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Mast Cell Degranulation and Fibroblast Activation in the Morphine-induced Spinal Mass: Role of Mas-related G Protein-coupled Receptor Signaling.

Yaksh TL, Eddinger KA, Kokubu S, Wang Z, DiNardo A, Ramachandran R, Zhu Y, He Y, Weren F, Quang D, Malkmus SA, Lansu K, Kroeze WK, Eliceiri B, Steinauer JJ, Schiller PW, Gmeiner P, Page LM, Hildebrand KR.

Anesthesiology. 2019 Jul;131(1):132-147. doi: 10.1097/ALN.0000000000002730.


Solid-Phase Azopeptide Diels-Alder Chemistry for Aza-pipecolyl Residue Synthesis To Study Peptide Conformation.

Chingle R, Mulumba M, Chung NN, Nguyen TM, Ong H, Ballet S, Schiller PW, Lubell WD.

J Org Chem. 2019 May 17;84(10):6006-6016. doi: 10.1021/acs.joc.8b03283. Epub 2019 Apr 26.


Equipotent enantiomers of cyclic opioid peptides at μ opioid receptor.

Weltrowska G, Nguyen TM, Chung NN, Wilkes BC, Schiller PW.

Pept Sci (Hoboken). 2019 Jan;111(1). pii: e24078. doi: 10.1002/pep2.24078. Epub 2018 May 25.


Characterization of Analgesic Actions of the Chronic Intrathecal Infusion of H-Dmt-D-Arg-Phe-Lys-NH2 in Rat.

Kokubu S, Eddinger KA, Yamaguchi S, Huerta-Esquivel LL, Schiller PW, Yaksh TL.

Neuromodulation. 2019 Oct;22(7):781-789. doi: 10.1111/ner.12925. Epub 2019 Feb 22.


Characterization of the antinociceptive effects of intrathecal DALDA peptides following bolus intrathecal delivery.

Kokubu S, Eddinger KA, Nguyen TM, Huerta-Esquivel LL, Yamaguchi S, Schiller PW, Yaksh TL.

Scand J Pain. 2019 Jan 28;19(1):193-206. doi: 10.1515/sjpain-2018-0120.


Strengthening peptide-based drug activity with novel glyconanoparticle.

Lewicky JD, Martel AL, Fraleigh NL, Boraman A, Nguyen TM, Schiller PW, Shiao TC, Roy R, Le HT.

PLoS One. 2018 Sep 27;13(9):e0204472. doi: 10.1371/journal.pone.0204472. eCollection 2018.


Corrigendum to "Chemical space screening around Phe3 in opioid peptides: Modulating µ versus δ agonism by Suzuki-Miyaura cross-couplings" [Bioorg. Med. Chem. Lett. 28(13) (2018) 2320-2323].

Willemse T, Eiselt E, Hollanders K, Schepens W, van Vlijmen HWT, Chung NN, Blais V, Holleran B, Longpré JM, Schiller PW, Maes BUW, Sarret P, Gendron L, Ballet S.

Bioorg Med Chem Lett. 2018 Nov 1;28(20):3418. doi: 10.1016/j.bmcl.2018.08.023. Epub 2018 Sep 5. No abstract available.


Chemical space screening around Phe3 in opioid peptides: Modulating µ versus δ agonism by Suzuki-Miyaura cross-couplings.

Willemse T, Eiselt E, Hollanders K, Schepens W, van Vlijmen HWT, Chung NN, Blais V, Holleran B, Longpré JM, Schiller PW, Maes BUW, Sarret P, Gendron L, Ballet S.

Bioorg Med Chem Lett. 2018 Jul 15;28(13):2320-2323. doi: 10.1016/j.bmcl.2018.05.015. Epub 2018 May 12. Erratum in: Bioorg Med Chem Lett. 2018 Nov 1;28(20):3418.


A Genetically Encoded Biosensor Reveals Location Bias of Opioid Drug Action.

Stoeber M, Jullié D, Lobingier BT, Laeremans T, Steyaert J, Schiller PW, Manglik A, von Zastrow M.

Neuron. 2018 Jun 6;98(5):963-976.e5. doi: 10.1016/j.neuron.2018.04.021. Epub 2018 May 10.


Protective Effect of a Mitochondria-Targeted Peptide against the Development of Chemotherapy-Induced Peripheral Neuropathy in Mice.

Toyama S, Shimoyama N, Szeto HH, Schiller PW, Shimoyama M.

ACS Chem Neurosci. 2018 Jul 18;9(7):1566-1571. doi: 10.1021/acschemneuro.8b00013. Epub 2018 Apr 18.


χ-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.

Van der Poorten O, Van Den Hauwe R, Eiselt E, Betti C, Guillemyn K, Chung NN, Hallé F, Bihel F, Schiller PW, Tourwé D, Sarret P, Gendron L, Ballet S.

ACS Med Chem Lett. 2017 Oct 4;8(11):1177-1182. doi: 10.1021/acsmedchemlett.7b00347. eCollection 2017 Nov 9.


Analgesic Properties of Opioid/NK1 Multitarget Ligands with Distinct in Vitro Profiles in Naive and Chronic Constriction Injury Mice.

Starnowska J, Costante R, Guillemyn K, Popiolek-Barczyk K, Chung NN, Lemieux C, Keresztes A, Van Duppen J, Mollica A, Streicher J, Vanden Broeck J, Schiller PW, Tourwé D, Mika J, Ballet S, Przewlocka B.

ACS Chem Neurosci. 2017 Oct 18;8(10):2315-2324. doi: 10.1021/acschemneuro.7b00226. Epub 2017 Jul 26.


A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinity μ Opioid Receptor Antagonists.

Weltrowska G, Nguyen TM, Chung NN, Wood J, Ma X, Guo J, Wilkes BC, Ge Y, Laferrière A, Coderre TJ, Schiller PW.

J Med Chem. 2016 Oct 13;59(19):9243-9254. doi: 10.1021/acs.jmedchem.6b01200. Epub 2016 Oct 3.


Prorenin/renin receptor blockade promotes a healthy fat distribution in obese mice.

Tan P, Blais C, Nguyen TM, Schiller PW, Gutkowska J, Lavoie JL.

Obesity (Silver Spring). 2016 Sep;24(9):1946-54. doi: 10.1002/oby.21592. Epub 2016 Jul 26.


Molecular Pharmacology of δ-Opioid Receptors.

Gendron L, Cahill CM, von Zastrow M, Schiller PW, Pineyro G.

Pharmacol Rev. 2016 Jul;68(3):631-700. doi: 10.1124/pr.114.008979. Review.


[Dmt(1)]DALDA analogues modified with tyrosine analogues at position 1.

Cai Y, Lu D, Chen Z, Ding Y, Chung NN, Li T, Schiller PW.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3629-31. doi: 10.1016/j.bmcl.2016.06.003. Epub 2016 Jun 3.


Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.

Guillemyn K, Starnowska J, Lagard C, Dyniewicz J, Rojewska E, Mika J, Chung NN, Utard V, Kosson P, Lipkowski AW, Chevillard L, Arranz-Gibert P, Teixidó M, Megarbane B, Tourwé D, Simonin F, Przewlocka B, Schiller PW, Ballet S.

J Med Chem. 2016 Apr 28;59(8):3777-92. doi: 10.1021/acs.jmedchem.5b01976. Epub 2016 Apr 14.


Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.

Betti C, Starnowska J, Mika J, Dyniewicz J, Frankiewicz L, Novoa A, Bochynska M, Keresztes A, Kosson P, Makuch W, Van Duppen J, Chung NN, Vanden Broeck J, Lipkowski AW, Schiller PW, Janssens F, Ceusters M, Sommen F, Meert T, Przewlocka B, Tourwé D, Ballet S.

ACS Med Chem Lett. 2015 Oct 31;6(12):1209-14. doi: 10.1021/acsmedchemlett.5b00359. eCollection 2015 Dec 10.


The bifunctional μ opioid agonist/antioxidant [Dmt(1)]DALDA is a superior analgesic in an animal model of complex regional pain syndrome-type i.

Schiller PW, Nguyen TM, Saray A, Poon AW, Laferrière A, Coderre TJ.

ACS Chem Neurosci. 2015 Nov 18;6(11):1789-93. doi: 10.1021/acschemneuro.5b00228. Epub 2015 Sep 14.


Structural basis for bifunctional peptide recognition at human δ-opioid receptor.

Fenalti G, Zatsepin NA, Betti C, Giguere P, Han GW, Ishchenko A, Liu W, Guillemyn K, Zhang H, James D, Wang D, Weierstall U, Spence JC, Boutet S, Messerschmidt M, Williams GJ, Gati C, Yefanov OM, White TA, Oberthuer D, Metz M, Yoon CH, Barty A, Chapman HN, Basu S, Coe J, Conrad CE, Fromme R, Fromme P, Tourwé D, Schiller PW, Roth BL, Ballet S, Katritch V, Stevens RC, Cherezov V.

Nat Struct Mol Biol. 2015 Mar;22(3):265-8. doi: 10.1038/nsmb.2965. Epub 2015 Feb 16.


Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics.

Guillemyn K, Kleczkowska P, Lesniak A, Dyniewicz J, Van der Poorten O, Van den Eynde I, Keresztes A, Varga E, Lai J, Porreca F, Chung NN, Lemieux C, Mika J, Rojewska E, Makuch W, Van Duppen J, Przewlocka B, Vanden Broeck J, Lipkowski AW, Schiller PW, Tourwé D, Ballet S.

Eur J Med Chem. 2015 Mar 6;92:64-77. doi: 10.1016/j.ejmech.2014.12.033. Epub 2014 Dec 19.


'Carba'-carfentanil (trans isomer): a μ opioid receptor (MOR) partial agonist with a distinct binding mode.

Weltrowska G, Lemieux C, Chung NN, Guo JJ, Wilkes BC, Schiller PW.

Bioorg Med Chem. 2014 Sep 1;22(17):4581-6. doi: 10.1016/j.bmc.2014.07.033. Epub 2014 Jul 29.


Impact of the prorenin/renin receptor on the development of obesity and associated cardiometabolic risk factors.

Tan P, Shamansurova Z, Bisotto S, Michel C, Gauthier MS, Rabasa-Lhoret R, Nguyen TM, Schiller PW, Gutkowska J, Lavoie JL.

Obesity (Silver Spring). 2014 Oct;22(10):2201-9. doi: 10.1002/oby.20844. Epub 2014 Jul 10.


One-pot isomerization-cross metathesis-reduction (ICMR) synthesis of lipophilic tetrapeptides.

Jida M, Betti C, Schiller PW, Tourwé D, Ballet S.

ACS Comb Sci. 2014 Jul 14;16(7):342-51. doi: 10.1021/co500020a. Epub 2014 Jun 18.


Inhibition of calpain reduces oxidative stress and attenuates endothelial dysfunction in diabetes.

Chen B, Zhao Q, Ni R, Tang F, Shan L, Cepinskas I, Cepinskas G, Wang W, Schiller PW, Peng T.

Cardiovasc Diabetol. 2014 May 3;13:88. doi: 10.1186/1475-2840-13-88.


In Vitro Membrane Permeation Studies and in Vivo Antinociception of Glycosylated Dmt1-DALDA Analogues.

Ballet S, Betti C, Novoa A, Tömböly C, Nielsen CU, Helms HC, Lesniak A, Kleczkowska P, Chung NN, Lipkowski AW, Brodin B, Tourwé D, Schiller PW.

ACS Med Chem Lett. 2014 Apr 10;5(4):352-357.


[Dmt(1)]DALDA analogues with enhanced μ opioid agonist potency and with a mixed μ/κ opioid activity profile.

Bai L, Li Z, Chen J, Chung NN, Wilkes BC, Li T, Schiller PW.

Bioorg Med Chem. 2014 Apr 1;22(7):2333-8. doi: 10.1016/j.bmc.2014.02.011. Epub 2014 Feb 19.


Endocytic profiles of δ-opioid receptor ligands determine the duration of rapid but not sustained cAMP responses.

Tudashki HB, Robertson DN, Schiller PW, Pineyro G.

Mol Pharmacol. 2014 Jan;85(1):148-61. doi: 10.1124/mol.113.089003. Epub 2013 Oct 30.


Ligand- and cell-dependent determinants of internalization and cAMP modulation by delta opioid receptor (DOR) agonists.

Charfi I, Nagi K, Mnie-Filali O, Thibault D, Balboni G, Schiller PW, Trudeau LE, Pineyro G.

Cell Mol Life Sci. 2014 Apr;71(8):1529-46.


N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile.

Weltrowska G, Nguyen TM, Chung NN, Wilkes BC, Schiller PW.

Bioorg Med Chem Lett. 2013 Sep 15;23(18):5082-5. doi: 10.1016/j.bmcl.2013.07.036. Epub 2013 Jul 23.


Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations.

Touati-Jallabe Y, Bojnik E, Legrand B, Mauchauffée E, Chung NN, Schiller PW, Benyhe S, Averlant-Petit MC, Martinez J, Hernandez JF.

J Med Chem. 2013 Jul 25;56(14):5964-5973. doi: 10.1021/jm4008592. Epub 2013 Jul 12.


Antinociceptive effects of two deltorphins analogs in the tail-immersion test in rats.

Kotlinska JH, Gibula-Bruzda E, Witkowska E, Chung NN, Schiller PW, Izdebski J.

Peptides. 2013 Jan;39:103-10. doi: 10.1016/j.peptides.2012.11.008. Epub 2012 Nov 23.


Conformational dynamics of Kir3.1/Kir3.2 channel activation via δ-opioid receptors.

Richard-Lalonde M, Nagi K, Audet N, Sleno R, Amraei M, Hogue M, Balboni G, Schiller PW, Bouvier M, Hébert TE, Pineyro G.

Mol Pharmacol. 2013 Feb;83(2):416-28. doi: 10.1124/mol.112.081950. Epub 2012 Nov 21.


Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.

Novoa A, Van Dorpe S, Wynendaele E, Spetea M, Bracke N, Stalmans S, Betti C, Chung NN, Lemieux C, Zuegg J, Cooper MA, Tourwé D, De Spiegeleer B, Schiller PW, Ballet S.

J Med Chem. 2012 Nov 26;55(22):9549-61. doi: 10.1021/jm3008079. Epub 2012 Nov 12.


Superior analgesic effect of H-Dmt-D-Arg-Phe-Lys-NH2 ([Dmt1]DALDA), a multifunctional opioid peptide, compared to morphine in a rat model of neuropathic pain.

Shimoyama M, Schiller PW, Shimoyama N, Toyama S, Szeto HH.

Chem Biol Drug Des. 2012 Nov;80(5):771-4. doi: 10.1111/cbdd.12003. Epub 2012 Sep 3.


Novel TIPP (H-Tyr-Tic-Phe-Phe-OH) analogues displaying a wide range of efficacies at the δ opioid receptor. Discovery of two highly potent and selective δ opioid agonists.

Berezowska I, Lemieux C, Chung NN, Ding J, Schiller PW.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1899-902. doi: 10.1016/j.bmcl.2012.01.063. Epub 2012 Jan 28.


In vivo antinociception of potent mu opioid agonist tetrapeptide analogues and comparison with a compact opioid agonist-neurokinin 1 receptor antagonist chimera.

Guillemyn K, Kleczkowska P, Novoa A, Vandormael B, Van den Eynde I, Kosson P, Asim MF, Schiller PW, Spetea M, Lipkowski AW, Tourwé D, Ballet S.

Mol Brain. 2012 Jan 30;5:4. doi: 10.1186/1756-6606-5-4.


Bifunctional μ/δ opioid peptides: variation of the type and length of the linker connecting the two components.

Ding J, Lemieux C, Chung NN, Schiller PW.

Chem Biol Drug Des. 2012 Feb;79(2):186-93. doi: 10.1111/j.1747-0285.2011.01268.x. Epub 2012 Jan 4.


Novel therapies targeting inner mitochondrial membrane--from discovery to clinical development.

Szeto HH, Schiller PW.

Pharm Res. 2011 Nov;28(11):2669-79. doi: 10.1007/s11095-011-0476-8. Epub 2011 Jun 3. Review.


MicroRNA-195 promotes palmitate-induced apoptosis in cardiomyocytes by down-regulating Sirt1.

Zhu H, Yang Y, Wang Y, Li J, Schiller PW, Peng T.

Cardiovasc Res. 2011 Oct 1;92(1):75-84. doi: 10.1093/cvr/cvr145. Epub 2011 May 27.


Cyclic enkephalin-deltorphin hybrids containing a carbonyl bridge: structure and opioid activity.

Ciszewska M, Ruszczyńska K, Oleszczuk M, Chung NN, Witkowska E, Schiller PW, Wójcik J, Izdebski J.

Acta Biochim Pol. 2011;58(2):225-30. Epub 2011 May 17.


Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist.

Ballet S, Feytens D, Buysse K, Chung NN, Lemieux C, Tumati S, Keresztes A, Van Duppen J, Lai J, Varga E, Porreca F, Schiller PW, Vanden Broeck J, Tourwé D.

J Med Chem. 2011 Apr 14;54(7):2467-76. doi: 10.1021/jm1016285. Epub 2011 Mar 17.


Influence of new deltorphin analogues on reinstatement of cocaine-induced conditioned place preference in rats.

Kotlinska JH, Gibula-Bruzda E, Pachuta A, Kunce D, Witkowska E, Chung NN, Schiller PW, Izdebski J.

Behav Pharmacol. 2010 Oct;21(7):638-48. doi: 10.1097/FBP.0b013e32833e7e97.


"Carba"-analogues of fentanyl are opioid receptor agonists.

Weltrowska G, Chung NN, Lemieux C, Guo J, Lu Y, Wilkes BC, Schiller PW.

J Med Chem. 2010 Apr 8;53(7):2875-81. doi: 10.1021/jm9019068.


Histone deacetylase-3 activation promotes tumor necrosis factor-alpha (TNF-alpha) expression in cardiomyocytes during lipopolysaccharide stimulation.

Zhu H, Shan L, Schiller PW, Mai A, Peng T.

J Biol Chem. 2010 Mar 26;285(13):9429-36. doi: 10.1074/jbc.M109.071274. Epub 2010 Jan 22.


N-methylated cyclic enkephalin analogues retain high opioid receptor binding affinity.

Weltrowska G, Berezowska I, Lemieux C, Chung NN, Wilkes BC, Schiller PW.

Chem Biol Drug Des. 2010 Feb;75(2):182-8. doi: 10.1111/j.1747-0285.2009.00919.x. Epub 2009 Dec 17.


Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1).

Berezowska I, Chung NN, Lemieux C, Wilkes BC, Schiller PW.

J Med Chem. 2009 Nov 12;52(21):6941-5. doi: 10.1021/jm9004913.


Cyclic opioid peptide agonists and antagonists obtained via ring-closing metathesis.

Berezowska I, Lemieux C, Chung NN, Wilkes BC, Schiller PW.

Chem Biol Drug Des. 2009 Oct;74(4):329-34. doi: 10.1111/j.1747-0285.2009.00867.x. Epub 2009 Aug 20.


Deltorphin analogs restricted via a urea bridge: structure and opioid activity.

Ciarkowski J, Zieleniak A, Rodziewicz-Motowidło S, Rusak Ł, Chung NN, Czaplewski C, Witkowska E, Schiller PW, Izdebski J.

Adv Exp Med Biol. 2009;611:491-2. No abstract available.


Conformation-activity relationships of cyclo-constrained mu/delta opioid agonists derived from the N-terminal tetrapeptide segment of dermorphin/deltorphin.

Ciarkowski J, Czaplewski C, Łuczak S, Rodziewicz-Motowidło S, Berezowska I, Schiller PW.

Adv Exp Med Biol. 2009;611:489-90. No abstract available.

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