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Safety, Biodistribution, and Radiation Dosimetry of 68Ga-OPS202 in Patients with Gastroenteropancreatic Neuroendocrine Tumors: A Prospective Phase I Imaging Study.

Nicolas GP, Beykan S, Bouterfa H, Kaufmann J, Bauman A, Lassmann M, Reubi JC, Rivier JEF, Maecke HR, Fani M, Wild D.

J Nucl Med. 2018 Jun;59(6):909-914. doi: 10.2967/jnumed.117.199737. Epub 2017 Oct 12.


Distribution of corticotropin-releasing factor (CRF) receptor binding in the mouse brain using a new, high-affinity radioligand, [125 I]-PD-Sauvagine.

Tan LA, Vaughan JM, Perrin MH, Rivier JE, Sawchenko PE.

J Comp Neurol. 2017 Dec 15;525(18):3840-3864. doi: 10.1002/cne.24307. Epub 2017 Sep 13.


Prospective Clinical Applications of CRF Peptide Antagonists.

Rivier JE.

Curr Mol Pharmacol. 2017;10(4):264-269. doi: 10.2174/1874467210666170110112914. Review.


A minimized human insulin-receptor-binding motif revealed in a Conus geographus venom insulin.

Menting JG, Gajewiak J, MacRaild CA, Chou DH, Disotuar MM, Smith NA, Miller C, Erchegyi J, Rivier JE, Olivera BM, Forbes BE, Smith BJ, Norton RS, Safavi-Hemami H, Lawrence MC.

Nat Struct Mol Biol. 2016 Oct;23(10):916-920. doi: 10.1038/nsmb.3292. Epub 2016 Sep 12.


Structural Basis for the Inhibition of Voltage-gated Sodium Channels by Conotoxin μO§-GVIIJ.

Green BR, Gajewiak J, Chhabra S, Skalicky JJ, Zhang MM, Rivier JE, Bulaj G, Olivera BM, Yoshikami D, Norton RS.

J Biol Chem. 2016 Mar 25;291(13):7205-20. doi: 10.1074/jbc.M115.697672. Epub 2016 Jan 27.


Characterization of a Pachymedusa dacnicolor-Sauvagine analog as a new high-affinity radioligand for corticotropin-releasing factor receptor studies.

Perrin MH, Tan LA, Vaughan JM, Lewis KA, Donaldson CJ, Miller C, Erchegyi J, Rivier JE, Sawchenko PE.

J Pharmacol Exp Ther. 2015 May;353(2):307-17. doi: 10.1124/jpet.114.222307. Epub 2015 Mar 3.


Α- and β-subunit composition of voltage-gated sodium channels investigated with μ-conotoxins and the recently discovered μO§-conotoxin GVIIJ.

Wilson MJ, Zhang MM, Gajewiak J, Azam L, Rivier JE, Olivera BM, Yoshikami D.

J Neurophysiol. 2015 Apr 1;113(7):2289-301. doi: 10.1152/jn.01004.2014. Epub 2015 Jan 28.


Comparison of somatostatin receptor agonist and antagonist for peptide receptor radionuclide therapy: a pilot study.

Wild D, Fani M, Fischer R, Del Pozzo L, Kaul F, Krebs S, Fischer R, Rivier JE, Reubi JC, Maecke HR, Weber WA.

J Nucl Med. 2014 Aug;55(8):1248-52. doi: 10.2967/jnumed.114.138834. Epub 2014 Jun 24.


Expression and functional characterization of membrane-integrated mammalian corticotropin releasing factor receptors 1 and 2 in Escherichia coli.

Jappelli R, Perrin MH, Lewis KA, Vaughan JM, Tzitzilonis C, Rivier JE, Vale WW, Riek R.

PLoS One. 2014 Jan 17;9(1):e84013. doi: 10.1371/journal.pone.0084013. eCollection 2014.


Corticotropin-releasing factor peptide antagonists: design, characterization and potential clinical relevance.

Rivier JE, Rivier CL.

Front Neuroendocrinol. 2014 Apr;35(2):161-70. doi: 10.1016/j.yfrne.2013.10.006. Epub 2013 Nov 20. Review.


Anxiolytic-like effects of antisauvagine-30 in mice are not mediated by CRF2 receptors.

Zorrilla EP, Roberts AJ, Rivier JE, Koob GF.

PLoS One. 2013 Aug 28;8(8):e63942. doi: 10.1371/journal.pone.0063942. eCollection 2013.


Mammalian neuronal sodium channel blocker μ-conotoxin BuIIIB has a structured N-terminus that influences potency.

Kuang Z, Zhang MM, Gupta K, Gajewiak J, Gulyas J, Balaram P, Rivier JE, Olivera BM, Yoshikami D, Bulaj G, Norton RS.

ACS Chem Biol. 2013;8(6):1344-51. doi: 10.1021/cb300674x. Epub 2013 Apr 16.


Posttranslational processing of human and mouse urocortin 2: characterization and bioactivity of gene products.

Vaughan JM, Donaldson CJ, Fischer WH, Perrin MH, Rivier JE, Sawchenko PE, Vale WW.

Endocrinology. 2013 Apr;154(4):1553-64. doi: 10.1210/en.2012-2011. Epub 2013 Mar 14.


Pharmacological fractionation of tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons by μ-conotoxins.

Zhang MM, Wilson MJ, Gajewiak J, Rivier JE, Bulaj G, Olivera BM, Yoshikami D.

Br J Pharmacol. 2013 May;169(1):102-14. doi: 10.1111/bph.12119.


Co-expression of Na(V)β subunits alters the kinetics of inhibition of voltage-gated sodium channels by pore-blocking μ-conotoxins.

Zhang MM, Wilson MJ, Azam L, Gajewiak J, Rivier JE, Bulaj G, Olivera BM, Yoshikami D.

Br J Pharmacol. 2013 Apr;168(7):1597-610. doi: 10.1111/bph.12051.


Unexpected sensitivity of sst2 antagonists to N-terminal radiometal modifications.

Fani M, Braun F, Waser B, Beetschen K, Cescato R, Erchegyi J, Rivier JE, Weber WA, Maecke HR, Reubi JC.

J Nucl Med. 2012 Sep;53(9):1481-9. doi: 10.2967/jnumed.112.102764. Epub 2012 Jul 31.


Characterization of two neuronal subclasses through constellation pharmacology.

Teichert RW, Raghuraman S, Memon T, Cox JL, Foulkes T, Rivier JE, Olivera BM.

Proc Natl Acad Sci U S A. 2012 Jul 31;109(31):12758-63. doi: 10.1073/pnas.1209759109. Epub 2012 Jul 9.


CRF induces intestinal epithelial barrier injury via the release of mast cell proteases and TNF-α.

Overman EL, Rivier JE, Moeser AJ.

PLoS One. 2012;7(6):e39935. doi: 10.1371/journal.pone.0039935. Epub 2012 Jun 29.


Wylie Vale: neuroendocrine master.

Montminy M, Lee KF, Rivier JE, Rivier C, Reichlin S.

Proc Natl Acad Sci U S A. 2012 Mar 6;109(10):3604-5. doi: 10.1073/pnas.1201696109. Epub 2012 Feb 21. No abstract available.


Novel dimeric DOTA-coupled peptidic Y1-receptor antagonists for targeting of neuropeptide Y receptor-expressing cancers.

Chatenet D, Cescato R, Waser B, Erchegyi J, Rivier JE, Reubi JC.

EJNMMI Res. 2011 Sep 2;1(1):21. doi: 10.1186/2191-219X-1-21.


Lactam-stabilized helical analogues of the analgesic μ-conotoxin KIIIA.

Khoo KK, Wilson MJ, Smith BJ, Zhang MM, Gulyas J, Yoshikami D, Rivier JE, Bulaj G, Norton RS.

J Med Chem. 2011 Nov 10;54(21):7558-66. doi: 10.1021/jm200839a. Epub 2011 Oct 12.


First clinical evidence that imaging with somatostatin receptor antagonists is feasible.

Wild D, Fani M, Behe M, Brink I, Rivier JE, Reubi JC, Maecke HR, Weber WA.

J Nucl Med. 2011 Sep;52(9):1412-7. doi: 10.2967/jnumed.111.088922. Epub 2011 Aug 18.


N-imidazolebenzyl-histidine substitution in somatostatin and in its octapeptide analogue modulates receptor selectivity and function.

Erchegyi J, Cescato R, Waser B, Rivier JE, Reubi JC.

J Med Chem. 2011 Sep 8;54(17):5981-7. doi: 10.1021/jm200307v. Epub 2011 Aug 16.


NMR structure of the first extracellular domain of corticotropin-releasing factor receptor 1 (ECD1-CRF-R1) complexed with a high affinity agonist.

Grace CR, Perrin MH, Gulyas J, Rivier JE, Vale WW, Riek R.

J Biol Chem. 2010 Dec 3;285(49):38580-9. doi: 10.1074/jbc.M110.121897. Epub 2010 Sep 15.


Switch from antagonist to agonist after addition of a DOTA chelator to a somatostatin analog.

Reubi JC, Erchegyi J, Cescato R, Waser B, Rivier JE.

Eur J Nucl Med Mol Imaging. 2010 Aug;37(8):1551-8. doi: 10.1007/s00259-010-1445-x. Epub 2010 Apr 16.


Early weaning stress impairs development of mucosal barrier function in the porcine intestine.

Smith F, Clark JE, Overman BL, Tozel CC, Huang JH, Rivier JE, Blikslager AT, Moeser AJ.

Am J Physiol Gastrointest Liver Physiol. 2010 Mar;298(3):G352-63. doi: 10.1152/ajpgi.00081.2009. Epub 2009 Nov 19.


Agonist-biased signaling at the sst2A receptor: the multi-somatostatin analogs KE108 and SOM230 activate and antagonize distinct signaling pathways.

Cescato R, Loesch KA, Waser B, Mäcke HR, Rivier JE, Reubi JC, Schonbrunn A.

Mol Endocrinol. 2010 Jan;24(1):240-9. doi: 10.1210/me.2009-0321. Epub 2009 Nov 12.


Novel, potent, and radio-iodinatable somatostatin receptor 1 (sst1) selective analogues.

Erchegyi J, Cescato R, Grace CR, Waser B, Piccand V, Hoyer D, Riek R, Rivier JE, Reubi JC.

J Med Chem. 2009 May 14;52(9):2733-46. doi: 10.1021/jm801314f.


Four functional GnRH receptors in zebrafish: analysis of structure, signaling, synteny and phylogeny.

Tello JA, Wu S, Rivier JE, Sherwood NM.

Integr Comp Biol. 2008 Nov;48(5):570-87. doi: 10.1093/icb/icn070. Epub 2008 Jul 21.


Newly-identified receptors for peptide histidine-isoleucine and GHRH-like peptide in zebrafish help to elucidate the mammalian secretin superfamily.

Wu S, Roch GJ, Cervini LA, Rivier JE, Sherwood NM.

J Mol Endocrinol. 2008 Nov;41(5):343-66. doi: 10.1677/JME-08-0083. Epub 2008 Aug 29.


Three-dimensional consensus structure of sst2-selective somatostatin (SRIF) antagonists by NMR.

Grace CR, Erchegyi J, Reubi JC, Rivier JE, Riek R.

Biopolymers. 2008 Dec;89(12):1077-87. doi: 10.1002/bip.21060.


Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting.

Cescato R, Erchegyi J, Waser B, Piccand V, Maecke HR, Rivier JE, Reubi JC.

J Med Chem. 2008 Jul 10;51(13):4030-7. doi: 10.1021/jm701618q. Epub 2008 Jun 11.


Ring size of somatostatin analogues (ODT-8) modulates receptor selectivity and binding affinity.

Erchegyi J, Grace CR, Samant M, Cescato R, Piccand V, Riek R, Reubi JC, Rivier JE.

J Med Chem. 2008 May 8;51(9):2668-75. doi: 10.1021/jm701444y. Epub 2008 Apr 12.


Ring size in octreotide amide modulates differently agonist versus antagonist binding affinity and selectivity.

Grace CR, Erchegyi J, Samant M, Cescato R, Piccand V, Riek R, Reubi JC, Rivier JE.

J Med Chem. 2008 May 8;51(9):2676-81. doi: 10.1021/jm701445q. Epub 2008 Apr 12.


Amyloid as a depot for the formulation of long-acting drugs.

Maji SK, Schubert D, Rivier C, Lee S, Rivier JE, Riek R.

PLoS Biol. 2008 Feb;6(2):e17. doi: 10.1371/journal.pbio.0060017.


Common and divergent structural features of a series of corticotropin releasing factor-related peptides.

Grace CR, Perrin MH, Cantle JP, Vale WW, Rivier JE, Riek R.

J Am Chem Soc. 2007 Dec 26;129(51):16102-14. Epub 2007 Dec 6.


Subtype-selective corticotropin-releasing factor receptor agonists exert contrasting, but not opposite, effects on anxiety-related behavior in rats.

Zhao Y, Valdez GR, Fekete EM, Rivier JE, Vale WW, Rice KC, Weiss F, Zorrilla EP.

J Pharmacol Exp Ther. 2007 Dec;323(3):846-54. Epub 2007 Sep 12.


Structure/function characterization of micro-conotoxin KIIIA, an analgesic, nearly irreversible blocker of mammalian neuronal sodium channels.

Zhang MM, Green BR, Catlin P, Fiedler B, Azam L, Chadwick A, Terlau H, McArthur JR, French RJ, Gulyas J, Rivier JE, Smith BJ, Norton RS, Olivera BM, Yoshikami D, Bulaj G.

J Biol Chem. 2007 Oct 19;282(42):30699-706. Epub 2007 Aug 27.


Synthesis of protected norcysteines for SPPS compatible with Fmoc-strategy.

Samant MP, Rivier JE.

Tetrahedron Lett. 2007 Jul 16;48(29):5107-5110.


Structure of the N-terminal domain of a type B1 G protein-coupled receptor in complex with a peptide ligand.

Grace CR, Perrin MH, Gulyas J, Digruccio MR, Cantle JP, Rivier JE, Vale WW, Riek R.

Proc Natl Acad Sci U S A. 2007 Mar 20;104(12):4858-63. Epub 2007 Mar 12.


Norcystine, a new tool for the study of the structure-activity relationship of peptides.

Samant MP, Rivier JE.

Org Lett. 2006 May 25;8(11):2361-4.


Biochemical characterization of Drosophila gamma-glutamyl carboxylase and its role in fly development.

Bandyopadhyay PK, Clark K, Stevenson BJ, Rivier JE, Olivera BM, Golic KG, Rong YS.

Insect Mol Biol. 2006 Apr;15(2):147-56.


Internalization of sst2, sst3, and sst5 receptors: effects of somatostatin agonists and antagonists.

Cescato R, Schulz S, Waser B, Eltschinger V, Rivier JE, Wester HJ, Culler M, Ginj M, Liu Q, Schonbrunn A, Reubi JC.

J Nucl Med. 2006 Mar;47(3):502-11.


Conformational analysis of a potent SSTR3-selective somatostatin analogue by NMR in water solution.

Gairí M, Saiz P, Madurga S, Roig X, Erchegyi J, Koerber SC, Reubi JC, Rivier JE, Giralt E.

J Pept Sci. 2006 Feb;12(2):82-91.


Identification of a novel pharmacophore for peptide toxins interacting with K+ channels.

Verdier L, Al-Sabi A, Rivier JE, Olivera BM, Terlau H, Carlomagno T.

J Biol Chem. 2005 Jun 3;280(22):21246-55. Epub 2005 Mar 30.


Characterization of four receptor cDNAs: PAC1, VPAC1, a novel PAC1 and a partial GHRH in zebrafish.

Fradinger EA, Tello JA, Rivier JE, Sherwood NM.

Mol Cell Endocrinol. 2005 Feb 28;231(1-2):49-63.


Synthesis and biological activity of GnRH antagonists modified at position 3 with 3-(2-methoxy-5-pyridyl)-alanine.

Samant MP, Miller C, Hong DJ, Koerber SC, Croston G, Rivier CL, Rivier JE.

J Pept Res. 2005 Feb;65(2):284-91.


A soluble mouse brain splice variant of type 2alpha corticotropin-releasing factor (CRF) receptor binds ligands and modulates their activity.

Chen AM, Perrin MH, Digruccio MR, Vaughan JM, Brar BK, Arias CM, Lewis KA, Rivier JE, Sawchenko PE, Vale WW.

Proc Natl Acad Sci U S A. 2005 Feb 15;102(7):2620-5. Epub 2005 Feb 8.

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