Vitoria Gomes M, Landwerlin P, Diebold-Durand ML, Shaik TB, Durand A, Troesch E, Weber C, Brillet K, Lemée MV, Decroos C, Dulac L, Antony P, Watrin E, Ennifar E, Golzio C, Romier C

Cell Rep. 2024 09 5;43(9):114656

Structure-Activity Studies of 1,2,4-Oxadiazoles for the Inhibition of the NAD-Dependent Lysine Deacylase Sirtuin 2.

Colcerasa A, Friedrich F, Melesina J, Moser P, Vogelmann A, Tzortzoglou P, Neuwirt E, Sum M, Robaa D, Zhang L, Ramos-Morales E, Romier C, Einsle O, Metzger E, Schüle R, Groß O, Sippl W, Jung M

J Med Chem. 2024 06 7;:

Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation.

Sinatra L, Vogelmann A, Friedrich F, Tararina MA, Neuwirt E, Colcerasa A, König P, Toy L, Yesiloglu TZ, Hilscher S, Gaitzsch L, Papenkordt N, Zhai S, Zhang L, Romier C, Einsle O, Sippl W, Schutkowski M, Gross O, Bendas G, Christianson DW, Hansen FK, Jung M, Schiedel M

J Med Chem. 2023 10 30;:

In cellulo and in vivo assays for compound testing against Trypanosoma cruzi.

Guerra-Slompo EP, Picchi-Constante GFA, Marek M, Romier C, Sippl W, Zanchin NIT

STAR Protoc. 2023 01 24;4(1):102058

Synthesis, Biochemical, and Cellular Evaluation of HDAC6 Targeting Proteolysis Targeting Chimeras.

Darwish S, Heimburg T, Ridinger J, Herp D, Schmidt M, Romier C, Jung M, Oehme I, Sippl W

Methods Mol Biol. 2023 ;2589:179-193

Development of Alkylated Hydrazides as Highly Potent and Selective Class I Histone Deacetylase Inhibitors with T cell Modulatory Properties.

Sun P, Wang J, Khan KS, Yang W, Ng BW, Ilment N, Zessin M, Bülbül EF, Robaa D, Erdmann F, Schmidt M, Romier C, Schutkowski M, Cheng AS, Sippl W

J Med Chem. 2022 11 30;:

Chemically Diverse S. mansoni HDAC8 Inhibitors Reduced Viability in Worm Larval and Adult Stages.

Noce B, Di Bello E, Zwergel C, Fioravanti R, Valente S, Rotili D, Masotti A, Ansari MSZ, Trisciuoglio D, Chakrabarti A, Romier C, Robaa D, Sippl W, Jung M, Häberli C, Keiser J, Mai A

ChemMedChem. 2022 10 17;:

Phenotypic Screening of Histone Deacetylase (HDAC) Inhibitors against Schistosoma mansoni.

Hassan MM, Sedighi A, Olaoye OO, Häberli C, Merz A, Ramos-Morales E, de Araujo ED, Romier C, Jung M, Keiser J, Gunning PT

ChemMedChem. 2022 08 19;:e202100622

Design, Synthesis and Biological Characterization of Histone Deacetylase 8 (HDAC8) Proteolysis Targeting Chimeras (PROTACs) with Anti-Neuroblastoma Activity.

Darwish S, Ghazy E, Heimburg T, Herp D, Zeyen P, Salem-Altintas R, Ridinger J, Robaa D, Schmidtkunz K, Erdmann F, Schmidt M, Romier C, Jung M, Oehme I, Sippl W

Int J Mol Sci. 2022 07 7;23(14):

Efficient CRISPR-Cas9-mediated genome editing for characterization of essential genes in .

Picchi-Constante GFA, Hiraiwa PM, Marek M, Rogerio VZ, Guerra-Slompo EP, Romier C, Zanchin NIT

STAR Protoc. 2022 Jun 17;3(2):101324

Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells.

Zeyen P, Zeyn Y, Herp D, Mahmoudi F, Yesiloglu TZ, Erdmann F, Schmidt M, Robaa D, Romier C, Ridinger J, Herbst-Gervasoni CJ, Christianson DW, Oehme I, Jung M, Krämer OH, Sippl W

Eur J Med Chem. 2022 Mar 11;234:114272

Synthesis, Molecular Docking and Biological Characterization of Pyrazine Linked 2-Aminobenzamides as New Class I Selective Histone Deacetylase (HDAC) Inhibitors with Anti-Leukemic Activity.

Ibrahim HS, Abdelsalam M, Zeyn Y, Zessin M, Mustafa AM, Fischer MA, Zeyen P, Sun P, Bülbül EF, Vecchio A, Erdmann F, Schmidt M, Robaa D, Barinka C, Romier C, Schutkowski M, Krämer OH, Sippl W

Int J Mol Sci. 2021 Dec 29;23(1):

Species-selective targeting of pathogens revealed by the atypical structure and active site of Trypanosoma cruzi histone deacetylase DAC2.

Marek M, Ramos-Morales E, Picchi-Constante GFA, Bayer T, Norström C, Herp D, Sales-Junior PA, Guerra-Slompo EP, Hausmann K, Chakrabarti A, Shaik TB, Merz A, Troesch E, Schmidtkunz K, Goldenberg S, Pierce RJ, Mourão MM, Jung M, Schultz J, Sippl W, Zanchin NIT, Romier C

Cell Rep. 2021 Dec 21;37(12):110129

Synthesis, structure-activity relationships, cocrystallization and cellular characterization of novel smHDAC8 inhibitors for the treatment of schistosomiasis.

Ghazy E, Heimburg T, Lancelot J, Zeyen P, Schmidtkunz K, Truhn A, Darwish S, Simoben CV, Shaik TB, Erdmann F, Schmidt M, Robaa D, Romier C, Jung M, Pierce R, Sippl W

Eur J Med Chem. 2021 Aug 8;225:113745

The structure of the mouse ADAT2/ADAT3 complex reveals the molecular basis for mammalian tRNA wobble adenosine-to-inosine deamination.

Ramos-Morales E, Bayam E, Del-Pozo-Rodríguez J, Salinas-Giegé T, Marek M, Tilly P, Wolff P, Troesch E, Ennifar E, Drouard L, Godin JD, Romier C

Nucleic Acids Res. 2021 May 31;:

Binding Free Energy (BFE) Calculations and Quantitative Structure-Activity Relationship (QSAR) Analysis of Histone Deacetylase 8 (HDAC8) Inhibitors.

Simoben CV, Ghazy E, Zeyen P, Darwish S, Schmidt M, Romier C, Robaa D, Sippl W

Molecules. 2021 Apr 28;26(9):

Citrullination of pyruvate kinase M2 by PADI1 and PADI3 regulates glycolysis and cancer cell proliferation.

Coassolo S, Davidson G, Negroni L, Gambi G, Daujat S, Romier C, Davidson I

Nat Commun. 2021 Mar 19;12(1):1718

Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.

Ghazy E, Zeyen P, Herp D, Hügle M, Schmidtkunz K, Erdmann F, Robaa D, Schmidt M, Morales ER, Romier C, Günther S, Jung M, Sippl W

Eur J Med Chem. 2020 May 18;200:112338

La Société de Biologie de Strasbourg : 100 ans au service de la science et de la société

Antony P, Fournel S, Zoll J, Mantz JM, Befort K, Massotte D, Giégé P, Céraline J, Metzger D, Becker H, Drouard L, Florentz C, Martin R, Nébigil C, Potier S, Schaefer A, Schaeffer E, Schuster C, Bresson A, Quéméneur E, Choulier L, Matt N, Monassier L, Lugnier C, Freysz L, Hoffmann J, Dreyfus H, Romier C

Biol Aujourdhui. 2020 ;214(3-4):137-148

Structure-Based Design, Synthesis, and Biological Evaluation of Triazole-Based smHDAC8 Inhibitors.

Holl R, Kalinin DV, Jana SK, Pfafenrot M, Chakrabarti A, Melesina J, Shaik TB, Lancelot J, Pierce RJ, Sippl W, Romier C, Jung M

ChemMedChem. 2019 Dec 9;:

One-Atom-Substitution Enables Direct and Continuous Monitoring of Histone Deacylase Activity.

Zessin M, Kutil Z, Meleshin M, Novakova Z, Ghazy E, Kalbas D, Marek M, Romier C, Sippl W, Bařinka C, Schutkowski M

Biochemistry. 2019 Nov 4;:

Characterization of histone deacetylase 8 (HDAC8) selective inhibition reveals specific active site structural and functional determinants.

Marek M, Shaik TB, Heimburg T, Chakrabarti A, Lancelot J, Ramos Morales E, Da Veiga C, Kalinin DV, Melesina J, Robaa D, Schmidtkunz K, Suzuki T, Holl R, Ennifar E, Pierce R, Jung M, Sippl W, Romier C

J. Med. Chem.. 2018 Oct 22;:

Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.

Brindisi M, Senger J, Cavella C, Grillo A, Chemi G, Gemma S, Cucinella DM, Lamponi S, Sarno F, Iside C, Nebbioso A, Novellino E, Shaik TB, Romier C, Herp D, Jung M, Butini S, Campiani G, Altucci L, Brogi S

Eur J Med Chem. 2018 Jul 31;157:127-138

Isoform-selective HDAC1/6/8 inhibitors with an imidazo-ketopiperazine cap containing stereochemical diversity.

Lecointre B, Narozny R, Borrello MT, Senger J, Chakrabarti A, Jung M, Marek M, Romier C, Melesina J, Sippl W, Bischoff L, Ganesan A

Philos. Trans. R. Soc. Lond., B, Biol. Sci.. 2018 Jun 5;373(1748):

Synthesis, crystallization studies and in vitro characterization of novel cinnamic acid derivatives as SmHDAC8 inhibitors for the treatment of Schistosomiasis.

Bayer T, Chakrabarti A, Lancelot J, Shaik TB, Hausmann K, Melesina J, Schmidtkunz K, Marek M, Erdmann F, Schmidt M, Robaa D, Romier C, Pierce RJ, Jung M, Sippl W

ChemMedChem. 2018 May 27;:

A Novel Class of Schistosoma mansoni Histone Deacetylase 8 (HDAC8) Inhibitors Identified by Structure-Based Virtual Screening and In Vitro Testing.

Simoben CV, Robaa D, Chakrabarti A, Schmidtkunz K, Marek M, Lancelot J, Kannan S, Melesina J, Shaik TB, Pierce RJ, Romier C, Jung M, Sippl W

Molecules. 2018 Mar 2;23(3):

Structure-Based Design and Biological Characterization of Selective Histone Deacetylase 8 (HDAC8) Inhibitors with Anti-Neuroblastoma Activity.

Heimburg T, Kolbinger FR, Zeyen P, Ghazy E, Herp D, Schmidtkunz K, Melesina J, Shaik TB, Erdmann F, Schmidt M, Romier C, Robaa D, Witt O, Oehme I, Jung M, Sippl W

J. Med. Chem.. 2017 Dec 28;60(24):10188-10204

Alkoxyurea-based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.

Stenzel K, Hamacher A, Hansen FK, Gertzen CGW, Senger J, Marquardt V, Marek L, Marek M, Romier C, Remke M, Jung M, Gohlke H, Kassack MU, Kurz T

J. Med. Chem.. 2017 Jul 13;60(13):5334-5348

Design, multicomponent synthesis and anticancer activity of a focused histone deacetylase (HDAC) inhibitor library with peptoid-based cap groups.

Krieger V, Hamacher A, Gertzen CGW, Senger J, Zwinderman MRH, Marek M, Romier C, Dekker FJ, Kurz T, Jung M, Gohlke H, Kassack MU, Hansen FK

J. Med. Chem.. 2017 Jul 13;60(13):5493-5506

Isophthalic Acid-Based HDAC Inhibitors as Potent Inhibitors of HDAC8 from Schistosoma mansoni.

Stenzel K, Chakrabarti A, Melesina J, Hansen FK, Lancelot J, Herkenhöhner S, Lungerich B, Marek M, Romier C, Pierce RJ, Sippl W, Jung M, Kurz T

Arch. Pharm. (Weinheim). 2017 Jun;:

Histone deacetylase inhibition modulates histone acetylation at gene promoter regions and affects genome-wide gene transcription in Schistosoma mansoni.

Anderson L, Gomes MR, daSilva LF, Pereira ADSA, Mourão MM, Romier C, Pierce R, Verjovski-Almeida S

PLoS Negl Trop Dis. 2017 Apr;11(4):e0005539

[History of the Strasbourg Society of Biology].

Antony P, Romier C, Mantz JM

Biol Aujourdhui. 2017 ;211(1):117-125

Molecular basis and specificity of H2A.Z-H2B recognition and deposition by the histone chaperone YL1.

Latrick CM, Marek M, Ouararhni K, Papin C, Stoll I, Ignatyeva M, Obri A, Ennifar E, Dimitrov S, Romier C, Hamiche A

Nat. Struct. Mol. Biol.. 2016 Apr;23(4):309-16

Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis.

Heimburg T, Chakrabarti A, Lancelot J, Marek M, Melesina J, Hauser AT, Shaik TB, Duclaud S, Robaa D, Erdmann F, Schmidt M, Romier C, Pierce RJ, Jung M, Sippl W

J. Med. Chem.. 2016 Mar;59(6):2423-35

Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.

Senger J, Melesina J, Marek M, Romier C, Oehme I, Witt O, Sippl W, Jung M

J. Med. Chem.. 2016 Feb;59(4):1545-55

Marek M, Shaik TB, Jung M, Sippl W, Pierce RJ, Romier C

Biol Aujourdhui. 2016 ;210(4):311-320

Complex Reconstitution and Characterization by Combining Co-expression Techniques in Escherichia coli with High-Throughput.

Vincentelli R, Romier C

Adv. Exp. Med. Biol.. 2016 ;896:43-58

Large-Scale Overproduction and Purification of Recombinant Histone Deacetylase 8 (HDAC8) from the Human-Pathogenic Flatworm Schistosoma mansoni.

Marek M, Shaik TB, Duclaud S, Pierce RJ, Romier C

Methods Mol. Biol.. 2016 ;1436:109-18

Homology modeling of parasite histone deacetylases to guide the structure-based design of selective inhibitors.

Melesina J, Robaa D, Pierce RJ, Romier C, Sippl W

J. Mol. Graph. Model.. 2015 Nov;62:342-61

HDAC8: a multifaceted target for therapeutic interventions.

Chakrabarti A, Oehme I, Witt O, Oliveira G, Sippl W, Romier C, Pierce RJ, Jung M

Trends Pharmacol Sci. 2015 May 23. pii: S0165-6147(15)00089-9

Drugging the schistosome zinc-dependent HDACs: current progress and future perspectives.

Marek M, Oliveira G, Pierce RJ, Jung M, Sippl W, Romier C

Future Med Chem. 2015 Apr;7(6):783-800

Characterization and production of protein complexes by co-expression in Escherichia coli.

Haffke M, Marek M, Pelosse M, Diebold ML, Schlattner U, Berger I, Romier C

Methods Mol Biol. 2015;1261:63-89

Fluorescence-based screening assays for the NAD(+)-dependent histone deacetylase smSirt2 from Schistosoma mansoni.

Schiedel M, Marek M, Lancelot J, Karaman B, Almlof I, Schultz J, Sippl W, Pierce RJ, Romier C, Jung M

J Biomol Screen. 2015 Jan;20(1):112-21

Schistosome sirtuins as drug targets.

Lancelot J, Cabezas-Cruz A, Caby S, Marek M, Schultz J, Romier C, Sippl W, Jung M, Pierce RJ

Future Med Chem. 2015 ;7(6):765-82

Hydroxamates of para-aminobenzoic acid as selective inhibitors of HDAC8.

Kulandaivelu U, Chilakamari LM, Jadav SS, Rao TR, Jayaveera KN, Shireesha B, Hauser AT, Senger J, Marek M, Romier C, Jung M, Jayaprakash V

Bioorg Chem. 2014 Dec;57:116-20

Discovery of inhibitors of Schistosoma mansoni HDAC8 by combining homology modeling, virtual screening, and in vitro validation.

Kannan S, Melesina J, Hauser AT, Chakrabarti A, Heimburg T, Schmidtkunz K, Walter A, Marek M, Pierce RJ, Romier C, Jung M, Sippl W

J Chem Inf Model. 2014 Oct 27;54(10):3005-19

Molecular basis for the antiparasitic activity of a mercaptoacetamide derivative that inhibits histone deacetylase 8 (HDAC8) from the human pathogen schistosoma mansoni.

Stolfa DA, Marek M, Lancelot J, Hauser AT, Walter A, Leproult E, Melesina J, Rumpf T, Wurtz JM, Cavarelli J, Sippl W, Pierce RJ, Romier C, Jung M

J Mol Biol. 2014 Oct 9;426(20):3442-53

DNA binding by Sgf11 protein affects histone H2B deubiquitination by Spt-Ada-Gcn5-acetyltransferase (SAGA).

Koehler C, Bonnet J, Stierle M, Romier C, Devys D, Kieffer B

J Biol Chem. 2014 Mar 28;289(13):8989-99

Characterization of the interaction between protein Snu13p/15.5K and the Rsa1p/NUFIP factor and demonstration of its functional importance for snoRNP assembly.

Rothe B, Back R, Quinternet M, Bizarro J, Robert MC, Blaud M, Romier C, Manival X, Charpentier B, Bertrand E, Branlant C

Nucleic Acids Res. 2014 Feb;42(3):2015-36

ANP32E is a histone chaperone that removes H2A.Z from chromatin.

Obri A, Ouararhni K, Papin C, Diebold ML, Padmanabhan K, Marek M, Stoll I, Roy L, Reilly PT, Mak TW, Dimitrov S, Romier C, Hamiche A

Nature. 2014 Jan 30;505(7485):648-53

TAF4, a subunit of transcription factor II D, directs promoter occupancy of nuclear receptor HNF4A during post-natal hepatocyte differentiation.

Alpern D, Langer D, Ballester B, Le Gras S, Romier C, Mengus G, Davidson I

Elife. 2014 Sep 10;3:e03613

Baculovirus VP1054 is an acquired cellular PURalpha, a nucleic acid-binding protein specific for GGN repeats.

Marek M, Romier C, Galibert L, Merten OW, van Oers MM

J Virol. 2013 Aug;87(15):8465-80

Expression in Escherichia coli: becoming faster and more complex.

Vincentelli R, Romier C

Curr Opin Struct Biol. 2013 Jun;23(3):326-34

Sequence-specific transcription factor NF-Y displays histone-like DNA binding and H2B-like ubiquitination.

Nardini M, Gnesutta N, Donati G, Gatta R, Forni C, Fossati A, Vonrhein C, Moras D, Romier C, Bolognesi M, Mantovani R

Cell. 2013 Jan 17;152(1-2):132-43

TFIID TAF6-TAF9 complex formation involves the HEAT repeat-containing C-terminal domain of TAF6 and is modulated by TAF5 protein.

Scheer E, Delbac F, Tora L, Moras D, Romier C

J Biol Chem. 2012 Aug 10;287(33):27580-92

Sequence and structure requirements for specific recognition of HIV-1 TAR and DIS RNA by the HIV-1 Vif protein.

Freisz S, Mezher J, Hafirassou L, Wolff P, Nomine Y, Romier C, Dumas P, Ennifar E

RNA Biol. 2012 Jul;9(7):966-77

Strategies for bacterial expression of protein-peptide complexes: application to solubilization of papillomavirus E6.

Sidi AO, Babah KO, Brimer N, Nomine Y, Romier C, Kieffer B, Pol SV, Trave G, Zanier K

Protein Expr Purif. 2011 Nov;80(1):8-16

Deciphering correct strategies for multiprotein complex assembly by co-expression: application to complexes as large as the histone octamer.

Diebold ML, Fribourg S, Koch M, Metzger T, Romier C

J Struct Biol. 2011 Aug;175(2):178-88

Robots, pipelines, polyproteins: enabling multiprotein expression in prokaryotic and eukaryotic cells.

Vijayachandran LS, Viola C, Garzoni F, Trowitzsch S, Bieniossek C, Chaillet M, Schaffitzel C, Busso D, Romier C, Poterszman A, Richmond TJ, Berger I

J Struct Biol. 2011 Aug;175(2):198-208

Noncanonical tandem SH2 enables interaction of elongation factor Spt6 with RNA polymerase II.

Diebold ML, Loeliger E, Koch M, Winston F, Cavarelli J, Romier C

J Biol Chem. 2010 Dec 3;285(49):38389-98

The structure of an Iws1/Spt6 complex reveals an interaction domain conserved in TFIIS, Elongin A and Med26.

Diebold ML, Koch M, Loeliger E, Cura V, Winston F, Cavarelli J, Romier C

EMBO J. 2010 Dec 1;29(23):3979-91

The structural plasticity of SCA7 domains defines their differential nucleosome-binding properties.

Bonnet J, Wang YH, Spedale G, Atkinson RA, Romier C, Hamiche A, Pijnappel WW, Timmers HT, Tora L, Devys D, Kieffer B

EMBO Rep. 2010 Aug;11(8):612-8

Crystallization and preliminary crystallographic analysis of eukaryotic transcription and mRNA export factor Iws1 from Encephalitozoon cuniculi.

Koch M, Diebold ML, Cavarelli J, Romier C

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2010 Feb 1;66(Pt

Crystal structure, biochemical and genetic characterization of yeast and E. cuniculi TAF(II)5 N-terminal domain: implications for TFIID assembly.

Romier C, James N, Birck C, Cavarelli J, Vivares C, Collart MA, Moras D

J Mol Biol. 2007 May 18;368(5):1292-306

Co-expression of protein complexes in prokaryotic and eukaryotic hosts: experimental procedures, database tracking and case studies.

Romier C, Ben Jelloul M, Albeck S, Buchwald G, Busso D, Celie PH, Christodoulou E, De Marco V, van Gerwen S, Knipscheer P, Lebbink JH, Notenboom V, Poterszman A, Rochel N, Cohen SX, Unger T, Sussman JL, Moras D, Sixma TK, Perrakis A

Acta Crystallogr D Biol Crystallogr. 2006 Oct;62(Pt 10):1232-42

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