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Items: 1 to 20 of 44

1.

Structure-Activity Relationships (SARs) of α-Ketothioamides as Inhibitors of Phosphoglycerate Dehydrogenase (PHGDH).

Spillier Q, Ravez S, Unterlass J, Corbet C, Degavre C, Feron O, Frédérick R.

Pharmaceuticals (Basel). 2020 Jan 22;13(2). pii: E20. doi: 10.3390/ph13020020.

PMID:
31979167
2.

Anti-alcohol abuse drug disulfiram inhibits human PHGDH via disruption of its active tetrameric form through a specific cysteine oxidation.

Spillier Q, Vertommen D, Ravez S, Marteau R, Thémans Q, Corbet C, Feron O, Wouters J, Frédérick R.

Sci Rep. 2019 Mar 18;9(1):4737. doi: 10.1038/s41598-019-41187-0.

3.

Current state on tryptophan 2,3-dioxygenase inhibitors: a patent review.

Kozlova A, Frédérick R.

Expert Opin Ther Pat. 2019 Jan;29(1):11-23. doi: 10.1080/13543776.2019.1556638. Epub 2019 Jan 16. Review.

PMID:
30526149
4.

1-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.

Ameryckx A, Thabault L, Pochet L, Leimanis S, Poupaert JH, Wouters J, Joris B, Van Bambeke F, Frédérick R.

Eur J Med Chem. 2018 Nov 5;159:324-338. doi: 10.1016/j.ejmech.2018.09.067. Epub 2018 Sep 28.

PMID:
30300845
5.

31ièmes Journées Franco-Belges de Pharmacochimie: Meeting Report.

Frédérick R, Pochet L, De Tullio P, Dufrasne F.

Pharmaceuticals (Basel). 2017 Dec 4;10(4). pii: E94. doi: 10.3390/ph10040094.

6.

Arginase Structure and Inhibition: Catalytic Site Plasticity Reveals New Modulation Possibilities.

Mortier J, Prévost JRC, Sydow D, Teuchert S, Omieczynski C, Bermudez M, Frédérick R, Wolber G.

Sci Rep. 2017 Oct 19;7(1):13616. doi: 10.1038/s41598-017-13366-4.

7.

Radiosynthesis and validation of (±)-[18F]-3-fluoro-2-hydroxypropionate ([18F]-FLac) as a PET tracer of lactate to monitor MCT1-dependent lactate uptake in tumors.

Van Hée VF, Labar D, Dehon G, Grasso D, Grégoire V, Muccioli GG, Frédérick R, Sonveaux P.

Oncotarget. 2017 Apr 11;8(15):24415-24428. doi: 10.18632/oncotarget.14705.

8.

α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH).

Ravez S, Corbet C, Spillier Q, Dutu A, Robin AD, Mullarky E, Cantley LC, Feron O, Frédérick R.

J Med Chem. 2017 Feb 23;60(4):1591-1597. doi: 10.1021/acs.jmedchem.6b01166. Epub 2017 Jan 27.

9.

Challenges and Opportunities in the Development of Serine Synthetic Pathway Inhibitors for Cancer Therapy.

Ravez S, Spillier Q, Marteau R, Feron O, Frédérick R.

J Med Chem. 2017 Feb 23;60(4):1227-1237. doi: 10.1021/acs.jmedchem.6b01167. Epub 2016 Dec 22. Review.

PMID:
27959531
10.

Lactate Dehydrogenase B Controls Lysosome Activity and Autophagy in Cancer.

Brisson L, Bański P, Sboarina M, Dethier C, Danhier P, Fontenille MJ, Van Hée VF, Vazeille T, Tardy M, Falces J, Bouzin C, Porporato PE, Frédérick R, Michiels C, Copetti T, Sonveaux P.

Cancer Cell. 2016 Sep 12;30(3):418-431. doi: 10.1016/j.ccell.2016.08.005.

11.

Intestinal Sucrase as a Novel Target Contributing to the Regulation of Glycemia by Prebiotics.

Neyrinck AM, Pachikian B, Taminiau B, Daube G, Frédérick R, Cani PD, Bindels LB, Delzenne NM.

PLoS One. 2016 Aug 17;11(8):e0160488. doi: 10.1371/journal.pone.0160488. eCollection 2016.

12.

Synthesis and In Vitro Evaluation of Polyethylene Glycol-Paclitaxel Conjugates for Lung Cancer Therapy.

Luo T, Magnusson J, Préat V, Frédérick R, Alexander C, Bosquillon C, Vanbever R.

Pharm Res. 2016 Jul;33(7):1671-81. doi: 10.1007/s11095-016-1908-2. Epub 2016 Mar 16.

PMID:
26984129
13.

Synthesis, evaluation and structure-activity relationship of new 3-carboxamide coumarins as FXIIa inhibitors.

Bouckaert C, Serra S, Rondelet G, Dolušić E, Wouters J, Dogné JM, Frédérick R, Pochet L.

Eur J Med Chem. 2016 Mar 3;110:181-94. doi: 10.1016/j.ejmech.2016.01.023. Epub 2016 Jan 16.

PMID:
26827162
14.

Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.

Ravez S, Arsenlis S, Barczyk A, Dupont A, Frédérick R, Hesse S, Kirsch G, Depreux P, Goossens L.

Bioorg Med Chem. 2015 Nov 15;23(22):7340-7. doi: 10.1016/j.bmc.2015.10.035. Epub 2015 Oct 24.

PMID:
26526740
15.

3D-QSAR, design, synthesis and characterization of trisubstituted harmine derivatives with in vitro antiproliferative properties.

Meinguet C, Bruyère C, Frédérick R, Mathieu V, Vancraeynest C, Pochet L, Laloy J, Mortier J, Wolber G, Kiss R, Masereel B, Wouters J.

Eur J Med Chem. 2015 Apr 13;94:45-55. doi: 10.1016/j.ejmech.2015.02.044. Epub 2015 Feb 24.

16.

Thiosemicarbazide, a fragment with promising indolamine-2,3-dioxygenase (IDO) inhibition properties.

Serra S, Moineaux L, Vancraeynest C, Masereel B, Wouters J, Pochet L, Frédérick R.

Eur J Med Chem. 2014 Jul 23;82:96-105. doi: 10.1016/j.ejmech.2014.05.044. Epub 2014 May 15.

PMID:
24878638
17.

Indoleamine 2,3-dioxygenase inhibitors: a patent review (2008 - 2012).

Dolušić E, Frédérick R.

Expert Opin Ther Pat. 2013 Oct;23(10):1367-81. doi: 10.1517/13543776.2013.827662. Epub 2013 Aug 30. Review.

PMID:
23992582
18.

Indoleamine 2,3-dioxygenase inhibitory activity of derivatives of marine alkaloid tsitsikammamine A.

Dolušić E, Larrieu P, Meinguet C, Colette D, Rives A, Blanc S, Ferain T, Pilotte L, Stroobant V, Wouters J, Van den Eynde B, Masereel B, Delfourne E, Frédérick R.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):47-54. doi: 10.1016/j.bmcl.2012.11.036. Epub 2012 Nov 22.

PMID:
23218716
19.

New selective carbonic anhydrase IX inhibitors: synthesis and pharmacological evaluation of diarylpyrazole-benzenesulfonamides.

Rogez-Florent T, Meignan S, Foulon C, Six P, Gros A, Bal-Mahieu C, Supuran CT, Scozzafava A, Frédérick R, Masereel B, Depreux P, Lansiaux A, Goossens JF, Gluszok S, Goossens L.

Bioorg Med Chem. 2013 Mar 15;21(6):1451-64. doi: 10.1016/j.bmc.2012.10.029. Epub 2012 Oct 29.

PMID:
23168081
20.

Computational tools for in silico fragment-based drug design.

Mortier J, Rakers C, Frederick R, Wolber G.

Curr Top Med Chem. 2012;12(17):1935-43. Review.

PMID:
23116473

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