Schwarz PF, Perhal AF, Preglej T, Breit L, Schmetterer KG, Grienke U, Janneschütz J, Chen Y, Rochel N, Kirchmair J, Schützenmeister N, Rollinger JM, Bonelli M, Dirsch VM

Acta Pharm Sin B. 2026 06;16(6):3746-3763

25-nitro-20-epi-vitamin D analogue with anti-proliferative and cytoprotective properties: Biological and pharmacological evaluation.

Gómez-Bouzó U, Peluso-Iltis C, Barreiro S, Fernandes C, Verlinden L, Verstuyf A, Borges F, Rochel N, Gómez G, Fall Y

Exp Mol Pathol. 2026 02 23;145:105036

Targeted Inhibition of CBP/p300-NCOA3 Interactions with an α-Methylated Peptide.

Silvestri A, Osz J, Jouin A, Bauer V, Chalhoub S, Torbeev V, Rochel N

J Med Chem. 2025 12 16;:

Mechanism of Inhibition of the MeTC7 Ligand That Covalently Binds to VDR To Reduce PD-L1 Expression.

Castel J, Peluso-Iltis C, Sanchez Dafun A, Silvestri A, Osz J, Khazan N, Yano N, Kim KK, Rowswell-Turner RB, Guiberteau T, Teramoto Y, Miyamoto H, Moore RG, Singh RK, Cianférani S, Rochel N

J Med Chem. 2025 10 22;:

New structural insights into the control of the retinoic acid receptors RAR/RXR by DNA, ligands, and transcriptional coregulators.

Tambones I, Sagar A, Vankova P, Loginov D, Carivenc C, Rochel N, Bourguet W, Man P, Bernadó P, le Maire A

Nucleic Acids Res. 2025 09 23;53(18):

Hyperagonism of a Vitamin D Receptor Agonist/Histone Deacetylase Inhibitor Hybrid Molecule.

Sarmadi F, Caza A, Gao Z, Rochel N, Gleason JL, White JH

J Med Chem. 2025 09 18;:

Identification of New Lupane-Type Triterpenoids as Inverse Agonists of RAR-Related Orphan Receptor Gamma (RORγ).

Schwarz PF, Perhal AF, Guder F, Hernández González JE, Janssen K, Sağıroğlu E, Tahir A, Kirchmair J, Rochel N, Dirsch VM, Chen Y

J Nat Prod. 2025 07 28;:

Synthesis, Molecular Docking and Biological Evaluation of A-Ring-Carborane-Vitamin D Analogues.

Otero R, Seoane S, Fernández-Domínguez X, Bourguet M, Cianférani S, Peluso-Iltis C, Maestro MA, Pérez-Fernández R, Rochel N, Mouriño A

Molecules. 2025 06 18;30(12):

Design, synthesis and biological evaluation of a novel non-Gemini analog of UVB1 and crystal structure of its complex with the vitamin D receptor.

Gómez-Bouzó U, Peluso-Iltis C, Santalla H, Verlinden L, Verstuyf A, Rochel N, Gómez G, Fall Y

Bioorg Chem. 2025 02 4;157:108239

Guanidinium-Stapled Helical Peptides for Targeting Protein-Protein Interactions.

Perdriau C, Luton A, Zimmeter K, Neuville M, Saragaglia C, Peluso-Iltis C, Osz J, Kauffmann B, Collie GW, Rochel N, Guichard G, Pasco M

Angew Chem Int Ed Engl. 2024 12 23;:e202416348

First Sila-Vitamin D Analogues: Design, Synthesis, Structural Analysis and Biological Activity.

Loureiro J, Seoane S, Sampaio-Dias IE, Peluso-Iltis C, Guiberteau T, Brito B, Gregorio C, Pérez-Fernández R, Rochel N, Mouriño A, Rodríguez-Borges JE

J Med Chem. 2024 11 29;:

Retinoids Molecular Probes by Late-stage Azide Insertion - Functional Tools to Decrypt Retinoid Metabolism.

Coulleray J, Kindler A, Rima M, Cahuzac H, Rochel N, Chaubet G, Krezel W, Wagner A

Chembiochem. 2024 08 2;:e202300689

A vitamin D-based strategy overcomes chemoresistance in prostate cancer.

Len-Tayon K, Beraud C, Fauveau C, Belorusova AY, Chebaro Y, Mouriño A, Massfelder T, Chauchereau A, Metzger D, Rochel N, Laverny G

Br J Pharmacol. 2024 07 9;:

Design, Synthesis, and Biological Evaluation of New Type of Gemini Analogues with a Cyclopropane Moiety in Their Side Chain.

Gómez-Bouzó U, Peluso-Iltis C, Santalla H, Quevedo MA, Verlinden L, Verstuyf A, Fall Y, Gómez G, Rochel N

J Med Chem. 2024 06 10;:

4-Hydroxy-1α,25-Dihydroxyvitamin D: Synthesis and Structure-Function Study.

Peluso-Iltis C, Pierrat N, Rovito D, Osz J, Sawada D, Kittaka A, Laverny G, Rochel N

Biomolecules. 2024 05 3;14(5):

Design, synthesis, and biological activity of D-bishomo-1α,25-dihydroxyvitamin D analogs and their crystal structures with the vitamin D nuclear receptor.

Fabisiak A, Brzeminski P, Sicinski RR, Rochel N, Maj E, Filip-Psurska B, Wietrzyk J, Plum LA, DeLuca HF

Eur J Med Chem. 2024 04 10;271:116403

Further Studies on the Highly Active Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D (Calcitriol): Refinement of the Side Chain.

Zárate-Ruíz A, Seoane S, Peluso-Iltis C, Peters S, Gregorio C, Guiberteau T, Maestro M, Pérez-Fernández R, Rochel N, Mouriño A

J Med Chem. 2023 11 1;:

Vitamin D Receptor Antagonist MeTC7 Inhibits PD-L1.

Khazan N, Quarato ER, Singh NA, Snyder CWA, Moore T, Miller JP, Yasui M, Teramoto Y, Goto T, Reshi S, Hong J, Zhang N, Pandey D, Srivastava P, Morell A, Kawano H, Kawano Y, Conley T, Sahasrabudhe DM, Yano N, Miyamoto H, Aljitawi O, Liesveld J, Becker MW, Calvi LM, Zhovmer AS, Tabdanov ED, Dokholyan NV, Linehan DC, Hansen JN, Gerber SA, Sharon A, Khera MK, Jurutka PW, Rochel N, Kim KK, Rowswell-Turner RB, Singh RK, Moore RG

Cancers (Basel). 2023 06 30;15(13):

Structural analysis and biological activities of C25-amino and C25-nitro vitamin D analogs.

Gómez-Bouzó U, Belorusova AY, Rivadulla ML, Santalla H, Verlinden L, Verstuyf A, Ferronato MJ, Curino AC, Facchinetti MM, Fall Y, Gómez G, Rochel N

Bioorg Chem. 2023 04 6;136:106528

FGFR3 Mutational Activation Can Induce Luminal-like Papillary Bladder Tumor Formation and Favors a Male Sex Bias.

Shi MJ, Fontugne J, Moreno-Vega A, Meng XY, Groeneveld C, Dufour F, Kamoun A, Viborg Lindskrog S, Cabel L, Krucker C, Rapinat A, Dunois-Larde C, Lepage ML, Chapeaublanc E, Levrel O, Dixon V, Lebret T, Almeida A, De Reynies A, Rochel N, Dyrskjøt L, Allory Y, Radvanyi F, Bernard-Pierrot I

Eur Urol. 2022 10 20;:

Design, Synthesis, Biological Activity, and Structural Analysis of Novel Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D.

Seoane S, Gogoi P, Zárate-Ruíz A, Peluso-Iltis C, Peters S, Guiberteau T, Maestro MA, Pérez-Fernández R, Rochel N, Mouriño A

J Med Chem. 2022 09 27;:

Vitamin D Analogs Bearing C-20 Modifications Stabilize the Agonistic Conformation of Non-Responsive Vitamin D Receptor Variants.

Belorusova AY, Rovito D, Chebaro Y, Doms S, Verlinden L, Verstuyf A, Metzger D, Rochel N, Laverny G

Int J Mol Sci. 2022 07 30;23(15):

Vitamin D and Its Receptor from a Structural Perspective.

Rochel N

Nutrients. 2022 07 12;14(14):

Advances in Vitamin D Receptor Function and Evolution Based on the 3D Structure of the Lamprey Ligand-Binding Domain.

Sigüeiro R, Bianchetti L, Peluso-Iltis C, Chalhoub S, Dejaegere A, Osz J, Rochel N

J Med Chem. 2022 Mar 18;:

HR-Bac, a toolbox based on homologous recombination for expression, screening and production of multiprotein complexes using the baculovirus expression system.

Kolesnikova O, Zachayus A, Pichard S, Osz J, Rochel N, Rossolillo P, Kolb-Cheynel I, Troffer-Charlier N, Compe E, Bensaude O, Berger I, Poterszman A

Sci Rep. 2022 02 7;12(1):2030

Biological evaluation and synthesis of calcitroic acid.

Yu OB, Webb DA, Di Milo ES, Mutchie TR, Teske KA, Chen T, Lin W, Peluso-Iltis C, Rochel N, Helmstädter M, Merk D, Arnold LA

Bioorg Chem. 2021 Aug 28;116:105310

Ligands and DNA in the allosteric control of retinoid receptors function.

Germain P, Rochel N, Bourguet W

Essays Biochem. 2021 Jul 23;:

Design, synthesis and evaluation of side-chain hydroxylated derivatives of lithocholic acid as potent agonists of the vitamin D receptor (VDR).

González CM, Gaikwad S, Lasanta G, Loureiro J, Nilsson N, Peluso-Iltis C, Rochel N, Mouriño A

Bioorg Chem. 2021 Jul 22;115:105202

Design, Synthesis, Evaluation and Structure of Allenic 1a,25- Dihydroxyvitamin D3 Analogs with Locked Mobility at C-17.

Mourino A, Fraga R, Len K, Lutzing G, Laverny G, Loureiro J, Maestro M, Rochel N, Rodriguez-Borges JE

Chemistry. 2021 Jul 5;:

Cytosolic sequestration of the vitamin D receptor as a therapeutic option for vitamin D-induced hypercalcemia.

Rovito D, Belorusova AY, Chalhoub S, Rerra AI, Guiot E, Molin A, Linglart A, Rochel N, Laverny G, Metzger D

Nat Commun. 2020 12 7;11(1):6249

Conformational editing of intrinsically disordered protein by α-methylation.

Bauer V, Schmidtgall B, Gógl G, Dolenc J, Osz J, Nominé Y, Kostmann C, Cousido-Siah A, Mitschler A, Rochel N, Travé G, Kieffer B, Torbeev V

Chem Sci. 2020 Nov 4;12(3):1080-1089

Molecular determinants of MED1 interaction with the DNA bound VDR-RXR heterodimer.

Belorusova AY, Bourguet M, Hessmann S, Chalhoub S, Kieffer B, Cianférani S, Rochel N

Nucleic Acids Res.. 2020 Sep 29;:

Structural basis for DNA recognition and allosteric control of the retinoic acid receptors RAR-RXR.

Osz J, McEwen AG, Bourguet M, Przybilla F, Peluso-Iltis C, Poussin-Courmontagne P, Mély Y, Cianférani S, Jeffries CM, Svergun DI, Rochel N

Nucleic Acids Res.. 2020 Sep 25;48(17):9969-9985

Structural basis for α-helix mimicry and inhibition of protein-protein interactions with oligourea foldamers.

Guichard G, Cussol L, Mauran L, Buratto J, Belorusova AY, Neuville M, Osz J, Fribourg S, Fremaux J, Dolain C, Goudreau S, Rochel N

Angew. Chem. Int. Ed. Engl.. 2020 Sep 16;:

DNA recognition by retinoic acid nuclear receptors.

Peluso-Iltis C, Osz J, Rochel N

Meth. Enzymol.. 2020 ;637:235-260

Quercetin potentializes the respective cytotoxic activity of gemcitabine or doxorubicin on 3D culture of AsPC-1 or HepG2 cells, through the inhibition of HIF-1α and MDR1.

Hassan S, Peluso J, Chalhoub S, Idoux Gillet Y, Benkirane-Jessel N, Rochel N, Fuhrmann G, Ubeaud-Sequier G

PLoS One. 2020 ;15(10):e0240676

Recurrent activating mutations of PPARγ associated with luminal bladder tumors.

Rochel N, Krucker C, Coutos-Thévenot L, Osz J, Zhang R, Guyon E, Zita W, Vanthong S, Hernandez OA, Bourguet M, Badawy KA, Dufour F, Peluso-Iltis C, Heckler-Beji S, Dejaegere A, Kamoun A, de Reyniès A, Neuzillet Y, Rebouissou S, Béraud C, Lang H, Massfelder T, Allory Y, Cianférani S, Stote RH, Radvanyi F, Bernard-Pierrot I

Nat Commun. 2019 Jan 16;10(1):253

The tumor suppressor FBW7 and the vitamin D receptor are mutual cofactors in protein turnover and transcriptional regulation.

Salehi-Tabar R, Memari B, Wong H, Dimitrov V, Rochel N, White JH

Mol. Cancer Res.. 2019 Jan 3;:

Modulation of RXR-DNA complex assembly by DNA context.

Osz J, McEwen AG, Wolf J, Poussin-Courmontagne P, Peluso-Iltis C, Chebaro Y, Kieffer B, Rochel N

Mol. Cell. Endocrinol.. 2018 Nov 23;:

Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.

Gogoi P, Seoane S, Sigüeiro R, Guiberteau T, Maestro MA, Pérez-Fernández R, Rochel N, Mouriño A

J. Med. Chem.. 2018 Jun 14;61(11):4928-4937

Investigation of 20S-hydroxyvitamin D analogs and their 1α-OH derivatives as potent vitamin D receptor agonists with anti-inflammatory activities.

Lin Z, Marepally SR, Goh ESY, Cheng CYS, Janjetovic Z, Kim TK, Miller DD, Postlethwaite AE, Slominski AT, Tuckey RC, Peluso-Iltis C, Rochel N, Li W

Sci Rep. 2018 01 24;8(1):1478

Structural analysis and biological activities of BXL0124, a gemini analog of vitamin D.

Belorusova AY, Suh N, Lee HJ, So JY, Maehr H, Rochel N

J. Steroid Biochem. Mol. Biol.. 2017 10;173:69-74

Structural aspects of Vitamin D endocrinology.

Rochel N, Molnár F

Mol. Cell. Endocrinol.. 2017 09 15;453:22-35

1α,20S-Dihydroxyvitamin D Interacts with Vitamin D Receptor: Crystal Structure and Route of Chemical Synthesis.

Lin Z, Chen H, Belorusova AY, Bollinger JC, Tang EKY, Janjetovic Z, Kim TK, Wu Z, Miller DD, Slominski AT, Postlethwaite AE, Tuckey RC, Rochel N, Li W

Sci Rep. 2017 Aug 31;7(1):10193

Structure-activity relationship study of vitamin D analogs with oxolane group in their side chain.

Belorusova AY, Martínez A, Gándara Z, Gómez G, Fall Y, Rochel N

Eur J Med Chem. 2017 Jul 7;134:86-96

Allosteric Regulation in the Ligand Binding Domain of Retinoic Acid Receptorγ.

Chebaro Y, Sirigu S, Amal I, Lutzing R, Stote RH, Rochette-Egly C, Rochel N, Dejaegere A

PLoS ONE. 2017 ;12(1):e0171043

The molecular mechanisms underlying the ERα-36-mediated signaling in breast cancer.

Omarjee S, Jacquemetton J, Poulard C, Rochel N, Dejaegere A, Chebaro Y, Treilleux I, Marangoni E, Corbo L, Le Romancer M

Oncogene. 2016 12;:

Monitoring of the retinoic acid receptor-retinoid X receptor dimerization upon DNA binding by native mass spectrometry.

Nguyen-Huynh NT, Osz J, Peluso-Iltis C, Rochel N, Potier N, Leize-Wagner E

Biophys. Chem.. 2016 Mar;210:2-8

Solution Behavior of the Intrinsically Disordered N-Terminal Domain of Retinoid X Receptor α in the Context of the Full-Length Protein.

Belorusova AY, Osz J, Petoukhov MV, Peluso-Iltis C, Kieffer B, Svergun DI, Rochel N

Biochemistry. 2016 Mar;55(12):1741-8

Carborane-based design of a potent vitamin D receptor agonist.

Otero R, Seoane S, Sigüeiro R, Belorusova AY, Maestro MA, Pérez-Fernández R, Rochel N, Mouriño A

Chem Sci. 2016 Feb 1;7(2):1033-1037

Structural Studies of Vitamin D Nuclear Receptor Ligand-Binding Properties.

Belorusova AY, Rochel N

Vitam. Horm.. 2016 ;100:83-116

9-cis-13,14-Dihydroretinoic Acid Is an Endogenous Retinoid Acting as RXR Ligand in Mice.

Ruhl R, Krzyzosiak A, Niewiadomska-Cimicka A, Rochel N, Szeles L, Vaz B, Wietrzych-Schindler M, Alvarez S, Szklenar M, Nagy L, de Lera AR, Krezel W

PLoS Genet. 2015 Jun 1;11(6):e1005213

Structure-function relationships in nuclear receptors: the facts.

Moras D, Billas IM, Rochel N, Klaholz BP

Trends Biochem Sci. 2015 Jun;40(6):287-90

A Vitamin D Receptor Selectively Activated by Gemini Analogs Reveals Ligand Dependent and Independent Effects.

Huet T, Laverny G, Ciesielski F, Molnar F, Ramamoorthy TG, Belorusova AY, Antony P, Potier N, Metzger D, Moras D, Rochel N

Cell Rep. 2015 Jan 21. pii: S2211-1247(14)01098-5

Structural basis of natural promoter recognition by the retinoid X nuclear receptor.

Osz J, McEwen AG, Poussin-Courmontagne P, Moutier E, Birck C, Davidson I, Moras D, Rochel N

Sci Rep. 2015 Feb 3;5:8216

Restricted diversity of antigen binding residues of antibodies revealed by computational alanine scanning of 227 antibody-antigen complexes.

Robin G, Sato Y, Desplancq D, Rochel N, Weiss E, Martineau P

J Mol Biol. 2014 Nov 11;426(22):3729-43

Structural insights into the molecular mechanism of vitamin D receptor activation by lithocholic acid involving a new mode of ligand recognition.

Belorusova AY, Eberhardt J, Potier N, Stote RH, Dejaegere A, Rochel N

J Med Chem. 2014 Jun 12;57(11):4710-9

Architecture of DNA Bound RAR heterodimers.

Rochel N, Moras D

Subcell Biochem. 2014;70:21-36

Modulators of vitamin D nuclear receptor: recent advances from structural studies.

Belorusova AY, Rochel N

Curr Top Med Chem. 2014;14(21):2368-77.

Diastereotopic and deuterium effects in gemini.

Maehr H, Rochel N, Lee HJ, Suh N, Uskokovic MR

J Med Chem. 2013 May 23;56(10):3878-88

Phosphorylation of the retinoic acid receptor alpha induces a mechanical allosteric regulation and changes in internal dynamics.

Chebaro Y, Amal I, Rochel N, Rochette-Egly C, Stote RH, Dejaegere A

PLoS Comput Biol. 2013 Apr;9(4):e1003012

Purification of the human RARgamma ligand-binding domain and crystallization of its complex with all-trans retinoic acid.

Rochel N, Renaud JP, Ruff M, Vivat V, Granger F, Bonnier D, Lerouge T, Chambon P, Gronemeyer H, Moras D

Biochem. Biophys. Res. Commun.. 1997 Jan;230(2):293-6

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