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Items: 31

1.

Identification of a novel quinoline-based DNA demethylating compound highly potent in cancer cells.

Zwergel C, Schnekenburger M, Sarno F, Battistelli C, Manara MC, Stazi G, Mazzone R, Fioravanti R, Gros C, Ausseil F, Florean C, Nebbioso A, Strippoli R, Ushijima T, Scotlandi K, Tripodi M, Arimondo PB, Altucci L, Diederich M, Mai A, Valente S.

Clin Epigenetics. 2019 May 6;11(1):68. doi: 10.1186/s13148-019-0663-8.

2.

The emerging role of epigenetics in human autoimmune disorders.

Mazzone R, Zwergel C, Artico M, Taurone S, Ralli M, Greco A, Mai A.

Clin Epigenetics. 2019 Feb 26;11(1):34. doi: 10.1186/s13148-019-0632-2. Review.

3.

Acute and chronic neurobehavioral effects of the designer drug and bath salt constituent 3,4-methylenedioxypyrovalerone in the rat.

Atehortua-Martinez LA, Masniere C, Campolongo P, Chasseigneaux S, Callebert J, Zwergel C, Mai A, Laplanche JL, Chen H, Etheve-Quelquejeu M, Mégarbane B, Benturquia N.

J Psychopharmacol. 2019 Mar;33(3):392-405. doi: 10.1177/0269881118822151. Epub 2019 Jan 15.

PMID:
30644332
4.

Development of alkyl glycerone phosphate synthase inhibitors: Structure-activity relationship and effects on ether lipids and epithelial-mesenchymal transition in cancer cells.

Stazi G, Battistelli C, Piano V, Mazzone R, Marrocco B, Marchese S, Louie SM, Zwergel C, Antonini L, Patsilinakos A, Ragno R, Viviano M, Sbardella G, Ciogli A, Fabrizi G, Cirilli R, Strippoli R, Marchetti A, Tripodi M, Nomura DK, Mattevi A, Mai A, Valente S.

Eur J Med Chem. 2019 Feb 1;163:722-735. doi: 10.1016/j.ejmech.2018.11.050. Epub 2018 Nov 28.

PMID:
30576903
5.

Application of Small Epigenetic Modulators in Pediatric Medulloblastoma.

Zwergel C, Romanelli A, Stazi G, Besharat ZM, Catanzaro G, Tafani M, Valente S, Mai A.

Front Pediatr. 2018 Dec 3;6:370. doi: 10.3389/fped.2018.00370. eCollection 2018. Review.

6.

Six Years (2012-2018) of Researches on Catalytic EZH2 Inhibitors: The Boom of the 2-Pyridone Compounds.

Fioravanti R, Stazi G, Zwergel C, Valente S, Mai A.

Chem Rec. 2018 Dec;18(12):1818-1832. doi: 10.1002/tcr.201800091. Epub 2018 Oct 19. Review.

PMID:
30338896
7.

Nucleocytoplasmic export of HDAC5 and SIRT2 downregulation: two epigenetic mechanisms by which antidepressants enhance synaptic plasticity markers.

Muñoz-Cobo I, Erburu MM, Zwergel C, Cirilli R, Mai A, Valente S, Puerta E, Tordera RM.

Psychopharmacology (Berl). 2018 Oct;235(10):2831-2846. doi: 10.1007/s00213-018-4975-8. Epub 2018 Aug 8.

PMID:
30091005
8.

Correction to 'Pyrazole-based inhibitors of enhancer of zeste homologue 2 induce apoptosis and autophagy in cancer cells'.

Mellini P, Marrocco B, Borovika D, Polletta L, Carnevale I, Saladini S, Stazi G, Zwergel C, Trapencieris P, Ferretti E, Tafani M, Valente S, Mai A.

Philos Trans R Soc Lond B Biol Sci. 2018 Sep 19;373(1755). pii: 20180305. doi: 10.1098/rstb.2018.0305. No abstract available.

9.

A Quinoline-Based DNA Methyltransferase Inhibitor as a Possible Adjuvant in Osteosarcoma Therapy.

Manara MC, Valente S, Cristalli C, Nicoletti G, Landuzzi L, Zwergel C, Mazzone R, Stazi G, Arimondo PB, Pasello M, Guerzoni C, Picci P, Nanni P, Lollini PL, Mai A, Scotlandi K.

Mol Cancer Ther. 2018 Sep;17(9):1881-1892. doi: 10.1158/1535-7163.MCT-17-0818. Epub 2018 Jun 29.

10.

HDAC1 inhibition by MS-275 in mesothelial cells limits cellular invasion and promotes MMT reversal.

Rossi L, Battistelli C, de Turris V, Noce V, Zwergel C, Valente S, Moioli A, Manzione A, Palladino M, Bordoni V, Domenici A, Menè P, Mai A, Tripodi M, Strippoli R.

Sci Rep. 2018 May 31;8(1):8492. doi: 10.1038/s41598-018-26319-2.

11.

Trends of LSD1 inhibitors in viral infections.

Zwergel C, Stazi G, Mai A, Valente S.

Future Med Chem. 2018 May 1;10(10):1133-1136. doi: 10.4155/fmc-2018-0065. Epub 2018 May 22. No abstract available.

12.

Pyrazole-based inhibitors of enhancer of zeste homologue 2 induce apoptosis and autophagy in cancer cells.

Mellini P, Marrocco B, Borovika D, Polletta L, Carnevale I, Saladini S, Stazi G, Zwergel C, Trapencieris P, Ferretti E, Tafani M, Valente S, Mai A.

Philos Trans R Soc Lond B Biol Sci. 2018 Jun 5;373(1748). pii: 20170150. doi: 10.1098/rstb.2017.0150. Erratum in: Philos Trans R Soc Lond B Biol Sci. 2018 Sep 19;373(1755):.

13.

Effects of Class II-Selective Histone Deacetylase Inhibitor on Neuromuscular Function and Disease Progression in SOD1-ALS Mice.

Buonvicino D, Felici R, Ranieri G, Caramelli R, Lapucci A, Cavone L, Muzzi M, Di Pietro L, Bernardini C, Zwergel C, Valente S, Mai A, Chiarugi A.

Neuroscience. 2018 May 21;379:228-238. doi: 10.1016/j.neuroscience.2018.03.022. Epub 2018 Mar 26.

PMID:
29588251
14.

Anti-inflammatory Effects of Heme Oxygenase-1 Depend on Adenosine A2A- and A2B-Receptor Signaling in Acute Pulmonary Inflammation.

Konrad FM, Zwergel C, Ngamsri KC, Reutershan J.

Front Immunol. 2017 Dec 20;8:1874. doi: 10.3389/fimmu.2017.01874. eCollection 2017.

15.

The histone methyltransferase EZH2 as a druggable target in SHH medulloblastoma cancer stem cells.

Miele E, Valente S, Alfano V, Silvano M, Mellini P, Borovika D, Marrocco B, Po A, Besharat ZM, Catanzaro G, Battaglia G, Abballe L, Zwergel C, Stazi G, Milite C, Castellano S, Tafani M, Trapencieris P, Mai A, Ferretti E.

Oncotarget. 2017 Aug 2;8(40):68557-68570. doi: 10.18632/oncotarget.19782. eCollection 2017 Sep 15.

16.

Effect of Class II HDAC inhibition on glutamate transporter expression and survival in SOD1-ALS mice.

Lapucci A, Cavone L, Buonvicino D, Felici R, Gerace E, Zwergel C, Valente S, Mai A, Chiarugi A.

Neurosci Lett. 2017 Aug 24;656:120-125. doi: 10.1016/j.neulet.2017.07.033. Epub 2017 Jul 19.

PMID:
28732762
17.

Epi-drugs in combination with immunotherapy: a new avenue to improve anticancer efficacy.

Mazzone R, Zwergel C, Mai A, Valente S.

Clin Epigenetics. 2017 May 30;9:59. doi: 10.1186/s13148-017-0358-y. eCollection 2017. Review.

18.

Novel coumarin- and quinolinone-based polycycles as cell division cycle 25-A and -C phosphatases inhibitors induce proliferation arrest and apoptosis in cancer cells.

Zwergel C, Czepukojc B, Evain-Bana E, Xu Z, Stazi G, Mori M, Patsilinakos A, Mai A, Botta B, Ragno R, Bagrel D, Kirsch G, Meiser P, Jacob C, Montenarh M, Valente S.

Eur J Med Chem. 2017 Jul 7;134:316-333. doi: 10.1016/j.ejmech.2017.04.012. Epub 2017 Apr 10.

PMID:
28431339
19.

EZH2 inhibitors: a patent review (2014-2016).

Stazi G, Zwergel C, Mai A, Valente S.

Expert Opin Ther Pat. 2017 Jul;27(7):797-813. doi: 10.1080/13543776.2017.1316976. Epub 2017 Apr 20. Review.

PMID:
28394193
20.

Metabolite profiling of ascidian Styela plicata using LC-MS with multivariate statistical analysis and their antitumor activity.

Palanisamy SK, Trisciuoglio D, Zwergel C, Del Bufalo D, Mai A.

J Enzyme Inhib Med Chem. 2017 Dec;32(1):614-623. doi: 10.1080/14756366.2016.1266344.

21.

Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity.

Ourailidou ME, Lenoci A, Zwergel C, Rotili D, Mai A, Dekker FJ.

Bioorg Med Chem. 2017 Feb 1;25(3):847-856. doi: 10.1016/j.bmc.2016.11.043. Epub 2016 Dec 1.

22.

MC1568 inhibits HDAC6/8 activity and influenza A virus replication in lung epithelial cells: role of Hsp90 acetylation.

Panella S, Marcocci ME, Celestino I, Valente S, Zwergel C, Li Puma DD, Nencioni L, Mai A, Palamara AT, Simonetti G.

Future Med Chem. 2016 Nov;8(17):2017-2031. doi: 10.4155/fmc-2016-0073. Epub 2016 Oct 14.

PMID:
27739328
23.

LSD1 inhibitors: a patent review (2010-2015).

Stazi G, Zwergel C, Valente S, Mai A.

Expert Opin Ther Pat. 2016 May;26(5):565-80. doi: 10.1517/13543776.2016.1165209. Epub 2016 Mar 28. Review.

PMID:
27019002
24.

Histone deacetylase inhibitors restore IL-10 expression in lipopolysaccharide-induced cell inflammation and reduce IL-1β and IL-6 production in breast silicone implant in C57BL/6J wild-type murine model.

Di Liddo R, Valente S, Taurone S, Zwergel C, Marrocco B, Turchetta R, Conconi MT, Scarpa C, Bertalot T, Schrenk S, Mai A, Artico M.

Autoimmunity. 2016 Jan 20:1-11. doi: 10.3109/08916934.2015.1134510. [Epub ahead of print]

PMID:
26789595
25.

1,4-Dihydropyridines Active on the SIRT1/AMPK Pathway Ameliorate Skin Repair and Mitochondrial Function and Exhibit Inhibition of Proliferation in Cancer Cells.

Valente S, Mellini P, Spallotta F, Carafa V, Nebbioso A, Polletta L, Carnevale I, Saladini S, Trisciuoglio D, Gabellini C, Tardugno M, Zwergel C, Cencioni C, Atlante S, Moniot S, Steegborn C, Budriesi R, Tafani M, Del Bufalo D, Altucci L, Gaetano C, Mai A.

J Med Chem. 2016 Feb 25;59(4):1471-91. doi: 10.1021/acs.jmedchem.5b01117. Epub 2016 Jan 5.

PMID:
26689352
26.

DNA Methyltransferases Inhibitors from Natural Sources.

Zwergel C, Valente S, Mai A.

Curr Top Med Chem. 2016;16(7):680-96. Review.

PMID:
26303417
27.

Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells.

Di Pompo G, Salerno M, Rotili D, Valente S, Zwergel C, Avnet S, Lattanzi G, Baldini N, Mai A.

J Med Chem. 2015 May 14;58(9):4073-9. doi: 10.1021/acs.jmedchem.5b00126. Epub 2015 Apr 30.

PMID:
25905694
28.

Emerging approaches for histone deacetylase inhibitor drug discovery.

Zwergel C, Valente S, Jacob C, Mai A.

Expert Opin Drug Discov. 2015 Jun;10(6):599-613. doi: 10.1517/17460441.2015.1038236. Epub 2015 Apr 20. Review.

PMID:
25895649
29.

Novel inhibitors of human histone deacetylases: design, synthesis and bioactivity of 3-alkenoylcoumarines.

Seidel C, Schnekenburger M, Zwergel C, Gaascht F, Mai A, Dicato M, Kirsch G, Valente S, Diederich M.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3797-801. doi: 10.1016/j.bmcl.2014.06.067. Epub 2014 Jun 28.

PMID:
25042254
30.

Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.

Valente S, Liu Y, Schnekenburger M, Zwergel C, Cosconati S, Gros C, Tardugno M, Labella D, Florean C, Minden S, Hashimoto H, Chang Y, Zhang X, Kirsch G, Novellino E, Arimondo PB, Miele E, Ferretti E, Gulino A, Diederich M, Cheng X, Mai A.

J Med Chem. 2014 Feb 13;57(3):701-13. doi: 10.1021/jm4012627. Epub 2014 Jan 15.

31.

Aurones: interesting natural and synthetic compounds with emerging biological potential.

Zwergel C, Gaascht F, Valente S, Diederich M, Bagrel D, Kirsch G.

Nat Prod Commun. 2012 Mar;7(3):389-94. Review.

PMID:
22545415

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