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Toward a Universal μ-Agonist Template for Template-Based Alignment Modeling of Opioid Ligands.

Wu Z, Hruby VJ.

ACS Omega. 2019 Oct 9;4(17):17457-17476. doi: 10.1021/acsomega.9b02244. eCollection 2019 Oct 22.


Development of N-Acetylated Dipalmitoyl-S-Glyceryl Cysteine Analogs as Efficient TLR2/TLR6 Agonists.

Zhou Y, Banday AH, Hruby VJ, Cai M.

Molecules. 2019 Sep 27;24(19). pii: E3512. doi: 10.3390/molecules24193512.


Multivalent peptide and peptidomimetic ligands for the treatment of pain without toxicities and addiction.

Hruby VJ.

Peptides. 2019 Jun;116:63-67. doi: 10.1016/j.peptides.2019.02.004. Epub 2019 Apr 20. Review.


Hypothalamic γ-melanocyte stimulating hormone gene delivery reduces fat mass in male mice

Eerola K, Virtanen S, Vähätalo L, Ailanen L, Cai M, Hruby V, Savontaus M, Savontaus E.

J Endocrinol. 2018 Oct 1;239(1):19–31. doi: 10.1530/JOE-18-0009.


Correction to Design of MC1R Selective γ-MSH Analogues with Canonical Amino Acids Leads to Potency and Pigmentation.

Zhou Y, Mowlazadeh Haghighi S, Zoi I, Sawyer JR, Hruby VJ, Cai M.

J Med Chem. 2018 Oct 11;61(19):8945. doi: 10.1021/acs.jmedchem.8b01423. Epub 2018 Sep 25. No abstract available.


Hypothalamic γ-melanocyte stimulating hormone gene delivery reduces fat mass in male mice.

Eerola K, Virtanen S, Vähätalo L, Ailanen L, Cai M, Hruby V, Savontaus M, Savontaus E.

J Endocrinol. 2018 Jul 13. pii: JOE-18-0009. doi: 10.1530/JOE-18-0009. [Epub ahead of print]


Synthesis and Evaluation of a Novel Bivalent Selective Antagonist for the Mu-Delta Opioid Receptor Heterodimer that Reduces Morphine Withdrawal in Mice.

Olson KM, Keresztes A, Tashiro JK, Daconta LV, Hruby VJ, Streicher JM.

J Med Chem. 2018 Jul 26;61(14):6075-6086. doi: 10.1021/acs.jmedchem.8b00403. Epub 2018 Jul 16.


Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors.

Remesic M, Macedonio G, Mollica A, Porreca F, Hruby V, Lee YS.

Bioorg Med Chem. 2018 Jul 23;26(12):3664-3667. doi: 10.1016/j.bmc.2018.05.045. Epub 2018 May 26.


Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH2, leads to hMC1R selectivity and pigmentation.

Mowlazadeh Haghighi S, Zhou Y, Dai J, Sawyer JR, Hruby VJ, Cai M.

Eur J Med Chem. 2018 May 10;151:815-823. doi: 10.1016/j.ejmech.2018.04.021. Epub 2018 Apr 11.


Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.

Merlino F, Zhou Y, Cai M, Carotenuto A, Yousif AM, Brancaccio D, Di Maro S, Zappavigna S, Limatola A, Novellino E, Grieco P, Hruby VJ.

J Med Chem. 2018 May 10;61(9):4263-4269. doi: 10.1021/acs.jmedchem.8b00488. Epub 2018 Apr 25.


Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.

Durek T, Cromm PM, White AM, Schroeder CI, Kaas Q, Weidmann J, Ahmad Fuaad A, Cheneval O, Harvey PJ, Daly NL, Zhou Y, Dellsén A, Österlund T, Larsson N, Knerr L, Bauer U, Kessler H, Cai M, Hruby VJ, Plowright AT, Craik DJ.

J Med Chem. 2018 Apr 26;61(8):3674-3684. doi: 10.1021/acs.jmedchem.8b00170. Epub 2018 Apr 11.


Protection against β-amyloid neurotoxicity by a non-toxic endogenous N-terminal β-amyloid fragment and its active hexapeptide core sequence.

Forest KH, Alfulaij N, Arora K, Taketa R, Sherrin T, Todorovic C, Lawrence JLM, Yoshikawa GT, Ng HL, Hruby VJ, Nichols RA.

J Neurochem. 2018 Jan;144(2):201-217. doi: 10.1111/jnc.14257. Epub 2017 Dec 18.


Design of MC1R Selective γ-MSH Analogues with Canonical Amino Acids Leads to Potency and Pigmentation.

Zhou Y, Mowlazadeh Haghighi S, Zoi I, Sawyer JR, Hruby VJ, Cai M.

J Med Chem. 2017 Nov 22;60(22):9320-9329. doi: 10.1021/acs.jmedchem.7b01295. Epub 2017 Nov 13. Erratum in: J Med Chem. 2018 Oct 11;61(19):8945.


Synthesis and Investigation of Mixed μ-Opioid and δ-Opioid Agonists as Possible Bivalent Ligands for Treatment of Pain.

Vardanyan RS, Cain JP, Haghighi SM, Kumirov VK, McIntosh MI, Sandweiss AJ, Porreca F, Hruby VJ.

J Heterocycl Chem. 2017 Mar;54(2):1228-1235. doi: 10.1002/jhet.2696. Epub 2016 Jun 1.


Structural Insights into Selective Ligand-Receptor Interactions Leading to Receptor Inactivation Utilizing Selective Melanocortin 3 Receptor Antagonists.

Cai M, Marelli UK, Mertz B, Beck JG, Opperer F, Rechenmacher F, Kessler H, Hruby VJ.

Biochemistry. 2017 Aug 15;56(32):4201-4209. doi: 10.1021/acs.biochem.7b00407. Epub 2017 Aug 1.


Fluorescent-labeled bioconjugates of the opioid peptides biphalin and DPDPE incorporating fluorescein-maleimide linkers.

Stefanucci A, Lei W, Hruby VJ, Macedonio G, Luisi G, Carradori S, Streicher JM, Mollica A.

Future Med Chem. 2017 Jun;9(9):859-869. doi: 10.4155/fmc-2016-0232. Epub 2017 Jun 21.


Genetic and pharmacological antagonism of NK1 receptor prevents opiate abuse potential.

Sandweiss AJ, McIntosh MI, Moutal A, Davidson-Knapp R, Hu J, Giri AK, Yamamoto T, Hruby VJ, Khanna R, Largent-Milnes TM, Vanderah TW.

Mol Psychiatry. 2018 Aug;23(8):1745-1755. doi: 10.1038/mp.2017.102. Epub 2017 May 9.


Melanocortin 1 Receptor Signaling Regulates Cholesterol Transport in Macrophages.

Rinne P, Rami M, Nuutinen S, Santovito D, van der Vorst EPC, Guillamat-Prats R, Lyytikäinen LP, Raitoharju E, Oksala N, Ring L, Cai M, Hruby VJ, Lehtimäki T, Weber C, Steffens S.

Circulation. 2017 Jul 4;136(1):83-97. doi: 10.1161/CIRCULATIONAHA.116.025889. Epub 2017 Apr 27.


Recent Advances in the Realm of Allosteric Modulators for Opioid Receptors for Future Therapeutics.

Remesic M, Hruby VJ, Porreca F, Lee YS.

ACS Chem Neurosci. 2017 Jun 21;8(6):1147-1158. doi: 10.1021/acschemneuro.7b00090. Epub 2017 Apr 7. Review.


Structure-Activity Relationships of [des-Arg7]Dynorphin A Analogues at the κ Opioid Receptor.

Ramos-Colon CN, Lee YS, Remesic M, Hall SM, LaVigne J, Davis P, Sandweiss AJ, McIntosh MI, Hanson J, Largent-Milnes TM, Vanderah TW, Streicher J, Porreca F, Hruby VJ.

J Med Chem. 2016 Nov 23;59(22):10291-10298. Epub 2016 Nov 8.


Cyclic non-opioid dynorphin A analogues for the bradykinin receptors.

Lee YS, Remesic M, Ramos-Colon C, Hall SM, Kuzmin A, Rankin D, Porreca F, Lai J, Hruby VJ.

Bioorg Med Chem Lett. 2016 Nov 15;26(22):5513-5516. doi: 10.1016/j.bmcl.2016.10.010. Epub 2016 Oct 6.


Discovery of Stable Non-opioid Dynorphin A Analogues Interacting at the Bradykinin Receptors for the Treatment of Neuropathic Pain.

Hall SM, LeBaron L, Ramos-Colon C, Qu C, Xie JY, Porreca F, Lai J, Lee YS, Hruby VJ.

ACS Chem Neurosci. 2016 Dec 21;7(12):1746-1752. doi: 10.1021/acschemneuro.6b00258. Epub 2016 Sep 27.


Design of cyclized selective melanotropins.

Cai M, Hruby VJ.

Biopolymers. 2016 Nov;106(6):876-883. doi: 10.1002/bip.22976. Review.


Enkephalin-Fentanyl Multifunctional Opioids as Potential Neuroprotectants for Ischemic Stroke Treatment.

Islam MR, Yang L, Lee YS, Hruby VJ, Karamyan VT, Abbruscato TJ.

Curr Pharm Des. 2016;22(42):6459-6468. doi: 10.2174/1381612822666160720170124.


Various modifications of the amphipathic dynorphin A pharmacophore for rat brain bradykinin receptors.

Lee YS, Kupp R, Remesic MV, Ramos-Colon C, Hall SM, Chan C, Rankin D, Lai J, Porreca F, Hruby VJ.

Chem Biol Drug Des. 2016 Oct;88(4):615-9. doi: 10.1111/cbdd.12789. Epub 2016 Jun 6.


Cyclic Opioid Peptides.

Remesic M, Lee YS, Hruby VJ.

Curr Med Chem. 2016;23(13):1288-303. Review.


The Melanocortin Receptor System: A Target for Multiple Degenerative Diseases.

Cai M, Hruby VJ.

Curr Protein Pept Sci. 2016;17(5):488-96. Review.


Dynorphin A analogs for the treatment of chronic neuropathic pain.

Hall SM, Lee YS, Hruby VJ.

Future Med Chem. 2016;8(2):165-77. doi: 10.4155/fmc.15.164. Epub 2016 Jan 29. Review.


Tumor Targeting and Pharmacokinetics of a Near-Infrared Fluorescent-Labeled δ-Opioid Receptor Antagonist Agent, Dmt-Tic-Cy5.

Huynh AS, Estrella V, Stark VE, Cohen AS, Chen T, Casagni TJ, Josan JS, Lloyd MC, Johnson J, Kim J, Hruby VJ, Vagner J, Morse DL.

Mol Pharm. 2016 Feb 1;13(2):534-44. doi: 10.1021/acs.molpharmaceut.5b00760. Epub 2016 Jan 8.


Design synthesis and structure-activity relationship of 5-substituted (tetrahydronaphthalen-2yl)methyl with N-phenyl-N-(piperidin-2-yl)propionamide derivatives as opioid ligands.

Deekonda S, Rankin D, Davis P, Lai J, Vanderah TW, Porecca F, Hruby VJ.

Bioorg Med Chem. 2016 Jan 15;24(2):85-91. doi: 10.1016/j.bmc.2015.11.030. Epub 2015 Nov 23.


Enkephalin analogues with N-phenyl-N-(piperidin-2-ylmethyl)propionamide derivatives: Synthesis and biological evaluations.

Deekonda S, Cole J, Sunna S, Rankin D, Largent-Milnes TM, Davis P, BassiriRad NM, Lai J, Vanderah TW, Porecca F, Hruby VJ.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):222-7. doi: 10.1016/j.bmcl.2015.10.081. Epub 2015 Nov 3.


Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.

Carotenuto A, Merlino F, Cai M, Brancaccio D, Yousif AM, Novellino E, Hruby VJ, Grieco P.

J Med Chem. 2015 Dec 24;58(24):9773-8. doi: 10.1021/acs.jmedchem.5b01285. Epub 2015 Dec 16.


Discovery of Novel Multifunctional Ligands with μ/δ Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain.

Giri AK, Apostol CR, Wang Y, Forte BL, Largent-Milnes TM, Davis P, Rankin D, Molnar G, Olson KM, Porreca F, Vanderah TW, Hruby VJ.

J Med Chem. 2015 Nov 12;58(21):8573-83. doi: 10.1021/acs.jmedchem.5b01170. Epub 2015 Oct 30.


Contribution of regional brain melanocortin receptor subtypes to elevated activity energy expenditure in lean, active rats.

Shukla C, Koch LG, Britton SL, Cai M, Hruby VJ, Bednarek M, Novak CM.

Neuroscience. 2015 Dec 3;310:252-67. doi: 10.1016/j.neuroscience.2015.09.035. Epub 2015 Sep 25.


Design and synthesis of novel bivalent ligands (MOR and DOR) by conjugation of enkephalin analogues with 4-anilidopiperidine derivatives.

Deekonda S, Wugalter L, Rankin D, Largent-Milnes TM, Davis P, Wang Y, Bassirirad NM, Lai J, Kulkarni V, Vanderah TW, Porreca F, Hruby VJ.

Bioorg Med Chem Lett. 2015 Oct 15;25(20):4683-8. doi: 10.1016/j.bmcl.2015.07.064. Epub 2015 Jul 29.


Design, synthesis and biological evaluation of multifunctional ligands targeting opioid and bradykinin 2 receptors.

Deekonda S, Rankin D, Davis P, Lai J, Porreca F, Hruby VJ.

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4148-52. doi: 10.1016/j.bmcl.2015.08.014. Epub 2015 Aug 14.


Discovery of 5-substituted tetrahydronaphthalen-2yl-methyl with N-phenyl-N-(piperidin-4-yl)propionamide derivatives as potent opioid receptor ligands.

Deekonda S, Wugalter L, Kulkarni V, Rankin D, Largent-Milnes TM, Davis P, Bassirirad NM, Lai J, Vanderah TW, Porreca F, Hruby VJ.

Bioorg Med Chem. 2015 Sep 15;23(18):6185-94. doi: 10.1016/j.bmc.2015.07.071. Epub 2015 Aug 4.


Blockade of non-opioid excitatory effects of spinal dynorphin A at bradykinin receptors.

Lee YS, Hall SM, Ramos-Colon C, Remesic M, Rankin D, Vanderah TW, Porreca F, Lai J, Hruby VJ.

Receptors Clin Investig. 2015;2(1). pii: 517.


Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors.

Cai M, Marelli UK, Bao J, Beck JG, Opperer F, Rechenmacher F, McLeod KR, Zingsheim MR, Doedens L, Kessler H, Hruby VJ.

J Med Chem. 2015 Aug 27;58(16):6359-67. doi: 10.1021/acs.jmedchem.5b00102. Epub 2015 Aug 11.


Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities.

Nair P, Yamamoto T, Cowell S, Kulkarni V, Moye S, Navratilova E, Davis P, Ma SW, Vanderah TW, Lai J, Porreca F, Hruby VJ.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3716-20. doi: 10.1016/j.bmcl.2015.06.030. Epub 2015 Jun 15.


Design, synthesis, and biological evaluation of a series of bifunctional ligands of opioids/SSRIs.

Mehr-un-Nisa, Munawar MA, Lee YS, Rankin D, Munir J, Lai J, Khan MA, Hruby VJ.

Bioorg Med Chem. 2015 Mar 15;23(6):1251-9. doi: 10.1016/j.bmc.2015.01.047. Epub 2015 Feb 3.


Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.

Van der Poorten O, Fehér K, Buysse K, Feytens D, Zoi I, Schwartz SD, Martins JC, Tourwé D, Cai M, Hruby VJ, Ballet S.

ACS Med Chem Lett. 2014 Dec 3;6(2):192-7. doi: 10.1021/ml500436s. eCollection 2015 Feb 12.


Development and characterisation of novel fentanyl-delta opioid receptor antagonist based bivalent ligands.

Bird MF, Vardanyan RS, Hruby VJ, Calò G, Guerrini R, Salvadori S, Trapella C, McDonald J, Rowbotham DJ, Lambert DG.

Br J Anaesth. 2015 Apr;114(4):646-56. doi: 10.1093/bja/aeu454. Epub 2015 Feb 13.


Mechanical properties and microstructure of Ti-35.5Nb-5.7Ta beta alloy.

Bartakova S, Prachar P, Dvorak I, Hruby V, Vanek J, Pospichal M, Svoboda E, Martikan A, Konecna H, Sedlak I.

Bratisl Lek Listy. 2015;116(2):88-92.


Synthesis and evaluation of bivalent ligands for binding to the human melanocortin-4 receptor.

Fernandes SM, Lee YS, Gillies RJ, Hruby VJ.

Bioorg Med Chem. 2014 Nov 15;22(22):6360-5. doi: 10.1016/j.bmc.2014.09.055. Epub 2014 Oct 2.


Modification of amphipathic non-opioid dynorphin A analogues for rat brain bradykinin receptors.

Lee YS, Hall SM, Ramos-Colon C, Remesic M, LeBaron L, Nguyen A, Rankin D, Porreca F, Lai J, Hruby VJ.

Bioorg Med Chem Lett. 2015 Jan 1;25(1):30-3. doi: 10.1016/j.bmcl.2014.11.026. Epub 2014 Nov 15.


Cancer vaccine adjuvants--recent clinical progress and future perspectives.

Banday AH, Jeelani S, Hruby VJ.

Immunopharmacol Immunotoxicol. 2015 Feb;37(1):1-11. doi: 10.3109/08923973.2014.971963. Epub 2014 Oct 16. Review.


Structure-activity relationships of non-opioid [des-Arg(7)]-dynorphin A analogues for bradykinin receptors.

Lee YS, Rankin D, Hall SM, Ramos-Colon C, Ortiz JJ, Kupp R, Porreca F, Lai J, Hruby VJ.

Bioorg Med Chem Lett. 2014 Nov 1;24(21):4976-9. doi: 10.1016/j.bmcl.2014.09.033. Epub 2014 Sep 19.


Novel cyclic biphalin analogue with improved antinociceptive properties.

Mollica A, Carotenuto A, Novellino E, Limatola A, Costante R, Pinnen F, Stefanucci A, Pieretti S, Borsodi A, Samavati R, Zador F, Benyhe S, Davis P, Porreca F, Hruby VJ.

ACS Med Chem Lett. 2014 Jul 14;5(9):1032-6. doi: 10.1021/ml500241n. eCollection 2014 Sep 11.

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