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Peptide-based protease inhibitors from plants.

Hellinger R, Gruber CW.

Drug Discov Today. 2019 Sep;24(9):1877-1889. doi: 10.1016/j.drudis.2019.05.026. Epub 2019 Jun 3. Review.


Nature-Derived Peptides: A Growing Niche for GPCR Ligand Discovery.

Muratspahić E, Freissmuth M, Gruber CW.

Trends Pharmacol Sci. 2019 May;40(5):309-326. doi: 10.1016/ Epub 2019 Apr 5. Review.


Discovery of peptide probes to modulate oxytocin-type receptors of insects.

Keov P, Liutkevičiūtė Z, Hellinger R, Clark RJ, Gruber CW.

Sci Rep. 2018 Jul 3;8(1):10020. doi: 10.1038/s41598-018-28380-3.


Oxytocin-like signaling in ants influences metabolic gene expression and locomotor activity.

Liutkevičiūtė Z, Gil-Mansilla E, Eder T, Casillas-Pérez B, Di Giglio MG, Muratspahić E, Grebien F, Rattei T, Muttenthaler M, Cremer S, Gruber CW.

FASEB J. 2018 Jun 25:fj201800443. doi: 10.1096/fj.201800443. [Epub ahead of print]


Inhibition of Breast Cancer Cell Migration by Cyclotides Isolated from Pombalia calceolaria.

Pinto MEF, Najas JZG, Magalhães LG, Bobey AF, Mendonça JN, Lopes NP, Leme FM, Teixeira SP, Trovó M, Andricopulo AD, Koehbach J, Gruber CW, Cilli EM, Bolzani VS.

J Nat Prod. 2018 May 25;81(5):1203-1208. doi: 10.1021/acs.jnatprod.7b00969. Epub 2018 May 14.


Contractility Measurements of Human Uterine Smooth Muscle to Aid Drug Development.

Arrowsmith S, Keov P, Muttenthaler M, Gruber CW.

J Vis Exp. 2018 Jan 26;(131). doi: 10.3791/56639.


Subtle modifications to oxytocin produce ligands that retain potency and improved selectivity across species.

Muttenthaler M, Andersson Å, Vetter I, Menon R, Busnelli M, Ragnarsson L, Bergmayr C, Arrowsmith S, Deuis JR, Chiu HS, Palpant NJ, O'Brien M, Smith TJ, Wray S, Neumann ID, Gruber CW, Lewis RJ, Alewood PF.

Sci Signal. 2017 Dec 5;10(508). pii: eaan3398. doi: 10.1126/scisignal.aan3398.


Chemical Proteomics for Target Discovery of Head-to-Tail Cyclized Mini-Proteins.

Hellinger R, Thell K, Vasileva M, Muhammad T, Gunasekera S, Kümmel D, Göransson U, Becker CW, Gruber CW.

Front Chem. 2017 Oct 11;5:73. doi: 10.3389/fchem.2017.00073. eCollection 2017.


Cyclotides Isolated from an Ipecac Root Extract Antagonize the Corticotropin Releasing Factor Type 1 Receptor.

Fahradpour M, Keov P, Tognola C, Perez-Santamarina E, McCormick PJ, Ghassempour A, Gruber CW.

Front Pharmacol. 2017 Sep 25;8:616. doi: 10.3389/fphar.2017.00616. eCollection 2017.


Development of a human vasopressin V1a-receptor antagonist from an evolutionary-related insect neuropeptide.

Di Giglio MG, Muttenthaler M, Harpsøe K, Liutkeviciute Z, Keov P, Eder T, Rattei T, Arrowsmith S, Wray S, Marek A, Elbert T, Alewood PF, Gloriam DE, Gruber CW.

Sci Rep. 2017 Feb 1;7:41002. doi: 10.1038/srep41002.


Global map of oxytocin/vasopressin-like neuropeptide signalling in insects.

Liutkeviciute Z, Koehbach J, Eder T, Gil-Mansilla E, Gruber CW.

Sci Rep. 2016 Dec 13;6:39177. doi: 10.1038/srep39177.


An exploration of village-level uterotonic practices in Fenerive-Est, Madagascar.

Collins L, Mmari K, Mullany LC, Gruber CW, Favero R.

BMC Pregnancy Childbirth. 2016 Apr 1;16:69. doi: 10.1186/s12884-016-0858-3.


Oral activity of a nature-derived cyclic peptide for the treatment of multiple sclerosis.

Thell K, Hellinger R, Sahin E, Michenthaler P, Gold-Binder M, Haider T, Kuttke M, Liutkevičiūtė Z, Göransson U, Gründemann C, Schabbauer G, Gruber CW.

Proc Natl Acad Sci U S A. 2016 Apr 12;113(15):3960-5. doi: 10.1073/pnas.1519960113. Epub 2016 Mar 28.


MALDI TOF/TOF-Based Approach for the Identification of d- Amino Acids in Biologically Active Peptides and Proteins.

Koehbach J, Gruber CW, Becker C, Kreil DP, Jilek A.

J Proteome Res. 2016 May 6;15(5):1487-96. doi: 10.1021/acs.jproteome.5b01067. Epub 2016 Mar 25.


Rapid expansion of the protein disulfide isomerase gene family facilitates the folding of venom peptides.

Safavi-Hemami H, Li Q, Jackson RL, Song AS, Boomsma W, Bandyopadhyay PK, Gruber CW, Purcell AW, Yandell M, Olivera BM, Ellgaard L.

Proc Natl Acad Sci U S A. 2016 Mar 22;113(12):3227-32. doi: 10.1073/pnas.1525790113. Epub 2016 Mar 8.


Viola plant cyclotide vigno 5 induces mitochondria-mediated apoptosis via cytochrome C release and caspases activation in cervical cancer cells.

Esmaeili MA, Abagheri-Mahabadi N, Hashempour H, Farhadpour M, Gruber CW, Ghassempour A.

Fitoterapia. 2016 Mar;109:162-8. doi: 10.1016/j.fitote.2015.12.021. Epub 2016 Jan 2.


Ethnobotanical survey of Rinorea dentata (Violaceae) used in South-Western Nigerian ethnomedicine and detection of cyclotides.

Attah AF, Hellinger R, Sonibare MA, Moody JO, Arrowsmith S, Wray S, Gruber CW.

J Ethnopharmacol. 2016 Feb 17;179:83-91. doi: 10.1016/j.jep.2015.12.038. Epub 2015 Dec 22.


Microwave-assisted extraction of cyclotides from Viola ignobilis.

Farhadpour M, Hashempour H, Talebpour Z, A-Bagheri N, Shushtarian MS, Gruber CW, Ghassempour A.

Anal Biochem. 2016 Mar 15;497:83-9. doi: 10.1016/j.ab.2015.12.001. Epub 2015 Dec 17.


Peptidomics of Circular Cysteine-Rich Plant Peptides: Analysis of the Diversity of Cyclotides from Viola tricolor by Transcriptome and Proteome Mining.

Hellinger R, Koehbach J, Soltis DE, Carpenter EJ, Wong GK, Gruber CW.

J Proteome Res. 2015 Nov 6;14(11):4851-62. doi: 10.1021/acs.jproteome.5b00681. Epub 2015 Oct 8.


Isolation and Characterization of a Thionin Proprotein-processing Enzyme from Barley.

Plattner S, Gruber C, Stadlmann J, Widmann S, Gruber CW, Altmann F, Bohlmann H.

J Biol Chem. 2015 Jul 17;290(29):18056-67. doi: 10.1074/jbc.M115.647859. Epub 2015 May 26.


Inhibition of Human Prolyl Oligopeptidase Activity by the Cyclotide Psysol 2 Isolated from Psychotria solitudinum.

Hellinger R, Koehbach J, Puigpinós A, Clark RJ, Tarragó T, Giralt E, Gruber CW.

J Nat Prod. 2015 May 22;78(5):1073-82. doi: 10.1021/np501061t. Epub 2015 Apr 20.


Ribifolin, an orbitide from Jatropha ribifolia, and its potential antimalarial activity.

Pinto ME, Batista JM Jr, Koehbach J, Gaur P, Sharma A, Nakabashi M, Cilli EM, Giesel GM, Verli H, Gruber CW, Blanch EW, Tavares JF, da Silva MS, Garcia CR, Bolzani VS.

J Nat Prod. 2015 Mar 27;78(3):374-80. doi: 10.1021/np5007668. Epub 2015 Feb 20.


Chaperoning of the A1-adenosine receptor by endogenous adenosine - an extension of the retaliatory metabolite concept.

Kusek J, Yang Q, Witek M, Gruber CW, Nanoff C, Freissmuth M.

Mol Pharmacol. 2015 Jan;87(1):39-51. doi: 10.1124/mol.114.094045. Epub 2014 Oct 29.


κB-Ras proteins regulate both NF-κB-dependent inflammation and Ral-dependent proliferation.

Oeckinghaus A, Postler TS, Rao P, Schmitt H, Schmitt V, Grinberg-Bleyer Y, Kühn LI, Gruber CW, Lienhard GE, Ghosh S.

Cell Rep. 2014 Sep 25;8(6):1793-1807. doi: 10.1016/j.celrep.2014.08.015. Epub 2014 Sep 15.


From ethnopharmacology to drug design.

Koehbach J, Gruber CW.

Commun Integr Biol. 2013 Nov 1;6(6):e27583. doi: 10.4161/cib.27583. Epub 2014 Jan 8.


Immunosuppressive peptides and their therapeutic applications.

Thell K, Hellinger R, Schabbauer G, Gruber CW.

Drug Discov Today. 2014 May;19(5):645-53. doi: 10.1016/j.drudis.2013.12.002. Epub 2013 Dec 11. Review.


Oxytocic plant cyclotides as templates for peptide G protein-coupled receptor ligand design.

Koehbach J, O'Brien M, Muttenthaler M, Miazzo M, Akcan M, Elliott AG, Daly NL, Harvey PJ, Arrowsmith S, Gunasekera S, Smith TJ, Wray S, Göransson U, Dawson PE, Craik DJ, Freissmuth M, Gruber CW.

Proc Natl Acad Sci U S A. 2013 Dec 24;110(52):21183-8. doi: 10.1073/pnas.1311183110. Epub 2013 Nov 18.


Immunosuppressive activity of an aqueous Viola tricolor herbal extract.

Hellinger R, Koehbach J, Fedchuk H, Sauer B, Huber R, Gruber CW, Gründemann C.

J Ethnopharmacol. 2014;151(1):299-306. doi: 10.1016/j.jep.2013.10.044. Epub 2013 Nov 8.


Molecular grafting onto a stable framework yields novel cyclic peptides for the treatment of multiple sclerosis.

Wang CK, Gruber CW, Cemazar M, Siatskas C, Tagore P, Payne N, Sun G, Wang S, Bernard CC, Craik DJ.

ACS Chem Biol. 2014 Jan 17;9(1):156-63. doi: 10.1021/cb400548s. Epub 2013 Nov 7.


Recruitment of a cytoplasmic chaperone relay by the A2A adenosine receptor.

Bergmayr C, Thurner P, Keuerleber S, Kudlacek O, Nanoff C, Freissmuth M, Gruber CW.

J Biol Chem. 2013 Oct 4;288(40):28831-44. doi: 10.1074/jbc.M113.464776. Epub 2013 Aug 21.


Physiology of invertebrate oxytocin and vasopressin neuropeptides.

Gruber CW.

Exp Physiol. 2014 Jan;99(1):55-61. doi: 10.1113/expphysiol.2013.072561. Epub 2013 Aug 16. Review.


A systematic approach to document cyclotide distribution in plant species from genomic, transcriptomic, and peptidomic analysis.

Gerlach SL, Göransson U, Kaas Q, Craik DJ, Mondal D, Gruber CW.

Biopolymers. 2013 Sep;100(5):433-7. doi: 10.1002/bip.22258.


Cyclotide discovery in Gentianales revisited--identification and characterization of cyclic cystine-knot peptides and their phylogenetic distribution in Rubiaceae plants.

Koehbach J, Attah AF, Berger A, Hellinger R, Kutchan TM, Carpenter EJ, Rolf M, Sonibare MA, Moody JO, Wong GK, Dessein S, Greger H, Gruber CW.

Biopolymers. 2013 Sep;100(5):438-52. doi: 10.1002/bip.22328.


Cyclotides Suppress Human T-Lymphocyte Proliferation by an Interleukin 2-Dependent Mechanism.

Gründemann C, Thell K, Lengen K, Garcia-Käufer M, Huang YH, Huber R, Craik DJ, Schabbauer G, Gruber CW.

PLoS One. 2013 Jun 26;8(6):e68016. doi: 10.1371/journal.pone.0068016. Print 2013.


Insights into the molecular evolution of oxytocin receptor ligand binding.

Koehbach J, Stockner T, Bergmayr C, Muttenthaler M, Gruber CW.

Biochem Soc Trans. 2013 Feb 1;41(1):197-204. doi: 10.1042/BST20120256. Review.


Ribosomally synthesized and post-translationally modified peptide natural products: overview and recommendations for a universal nomenclature.

Arnison PG, Bibb MJ, Bierbaum G, Bowers AA, Bugni TS, Bulaj G, Camarero JA, Campopiano DJ, Challis GL, Clardy J, Cotter PD, Craik DJ, Dawson M, Dittmann E, Donadio S, Dorrestein PC, Entian KD, Fischbach MA, Garavelli JS, Göransson U, Gruber CW, Haft DH, Hemscheidt TK, Hertweck C, Hill C, Horswill AR, Jaspars M, Kelly WL, Klinman JP, Kuipers OP, Link AJ, Liu W, Marahiel MA, Mitchell DA, Moll GN, Moore BS, Müller R, Nair SK, Nes IF, Norris GE, Olivera BM, Onaka H, Patchett ML, Piel J, Reaney MJ, Rebuffat S, Ross RP, Sahl HG, Schmidt EW, Selsted ME, Severinov K, Shen B, Sivonen K, Smith L, Stein T, Süssmuth RD, Tagg JR, Tang GL, Truman AW, Vederas JC, Walsh CT, Walton JD, Wenzel SC, Willey JM, van der Donk WA.

Nat Prod Rep. 2013 Jan;30(1):108-60. doi: 10.1039/c2np20085f. Review.


Reengineering the collision coupling and diffusion mode of the A2A-adenosine receptor: palmitoylation in helix 8 relieves confinement.

Keuerleber S, Thurner P, Gruber CW, Zezula J, Freissmuth M.

J Biol Chem. 2012 Dec 7;287(50):42104-18. doi: 10.1074/jbc.M112.393579. Epub 2012 Oct 15.


Exploring bioactive peptides from natural sources for oxytocin and vasopressin drug discovery.

Gruber CW, Koehbach J, Muttenthaler M.

Future Med Chem. 2012 Sep;4(14):1791-8. doi: 10.4155/fmc.12.108. No abstract available.


Creativity in context; the courage in Therivel's GAM/DP.

Gruber CW.

Integr Psychol Behav Sci. 2013 Mar;47(1):176-83. doi: 10.1007/s12124-012-9209-8.


Characterizing circular peptides in mixtures: sequence fragment assembly of cyclotides from a violet plant by MALDI-TOF/TOF mass spectrometry.

Hashempour H, Koehbach J, Daly NL, Ghassempour A, Gruber CW.

Amino Acids. 2013 Feb;44(2):581-95. doi: 10.1007/s00726-012-1376-x. Epub 2012 Aug 14.


A combined proteomic and genetic analysis of the highly variable platelet proteome: from plasmatic proteins and SNPs.

Veitinger M, Umlauf E, Baumgartner R, Badrnya S, Porter J, Lamont J, Gerner C, Gruber CW, Oehler R, Zellner M.

J Proteomics. 2012 Oct 22;75(18):5848-60. doi: 10.1016/j.jprot.2012.07.042. Epub 2012 Aug 4.


Uterine contractility of plants used to facilitate childbirth in Nigerian ethnomedicine.

Attah AF, O'Brien M, Koehbach J, Sonibare MA, Moody JO, Smith TJ, Gruber CW.

J Ethnopharmacol. 2012 Aug 30;143(1):377-82. doi: 10.1016/j.jep.2012.06.042. Epub 2012 Jul 3.


The mechanistic basis for noncompetitive ibogaine inhibition of serotonin and dopamine transporters.

Bulling S, Schicker K, Zhang YW, Steinkellner T, Stockner T, Gruber CW, Boehm S, Freissmuth M, Rudnick G, Sitte HH, Sandtner W.

J Biol Chem. 2012 May 25;287(22):18524-34. doi: 10.1074/jbc.M112.343681. Epub 2012 Mar 26.


Discovery of defense- and neuropeptides in social ants by genome-mining.

Gruber CW, Muttenthaler M.

PLoS One. 2012;7(3):e32559. doi: 10.1371/journal.pone.0032559. Epub 2012 Mar 20.


The nonpeptide oxytocin receptor agonist WAY 267,464: receptor-binding profile, prosocial effects and distribution of c-Fos expression in adolescent rats.

Hicks C, Jorgensen W, Brown C, Fardell J, Koehbach J, Gruber CW, Kassiou M, Hunt GE, McGregor IS.

J Neuroendocrinol. 2012 Jul;24(7):1012-29. doi: 10.1111/j.1365-2826.2012.02311.x.


Do plant cyclotides have potential as immunosuppressant peptides?

Gründemann C, Koehbach J, Huber R, Gruber CW.

J Nat Prod. 2012 Feb 24;75(2):167-74. doi: 10.1021/np200722w. Epub 2012 Jan 24.


An aqueous birch leaf extract of Betula pendula inhibits the growth and cell division of inflammatory lymphocytes.

Gründemann C, Gruber CW, Hertrampf A, Zehl M, Kopp B, Huber R.

J Ethnopharmacol. 2011 Jul 14;136(3):444-51. doi: 10.1016/j.jep.2011.05.018. Epub 2011 May 17.


Uterotonic plants and their bioactive constituents.

Gruber CW, O'Brien M.

Planta Med. 2011 Feb;77(3):207-20. doi: 10.1055/s-0030-1250317. Epub 2010 Sep 15. Review.


Ligand-based peptide design and combinatorial peptide libraries to target G protein-coupled receptors.

Gruber CW, Muttenthaler M, Freissmuth M.

Curr Pharm Des. 2010;16(28):3071-88. Review.


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