Frédéric BIHEL

112
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Publications

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Multitarget μ-Opioid Receptor Agonists─Neuropeptide FF Receptor Antagonists Induce Potent Antinociception with Reduced Adverse Side Effects

Jolien de Neve , Khadija Elhabazi , Simon Gonzalez , Claire Herby , Séverine Schneider et al.
Journal of Medicinal Chemistry, 2024, 67 (9), pp.7603-7619. ⟨10.1021/acs.jmedchem.4c00442⟩
Article dans une revue hal-04631174 v1
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The IMS Library: from IN‐Stock to Virtual

Teodora Djikic‐stojsic , Guillaume Bret , Gaëlle Blond , Nicolas Girard , Clothilde Le Guen et al.
ChemMedChem, 2024, 19 (20), pp.e202400381. ⟨10.1002/cmdc.202400381⟩
Article dans une revue hal-04727478 v2
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Ethaverine and Papaverine Target Cyclin-Dependent Kinase 5 and Inhibit Lung Cancer Cell Proliferation and Migration

Arthur Laure , Chloe Royet , Frédéric Bihel , Blandine Baratte , Stéphane Bach et al.
ACS Pharmacology & Translational Science, 2024, 7 (5), pp.1377-1385. ⟨10.1021/acsptsci.4c00023⟩
Article dans une revue hal-04609131 v1
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Synthesis, Characterization, and Self-Assembling Properties of New Amphiphilic Dendrons Bearing Branched TRIS-Derived Oligomers as Polar Head Groups

Stéphane Desgranges , Valentin Lacanau , Françoise Bonneté , Marine Soulié , Frédéric Bihel et al.
Macromolecules, 2024, 57 (9), pp.4495-4507. ⟨10.1021/acs.macromol.3c02388⟩
Article dans une revue hal-04578834 v1
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New insights into the regulation of Cystathionine beta synthase (CBS), an enzyme involved in intellectual deficiency in Down syndrome

Pierre Conan , Alice Léon , Noéline Caroff , Claire Rollet , Loubna Chaïr et al.
Frontiers in Neuroscience, 2023, 16, ⟨10.3389/fnins.2022.1110163⟩
Article dans une revue hal-04170617 v1
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In Situ Formation of Cationic π-Allylpalladium Precatalysts in Alcoholic Solvents: Application to C–N Bond Formation

Philippe Steinsoultz , Aurélien Bailly , Patrick Wagner , Estefania Oliva , Martine Schmitt et al.
ACS Catalysis, 2022, 12 (1), pp.560-567. ⟨10.1021/acscatal.1c04641⟩
Article dans une revue hal-03546107 v1
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Identification of 8-Hydroxyquinoline Derivatives That Decrease Cystathionine Beta Synthase (CBS) Activity

Pierre Conan , Alice Léon , Mathilde Gourdel , Claire Rollet , Loubna Chaïr et al.
International Journal of Molecular Sciences, 2022, 23 (12), pp.6769. ⟨10.3390/ijms23126769⟩
Article dans une revue hal-03701324 v1
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Comprehensive overview of biased pharmacology at the opioid receptors: biased ligands and bias factors

Jolien de Neve , Thomas M A Barlow , Dirk Tourwé , Frédéric Bihel , Frédéric Simonin et al.
RSC Medicinal Chemistry, 2021, 12 (6), pp.828-870. ⟨10.1039/D1MD00041A⟩
Article dans une revue hal-03435229 v1
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Anti-prion Drugs Targeting the Protein Folding Activity of the Ribosome Reduce PABPN1 Aggregation

Aline Bamia , Maha Sinane , Rima Naït-Saïdi , Jamila Dhiab , Marc Keruzoré et al.
Neurotherapeutics, 2021, 18 (2), pp.1137-1150. ⟨10.1007/s13311-020-00992-6⟩
Article dans une revue hal-03158577 v1
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Identification of an N -acylated- D Arg-Leu-NH 2 Dipeptide as a Highly Selective Neuropeptide FF1 Receptor Antagonist That Potently Prevents Opioid-Induced Hyperalgesia

Raphaëlle Quillet , Séverine Schneider , Valérie Utard , Armand Drieu La Rochelle , Khadija Elhabazi et al.
Journal of Medicinal Chemistry, 2021, 64 (11), pp.7555-7564. ⟨10.1021/acs.jmedchem.1c00256⟩
Article dans une revue hal-03363456 v1
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Design, Synthesis and Biological Evaluation of Arylpyridin-2-yl Guanidine Derivatives and Cyclic Mimetics as Novel MSK1 Inhibitors. An Application in an Asthma Model

Maud Bollenbach , Simona Nemska , Patrick Wagner , Guillaume Camelin , François Daubeuf et al.
Molecules, 2021, 26 (2), pp.391. ⟨10.3390/molecules26020391⟩
Article dans une revue hal-03266504 v1
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Diastereoselective Synthesis of Nonplanar 3-Amino-1,2,4-oxadiazine Scaffold: Structure Revision of Alchornedine

Shuang-Qi Tang , Maeva Leloire , Severine Schneider , Julie Mohr , Jacques Bricard et al.
Journal of Organic Chemistry, In press, ⟨10.1021/acs.joc.0c01764⟩
Article dans une revue hal-03021041 v1
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From Electronic Waste to Suzuki−Miyaura Cross‐Coupling Reaction in Water: Direct Valuation of Recycled Palladium in Catalysis

Valentin Lacanau , Françoise Bonnete , Patrick Wagner , Martine Schmitt , Daniel Meyer et al.
ChemSusChem, 2020, 13 (19), pp.5224-5230. ⟨10.1002/cssc.202001155⟩
Article dans une revue hal-02999762 v1
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Minimizing HCN in DIC/Oxyma mediated amide bond forming reactions

Marion Erny , Marika Lundqvist , Jon Rasmussen , Olivier Ludemann-Hombourger , Frédéric Bihel et al.
Organic Process Research and Development, 2020, 24 (7), pp.1341-1349. ⟨10.1021/acs.oprd.0c00227⟩
Article dans une revue hal-02997255 v1
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Mitochondria modulatory effects of new TSPO ligands in a cellular model of tauopathies

Amandine Grimm , Imane Lejri , François Hallé , Martine Schmitt , Jürgen Götz et al.
Journal of Neuroendocrinology, 2019, ⟨10.1111/jne.12796⟩
Article dans une revue hal-02368671 v1
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POxAP Precatalysts and the Negishi Cross-Coupling Reaction

Shuang-Qi Tang , Martine Schmitt , Frédéric Bihel
Synthesis: Journal of Synthetic Organic Chemistry, 2019, 52 (01), pp.51-59. ⟨10.1055/s-0039-1690728⟩
Article dans une revue hal-02997250 v1
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Design and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model

Maud Bollenbach , Claire Lugnier , M Elanie Kremer , Eric Salvat , Salim Megat et al.
European Journal of Medicinal Chemistry, 2019, 177, pp.269-290. ⟨10.1016/j.ejmech.2019.05.026⟩
Article dans une revue hal-02322399 v1

Evolution of coumaroyl conjugate 3‐hydroxylases in land plants: lignin biosynthesis and defense

Annette Alber , Hugues Renault , Alexandra Basilio-Lopes , Jean-Etienne Bassard , Zhenhua Liu et al.
The Plant Journal, 2019, 99 (5), pp.924-936. ⟨10.1111/tpj.14373⟩
Article dans une revue hal-02437982 v1
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Fukuyama Cross-Coupling Approach to Isoprekinamycin: Discovery of the Highly Active and Bench-Stable Palladium Precatalyst POxAP

Shuang-Qi Tang , Jacques Bricard , Martine Schmitt , Frédéric Bihel
Organic Letters, 2019, 21 (3), pp.844-848. ⟨10.1021/acs.orglett.9b00031⟩
Article dans une revue hal-02323246 v1
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TSPO Ligands Boost Mitochondrial Function and Pregnenolone Synthesis

Imane Lejri , Amandine Grimm , François Hallé , Mustapha Abarghaz , Christian Klein et al.
Journal of Alzheimer's Disease, In press, pp.1-14. ⟨10.3233/JAD-190127⟩
Article dans une revue hal-02368657 v1

A bifunctional-biased mu-opioid agonist–neuropeptide FF receptor antagonist as analgesic with improved acute and chronic side effects

Armand Drieu La Rochelle , Karel Guillemyn , Maria Dumitrascuta , Charlotte Martin , Valérie Utard et al.
Pain, 2018, 159 (9), pp.1705-1718. ⟨10.1097/j.pain.0000000000001262⟩
Article dans une revue hal-02368742 v1
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Human erythrocytes release ATP by a novel pathway involving VDAC oligomerization independent of pannexin-1

Irene Marginedas-Freixa , Cora Lilia Alvarez , Martina Moras , María Florencia Leal Denis , Claude Hattab et al.
Scientific Reports, 2018, 8, pp.11384. ⟨10.1038/s41598-018-29885-7⟩
Article dans une revue hal-02368694 v1

Aminoguanidine Hydrazone Derivatives as Nonpeptide NPFF1 Receptor Antagonists Reverse Opioid Induced Hyperalgesia

Hassan Hammoud , Khadija Elhabazi , Isabelle Bertin , Valeŕie Utard , Emilie Laboureyras et al.
ACS Chemical Neuroscience, 2018, 9 (11), pp.2599-2609. ⟨10.1021/acschemneuro.8b00099⟩
Article dans une revue hal-02323065 v1

Dioxygenation of styrenes with molecular oxygen in water

Shuang-Qi Tang , An-Ping Wang , Martine Schmitt , Frédéric Bihel
Tetrahedron Letters, 2018, 59 (15), pp.1465-1468. ⟨10.1016/j.tetlet.2018.03.009⟩
Article dans une revue hal-02326129 v1
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Induction of ATP Release, PPIX Transport, and Cholesterol Uptake by Human Red Blood Cells Using a New Family of TSPO Ligands

Irene Marginedas-Freixa , Cora L Alvarez , Martina Moras , Claude Hattab , Guillaume Bouyer et al.
International Journal of Molecular Sciences, 2018, 19 (10), pp.3098. ⟨10.3390/ijms19103098⟩
Article dans une revue hal-01926983 v1
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WNK1 kinase and its partners Akt, SGK1 and NBC-family Na<sup>+</sup>/HCO3<sup>&#x2013;</sup> cotransporters are potential therapeutic targets for glioblastoma stem-like cells linked to Bisacodyl signaling

Wanyin Chen , Leonel Nguekeu Zebaze , Jihu Dong , Laëtitia Chezeau , Perrine Inquimbert et al.
Oncotarget, 2018, 9 (43), pp.27197-27219. ⟨10.18632/oncotarget.25509⟩
Article dans une revue hal-02349611 v1

Heteroarylguanidines as Allosteric Modulators of ASIC1a and ASIC3 Channels

Omar Alijevic , Hassan Hammoud , Anand Vaithia , Viktor Trendafilov , Maud Bollenbach et al.
ACS Chemical Neuroscience, 2018, 9 (6), pp.1357-1365. ⟨10.1021/acschemneuro.7b00529⟩
Article dans une revue hal-02368759 v1

Phenylpyridine-2-ylguanidines and rigid mimetics as novel inhibitors of TNFα overproduction: Beneficial action in models of neuropathic pain and of acute lung inflammation

Maud Bollenbach , Eric Salvat , Francois Daubeuf , Patrick Wagner , Ipek Yalcin et al.
European Journal of Medicinal Chemistry, 2018, 147, pp.163-182. ⟨10.1016/j.ejmech.2018.01.049⟩
Article dans une revue hal-02323729 v1

Development of a L-Tryptophan-Based Ligand for Regioselective Copper Catalyzed N 2 -Arylation of 1,2,3-Triazoles

Alexandra Basilio Lopes , Patrick Wagner , Arthur Eugen Kümmerle , Frédéric Bihel , Jean-Jacques Bourguignon et al.
ChemistrySelect, 2017, 2 (22), pp.6544-6548. ⟨10.1002/slct.201701498⟩
Article dans une revue hal-02368798 v1

Discovery of Imidazoquinazolinone Derivatives as TSPO Ligands Modulating Neurosteroidogenesis and Cellular Bioenergetics in Neuroblastoma Cells Expressing Amyloid Precursor Protein

François Hallé , Imane Lejri , Mustapha Abarghaz , Amandine Grimm , Christian Klein et al.
ChemistrySelect, 2017, 2 (22), pp.6452-6457. ⟨10.1002/slct.201701565⟩
Article dans une revue hal-02368811 v1

The translocator protein ligand XBD173 improves clinical symptoms and neuropathological markers in the SJL/J mouse model of multiple sclerosis

I. Marginedas-Freixa , C. Hattab , G. Bouyer , F. Halle , A. Chene et al.
Biochimica et Biophysica Acta - Molecular Basis of Disease, 2017, 1863 (12), pp.3016-3027. ⟨10.1016/j.bbadis.2017.09.007⟩
Article dans une revue hal-02290250 v1
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RF313, an orally bioavailable neuropeptide FF receptor antagonist, opposes effects of RF-amide-related peptide-3 and opioid-induced hyperalgesia in rodents

Khadija Elhabazi , Jean-Paul Humbert , Isabelle Bertin , Raphaelle Quillet , Valérie Utard et al.
Neuropsychopharmacology, 2017, 118, pp.188-198. ⟨10.1016/j.neuropharm.2017.03.012⟩
Article dans une revue hal-01603852 v1
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Efficient and Mild Ullmann-Type N-Arylation of Amides, Carbamates, and Azoles in Water

Maud Bollenbach , Pedro Aquino , João Xavier De araújo-Júnior , Jean-Jacques Bourguignon , Frédéric Bihel et al.
Chemistry - A European Journal, 2017, 23 (55), pp.13676-13683. ⟨10.1002/chem.201700832⟩
Article dans une revue hal-02368823 v1

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

Olivier van Der Poorten , Robin van den Hauwe , Emilie Eiselt , Cecilia Betti , Karel Guillemyn et al.
ACS Medicinal Chemistry Letters, 2017, 8 (11), pp.1177-1182. ⟨10.1021/acsmedchemlett.7b00347⟩
Article dans une revue hal-02368778 v1

RF-amide neuropeptides and their receptors in Mammals: Pharmacological properties, drug development and main physiological functions

Raphaelle Quillet , Safia Ayachi , Frédéric Bihel , Khadija Elhabazi , Brigitte Ilien et al.
Alimentary Pharmacology & Therapeutics (Suppl), 2016, 160, pp.84-132. ⟨10.1016/j.pharmthera.2016.02.005⟩
Article dans une revue hal-02368835 v1

Development of Dipeptidic hGPR54 Agonists

Christelle Doebelin , Isabelle I. Bertin , Séverine Schneider , Martine Schmitt , Jean-Jacques Bourguignon et al.
ChemMedChem, 2016, 11 (19), pp.2147-2154. ⟨10.1002/cmdc.201600331⟩
Article dans une revue istex hal-02368845 v1
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Erratum to: "CMTX1 patients' cells present genomic instability corrected by CamKII inhibitors

Saleh Mones , Burkhard Gess , Benoit Bordignon , Alexandre Altie , Peter Young et al.
Orphanet Journal of Rare Diseases, 2016, 11, ⟨10.1186/s13023-015-0354-2⟩
Article dans une revue hal-02630248 v1

The effect of neuropeptide FF in the amygdala kindling model

I. Buffel , A. Meurs , J. Portelli , R. Raedt , V. de Herdt et al.
Acta Neurologica Scandinavica Supplementum, 2016, 134 (3), pp.181-188. ⟨10.1111/ane.12526⟩
Article dans une revue istex hal-02368848 v1

Opioid adjuvant strategy: improving opioid effectiveness

Frédéric Bihel
Future Medicinal Chemistry, 2016, 8 (3), pp.339-354. ⟨10.4155/fmc.15.186⟩
Article dans une revue hal-02368859 v1

Synthesis of 3-amino-3,4-dihydro-1H-quinolin-2-ones through regioselective palladium-catalyzed intramolecular cyclization

François Hallé , Olivier van Der Poorten , Christelle Doebelin , Marie Niederst , Séverine Schneider et al.
Tetrahedron Letters, 2016, 57 (14), pp.1547-1550. ⟨10.1016/j.tetlet.2016.02.094⟩
Article dans une revue hal-02290245 v1
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TSPO ligands stimulate ZnPPIX transport and ROS accumulation leading to the inhibition of P. falciparum growth in human blood

I Marginedas-Freixa , C Hattab , G Bouyer , F Halle , A Chene et al.
Scientific Reports, 2016, 6, pp.33516 ⟨10.1038/srep33516⟩
Article dans une revue hal-01369499 v1
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CMTX Disorder and CamKinase

Frédéric Bihel , Burkhard Gess , Michel Fontés
Frontiers in Cellular Neuroscience, 2016, 10, pp.1-4. ⟨10.3389/fncel.2016.00049⟩
Article dans une revue hal-02630284 v1
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d -Glucose: An Efficient Reducing Agent for a Copper(II)-Mediated Arylation of Primary Amines in Water

Maud Bollenbach , Patrick Wagner , Pedro Aquino , Jean-Jacques Bourguignon , Frédéric Bihel et al.
ChemSusChem, 2016, 9 (22), pp.3244-3249. ⟨10.1002/cssc.201600801⟩
Article dans une revue istex hal-02368856 v1

Neuropeptide FF receptors as novel targets for limbic seizure attenuation

Jeanelle Portelli , Alfred Meurs , Frederic Bihel , Hassan Hammoud , Martine Schmitt et al.
Neuropharmacology, 2015, 95, pp.415-423. ⟨10.1016/j.neuropharm.2015.04.030⟩
Article dans une revue hal-03005155 v1

Effects of systematic N-terminus deletions and benzoylations of endogenous RF-amide peptides on NPFF1R, NPFF2R, GPR10, GPR54 and GPR103

Laurent Rouméas , Jean-Paul Humbert , Séverine Schneider , Christelle Doebelin , Isabelle Bertin et al.
Peptides, 2015, 71, pp.156-161. ⟨10.1016/j.peptides.2015.07.016⟩
Article dans une revue hal-02997151 v1
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Rapid and scalable synthesis of innovative unnatural α,β or γ-amino acids functionalized with tertiary amines on their side-chains

Séverine Schneider , Hussein Ftouni , Songlin Niu , Martine Schmitt , Frédéric Simonin et al.
Organic & Biomolecular Chemistry, 2015, 13 (25), pp.7020-7026. ⟨10.1039/c5ob00828j⟩
Article dans une revue hal-04720697 v1

Development of a Peptidomimetic Antagonist of Neuropeptide FF Receptors for the Prevention of Opioid-Induced Hyperalgesia

Frédéric Bihel , Jean-Paul Humbert , Severine Schneider , Isabelle Bertin , Patrick Wagner et al.
ACS Chemical Neuroscience, 2015, 6 (3), pp.438-445. ⟨10.1021/cn500219h⟩
Article dans une revue hal-03198603 v1

Design and validation of a homogeneous time-resolved fluorescence cell-based assay targeting the ligand-gated ion channel 5-HT3A

Emilie Blanc , Patrick Wagner , Fabrice Plaisier , M. Schmitt , Thierry Durroux et al.
Analytical Biochemistry, 2015, 484, pp.105-12. ⟨10.1016/j.ab.2015.03.035⟩
Article dans une revue hal-02064366 v1

A Yeast/ Drosophila Screen to Identify New Compounds Overcoming Frataxin Deficiency

Alexandra Seguin , Véronique Monnier , Amandine Palandri , Frédéric Bihel , Michael Rera et al.
Oxidative Medicine and Cellular Longevity, 2015, 2015, pp.1-10. ⟨10.1155/2015/565140⟩
Article dans une revue hal-03798926 v1
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CMTX1 patients' cells present genomic instability corrected by CamKII inhibitors

Saleh Mones , Burkhardt Gess , Benoit Bordignon , Alexandre Altie , Peter Young et al.
Orphanet Journal of Rare Diseases, 2015, 10, ⟨10.1186/s13023-015-0270-5⟩
Article dans une revue hal-02634560 v1

Neuropeptide FF and prolactin-releasing peptide decrease cortical excitability through activation of NPFF receptors.

Ine Buffel , Alfred Meurs , Jeanelle Portelli , Robrecht Raedt , Veerle de Herdt et al.
Epilepsia, 2015, 56 (3), pp.489-498. ⟨10.1111/epi.12928⟩
Article dans une revue hal-03005167 v1
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CamKII inhibitors reduce mitotic instability, connexon anomalies and progression of the <em>in vivo</em> behavioral phenotype in transgenic animals expressing a mutated Gjb1 gene

Saleh Mones , Benoit Bordignon , Franck Peiretti , Jean-Francois Landrier , Burkhardt Gess et al.
Frontiers in Neuroscience, 2014, 8, 10 p. ⟨10.3389/fnins.2014.00151⟩
Article dans une revue hal-02639042 v1

Fully regiocontrolled polyarylation of pyridine.

C. Doebelin , P. Wagner , F. Bihel , N. Humbert , C.A. Kenfack et al.
Journal of Organic Chemistry, 2014, 79, pp.908-918
Article dans une revue hal-01065061 v1

A Yeast/Drosophila Screen to Identify New Compounds Overcoming Frataxin Deficiency.

Alexandra Seguin , Véronique Monnier , Amandine Palandri , Frédéric Bihel , Michael Rera et al.
Oxidative Medicine and Cellular Longevity, 2014, 2015, pp.565140. ⟨10.1155/2015/565140⟩
Article dans une revue hal-01267591 v1

Structure-activity relationship study around guanabenz identifies two derivatives retaining antiprion activity but having lost alpha 2-adrenergic receptor agonistic activity

- Phu Hai Nguyen , Hassan Hammoud , Sophie Halliez , Yanhong Pang , Justine Evrard et al.
ACS Chemical Neuroscience, 2014, 5 (10), pp.1075-1082. ⟨10.1021/cn5001588⟩
Article dans une revue hal-02635473 v1

The neuroprotector kynurenic acid increases neuronal cell survival through neprilysin induction.

Christian Klein , Christine Mensah-Nyagan , Omar Taleb , Jean-Jacques Bourguignon , Martine Schmitt et al.
Neuropharmacology, 2013, 70, pp.254-260. ⟨10.1016/j.neuropharm.2013.02.006⟩
Article dans une revue istex hal-02612146 v1

Endogenous mammalian RF-amide peptides, including PrRP, kisspeptin and 26RFa, modulate nociception and morphine analgesia via NPFF receptors

Khadija Elhabazi , Jean-Paul Humbert , Isabelle Bertin , Martine Schmitt , Frédéric Bihel et al.
Neuropharmacology, 2013, 75, pp.164-171. ⟨10.1016/j.neuropharm.2013.07.012⟩
Article dans une revue istex hal-02650252 v1

Trisubstitution of pyridine through sequential and regioselective palladium cross-coupling reactions affording analogs of known GPR54 antagonists

Christelle Doebelin , Patrick Wagner , Isabelle Bertin , Frederic Simonin , Martine Schmitt et al.
RSC Advances, 2013, 3 (26), pp.10296. ⟨10.1039/c3ra41985a⟩
Article dans une revue hal-03005205 v1

Development of sub-nanomolar dipeptidic ligands of neuropeptide FF receptors

Ronan Gealageas , Severine Schneider , Jean-Paul Humbert , Isabelle Bertin , Martine Schmitt et al.
Bioorganic and Medicinal Chemistry Letters, 2012, 22 (24), pp.7471-7474. ⟨10.1016/j.bmcl.2012.10.049⟩
Article dans une revue istex hal-02993696 v1

New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.

F.J.J. Bihel , Hélène Justiniano , Martine Schmitt , Malik Hellal , Mohamed A. Ibrahim et al.
Bioorganic and Medicinal Chemistry Letters, 2011, 21, pp.6567-6572
Article dans une revue hal-00667395 v1

Involvement of neuropeptide FF receptors in neuroadaptive responses to acute and chronic opiate treatments

Khadija Elhabazi , J Trigo , C Mollereau , L Mouledous , J.-M. Zajac et al.
British Journal of Pharmacology, 2011, 165 (2), pp.424-435. ⟨10.1111/j.1476-5381.2011.01563.x⟩
Article dans une revue hal-04674971 v1

6-Endo-dig cyclization of heteroarylesters to alkynes promoted by Lewis acid catalyst in the presence of Bronsted acid

Hellal Malik , Bourguignon Jean-Jacques , Frédéric Bihel
Tetrahedron Letters, 2008, 49 (1), pp.62-65
Article dans une revue hal-00195333 v1

Synthesis and reactivity of 2,3-dihydro-1H-2,3-benzodiazepine-1,4(5H)-dione

Frédéric Bihel , Hellal Malik , Bourguignon Jean-Jacques
Synthesis: Journal of Synthetic Organic Chemistry, 2007, 24, pp.3791-3796
Article dans une revue hal-00195328 v1

Microwave-assisted cyclic amidine synthesis using TiCl4.

M. Hellal , F. Bihel , A. Mongeot , J.-J. Bourguignon
Organic & Biomolecular Chemistry, 2006, 4, pp.3142-3146
Article dans une revue hal-00129884 v1

Substituted thiazolamide coupled to a redox delivery system: a new gamma-secretase inhibitor with enhanced pharmacokinetic profile

Y. Laras , G. Quelever , C. Garino , N. Pietrancosta , M. Sheha et al.
Organic & Biomolecular Chemistry, 2005, 3, pp.612-618
Article dans une revue hal-00118749 v1

substituded thiazolamide coupled to a redox delivery system : a new gamma-secretase inhibitor with enhanced pharmacokinetic profile

Y. Younes , G. Quelever , C. Garino , N. Pietrancosta , M. Shela et al.
Organic & Biomolecular Chemistry, 2005, 21, pp.612-8
Article dans une revue hal-00159607 v1

Substituted thiazolamide coupled to a redox delivery system: a new γ-secretase inhibitor with enhanced pharmacokinetic profile

Younes Laras , Gilles Quéléver , Cédrik Garino , Nicolas Pietrancosta , Mahmoud Sheha et al.
Organic & Biomolecular Chemistry, 2005, 3 (4), pp.612-618. ⟨10.1039/b415090b⟩
Article dans une revue istex hal-02351730 v1

New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones. Synthesis and biological properties

C. Garino , F. Bihel , N. Pietrancosta , Y. Laras , G. Quelever et al.
Bioorganic and Medicinal Chemistry Letters, 2005, 15, pp.135-138
Article dans une revue hal-00117234 v1

Photoactivatable helical peptide inhibitors of y-secretase covalently bind to presenilin at a site close to but distinct from the active site.

A.Y. Kornilova , F. Bihel , C. Das , M.S. Wolfe
Proceedings of the National Academy of Sciences of the United States of America, 2005, 102, pp.3230-5
Article dans une revue hal-00159650 v1

New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones. Synthesis and biological properties

Cédrik Garino , Frédéric Bihel , Nicolas Pietrancosta , Younes Laras , Gilles Quéléver et al.
Bioorganic and Medicinal Chemistry Letters, 2005, 15 (1), pp.135-138. ⟨10.1016/j.bmcl.2004.10.018⟩
Article dans une revue istex hal-02351737 v1

N-acyl substituted 7-amino-4-chloroisocoumarin: a peptide degradation model via an imide mechanism

C. Garino , F. Bihel , F. Souard , G. Quelever , J.L. Kraus
Bioorganic and Medicinal Chemistry Letters, 2004, 14, pp.1771-1774
Article dans une revue hal-00305873 v1

New b-strand macrocyclic peptidomimetic analogues containing alpha-(O-, S- or NH-)aryl substituted glycine residues: synthesis, chemical and enzymatic properties

Gilles Quéléver , Frédéric Bihel , Jean-Louis Kraus
Organic & Biomolecular Chemistry, 2003, 1, pp.1676-1683
Article dans une revue hal-00154124 v1

Synthesis of new 3-alkoxy-7-amino-4-chloro-isocoumarin derivatives as new β-amyloid peptide production inhibitors and their activities on various classes of protease

Agnès Petit-Paitel , Frédéric Bihel , Gilles Quéléver , Hugues Lelouard , Agnès Petit et al.
Bioorganic and Medicinal Chemistry, 2003, 11 (14), pp.3141-3152. ⟨10.1016/s0968-0896(03)00235-9⟩
Article dans une revue istex hal-03016636 v1

Novel synthesis of 3,4-dihydro-5-bromo[1,4]oxazin-2-one derivatives, new protease inhibitor scaffold

F. Bihel , J.L. Kraus
Organic & Biomolecular Chemistry, 2003, 1, pp.793-799
Article dans une revue hal-00304322 v1

New beta-strand macrocyclic peptidomimetic analogues containing alpha-(O-, S- or NH-)aryl substituted glycine residues: synthesis, chemical and enzymatic properties

G. Quelever , F. Bihel , J.L. Kraus
Organic & Biomolecular Chemistry, 2003, 1, pp.1676-83
Article dans une revue hal-00304318 v1

Synthesis of new 3-alkoxy-7-amino-4-chloro-isocoumarin derivatives as new beta-amyloid peptide production inhibitors and their activities on various classes of protease

F. Bihel , G. Quelever , H. Lelouard , A. Petit , C. Alves da Costa et al.
Bioorganic and Medicinal Chemistry, 2003, 11, pp.3141-3152
Article dans une revue hal-00304333 v1

Novel synthesis of 3,4-dihydro-5-bromo[1,4]oxazin-2-one derivatives, new protease inhibitor scaffold

Frédéric Bihel , Jean-Louis Kraus
Organic & Biomolecular Chemistry, 2003, 1, pp.793-799
Article dans une revue hal-00154126 v1

Reactivity studies of 3-alkoxy-7-amino-4-chloroisocoumarins (beta-amyloid peptide inhibitors) versus different classes of amines

F. Bihel , R. Faure , J.L. Kraus
Organic & Biomolecular Chemistry, 2003, 1, pp.800-802
Article dans une revue hal-00304324 v1

Synthesis of new 3-alkoxy-7-amino-4-chloro-isocoumarin derivatives as new b-amyloid peptide production inhibitors and their activities on various classes of protease

Frédéric Bihel , Gilles Quéléver , Hugues Lelouard , Agnes Petit , Christine Alves da Costa et al.
Bioorganic and Medicinal Chemistry, 2003, 11, pp.3141-3152
Article dans une revue hal-00154122 v1

Synthesis and antiviral activity of new anti-HIV amprenavir bioisosteres

L. Rocheblave , F. Bihel , C. de Michelis , G. Priem , J. Courcambeck et al.
Journal of Medicinal Chemistry, 2002, 45, pp.3321-24
Article dans une revue hal-00304305 v1

Synthesis and antiviral activity of new Anti-HIV amprenavir bioisosteres

Luc Rocheblave , Frédéric Bihel , Céline de Michelis , Ghislaine Priem , Jérôme Courcambeck et al.
Journal of Medicinal Chemistry, 2002, 45, pp.3321-3324
Article dans une revue hal-00154120 v1

New protease inhibitors prevent gamma-secretase-mediated production of Ab40/42 without affecting Notch cleavage.

Frédéric Bihel , Agnes Petit , Christine Alves da Costa , Olivier Pourquié , Frédéric Checler et al.
Nature Cell Biology, 2001, 3, pp.507-511
Article dans une revue hal-00154118 v1

New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs: Synthesis and anti-HIV evaluation.

Patrick Vlieghe , Frédéric Bihel , Thierry Clerc , Christophe Pannecouque , Myriam Witvrouw et al.
Journal of Medicinal Chemistry, 2001, 44, pp.777-786
Article dans une revue hal-00154110 v1

Design of potential newHIV protease inhibitors: enantioconvergent synthesis of new pyrrolidin-3-ol, and pyrrolidin-3-one peptide conjugates.

Frédéric Bihel , Jérôme Courcambeck , Céline de Michelis , Gilles Quéléver , Jean-Louis Kraus
Journal of the Chemical Society Perkin Transactions 1, 2001, pp.1421-1430
Article dans une revue hal-00154116 v1

Anti-tumor activity of new ligands targeting LINGO1- a protein primarily expressed in CNS for the treatment of glioblastomas

Wanyin Chen , Anthony Guillemain , Lauren Blot , Fabienne Fasani , Esther Kellenberger et al.
Colloque Niche et épigénétique des tumeurs, Jul 2020, Online, France
Communication dans un congrès hal-03686680 v1

Allosteric Modulators of CDK4 for Lung Cancer Therapeutics

May Catherine Morris , Frédéric Bihel , Sebastien Diot , Clovis Peter , Céline Bouclier et al.
Annual Meeting on Experimental Biology, The Federation of American Societies for Experimental Biology (FASEB), Apr 2020, San Diego (California), United States. pp.1-1, ⟨10.1096/fasebj.2020.34.s1.00334⟩
Communication dans un congrès hal-04570635 v1

The research of new therapeutic targets and small chemical molecules for glioblastoma therapies

W. Chen , A. Guillemain , L. Blot , Fabienne Fasani , E. Kellenberger et al.
Central South University in HuNan, Dec 2019, Changsha, China
Communication dans un congrès hal-03686683 v1

6-Endo-dig cyclization of heteroarylesters to alkynes promoted by Lewis acid catalyst in presence of Brønsted acid

Hellal Malik , Bourguignon Jean-Jacques , Frédéric Bihel
SAJEC, Oct 2007, Paris, France
Communication dans un congrès hal-00195387 v1

6-Endo-dig cyclization of heteroarylesters to alkynes promoted by Lewis acid catalyst in presence of Brønsted acid

Frédéric Bihel , Hellal Malik , Bourguignon Jean-Jacques
XXVII REGIO, Sep 2007, Buhl, France
Communication dans un congrès hal-00195398 v1

Synthèse et fonctionnalisation de 2,3-benzodiazépines : Vers la construction d'une chimiothèque focalisée

Hellal Malik , Frédéric Bihel , Bourguignon Jean-Jacques
Journée Scientifique de l'Institut Gilbert Laustriat, Apr 2007, Illkirch, France
Communication dans un congrès hal-00195391 v1

Creation of a Chemical Diversity Space Around the 2,3-Benzodiazepine Scaffold

Frédéric Bihel , Hellal Malik , Bourguignon Jean-Jacques
International Symposium on Advances in Synthetic and Medicinal Chemistry, Aug 2007, Saint Petersbourg, Russia
Communication dans un congrès hal-00195383 v1

Microwave-assisted cyclic amidine synthesis using TiCl4

Hellal Malik , Frédéric Bihel , Bourguignon Jean-Jacques
Journée Scientifique de l'IFR Gilbert Laustriat, 2006, Illkirch, France
Communication dans un congrès hal-00195376 v1

Design and synthesis of Benzodiazepines as phthalazine structurally-related compounds

Hellal Malik , Frédéric Bihel , Bourguignon Jean-Jacques
10th International Symposium on the Chemistry and Pharmacology of Pyridazines, Jun 2006, Strasbourg, France
Communication dans un congrès hal-00195377 v1

Synthèse assistée par micro-onde d'amidines cycliques médiée par TiCl4

Hellal Malik , Frédéric Bihel , Bourguignon Jean-Jacques
SECO'43, May 2006, Fréjus, France
Communication dans un congrès hal-00195388 v1

P2Y1 Purinergic Receptor : Synthesis of a fluorescent Probe

Frédéric Bihel
Strep GPCR / Joint Meeting, Feb 2005, Barcelone, Spain
Communication dans un congrès hal-00195392 v1

Evaluation of the anti-tumoral acitivty of new ligands targeting LINGO-1 for the treatment of glioblastoma

W. Chen , A. Guillemain , L. Blot , F. Fasani , E. Kellenberger et al.
Journée du cancéropole Grand ouest, Oct 2020, Virtual, France
Poster de conférence hal-03686678 v1

Anti-tumor activity of new ligands targeting LINGO1- a protein primarily expressed in CNS for the treatment of glioblastomas

Wanyin Chen , Anthony Guillemain , Lauren Blot , Fabienne Fasani , Esther Kellenberger et al.
Colloque Niche et épigénétique des tumeurs, Jul 2020, Online, France.
Poster de conférence hal-03686675 v1

Etude de l’activité anti-tumorale de nouveaux ligands ciblant LINGO-1 pour le traitement des glioblastomes

Wanyin Chen , Anthony Guillemain , Lauren Blot , Fabienne Fasani , Esther Kellenberger et al.
Journée Fédération FR2708 Physique et Chimie du Vivant, Apr 2019, Orléans, France
Poster de conférence hal-03625295 v1

Etude de l’activité anti-tumorale de nouveaux ligands ciblant LINGO-1 pour le traitement des glioblastomes

Wanyin Chen , Anthony Guillemain , Lauren Blot , Fabienne Fasani , Esther Kellenberger et al.
Colloque de l’ADOC, Jul 2019, Orléans, France
Poster de conférence hal-03686230 v1

Nouvelles molécules chimiques anti-tumorales pour le traitement du glioblastomes

W. Chen , A. Guillemain , L. Blot , F. Fasani , E. Kellenberger et al.
13es journées du Cancéropôle Grand Ouest, Jul 2019, Tours, France
Poster de conférence hal-02973622 v1

Anti-tumoral activity of new ligands targeting LINGO-1 for the treatment of glioblastoma

Wanyin Chen , Anthony Guillemain , Laurent Blot , Fabienne Fasani , E. Kellenberger et al.
1st meeting « Niches and Epigenetic of tumors », Mar 2019, Nantes, France
Poster de conférence hal-02973567 v1

In vitro and in vivo characterization of RF313 the first orally available NPFF receptor antagonist.

Frédéric Simonin , J-P Humbert , I Bertin , Raphaelle Quillet , Valérie Utard et al.
SFN 45th Annual Meeting, Chicago, USA, (2015-10-17 / 2015-10-21), Oct 2015, Chicago, United States. 2015
Poster de conférence hal-04747309 v1

Pallado-catalyzed reactions applied to solid phase synthesis of dipeptidic GPR54 agonists

Christelle Doebelin , I Bertin , M Schmitt , Frédéric Simonin , Valérie Simonneaux et al.
18e Congrès du GFPP, Sète, France, (2013-05-26 / 2013-05-31), May 2013, Sète, France. 2013
Poster de conférence hal-04747272 v1

Modulation of nociception and morphine analgesia by endogenous RF−amide peptides.

Frédéric Simonin , J-P Humbert , I Bertin , M Schmitt , Frédéric Bihel et al.
Gordon Research Conference on Molecular Pharmacology, Il Ciocco, Italie (2013-05-08 / 2013-05-13), May 2013, Il Ciocco, Italy. 2013
Poster de conférence hal-04750860 v1

Development of the first orally available NPFF1-R antagonist capable of reversing opioid-induced hyperalgesia in rodents

Frédéric Bihel , S Schneider , M Schmitt , J-P Humbert , Khadija Elhabazi et al.
International conference on Medicinal Chemistry RICT 2012, Poitiers, France, (2012-07-04 /2012-07-06), Jul 2012, Poitiers, France. 2012
Poster de conférence hal-04754574 v1

Neuropeptide FF receptors as novel drug targets in epilepsy

I Smolders , J Portelli , Frédéric Bihel , M Schmitt , J Coppens et al.
SFN 42nd Annual Meeting, New Orleans, USA, (2012-10-13 / 2012-10-17), Oct 2012, New Orleans, United States. 2012
Poster de conférence hal-04747273 v1

Neuropeptide FF decreases Cortical and Amygdala Excitability Via NPFF1 and/or NPFF2 Receptors

A Meurs , I Buffel , J Portelli , R Raedt , L Sioncke et al.
SFN 42nd Annual Meeting, New Orleans, USA, (2012-10-13 / 2012-10-17), Oct 2012, New Orleans, United States. 2012
Poster de conférence hal-04747286 v1

Dérivés polysubstitués de pyridines comme ligands hétérocycliques de GPR54

Christelle Doebelin , P Wagner , M Messe , M Schmitt , Frédéric Bihel et al.
Journée jeunes chercheurs SCT, Mar 2012, Romainville, France. 2012
Poster de conférence hal-05035740 v1