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001-es BibID:BIBFORM003546
Első szerző:Amano, Masayuki
Cím:A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro / Amano M., Koh Y., Das D., Li J., Leschenko S., Wang Y.F., Boross P.I., Weber I.T., Ghosh A.K., Mitsuya H.
Dátum:2007
Megjegyzések:We designed, synthesized, and identified GRL-98065, a novel nonpeptidic human immunodeficiency virus type 1 (HIV-1) protease inhibitor (PI) containing the structure-based designed privileged cyclic ether-derived nonpeptide P2 ligand, 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane (bis-THF), and a sulfonamide isostere, which is highly potent against laboratory HIV-1 strains and primary clinical isolates (50% effective concentration [EC(50)], 0.0002 to 0.0005 microM) with minimal cytotoxicity (50% cytotoxicity, 35.7 microM in CD4(+) MT-2 cells). GRL-98065 blocked the infectivity and replication of each of the HIV-1(NL4-3) variants exposed to and selected by up to a 5 microM concentration of saquinavir, indinavir, nelfinavir, or ritonavir and a 1 microM concentration of lopinavir or atazanavir (EC(50), 0.0015 to 0.0075 microM), although it was less active against HIV-1(NL4-3) selected by amprenavir (EC(50), 0.032 microM). GRL-98065 was also potent against multiple-PI-resistant clinical HIV-1 variants isolated from patients who had no response to existing antiviral regimens after having received a variety of antiviral agents, HIV-1 isolates of various subtypes, and HIV-2 isolates examined. Structural analyses revealed that the close contact of GRL-98065 with the main chain of the protease active-site amino acids (Asp29 and Asp30) is important for its potency and wide-spectrum activity against multiple-PI-resistant HIV-1 variants. The present data demonstrate that the privileged nonpeptide P2 ligand, bis-THF, is critical for the binding of GRL-98065 to the HIV protease substrate binding site and that this scaffold can confer highly potent antiviral activity against a wide spectrum of HIV isolates.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Antimicrobial agents and chemotherapy. - 51 : 6 (2007), p. 2143-2155. -
További szerzők:Koh, Yasuhiro Das, Debananda Li, Jianfeng Leschenko, Sofiya Wang, Yuan-Fang Boross Péter (1972-) (biokémikus, vegyész) Weber, Irene T. Ghosh, Arun K. Mitsuya, Hiroaki
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2.

001-es BibID:BIBFORM076207
035-os BibID:(Cikkazonosító)e01777-18 (Scopus)85060825357 (WOS)000457110200035
Első szerző:Kovács Renátó László (molekuláris biológus)
Cím:In vivo applicability of Neosartorya fischeri antifungal protein 2 (NFAP2) in treatment of vulvovaginal candidiasis / Kovács Renátó, Holzknecht Jeanett, Hargitai Zoltán, Papp Csaba, Farkas Attila, Borics Attila, Tóth Liliána, Váradi Györgyi, Tóth Gábor K., Kovács Ilona, Dubrac Sandrine, Majoros László, Marx Florentine, Galgóczy László
Dátum:2019
ISSN:0066-4804 1098-6596
Megjegyzések:In the consequence of emerging number of vulvovaginitis caused by azole-resistant and biofilm-forming Candida species, the fast and efficient treatment of this infection has become challenging. The problem is further exacerbated by the severe side-effects of azoles as long-term use medications in the recurrent form. There is therefore an increasing demand for novel and safely applicable effective antifungal therapeutic strategies. The small, cysteine-rich and cationic antifungal proteins from filamentous ascomycetes are potential candidates as they inhibit the growth of several Candida spp. in vitro; however no information is available about their in vivo antifungal potency against yeasts. In the present study we investigated the possible therapeutic application of one of their representatives in the treatment of vulvovaginal candidiasis, the Neosartorya fischeri antifungal protein 2 (NFAP2). NFAP2 inhibited the growth of a fluconazole (FLC)-resistant Candida albicans strain isolated from vulvovaginal infection, and it was effective against both planktonic cells and biofilm in vitro We observed that the fungal cell killing activity of NFAP2 is connected to its pore-forming ability in the cell membrane. NFAP2 did not exert cytotoxic effects on primary human keratinocytes and dermal fibroblasts at the minimal inhibitory concentration in vitro In vivo murine vulvovaginitis model experiments showed that NFAP2 significantly decreases the cell number of the FLC-resistant C. albicans, and the combined application with FLC enhances the efficacy. These results suggest that NFAP2 provides a feasible base for the development of a fundamental new, safely applicable mono- or polytherapeutic topical agent in the treatment of superficial candidiasis.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
folyóiratcikk
Megjelenés:Antimicrobial Agents And Chemotherapy. - 63 : 2 (2019), p. 1-12. -
További szerzők:Holzknecht, Jeanett Hargitai Zoltán Papp Csaba (1966-) (aneszteziológus és intenzív terápiás szakorvos) Farkas Attila (1961-) (farmakológus) Borics Attila Tóth Liliána Váradi Györgyi Tóth Gábor K. Kovács Ilona (1965-) (patológus) Dubrac, Sandrine Majoros László (1966-) (szakorvos, klinikai mikrobiológus) Marx, Florentine Galgóczy László (1950-)
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3.

001-es BibID:BIBFORM004145
Első szerző:Leiter Éva (biológus)
Cím:Antifungal protein PAF severely affects the integrity of the plasma membrane of Aspergillus nidulans and induces an apoptosis-like phenotype / Éva Leiter, Henrietta Szappanos, Christoph Oberparleiter, Lydia Kaiserer, László Csernoch, Tünde Pusztahelyi, Tamás Emri, István Pócsi, Willibald Salvenmoser, and Florentine Marx
Dátum:2005
Megjegyzések:The small, basic, and cysteine-rich antifungal protein PAF is abundantly secreted into the supernatant by the beta-lactam producer Penicillium chrysogenum. PAF inhibits the growth of various important plant and zoopathogenic filamentous fungi. Previous studies revealed the active internalization of the antifungal protein and the induction of multifactorial detrimental effects, which finally resulted in morphological changes and growth inhibition in target fungi. In the present study, we offer detailed insights into the mechanism of action of PAF and give evidence for the induction of a programmed cell death-like phenotype. We proved the hyperpolarization of the plasma membrane in PAF-treated Aspergillus nidulans hyphae by using the aminonaphtylethenylpyridinium dye di-8-ANEPPS. The exposure of phosphatidylserine on the surface of A. nidulans protoplasts by Annexin V staining and the detection of DNA strand breaks by TUNEL (terminal deoxynucleotidyltransferase-mediated dUTP-biotin nick end labeling) gave evidence for a PAF-induced apoptotic-like mechanism in A. nidulans. The localization of reactive oxygen species (ROS) by dichlorodihydrofluorescein diacetate and the abnormal cellular ultrastructure analyzed by transmission electron microscopy suggested that ROS-elicited membrane damage and the disintegration of mitochondria played a major role in the cytotoxicity of PAF. Finally, the reduced PAF sensitivity of A. nidulans strain FGSC1053, which carries a dominant-interfering mutation in fadA, supported our assumption that G-protein signaling was involved in PAF-mediated toxicity.
Tárgyszavak:Természettudományok Biológiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Antimicrobial Agents and Chemotherapy. - 49 : 6 (2005), p. 2445-2453. -
További szerzők:Oberparleiter, Christoph Kaiserer, Lydia Csernoch László (1961-) (élettanász) Pusztahelyi Tünde (1969-) (biológus, angol-magyar szakfordító) Emri Tamás (1969-) (biológus) Pócsi István (1961-) (vegyész) Salvenmoser, Willibald Marx, Florentine Szappanos Henrietta (1976-) (biológus, élettanász)
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4.

001-es BibID:BIBFORM018119
Első szerző:Majoros László (szakorvos, klinikai mikrobiológus)
Cím:Caspofungin susceptibility testing of Candida inconspicua : correlation of different methods with the minimal fungicidal concentration / Majoros L., Kardos G., Szabó G., Sipiczki M.
Dátum:2005
ISSN:0066-4804
Megjegyzések:Minimal inhibitory and minimal fungicidal concentrations of caspofungin were determined for 48 Candida inconspicua isolates. By using CLSI (formerly NCCLS) methodology with the partial inhibition endpoint criterion, caspofungin exhibited a good fungicidal effect against C. inconspicua (the MIC90 was 0.25 ?g/ml and the minimum fungicidal concentration [MFC] was 0.5 ?g/ml after 24 h). Total inhibition yielded falsely elevated MICs, exceeding even the respective MFCs.
Tárgyszavak:Természettudományok Biológiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Antimicrobial Agents And Chemotherapy. - 49 : 8 (2005), p. 3486-3488. -
További szerzők:Kardos Gábor (1974-) (szakorvos, klinikai mikrobiológus) Szabó G. Sipiczki Mátyás (1948-) (biológus)
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5.

001-es BibID:BIBFORM001620
Első szerző:Sóczó Georgina
Cím:In vitro study of candida tropicalis isolates exhibiting paradoxical growth in the presence of high concentrations of caspofungin / Sóczó Georgina, Kardos Gábor, Varga István, Kelentey Barna, Gesztelyi Rudolf, Majoros László
Dátum:2007
Megjegyzések:Paradoxical growth was noted in RPMI 1640 and antibiotic medium 3 in the case of 14 and 1 of 15 Candida tropicalis strains, respectively, at a caspofungin concentration of 12.5 beta g/ml using minimum fungicidal concentration tests. Time-kill assays showed that against isolates killed at lower concentrations, caspofungin at a concentration of 12.5 beta g/ml was only fungistatic.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok Klinikai orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Candida tropicalis
caspofungin
Megjelenés:Antimicrobial Agents and Chemotherapy 51 : 12 (2007), p. 4474-4476. -
További szerzők:Kardos Gábor (1974-) (szakorvos, klinikai mikrobiológus) Varga István (1974-) (fogszakorvos) Kelentey Barna (1959-) (fogszakorvos) Gesztelyi Rudolf (1969-) (kísérletes farmakológus) Majoros László (1966-) (szakorvos, klinikai mikrobiológus)
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