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Items: 26

1.

Recent advances in drug discovery of GPCR allosteric modulators for neurodegenerative disorders.

Lütjens R, Rocher JP.

Curr Opin Pharmacol. 2017 Feb;32:91-95. doi: 10.1016/j.coph.2017.01.001. Epub 2017 Jan 27. Review.

PMID:
28135635
2.

The drug candidate, ADX71441, is a novel, potent and selective positive allosteric modulator of the GABAB receptor with a potential for treatment of anxiety, pain and spasticity.

Kalinichev M, Girard F, Haddouk H, Rouillier M, Riguet E, Royer-Urios I, Mutel V, Lütjens R, Poli S.

Neuropharmacology. 2017 Mar 1;114:34-47. doi: 10.1016/j.neuropharm.2016.11.016. Epub 2016 Nov 23.

PMID:
27889489
3.

Targeting type-2 metabotropic glutamate receptors to protect vulnerable hippocampal neurons against ischemic damage.

Motolese M, Mastroiacovo F, Cannella M, Bucci D, Gaglione A, Riozzi B, Lütjens R, Poli SM, Celanire S, Bruno V, Battaglia G, Nicoletti F.

Mol Brain. 2015 Oct 24;8(1):66. doi: 10.1186/s13041-015-0158-2.

4.

Preclinical evaluation of the antipsychotic potential of the mGlu2-positive allosteric modulator JNJ-40411813.

Lavreysen H, Langlois X, Donck LV, Nuñez JM, Pype S, Lütjens R, Megens A.

Pharmacol Res Perspect. 2015 Mar;3(2):e00097. doi: 10.1002/prp2.97. Epub 2015 Jan 30.

5.

Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor.

Lavreysen H, Ahnaou A, Drinkenburg W, Langlois X, Mackie C, Pype S, Lütjens R, Le Poul E, Trabanco AA, Nuñez JM.

Pharmacol Res Perspect. 2015 Feb;3(1):e00096. doi: 10.1002/prp2.96. Epub 2014 Dec 9.

6.

Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.

Cid JM, Tresadern G, Duvey G, Lütjens R, Finn T, Rocher JP, Poli S, Vega JA, de Lucas AI, Matesanz E, Linares ML, Andrés JI, Alcazar J, Alonso JM, Macdonald GJ, Oehlrich D, Lavreysen H, Ahnaou A, Drinkenburg W, Mackie C, Pype S, Gallacher D, Trabanco AA.

J Med Chem. 2014 Aug 14;57(15):6495-512. doi: 10.1021/jm500496m. Epub 2014 Jul 28.

PMID:
25032784
7.

New technologies enabling the industrialization of allosteric modulator discovery.

Lütjens R, Perry B, Schelshorn D, Rocher JP.

Drug Discov Today Technol. 2013 Summer;10(2):e253-60. doi: 10.1016/j.ddtec.2013.01.001. Review.

PMID:
24050276
8.

Pharmacological characterization of JNJ-40068782, a new potent, selective, and systemically active positive allosteric modulator of the mGlu2 receptor and its radioligand [3H]JNJ-40068782.

Lavreysen H, Langlois X, Ahnaou A, Drinkenburg W, te Riele P, Biesmans I, Van der Linden I, Peeters L, Megens A, Wintmolders C, Cid JM, Trabanco AA, Andrés JI, Dautzenberg FM, Lütjens R, Macdonald G, Atack JR.

J Pharmacol Exp Ther. 2013 Sep;346(3):514-27. doi: 10.1124/jpet.113.204990. Epub 2013 Jun 13.

PMID:
23766542
9.

ADX71743, a potent and selective negative allosteric modulator of metabotropic glutamate receptor 7: in vitro and in vivo characterization.

Kalinichev M, Rouillier M, Girard F, Royer-Urios I, Bournique B, Finn T, Charvin D, Campo B, Le Poul E, Mutel V, Poli S, Neale SA, Salt TE, Lütjens R.

J Pharmacol Exp Ther. 2013 Mar;344(3):624-36. doi: 10.1124/jpet.112.200915. Epub 2012 Dec 20. Erratum in: J Pharmacol Exp Ther. 2013 May;345(2):328.

PMID:
23257312
10.

Discovery of 1,4-disubstituted 3-cyano-2-pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor.

Cid JM, Duvey G, Tresadern G, Nhem V, Furnari R, Cluzeau P, Vega JA, de Lucas AI, Matesanz E, Alonso JM, Linares ML, Andrés JI, Poli SM, Lutjens R, Himogai H, Rocher JP, Macdonald GJ, Oehlrich D, Lavreysen H, Ahnaou A, Drinkenburg W, Mackie C, Trabanco AA.

J Med Chem. 2012 Mar 8;55(5):2388-405. doi: 10.1021/jm2016864. Epub 2012 Feb 24.

PMID:
22364337
11.

Lateral allosterism in the glucagon receptor family: glucagon-like peptide 1 induces G-protein-coupled receptor heteromer formation.

Schelshorn D, Joly F, Mutel S, Hampe C, Breton B, Mutel V, Lütjens R.

Mol Pharmacol. 2012 Mar;81(3):309-18. doi: 10.1124/mol.111.074757. Epub 2011 Nov 22.

PMID:
22108912
12.

mGluR5 negative allosteric modulators overview: a medicinal chemistry approach towards a series of novel therapeutic agents.

Rocher JP, Bonnet B, Boléa C, Lütjens R, Le Poul E, Poli S, Epping-Jordan M, Bessis AS, Ludwig B, Mutel V.

Curr Top Med Chem. 2011;11(6):680-95. Review.

PMID:
21261592
13.

New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): identification and synthesis of N-propyl-8-chloro-6-substituted isoquinolones.

Trabanco AA, Duvey G, Cid JM, Macdonald GJ, Cluzeau P, Nhem V, Furnari R, Behaj N, Poulain G, Finn T, Lavreysen H, Poli S, Raux A, Thollon Y, Poirier N, D'Addona D, Andrés JI, Lutjens R, Le Poul E, Imogai H, Rocher JP.

Bioorg Med Chem Lett. 2011 Feb 1;21(3):971-6. doi: 10.1016/j.bmcl.2010.12.048. Epub 2010 Dec 21.

PMID:
21232953
14.

Discovery of 1,5-disubstituted pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor.

Cid JM, Duvey G, Cluzeau P, Nhem V, Macary K, Raux A, Poirier N, Muller J, Boléa C, Finn T, Poli S, Epping-Jordan M, Chamelot E, Derouet F, Girard F, Macdonald GJ, Vega JA, de Lucas AI, Matesanz E, Lavreysen H, Linares ML, Oehlrich D, Oyarzábal J, Tresadern G, Trabanco AA, Andrés JI, Le Poul E, Imogai H, Lutjens R, Rocher JP.

ACS Chem Neurosci. 2010 Dec 15;1(12):788-95. doi: 10.1021/cn1000638. Epub 2010 Aug 23.

15.

Increased expression of protein kinase A inhibitor alpha (PKI-alpha) and decreased PKA-regulated genes in chronic intermittent alcohol exposure.

Repunte-Canonigo V, Lutjens R, van der Stap LD, Sanna PP.

Brain Res. 2007 Mar 23;1138:48-56. Epub 2007 Jan 30.

16.

Gene expression evidence for remodeling of lateral hypothalamic circuitry in cocaine addiction.

Ahmed SH, Lutjens R, van der Stap LD, Lekic D, Romano-Spica V, Morales M, Koob GF, Repunte-Canonigo V, Sanna PP.

Proc Natl Acad Sci U S A. 2005 Aug 9;102(32):11533-8. Epub 2005 Aug 2.

17.

Time-restricted role for dendritic activation of the mTOR-p70S6K pathway in the induction of late-phase long-term potentiation in the CA1.

Cammalleri M, Lütjens R, Berton F, King AR, Simpson C, Francesconi W, Sanna PP.

Proc Natl Acad Sci U S A. 2003 Nov 25;100(24):14368-73. Epub 2003 Nov 17.

18.

ERK regulation in chronic ethanol exposure and withdrawal.

Sanna PP, Simpson C, Lutjens R, Koob G.

Brain Res. 2002 Sep 6;948(1-2):186-91.

PMID:
12383974
19.

Phosphatidylinositol 3-kinase is required for the expression but not for the induction or the maintenance of long-term potentiation in the hippocampal CA1 region.

Sanna PP, Cammalleri M, Berton F, Simpson C, Lutjens R, Bloom FE, Francesconi W.

J Neurosci. 2002 May 1;22(9):3359-65. Erratum in: J Neurosci 2002 Dec 1;22(23):10507.

20.

Localization and targeting of SCG10 to the trans-Golgi apparatus and growth cone vesicles.

Lutjens R, Igarashi M, Pellier V, Blasey H, Di Paolo G, Ruchti E, Pfulg C, Staple JK, Catsicas S, Grenningloh G.

Eur J Neurosci. 2000 Jul;12(7):2224-34.

PMID:
10947801
21.

Identification of in vitro phosphorylation sites in the growth cone protein SCG10. Effect Of phosphorylation site mutants on microtubule-destabilizing activity.

Antonsson B, Kassel DB, Di Paolo G, Lutjens R, Riederer BM, Grenningloh G.

J Biol Chem. 1998 Apr 3;273(14):8439-46.

22.

Differential distribution of stathmin and SCG10 in developing neurons in culture.

Di Paolo G, Lutjens R, Osen-Sand A, Sobel A, Catsicas S, Grenningloh G.

J Neurosci Res. 1997 Dec 15;50(6):1000-9.

PMID:
9452014
23.

Purification, characterization, and in vitro phosphorylation of the neuron-specific membrane-associated protein SCG10.

Antonsson B, Lütjens R, Di Paolo G, Kassel D, Allet B, Bernard A, Catsicas S, Grenningloh G.

Protein Expr Purif. 1997 Apr;9(3):363-71.

PMID:
9126608
24.

Expression, purification, and characterization of a highly soluble N-terminal-truncated form of the neuron-specific membrane-associated phosphoprotein SCG10.

Antonsson B, Montessuit S, Di Paolo G, Lutjens R, Grenningloh G.

Protein Expr Purif. 1997 Mar;9(2):295-300.

PMID:
9056495
25.

Targeting of SCG10 to the area of the Golgi complex is mediated by its NH2-terminal region.

Di Paolo G, Lutjens R, Pellier V, Stimpson SA, Beuchat MH, Catsicas S, Grenningloh G.

J Biol Chem. 1997 Feb 21;272(8):5175-82.

26.

Regulation of microtubule dynamics by the neuronal growth-associated protein SCG10.

Riederer BM, Pellier V, Antonsson B, Di Paolo G, Stimpson SA, Lütjens R, Catsicas S, Grenningloh G.

Proc Natl Acad Sci U S A. 1997 Jan 21;94(2):741-5.

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