TY  - JOUR
AU  - Parravicini, Oscar
AU  - Somlai, Csaba
AU  - Andujar, Sebastian A
AU  - Garro, Adriana D
AU  - Lima, Beatriz
AU  - Tapia, Alejandro
AU  - Feresin, Gabriela
AU  - Perczel, András
AU  - Tóth, Gábor
AU  - Cascales, Javier Lopez
AU  - Rodriguez, Ana M
AU  - Enriz, Ricardo D
TI  - Small Peptides Derived from Penetratin as Antibacterial Agents
JF  - ARCHIV DER PHARMAZIE
J2  - ARCH PHARM
VL  - 349
PY  - 2016
IS  - 4
SP  - 242
EP  - 251
PG  - 10
SN  - 0365-6233
DO  - 10.1002/ardp.201500419
UR  - https://m2.mtmt.hu/api/publication/3054649
ID  - 3054649
N1  - Funding Agency and Grant Number: Universidad Nacional de San Luis; CICITCA Universidad Nacional de San Juan; Agencia de Promocion Cientifica y Tecnologica de la Argentina PICT [2010-1832]; Hungarian Scientific Research Fund (OTKA)Orszagos Tudomanyos Kutatasi Alapprogramok (OTKA) [NK101072]; CONICETConsejo Nacional de Investigaciones Cientificas y Tecnicas (CONICET)
            Funding text: This study is a part of the Hungarian-Argentine Intergovernmental S&T Cooperation Programme. This research was supported by grants from Universidad Nacional de San Luis, CICITCA Universidad Nacional de San Juan, and grants to R.D.E. (Agencia de Promocion Cientifica y Tecnologica de la Argentina PICT 2010-1832). This study was partly supported by grants from the Hungarian Scientific Research Fund (OTKA NK101072). R.D.E., S.A., B.L., A.D.G., and G.E.F. are researchers from CONICET (Argentina). O.P. holds a fellowship from CONICET. The authors would like to thank MSc. D.O. Zamo for technical assistance.
AB  - The synthesis, in vitro evaluation and conformational study of several small-size peptides acting as antibacterial agents are reported. Among the compds. evaluated, the peptides Arg-Gln-Ile-Lys-Ile-Trp-Arg-Arg-Met-Lys-Trp-Lys-Lys-NH2, Arg-Gln-Ile-Lys-Ile-Arg-Arg-Met-Lys-Trp-Arg-NH2, and Arg-Gln-Ile-Trp-Trp-Trp-Trp-Gln-Arg-NH2 exhibited significant antibacterial activity. These were found to be very active antibacterial compds., considering their small mol. size. To better understand the antibacterial activity obtained for these peptides, an exhaustive conformational anal. was performed, using both theor. calcns. and exptl. measurements. Mol. dynamics simulations using two different media (water and trifluoroethanol/water) were employed. The results of these theor. calcns. were corroborated by exptl. CD measurements. A brief discussion on the possible mechanism of action of these peptides at mol. level is also presented. Some of the peptides reported here constitute very interesting structures to be used as starting compds. for the design of new small-size peptides possessing antibacterial activity. [on SciFinder(R)]
LA  - English
DB  - MTMT
ER  - 

TY  - JOUR
AU  - Szőllősi, György
AU  - Csámpai, Antal
AU  - Somlai, Csaba
AU  - Fekete, M
AU  - Bartók, Mihály
TI  - Unusual enantioselectivities in heterogeneous organocatalyzed reactions: Reversal of direction using proline di- versus tri-peptides in the aldol addition
JF  - JOURNAL OF MOLECULAR CATALYSIS A-CHEMICAL
J2  - J MOL CATAL A-CHEM
VL  - 382
PY  - 2014
SP  - 86
EP  - 92
PG  - 7
SN  - 1381-1169
DO  - 10.1016/j.molcata.2013.11.011
UR  - https://m2.mtmt.hu/api/publication/2550508
ID  - 2550508
N1  - BM-401
Megjegyzés-24064001
BM-401
Admin megjegyzés-24064001
#tbldoc_author 0 Szerző ismeretlen #
#tbldoc_author 2 hozzárendelt szerző nem található #Bartok M
Megjegyzés-23568056
ref.[12];
Megjegyzés-23568077
ref.[29];
Megjegyzés-23568086
ref.[30];
Megjegyzés-23568131
ref.[34];
Megjegyzés-23568137
ref.[31];
Megjegyzés-23568149
ref.[32];
Megjegyzés-23568046
ref.[28];
Megjegyzés-23568034
ref.[10];
Megjegyzés-23568072
ref.[53];
Megjegyzés-23568111
ref.[11];
Megjegyzés-23568002
ref.[9];
LA  - English
DB  - MTMT
ER  - 

TY  - JOUR
AU  - Garro, AD
AU  - Olivella, MS
AU  - Bombasaro, JA
AU  - Lima, B
AU  - Tapia, A
AU  - Feresin, G
AU  - Perczel, András
AU  - Somlai, Csaba
AU  - Penke, Botond
AU  - López, Cascales J
AU  - Rodríguez, AM
AU  - Enriz, RD
TI  - Penetratin and derivatives acting as antibacterial agents
JF  - CHEMICAL BIOLOGY & DRUG DESIGN
J2  - CHEM BIOL DRUG DES
VL  - 82
PY  - 2013
IS  - 2
SP  - 167
EP  - 177
PG  - 11
SN  - 1747-0277
DO  - 10.1111/cbdd.12143
UR  - https://m2.mtmt.hu/api/publication/2386687
ID  - 2386687
AB  - The synthesis, in vitro evaluation and conformational study of penetratin and structurally related derivatives acting as antibacterial agents are reported. Among the compounds evaluated here, two methionine sulphoxide derivatives (RQIKIWFQNRRM[O]KWKK-NH2 and RQIKIFFQNRRM[O]KFKK-NH2) exhibited the strongest antibacterial effect in this series. In order to better understand the antimicrobial activity obtained for these peptides, we performed an exhaustive conformational analysis using different approaches. Molecular dynamics simulations were performed using two different media (water and trifluoroethanol/water). The results of these theoretical calculations were corroborated using experimental CD measurements. The electronic study for these peptides was carried out using molecular electrostatic potentials obtained from RHF/6-31G(d) calculations. In addition, the non-apeptide RQIRRWWQR-NH2 showed strong inhibitory action against the Gram-negative and Gram-positive bacteria tested in this study. In this study we report the synthesis, in vitro evaluation, and conformational study of penetratin and structurally related derivatives acting as antibacterial agents. Among the compounds evaluated two methionine sulfoxide derivatives (RQIKIWFQNRRM[O] KWKK-NH2 and RQIKIFFQNRRM[O]KFKK-NH2) and a nonapeptide (RQIRRWWQR-NH2) exhibited the strongest antibacterial effect against the Gram-negative and Gram-positive bacteria tested in this study.© 2013 John Wiley and Sons A/S.
LA  - English
DB  - MTMT
ER  - 

TY  - JOUR
AU  - Somlai, Csaba
AU  - Correche, Estela
AU  - Olivella, Monica
AU  - Tolosa, Laia
AU  - Lechon, Maria Jose Gomez
AU  - Dombi, György
AU  - Tóth, Gábor
AU  - Penke, Botond
AU  - Enriz, Ricardo D
TI  - Synthesis and cytotoxic activity of 4-N-carboxybutyl-5-fluorocytosyl-Arg-Gln-Trp-Arg-Arg-Trp-Trp-Gln-Arg-NH2
JF  - BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
J2  - BIOORG MED CHEM LETT
VL  - 22
PY  - 2012
IS  - 13
SP  - 4233
EP  - 4237
PG  - 5
SN  - 0960-894X
DO  - 10.1016/j.bmcl.2012.05.045
UR  - https://m2.mtmt.hu/api/publication/1993696
ID  - 1993696
N1  - M1: Copyright (C) 2012 American Chemical Society (ACS). All Rights Reserved.
CAPLUS AN 2012:803819(Journal; Online Computer File)
AB  - The chem. synthesis of 4-N-carboxybutyl-5-fluorocytosine in soln. phase starting from 5-fluorocytosine and the solid phase synthesis of Arg-Gln-Trp-Arg-Arg-Trp-Trp-Gln-Arg-NH2 attached to the 4-N-carboxybutyl-5-fluorocytosine residue at the N-terminus of the peptide via peptide bond formation is reported. The target compd. exhibited a significant cytotoxic activity against a culture of HepG2 cells. In addn. our results demonstrated that this new compd. affect cell viability, produce mitochondrial dysfunction as well as interfere with intracellular calcium homeostasis control; leading to cell malfunction and death. [on SciFinder(R)]
LA  - English
DB  - MTMT
ER  - 

TY  - JOUR
AU  - Czövek, Dorottya
AU  - Novák, Zoltán
AU  - Somlai, Csaba
AU  - Asztalos, T
AU  - Tiszlavicz, László
AU  - Bozóki, Zoltán
AU  - Ajtai, Tibor
AU  - Utry, Noémi
AU  - Filep, Ágnes
AU  - Bari, Ferenc
AU  - Peták, Ferenc
TI  - Respiratory consequences of red sludge dust inhalation in rats
JF  - TOXICOLOGY LETTERS
J2  - TOXICOL LETT
VL  - 209
PY  - 2012
IS  - 2
SP  - 113
EP  - 120
PG  - 8
SN  - 0378-4274
DO  - 10.1016/j.toxlet.2011.12.006
UR  - https://m2.mtmt.hu/api/publication/1845203
ID  - 1845203
AB  - The environmental disaster following flooding by red sludge in the Ajka region in Hungary poses a serious public health threat with particular concern regarding the potentially adverse respiratory effects of the inhalation of red sludge dust (RSD). The respiratory consequences of the inhalation of RSD obtained from field samples were investigated in rats. Rats were either exposed to RSD at a high concentration (2 weeks, 8h/day), or kept in room air. After the exposures, the airway resistance (R(aw)) and the respiratory tissues mechanics were measured under baseline condition, and following methacholine (MCh) challenges with the aim of establishing airway hyper-responsiveness (AH). Histopathology was performed to assess lung morphologic alterations. The physical properties and the chemical composition of the RSD were also characterized. The size distribution, chemical composition and topology of the RSD particles applied in our experiments were similar to those observed at the site of the disaster. The inhalation of RSD did not alter the basal respiratory mechanics, whereas it led to greater MCh-induced responses in R(aw), demonstrating the progression of mild AH. Histopathological investigations revealed fine, granular particles in the alveolar macrophages, as evidence that RSD had reached the lower respiratory tract and induced mild inflammation around the alveoli and the pulmonary vasculature. The mild respiratory symptoms that developed following short-term exposure of healthy individuals to high concentrations of airborne RSD do not appear to pose a greater respiratory hazard than the inhalation of urban dust at a comparable concentration.
LA  - English
DB  - MTMT
ER  - 

TY  - JOUR
AU  - Kasperkiewicz, M
AU  - Muller, R
AU  - Manz, R
AU  - Magens, M
AU  - Hammers, CM
AU  - Somlai, Csaba
AU  - Westermann, J
AU  - Schmidt, E
AU  - Zillikens, D
AU  - Ludwig, RJ
AU  - Orosz, Antal
TI  - Heat-shock protein 90 inhibition in autoimmunity to type VII collagen: evidence that nonmalignant plasma cells are not therapeutic targets
JF  - BLOOD
J2  - BLOOD
VL  - 117
PY  - 2011
IS  - 23
SP  - 6135
EP  - 6142
PG  - 8
SN  - 0006-4971
DO  - 10.1182/blood-2010-10-314609
UR  - https://m2.mtmt.hu/api/publication/1880324
ID  - 1880324
N1  - R.J.L. and A.O. contributed equally to this study.
AB  - Blocking heat-shock protein 90 (Hsp90) induces death of malignant plasma cells by activation of the unfolded protein response, a signaling pathway activated by accumulation of misfolded proteins within the endoplasmic reticulum. We hypothesized that nontransformed plasma cells are also hypersensitive to Hsp90 inhibition because of their high amount of protein biosynthesis. To investigate this hypothesis, 2 different Hsp90 inhibitors, the geldanamycin derivative 17-DMAG and the nontoxic peptide derivative TCBL-145, were applied to mice with experimental epidermolysis bullosa acquisita, an autoimmune bullous disease characterized by autoantibodies against type VII collagen of the dermal-epidermal junction. Both inhibitors ameliorated clinical disease of type VII collagen-immunized mice, suppressed auto-antibody production, and reduced dermal neutrophilic infiltrate. Interestingly, total plasma cell numbers, type VII collagen-specific plasma cells, and germinal center B cells were unaffected by anti-Hsp90 treatment in vivo. However, T-cell proliferation was potently inhibited, as evidenced by the reduced response of isolated lymph node cells from immunized mice to in vitro restimulation with anti-CD3/CD28 antibody or autoantigen in the presence of Hsp90 inhibitors. Our results suggest that Hsp90 blockade has no impact on normal or autoreactive plasma cells in vivo and indentify T cells as targets of anti-Hsp90 treatment in autoimmunity to type VII collagen. (Blood. 2011;117(23):6135-6142)
LA  - English
DB  - MTMT
ER  - 

TY  - JOUR
AU  - Kasperkiewicz, M
AU  - Muller, R
AU  - Manz, R
AU  - Magens, M
AU  - Hammers, C
AU  - Somlai, Csaba
AU  - Westermann, J
AU  - Schmidt, E
AU  - Zillikens, D
AU  - Ludwig, R
AU  - Orosz, Antal
TI  - Heat shock protein 90 inhibition in autoimmunity to type VII collagen
JF  - JOURNAL OF INVESTIGATIVE DERMATOLOGY
J2  - J INVEST DERMATOL
VL  - 131
PY  - 2011
SP  - S6
EP  - S6
SN  - 0022-202X
UR  - https://m2.mtmt.hu/api/publication/1880323
ID  - 1880323
LA  - English
DB  - MTMT
ER  - 

TY  - JOUR
AU  - Serly, Julianna
AU  - Vincze, Irén
AU  - Somlai, Csaba
AU  - Hodoniczki, László
AU  - Molnár, József
TI  - Synthesis and Comparison of the Antitumor Activities of Steroids on ABCB1-transfected Mouse Lymphoma and Human Ovary Carcinoma
JF  - LETTERS IN DRUG DESIGN AND DISCOVERY
J2  - LETT DRUG DES DISCOV
VL  - 8
PY  - 2011
IS  - 2
SP  - 138
EP  - 147
PG  - 10
SN  - 1570-1808
DO  - 10.2174/157018011794183833
UR  - https://m2.mtmt.hu/api/publication/1876499
ID  - 1876499
LA  - English
DB  - MTMT
ER  - 

TY  - JOUR
AU  - Garibotto, FM
AU  - Garro, AD
AU  - Rodriguez, AM
AU  - Raimondi, M
AU  - Zacchino, SA
AU  - Perczel, András
AU  - Somlai, Csaba
AU  - Penke, Botond
AU  - Enriz, RD
TI  - Penetratin analogues acting as antifungal agents
JF  - EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
J2  - EUR J MED CHEM
VL  - 46
PY  - 2011
IS  - 1
SP  - 370
EP  - 377
PG  - 8
SN  - 0223-5234
DO  - 10.1016/j.ejmech.2010.10.025
UR  - https://m2.mtmt.hu/api/publication/1842710
ID  - 1842710
N1  - WC: Chemistry, Medicinal
Funding Agency and Grant Number: Hungarian-Argentine Intergovernmental S&T Cooperation Programme; Universidad Nacional de San Luis
            Funding text: This work is part of the Hungarian-Argentine Intergovernmental S&T Cooperation Programme. This research was partially supported by grants from Universidad Nacional de San Luis and it is part of the Iberoamerican Project X.7 PIBEAFUN (Search and development of new antifungal part of the Iberoamerican Program of Science and Technology for the Development (CYTED)). R.D.E. is a member of the CONICET (Argentina) staff.
AB  - The synthesis, in vitro evaluation, and conformational study of penetratin analogues acting as antifungal agents are reported. Different peptides structurally related with penetratin were evaluated. Analogues of penetratin rich in Arg, Lys and Trp amino acids were tested. In addition, HFRWRQIKIWFQNRRM[O]KWKK-NH(2), a synthetic 20 amino acid peptide was also evaluated. These penetratin analogues displayed antifungal activity against human pathogenic strains including Candida albicans and Cryptococcus neoformans. In contrast, Tat peptide, a well-known cell penetrating peptide, did not show a significant antifungal activity against fungus tested here. We also performed a conformational study by means experimental and theoretical approaches (CD spectroscopic measurements and MD simulations). The electronic structure analysis was carried out from Molecular Electrostatic Potentials (MEP) obtained by using RHF/6-31G ab initio calculations. Our experimental and theoretical results permitted us to identify a topographical template which may provide a guide for the design of new peptides with antifungal effects. (C) 2010 Elsevier Masson SAS. All rights reserved.
LA  - English
DB  - MTMT
ER  - 

TY  - JOUR
AU  - Garro, AD
AU  - Garibotto, FM
AU  - Rodriguez, AM
AU  - Raimondi, M
AU  - Zacchino, SA
AU  - Perczel, András
AU  - Somlai, Csaba
AU  - Penke, Botond
AU  - Enriz, RD
TI  - New Small-Size Antifungal Peptides: Design, Synthesis and Antifungal Activity
JF  - LETTERS IN DRUG DESIGN AND DISCOVERY
J2  - LETT DRUG DES DISCOV
VL  - 8
PY  - 2011
IS  - 6
SP  - 562
EP  - 567
PG  - 6
SN  - 1570-1808
DO  - 10.2174/157018011795906785
UR  - https://m2.mtmt.hu/api/publication/1842707
ID  - 1842707
N1  - M1: Copyright (C) 2012 American Chemical Society (ACS). All Rights Reserved.
CAPLUS AN 2011:710047(Journal; Online Computer File)
AB  - The synthesis, in vitro evaluation and conformational study of small-size peptides acting as antifungal agents are reported. These peptides displayed antifungal activity against human pathogenic strains including Candida albicans and Cryptococcus neoformans. Among the peptides reported here, RQWRRWWQR-NH(2) exhibited the strongest activity against Cryptococcus neoformans. Our results allowed us to reduce in size these bioactive peptides from 16 to 11 and to 9 amino acid residues in total. Despite their reduction, they still maintained and even enhanced the antifungal activity detected for penetratin. A conformational and electronic structure analysis on these peptides was also performed by using molecular mechanics calculations in conjunction with Molecular Electrostatic Potentials (MEP) maps.
LA  - English
DB  - MTMT
ER  -