5b00344. eCollection 2015 Dec 10.


Further Optimization and Evaluation of Bioavailable, Mixed-Efficacy μ-Opioid Receptor (MOR) Agonists/δ-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.

Harland AA, Yeomans L, Griggs NW, Anand JP, Pogozheva ID, Jutkiewicz EM, Traynor JR, Mosberg HI.

J Med Chem. 2015 Nov 25;58(22):8952-69. doi: 10.1021/acs.jmedchem.5b01270. Epub 2015 Nov 13.


Use of Functional Polymorphisms To Elucidate the Peptide Binding Site of TAP Complexes.

Geng J, Pogozheva ID, Mosberg HI, Raghavan M.

J Immunol. 2015 Oct 1;195(7):3436-48. doi: 10.4049/jimmunol.1500985. Epub 2015 Aug 31.


Asymmetric synthesis and in vitro and in vivo activity of tetrahydroquinolines featuring a diverse set of polar substitutions at the 6 position as mixed-efficacy μ opioid receptor/δ opioid receptor ligands.

Bender AM, Griggs NW, Anand JP, Traynor JR, Jutkiewicz EM, Mosberg HI.

ACS Chem Neurosci. 2015 Aug 19;6(8):1428-35. doi: 10.1021/acschemneuro.5b00100. Epub 2015 May 13.


Life at the border: adaptation of proteins to anisotropic membrane environment.

Pogozheva ID, Mosberg HI, Lomize AL.

Protein Sci. 2014 Sep;23(9):1165-96. doi: 10.1002/pro.2508. Epub 2014 Jul 2. Review.


Development of a bioavailable μ opioid receptor (MOPr) agonist, δ opioid receptor (DOPr) antagonist peptide that evokes antinociception without development of acute tolerance.

Mosberg HI, Yeomans L, Anand JP, Porter V, Sobczyk-Kojiro K, Traynor JR, Jutkiewicz EM.

J Med Chem. 2014 Apr 10;57(7):3148-53. doi: 10.1021/jm5002088. Epub 2014 Mar 26.


Translation of structure-activity relationships from cyclic mixed efficacy opioid peptides to linear analogues.

Anand JP, Porter-Barrus VR, Waldschmidt HV, Yeomans L, Pogozheva ID, Traynor JR, Mosberg HI.

Biopolymers. 2014 Jan;102(1):107-14. doi: 10.1002/bip.22437. Erratum in: Biopolymers. 2014 Sep;102(5):426.


Unveiling the membrane-binding properties of N-terminal and C-terminal regions of G protein-coupled receptor kinase 5 by combined optical spectroscopies.

Ding B, Glukhova A, Sobczyk-Kojiro K, Mosberg HI, Tesmer JJ, Chen Z.

Langmuir. 2014 Jan 28;30(3):823-31. doi: 10.1021/la404055a. Epub 2014 Jan 16.


Synthesis and evaluation of 4-substituted piperidines and piperazines as balanced affinity μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands.

Bender AM, Clark MJ, Agius MP, Traynor JR, Mosberg HI.

Bioorg Med Chem Lett. 2014 Jan 15;24(2):548-51. doi: 10.1016/j.bmcl.2013.12.021. Epub 2013 Dec 11.


Structural adaptations of proteins to different biological membranes.

Pogozheva ID, Tristram-Nagle S, Mosberg HI, Lomize AL.

Biochim Biophys Acta. 2013 Nov;1828(11):2592-608. doi: 10.1016/j.bbamem.2013.06.023. Epub 2013 Jun 27.


Opioid peptidomimetics: leads for the design of bioavailable mixed efficacy μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands.

Mosberg HI, Yeomans L, Harland AA, Bender AM, Sobczyk-Kojiro K, Anand JP, Clark MJ, Jutkiewicz EM, Traynor JR.

J Med Chem. 2013 Mar 14;56(5):2139-49. doi: 10.1021/jm400050y. Epub 2013 Feb 27.


Modulation of opioid receptor ligand affinity and efficacy using active and inactive state receptor models.

Anand JP, Purington LC, Pogozheva ID, Traynor JR, Mosberg HI.

Chem Biol Drug Des. 2012 Nov;80(5):763-70. doi: 10.1111/cbdd.12014. Epub 2012 Sep 12.


Rescue of misrouted GnRHR mutants reveals its constitutive activity.

Janovick JA, Pogozheva ID, Mosberg HI, Cornea A, Conn PM.

Mol Endocrinol. 2012 Jul;26(7):1179-88. doi: 10.1210/me.2012-1089. Epub 2012 May 17.


Conformationally restricted analogs of the direct thrombin inhibitor FM 19.

Girnys EA, Porter VR, Mosberg HI.

Bioorg Med Chem. 2011 Dec 15;19(24):7425-34. doi: 10.1016/j.bmc.2011.10.045. Epub 2011 Oct 20.


Development and in vitro characterization of a novel bifunctional μ-agonist/δ-antagonist opioid tetrapeptide.

Purington LC, Sobczyk-Kojiro K, Pogozheva ID, Traynor JR, Mosberg HI.

ACS Chem Biol. 2011 Dec 16;6(12):1375-81. doi: 10.1021/cb200263q. Epub 2011 Oct 11.


OPM database and PPM web server: resources for positioning of proteins in membranes.

Lomize MA, Pogozheva ID, Joo H, Mosberg HI, Lomize AL.

Nucleic Acids Res. 2012 Jan;40(Database issue):D370-6. doi: 10.1093/nar/gkr703. Epub 2011 Sep 2.


Salt bridges overlapping the gonadotropin-releasing hormone receptor agonist binding site reveal a coincidence detector for G protein-coupled receptor activation.

Janovick JA, Pogozheva ID, Mosberg HI, Conn PM.

J Pharmacol Exp Ther. 2011 Aug;338(2):430-42. doi: 10.1124/jpet.111.180869. Epub 2011 Apr 28.


Anisotropic solvent model of the lipid bilayer. 1. Parameterization of long-range electrostatics and first solvation shell effects.

Lomize AL, Pogozheva ID, Mosberg HI.

J Chem Inf Model. 2011 Apr 25;51(4):918-29. doi: 10.1021/ci2000192. Epub 2011 Mar 25.


Anisotropic solvent model of the lipid bilayer. 2. Energetics of insertion of small molecules, peptides, and proteins in membranes.

Lomize AL, Pogozheva ID, Mosberg HI.

J Chem Inf Model. 2011 Apr 25;51(4):930-46. doi: 10.1021/ci200020k. Epub 2011 Mar 25.


Pharmacological chaperones restore function to MC4R mutants responsible for severe early-onset obesity.

René P, Le Gouill C, Pogozheva ID, Lee G, Mosberg HI, Farooqi IS, Valenzano KJ, Bouvier M.

J Pharmacol Exp Ther. 2010 Dec;335(3):520-32. doi: 10.1124/jpet.110.172098. Epub 2010 Sep 8.


Structure-based design of residue 1 analogs of the direct thrombin inhibitor pentapeptide FM 19.

Girnys EA, Sobczyk-Kojiro K, Mosberg HI.

Chem Biol Drug Des. 2010 Jan;75(1):35-9. doi: 10.1111/j.1747-0285.2009.00915.x.


Pentapeptides displaying mu opioid receptor agonist and delta opioid receptor partial agonist/antagonist properties.

Purington LC, Pogozheva ID, Traynor JR, Mosberg HI.

J Med Chem. 2009 Dec 10;52(23):7724-31. doi: 10.1021/jm9007483.


Purification and functional reconstitution of monomeric mu-opioid receptors: allosteric modulation of agonist binding by Gi2.

Kuszak AJ, Pitchiaya S, Anand JP, Mosberg HI, Walter NG, Sunahara RK.

J Biol Chem. 2009 Sep 25;284(39):26732-41. doi: 10.1074/jbc.M109.026922. Epub 2009 Jun 19.


A covalent peptide inhibitor of RGS4 identified in a focused one-bead, one compound library screen.

Roof RA, Roman DL, Clements ST, Sobczyk-Kojiro K, Blazer LL, Ota S, Mosberg HI, Neubig RR.

BMC Pharmacol. 2009 May 22;9:9. doi: 10.1186/1471-2210-9-9.


Discovery of a ligand that compensates for decreased endogenous agonist potency of melanocortin-4 receptor polymorphisms identified in obese humans.

Haskell-Luevano C, Xiang Z, Wilczynski AM, Haskell KR, Andreasen AM, Litherland SA, Millard WJ, Pogozheva ID, Mosberg HI, Sorenson NB.

Adv Exp Med Biol. 2009;611:509-10. No abstract available.


Functional characterization and structural modeling of obesity associated mutations in the melanocortin 4 receptor.

Tan K, Pogozheva ID, Yeo GS, Hadaschik D, Keogh JM, Haskell-Leuvano C, O'Rahilly S, Mosberg HI, Farooqi IS.

Endocrinology. 2009 Jan;150(1):114-25. doi: 10.1210/en.2008-0721. Epub 2008 Sep 18.


Novel peptide ligands of RGS4 from a focused one-bead, one-compound library.

Roof RA, Sobczyk-Kojiro K, Turbiak AJ, Roman DL, Pogozheva ID, Blazer LL, Neubig RR, Mosberg HI.

Chem Biol Drug Des. 2008 Aug;72(2):111-9. doi: 10.1111/j.1747-0285.2008.00687.x. Epub 2008 Jul 15.


Thrombostatin FM compounds: direct thrombin inhibitors - mechanism of action in vitro and in vivo.

Nieman MT, Burke F, Warnock M, Zhou Y, Sweigart J, Chen A, Ricketts D, Lucchesi BR, Chen Z, Di Cera E, Hilfinger J, Kim JS, Mosberg HI, Schmaier AH.

J Thromb Haemost. 2008 May;6(5):837-45. doi: 10.1111/j.1538-7836.2008.02937.x. Epub 2008 Feb 25.


The role of hydrophobic interactions in positioning of peripheral proteins in membranes.

Lomize AL, Pogozheva ID, Lomize MA, Mosberg HI.

BMC Struct Biol. 2007 Jun 29;7:44.


Peptide and small molecules rescue the functional activity and agonist potency of dysfunctional human melanocortin-4 receptor polymorphisms.

Xiang Z, Pogozheva ID, Sorenson NB, Wilczynski AM, Holder JR, Litherland SA, Millard WJ, Mosberg HI, Haskell-Luevano C.

Biochemistry. 2007 Jul 17;46(28):8273-87. Epub 2007 Jun 23.


Synthesis of novel peptide inhibitors of thrombin-induced platelet activation.

Burke FM, Warnock M, Schmaier AH, Mosberg HI.

Chem Biol Drug Des. 2006 Nov;68(5):235-8.


Positioning of proteins in membranes: a computational approach.

Lomize AL, Pogozheva ID, Lomize MA, Mosberg HI.

Protein Sci. 2006 Jun;15(6):1318-33.


Mechanism of action and structural requirements of constrained peptide inhibitors of RGS proteins.

Roof RA, Jin Y, Roman DL, Sunahara RK, Ishii M, Mosberg HI, Neubig RR.

Chem Biol Drug Des. 2006 Apr;67(4):266-74.


Molecular mechanism of the constitutive activation of the L250Q human melanocortin-4 receptor polymorphism.

Proneth B, Xiang Z, Pogozheva ID, Litherland SA, Gorbatyuk OS, Shaw AM, Millard WJ, Mosberg HI, Haskell-Luevano C.

Chem Biol Drug Des. 2006 Mar;67(3):215-29.


Behavioral and neurobiological effects of the enkephalinase inhibitor RB101 relative to its antidepressant effects.

Jutkiewicz EM, Torregrossa MM, Sobczyk-Kojiro K, Mosberg HI, Folk JE, Rice KC, Watson SJ, Woods JH.

Eur J Pharmacol. 2006 Feb 15;531(1-3):151-9. Epub 2006 Jan 25.


OPM: orientations of proteins in membranes database.

Lomize MA, Lomize AL, Pogozheva ID, Mosberg HI.

Bioinformatics. 2006 Mar 1;22(5):623-5. Epub 2006 Jan 5.


Peptidic delta opioid receptor agonists produce antidepressant-like effects in the forced swim test and regulate BDNF mRNA expression in rats.

Torregrossa MM, Jutkiewicz EM, Mosberg HI, Balboni G, Watson SJ, Woods JH.

Brain Res. 2006 Jan 19;1069(1):172-81. Epub 2005 Dec 20.


Homology modeling of opioid receptor-ligand complexes using experimental constraints.

Pogozheva ID, Przydzial MJ, Mosberg HI.

AAPS J. 2005 Oct 5;7(2):E434-48. Review.

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