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Items: 46

1.

Non-covalent immunoproteasome inhibitors induce cell cycle arrest in multiple myeloma MM.1R cells.

Ettari R, Pallio G, Pizzino G, Irrera N, Zappalà M, Maiorana S, Di Chio C, Altavilla D, Squadrito F, Bitto A.

J Enzyme Inhib Med Chem. 2019 Dec;34(1):1307-1313. doi: 10.1080/14756366.2019.1594802.

PMID:
31307247
2.

Role of the microbiota in hematologic malignancies.

Allegra A, Innao V, Allegra AG, Ettari R, Pugliese M, Pulvirenti N, Musolino C.

Neth J Med. 2019 Feb;77(2):67-80.

3.

Development of Novel Amides as Noncovalent Inhibitors of Immunoproteasomes.

Ettari R, Cerchia C, Maiorana S, Guccione M, Novellino E, Bitto A, Grasso S, Lavecchia A, Zappalà M.

ChemMedChem. 2019 Apr 17;14(8):842-852. doi: 10.1002/cmdc.201900028. Epub 2019 Mar 26.

PMID:
30829448
4.

Evaluation of curcumin irreversibility.

Ettari R, Previti S, Maiorana S, Allegra A, Schirmeister T, Grasso S, Zappalà M.

Nat Prod Res. 2019 Jan 24:1-4. doi: 10.1080/14786419.2018.1557658. [Epub ahead of print] No abstract available.

PMID:
30676764
5.

Drug combination studies of curcumin and genistein against rhodesain of Trypanosoma brucei rhodesiense.

Ettari R, Previti S, Maiorana S, Allegra A, Schirmeister T, Grasso S, Zappalà M.

Nat Prod Res. 2018 Jun 13:1-5. doi: 10.1080/14786419.2018.1483927. [Epub ahead of print]

PMID:
29897253
6.

Identification of 2-thioxoimidazolidin-4-one derivatives as novel noncovalent proteasome and immunoproteasome inhibitors.

Maccari R, Ettari R, Adornato I, Naß A, Wolber G, Bitto A, Mannino F, Aliquò F, Bruno G, Nicolò F, Previti S, Grasso S, Zappalà M, Ottanà R.

Bioorg Med Chem Lett. 2018 Feb 1;28(3):278-283. doi: 10.1016/j.bmcl.2017.12.053. Epub 2017 Dec 26.

PMID:
29292224
7.

Immunoproteasome-selective and non-selective inhibitors: A promising approach for the treatment of multiple myeloma.

Ettari R, Zappalà M, Grasso S, Musolino C, Innao V, Allegra A.

Pharmacol Ther. 2018 Feb;182:176-192. doi: 10.1016/j.pharmthera.2017.09.001. Epub 2017 Sep 11. Review.

PMID:
28911826
8.

Development of Novel Peptide-Based Michael Acceptors Targeting Rhodesain and Falcipain-2 for the Treatment of Neglected Tropical Diseases (NTDs).

Previti S, Ettari R, Cosconati S, Amendola G, Chouchene K, Wagner A, Hellmich UA, Ulrich K, Krauth-Siegel RL, Wich PR, Schmid I, Schirmeister T, Gut J, Rosenthal PJ, Grasso S, Zappalà M.

J Med Chem. 2017 Aug 24;60(16):6911-6923. doi: 10.1021/acs.jmedchem.7b00405. Epub 2017 Aug 11.

PMID:
28763614
9.

Development of novel N-3-bromoisoxazolin-5-yl substituted 2,3-benzodiazepines as noncompetitive AMPAR antagonists.

Espahbodinia M, Ettari R, Wen W, Wu A, Shen YC, Niu L, Grasso S, Zappalà M.

Bioorg Med Chem. 2017 Jul 15;25(14):3631-3637. doi: 10.1016/j.bmc.2017.05.036. Epub 2017 May 19.

PMID:
28571973
10.

BAY 11-7082 inhibits the NF-κB and NLRP3 inflammasome pathways and protects against IMQ-induced psoriasis.

Irrera N, Vaccaro M, Bitto A, Pallio G, Pizzino G, Lentini M, Arcoraci V, Minutoli L, Scuruchi M, Cutroneo G, Anastasi GP, Ettari R, Squadrito F, Altavilla D.

Clin Sci (Lond). 2017 Mar 1;131(6):487-498. doi: 10.1042/CS20160645. Epub 2017 Jan 17.

PMID:
28096316
11.

Development of novel 1,4-benzodiazepine-based Michael acceptors as antitrypanosomal agents.

Ettari R, Previti S, Cosconati S, Maiorana S, Schirmeister T, Grasso S, Zappalà M.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3453-6. doi: 10.1016/j.bmcl.2016.06.047. Epub 2016 Jun 21.

PMID:
27372809
12.

G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.

Guccione M, Ettari R, Taliani S, Da Settimo F, Zappalà M, Grasso S.

J Med Chem. 2016 Oct 27;59(20):9277-9294. Epub 2016 Jul 8. Review.

PMID:
27362616
13.

Identification of noncovalent proteasome inhibitors with high selectivity for chymotrypsin-like activity by a multistep structure-based virtual screening.

Di Giovanni C, Ettari R, Sarno S, Rotondo A, Bitto A, Squadrito F, Altavilla D, Schirmeister T, Novellino E, Grasso S, Zappalà M, Lavecchia A.

Eur J Med Chem. 2016 Oct 4;121:578-591. doi: 10.1016/j.ejmech.2016.05.049. Epub 2016 May 27.

PMID:
27318981
14.

A novel 2,3-benzodiazepine-4-one derivative AMPA antagonist inhibits G2/M transition and induces apoptosis in human leukemia Jurkat T cell line.

Parenti S, Casagrande G, Montanari M, Espahbodinia M, Ettari R, Grande A, Corsi L.

Life Sci. 2016 May 1;152:117-25. doi: 10.1016/j.lfs.2016.03.051. Epub 2016 Apr 6.

PMID:
27178220
15.

The Inhibition of Cysteine Proteases Rhodesain and TbCatB: A Valuable Approach to Treat Human African Trypanosomiasis.

Ettari R, Previti S, Tamborini L, Cullia G, Grasso S, Zappalà M.

Mini Rev Med Chem. 2016;16(17):1374-1391. Review.

PMID:
27156518
16.

Immunoproteasome-Selective Inhibitors: A Promising Strategy to Treat Hematologic Malignancies, Autoimmune and Inflammatory Diseases.

Ettari R, Previti S, Bitto A, Grasso S, Zappalà M.

Curr Med Chem. 2016;23(12):1217-38. Review.

PMID:
26965184
17.

Synthesis and biological evaluation of novel peptidomimetics as rhodesain inhibitors.

Ettari R, Previti S, Cosconati S, Kesselring J, Schirmeister T, Grasso S, Zappalà M.

J Enzyme Inhib Med Chem. 2016 Dec;31(6):1184-91. doi: 10.3109/14756366.2015.1108972. Epub 2015 Nov 16.

PMID:
26572904
18.

Development of novel dipeptide-like rhodesain inhibitors containing the 3-bromoisoxazoline warhead in a constrained conformation.

Ettari R, Pinto A, Previti S, Tamborini L, Angelo IC, La Pietra V, Marinelli L, Novellino E, Schirmeister T, Zappalà M, Grasso S, De Micheli C, Conti P.

Bioorg Med Chem. 2015 Nov 1;23(21):7053-60. doi: 10.1016/j.bmc.2015.09.029. Epub 2015 Sep 21.

PMID:
26432608
19.

Mechanism and site of inhibition of AMPA receptors: substitution of one and two methyl groups at the 4-aminophenyl ring of 2,3-benzodiazepine and implications in the "E" site.

Wang C, Wu A, Shen YC, Ettari R, Grasso S, Niu L.

ACS Chem Neurosci. 2015 Aug 19;6(8):1371-8. doi: 10.1021/acschemneuro.5b00064. Epub 2015 May 29.

PMID:
25967651
20.

Synthesis and Pharmacological Evaluation of α4β2 Nicotinic Ligands with a 3-Fluoropyrrolidine Nucleus.

Tamborini L, Pinto A, Ettari R, Gotti C, Fasoli F, Conti P, De Micheli C.

ChemMedChem. 2015 Jun;10(6):1071-8. doi: 10.1002/cmdc.201500073. Epub 2015 Apr 16.

PMID:
25882435
21.

Selected cytotoxic gold compounds cause significant inhibition of 20S proteasome catalytic activities.

Micale N, Schirmeister T, Ettari R, Cinellu MA, Maiore L, Serratrice M, Gabbiani C, Massai L, Messori L.

J Inorg Biochem. 2014 Dec;141:79-82. doi: 10.1016/j.jinorgbio.2014.08.001. Epub 2014 Aug 11.

PMID:
25217719
22.

Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors.

Troiano V, Scarbaci K, Ettari R, Micale N, Cerchia C, Pinto A, Schirmeister T, Novellino E, Grasso S, Lavecchia A, Zappalà M.

Eur J Med Chem. 2014 Aug 18;83:1-14. doi: 10.1016/j.ejmech.2014.06.017. Epub 2014 Jun 10.

PMID:
24946214
23.

Synthesis and biological evaluation of papain-family cathepsin L-like cysteine protease inhibitors containing a 1,4-benzodiazepine scaffold as antiprotozoal agents.

Ettari R, Pinto A, Tamborini L, Angelo IC, Grasso S, Zappalà M, Capodicasa N, Yzeiraj L, Gruber E, Aminake MN, Pradel G, Schirmeister T, De Micheli C, Conti P.

ChemMedChem. 2014 Aug;9(8):1817-25. doi: 10.1002/cmdc.201402079. Epub 2014 Jun 11.

PMID:
24919925
24.

Development of novel selective peptidomimetics containing a boronic acid moiety, targeting the 20S proteasome as anticancer agents.

Scarbaci K, Troiano V, Ettari R, Pinto A, Micale N, Di Giovanni C, Cerchia C, Schirmeister T, Novellino E, Lavecchia A, Zappalà M, Grasso S.

ChemMedChem. 2014 Aug;9(8):1801-16. doi: 10.1002/cmdc.201402075. Epub 2014 May 28.

PMID:
24891205
25.

Efficient synthesis of novel glutamate homologues and investigation of their affinity and selectivity profile at ionotropic glutamate receptors.

Pinto A, Tamborini L, Mastronardi F, Ettari R, Romano D, Nielsen B, De Micheli C, Conti P.

Bioorg Med Chem Lett. 2014 Apr 15;24(8):1980-2. doi: 10.1016/j.bmcl.2014.02.058. Epub 2014 Mar 1.

26.

Peptide-based proteasome inhibitors in anticancer drug design.

Micale N, Scarbaci K, Troiano V, Ettari R, Grasso S, Zappalà M.

Med Res Rev. 2014 Sep;34(5):1001-69. doi: 10.1002/med.21312. Epub 2014 Mar 1. Review.

PMID:
24585725
27.

Identification of a new series of amides as non-covalent proteasome inhibitors.

Scarbaci K, Troiano V, Micale N, Ettari R, Tamborini L, Di Giovanni C, Cerchia C, Grasso S, Novellino E, Schirmeister T, Lavecchia A, Zappalà M.

Eur J Med Chem. 2014 Apr 9;76:1-9. doi: 10.1016/j.ejmech.2014.01.022. Epub 2014 Jan 25.

PMID:
24561716
28.

Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors.

Pinto A, Tamborini L, Mastronardi F, Ettari R, Safoz Y, Bunch L, Nielsen B, Jensen AA, De Micheli C, Conti P.

Eur J Med Chem. 2014 Mar 21;75:151-8. doi: 10.1016/j.ejmech.2014.01.029. Epub 2014 Jan 25.

PMID:
24531228
29.

Development of rhodesain inhibitors with a 3-bromoisoxazoline warhead.

Ettari R, Tamborini L, Angelo IC, Grasso S, Schirmeister T, Lo Presti L, De Micheli C, Pinto A, Conti P.

ChemMedChem. 2013 Dec;8(12):2070-6. doi: 10.1002/cmdc.201300390. Epub 2013 Nov 15.

PMID:
24243827
30.

Development of peptidomimetic boronates as proteasome inhibitors.

Micale N, Ettari R, Lavecchia A, Di Giovanni C, Scarbaci K, Troiano V, Grasso S, Novellino E, Schirmeister T, Zappalà M.

Eur J Med Chem. 2013 Jun;64:23-34. doi: 10.1016/j.ejmech.2013.03.032. Epub 2013 Mar 27.

PMID:
23639651
31.

Inhibition of rhodesain as a novel therapeutic modality for human African trypanosomiasis.

Ettari R, Tamborini L, Angelo IC, Micale N, Pinto A, De Micheli C, Conti P.

J Med Chem. 2013 Jul 25;56(14):5637-58. doi: 10.1021/jm301424d. Epub 2013 May 7.

PMID:
23611656
32.

Mechanism of falcipain-2 inhibition by α,β-unsaturated benzo[1,4]diazepin-2-one methyl ester.

Grazioso G, Legnani L, Toma L, Ettari R, Micale N, De Micheli C.

J Comput Aided Mol Des. 2012 Sep;26(9):1035-43. doi: 10.1007/s10822-012-9596-4. Epub 2012 Sep 11.

PMID:
22965332
33.

Synthesis and molecular modeling studies of derivatives of a highly potent peptidomimetic vinyl ester as falcipain-2 inhibitors.

Ettari R, Micale N, Grazioso G, Bova F, Schirmeister T, Grasso S, Zappalà M.

ChemMedChem. 2012 Sep;7(9):1594-600. doi: 10.1002/cmdc.201200274. Epub 2012 Jun 29.

PMID:
22753258
34.

Glutamate binding-site ligands of NMDA receptors.

Bonaccorso C, Micale N, Ettari R, Grasso S, Zappalà M.

Curr Med Chem. 2011;18(36):5483-506. Review.

PMID:
22172060
36.

Development of novel peptidomimetics containing a vinyl sulfone moiety as proteasome inhibitors.

Ettari R, Bonaccorso C, Micale N, Heindl C, Schirmeister T, Calabrò ML, Grasso S, Zappalà M.

ChemMedChem. 2011 Jul 4;6(7):1228-37. doi: 10.1002/cmdc.201100093. Epub 2011 Apr 19.

PMID:
21506279
37.

Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.

Ettari R, Zappalà M, Micale N, Grazioso G, Giofrè S, Schirmeister T, Grasso S.

Eur J Med Chem. 2011 Jun;46(6):2058-65. doi: 10.1016/j.ejmech.2011.02.058. Epub 2011 Mar 3.

PMID:
21420760
38.

Design and synthesis of novel isoxazole-based HDAC inhibitors.

Conti P, Tamborini L, Pinto A, Sola L, Ettari R, Mercurio C, De Micheli C.

Eur J Med Chem. 2010 Sep;45(9):4331-8. doi: 10.1016/j.ejmech.2010.06.035. Epub 2010 Jun 30.

PMID:
20637529
39.

Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors.

Bova F, Ettari R, Micale N, Carnovale C, Schirmeister T, Gelhaus C, Leippe M, Grasso S, Zappalà M.

Bioorg Med Chem. 2010 Jul 15;18(14):4928-38. doi: 10.1016/j.bmc.2010.06.010. Epub 2010 Jun 10.

PMID:
20598553
40.

Synthesis of novel peptidomimetics as inhibitors of protozoan cysteine proteases falcipain-2 and rhodesain.

Ettari R, Zappalà M, Micale N, Schirmeister T, Gelhaus C, Leippe M, Evers A, Grasso S.

Eur J Med Chem. 2010 Jul;45(7):3228-33. doi: 10.1016/j.ejmech.2010.04.003. Epub 2010 Apr 14.

PMID:
20434817
41.

Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors.

Micale N, Ettari R, Schirmeister T, Evers A, Gelhaus C, Leippe M, Zappalà M, Grasso S.

Bioorg Med Chem. 2009 Sep 15;17(18):6505-11. doi: 10.1016/j.bmc.2009.08.013. Epub 2009 Aug 12.

PMID:
19709887
42.

Falcipain-2 inhibitors.

Ettari R, Bova F, Zappalà M, Grasso S, Micale N.

Med Res Rev. 2010 Jan;30(1):136-67. doi: 10.1002/med.20163. Review.

PMID:
19526594
43.

Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.

Ettari R, Micale N, Schirmeister T, Gelhaus C, Leippe M, Nizi E, Di Francesco ME, Grasso S, Zappalà M.

J Med Chem. 2009 Apr 9;52(7):2157-60. doi: 10.1021/jm900047j.

PMID:
19296600
44.

Nonpeptidic vinyl and allyl phosphonates as falcipain-2 inhibitors.

Ettari R, Nizi E, Di Francesco ME, Micale N, Grasso S, Zappalà M, Vicík R, Schirmeister T.

ChemMedChem. 2008 Jul;3(7):1030-3. doi: 10.1002/cmdc.200800050. No abstract available.

PMID:
18428116
45.

Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors.

Ettari R, Nizi E, Di Francesco ME, Dude MA, Pradel G, Vicík R, Schirmeister T, Micale N, Grasso S, Zappalà M.

J Med Chem. 2008 Feb 28;51(4):988-96. doi: 10.1021/jm701141u. Epub 2008 Jan 31.

PMID:
18232656
46.

Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents.

Micale N, Kozikowski AP, Ettari R, Grasso S, Zappalà M, Jeong JJ, Kumar A, Hanspal M, Chishti AH.

J Med Chem. 2006 Jun 1;49(11):3064-7.

PMID:
16722625

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