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1.

001-es BibID:BIBFORM099555
035-os BibID:(cikkazonosító)170716 (WoS)000740210200001 (Scopus)85121979229
Első szerző:Cai, Ren-Zhi
Cím:Synthesis of potent antagonists of receptors for growth hormone-releasing hormone with antitumor and anti-inflammatory activity / Renzhi Cai, Xianyang Zhang, Haibo Wang, Tengjiao Cui, Gabor Halmos, Wei Sha, Jinlin He, Petra Popovics, Irving Vidaurre, Chongxu Zhang, Mehdi Mirsaeidi, Andrew V. Schally
Dátum:2022
ISSN:0196-9781
Megjegyzések:The syntheses and biological evaluation of GHRH antagonists of AVR series with high anticancer and antiinflammatory activities are described. Compared to our previously reported GHRH antagonist 602 of MIAMI series, AVR analogs contain additional modifications at positions 0, 6, 8, 10, 11, 12, 20, 21, 29 and 30, which induce greater antitumor activities. Five of nineteen tested AVR analogs presented binding affinities to the membrane GHRH receptors on human pituitary, 2-4-fold better than MIA-602. The antineoplastic properties of these analogs were evaluated in vitro using proliferation assays and in vivo in nude mice xenografted with various human cancer cell lines including lung (NSCLC-ADC HCC827 and NSCLC H460), gastric (NCI-N87), pancreatic (PANC-1 and CFPAC-1), colorectal (HT-29), breast (MX-1), glioblastoma (U87), ovarian (SK-OV-3 and OVCAR-3) and prostatic (PC3) cancers. In vitro AVR analogs showed inhibition of cell viability equal to or greater than MIA602. After subcutaneous administration at 5 mu g/day doses, some AVR antagonists demonstrated better inhibition of tumor growth in nude mice bearing various human cancers, with analog AVR-353 inducing stronger suppression than MIA-602 in lung, gastric, pancreatic and colorectal cancers and AVR-352 in ovarian cancers and glioblastoma. Both antagonists induced greater inhibition of GH release than MIA-602 in vitro in cultured rat pituitary cells and in vivo in rats. AVR-352 also demonstrated stronger anti-inflammatory effects in lung granulomas from mice with lung inflammation. Our studies demonstrate the merit of further investigation of AVR GHRH antagonists and support their potential use for clinical therapy of human cancers and other diseases.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
folyóiratcikk
Megjelenés:Peptides. - 150 (2022), p. 1-13. -
További szerzők:Zhang, Xianyang Wang, Haibo Cui, Tengjiao Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus) Sha, Wei He, Jinlin Popovics Petra Vidaurre, Irving Zhang, Chongxu Mirsaeidi, Mehdi Schally, Andrew Victor
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2.

001-es BibID:BIBFORM049347
Első szerző:Cai, Ren-Zhi
Cím:Synthesis of new potent agonistic analogs of growth hormone-releasing hormone (GHRH) and evaluation of their endocrine and cardiac activities / Renzhi Cai, Andrew V. Schally, Tengjiao Cui, Luca Szalontay, Gabor Halmos, Wei Sha, Magdolna Kovacs, Miklos Jaszberenyi, Jinlin He, Ferenc G. Rick, Petra Popovics, Rosemeire Kanashiro-Takeuchi, Joshua M. Hare, Norman L. Block, Marta Zarandi
Dátum:2013
ISSN:0196-9781
Megjegyzések:AbstractIn view of the recent findings of stimulatory effects of GHRH analogs, JI-34, JI-36 and JI-38, on cardiomyocytes, pancreatic islets and wound healing, three series of new analogs of GHRH(1-29) have been synthesized and evaluated biologically in an endeavor to produce more potent compounds. "Agmatine analogs", MR-356 (N-Me-Tyr1-JI-38), MR-361(N-Me-Tyr1, D-Ala2-JI-38) and MR-367(N-Me-Tyr1, D-Ala2, Asn8-JI-38), in which Dat in JI-38 is replaced by N-Me-Tyr1, showed improved relative potencies on GH release upon subcutaneous administration in vivo and binding in vitro. Modification with N-Me-Tyr1 and Arg29-NHCH3 as in MR-403 (N-Me-Tyr1, D-Ala2, Arg29-NHCH3-JI-38), MR-406 (N-Me-Tyr1, Arg29-NHCH3-JI-38) and MR-409 (N-Me-Tyr1, D-Ala2, Asn8, Arg29-NHCH3-JI-38), and MR-410 (N-Me-Tyr1, D-Ala2, Thr8, Arg29-NHCH3-JI-38) resulted in dramatically increased endocrine activities. These appear to be the most potent GHRH agonistic analogs so far developed. Analogs with Apa30-NH2 such as MR-326 (N-Me-Tyr1, D-Ala2, Arg29, Apa30-NH2-JI-38), and with Gab30-NH2, as MR-502 (D-Ala2, 5F-Phe6, Ser28, Arg29,Gab30-NH2-JI-38) also exhibited much higher potency than JI-38 upon i.v. administration. The relationship between the GH-releasing potency and the analog structure is discussed. Fourteen GHRH agonists with the highest endocrine potencies were subjected to cardiologic tests. MR-409 and MR-356 exhibited higher potency than JI-38 in activating myocardial repair in rats with induced myocardial infarction. As the previous class of analogs, exemplified by JI-38, had shown promising results in multiple fields including cardiology, diabetes and wound healing, our new, more potent, GHRH agonists should manifest additional efficacy for possible medical applications.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
5-aminopentanoyl
Abu
Agm
Apa
Cardioprotection
Dat
EF
Fpa5
GH
GH-releasing hormone
GHRH
Gab
IGF
MI
MeCN
N-Me-Tyr
N-methyl-tyrosine
PKA
PKC
PLC
TOF
acetonitrile
agmatine
des-amino-tyrosine
ejection fraction
gamma-amino-butanoyl
growth hormone
hGHRH agonist
hGHRH(1-29)
human
i.v.
insulin-like growth factor
intravenous, myocardial infarction
pentafluoro-Phe, phospholipase C
protein kinase A
protein kinase C
s.c.
s.c. administration
subcutaneous
time-of-flight
Megjelenés:Peptides. - 52C (2013), p. 104-112. -
További szerzők:Schally, Andrew Victor Cui, Tengjiao Szalontay Luca Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus) Sha, Wei Kovács Magdolna Jászberényi Miklós He, Jinlin Rick Ferenc G. Popovics Petra Kanashiro-Takeuchi, Rosemeire Hare, Joshua M. Block, Norman L. Zarándi Márta
Pályázati támogatás:TÁMOP-4.2.2.A-11/1/KONV-2012-0025
TÁMOP
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3.

001-es BibID:BIBFORM030559
Első szerző:Kovács József
Cím:Asphyxia-induced release of alpha-melanocyte-stimulating hormone in newborn pigs / József Kovács, János Julesz, Mónika V. Mogyoróssy, Mária A. Deli, Csongor S. Ábrahám, Miklós Vecsernyés
Dátum:2001
ISSN:0196-9781
Megjegyzések:Asphyxia and reperfusion induced changes in the plasma and cerebrospinal fluid (CSF) concentrations of alpha-melanocyte-stimulating hormone (alpha-MSH) were studied in newborn pigs using a specific radioimmunoassay technique. Cardiovascular and metabolic failure induced by neonatal asphyxia resulted in a 3-fold, significant (P < 0.05) increase in plasma alpha-MSH levels, whereas the hormone concentration in CSF was significantly (P < 0.05) reduced by 50% during postasphyxial reperfusion. Our data indicate an asphyxia-induced release of alpha-MSH, and suggest a discordant regulation of plasma and CSF concentrations in newborn pigs.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
asphyxia
cerebrospinal fluid
alpha-melanocyte-stimulating hormone
newborn
plasma
resuscitation
egyetemen (Magyarországon) készült közlemény
Megjelenés:Peptides. - 22 : 7 (2001), p. 1049-1053. -
További szerzők:Julesz János Mogyoróssy Mónika V. Deli Mária A. Abrahám Csongor Vecsernyés Miklós (1959-) (gyógyszertechnológus, endokrinológus)
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4.

001-es BibID:BIBFORM011474
Első szerző:Treszl Andrea (molekuláris biológus)
Cím:Inhibition of human non-small cell lung cancers with a targeted cytotoxic somatostatin analog, AN-162 / Treszl A., Schally A. V., Seitz S., Szalontay L., Rick F. G., Szepeshazi K., Halmos G.
Dátum:2009
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Peptides. - 30 : 9 (2009), p. 1643-1650. -
További szerzők:Schally, Andrew Victor Seitz, Stephan Szalontay Luca Rick Ferenc G. Szepesházi Károly Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus)
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
DOI
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5.

001-es BibID:BIBFORM055517
Első szerző:Ujhelyi Judit Ágnes (farmakológus)
Cím:Analgesic and anti-inflammatory effectiveness of sitagliptin and vildagliptin in mice / Judit Újhelyi, Zoltán Újhelyi, Andrea Szalai, János F. László, Mayella Cayasso, Miklós Vecsernyés, Róbert Pórszász
Dátum:2014
ISSN:0167-0115
Megjegyzések:To validate the potential anti-inflammatory and analgesic role of sita- and vildagliptin, five different experimental 22modelswere used inmice: i)mustard oil-induced ear edema, ii) neutrophil accumulation, iii)mechanical and iv) 23thermal touch sensitivity in complete Freund's adjuvant-induced arthritis and v) capsaicin-induced plasma 24extravasation in the urinary bladder. For the complete examination period in i) the dose of 10 mg sitagliptin as 25well as 1?10 mg vildagliptin was found to significantly decrease ear edema as compared to positive control 26(p b 0.05, n = 8/group). All doses of sitagliptin provided an anti-inflammatory effect p b 0.005 (n = 10/ 27group) in test ii) and an analgesic effect in iii) except 3 mg. Vildagliptin was similarly effective in test ii) 28(p b 0.005, n = 10/group) as sitagliptin, but it failed to affect mechanical touch sensitivity. Unlike mechanical 29touch sensitivity, both gliptins could beneficially act on the thermal threshold (p b 0.05, n = 10/group). And 30only in tests v) could both gliptins reverse inflammation. Further studies are needed to support the suggestion 31that the utilization of these beneficial effects of gliptins may be considered in the treatment of Type 2 diabetic 32patients.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Arthritis
Mechanical and thermal touch sensitivity
mice
Mustard oil
sitagliptin
vildagliptin
Megjelenés:Regulatory Peptides. - 194-195 (2014), p. 23-29. -
További szerzők:Ujhelyi Zoltán (1984-) (gyógyszerész) Szalai Andrea (1968-) (analitikus) László F. János (1956-) (fizikus) Cayasso, Mayella Vecsernyés Miklós (1959-) (gyógyszertechnológus, endokrinológus) Pórszász Róbert (1965-) (farmakológus, klinikai farmakológus)
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6.

001-es BibID:BIBFORM072409
Első szerző:Zarándi Márta
Cím:Synthesis and structure-activity studies on novel analogs of human growth hormone releasing hormone (GHRH) with enhanced inhibitory activities on tumor growth / Marta Zarandi, Renzhi Cai, Magdolna Kovacs, Petra Popovics, Luca Szalontay, Tengjiao Cui, Wei Sha, Miklos Jaszberenyi, Jozsef Varga, XianYang Zhang, Norman L. Block, Ferenc G. Rick, Gabor Halmos, Andrew V. Schally
Dátum:2017
ISSN:0196-9781
Megjegyzések:The syntheses and biological evaluations of new GHRH analogs of Miami (MIA) series with greatly increased anticancer activity are described. In the design and synthesis of these analogs, the following previous substitutions were conserved: D-Arg(2), Har(9), Abuls(15), and Nle(27). Most new analogs had Ala at position 8. Since replacements of both Lys(12) and Lys(21) with Orn increased resistance against enzymatic degradation, these modifications were kept. The substitutions of Arg at both positions 11 and 20 by His were also conserved. We kept D-Arg(28), Har(29) -NH2 at the C-terminus or inserted Agm or 12-amino dodecanoic acid amide at position 30. We incorporated pentafluoro-Phe (Fpa(s)), instead of Cpa, at position 6 and Tyr(Me) at position 10 and omega-amino acids at N-terminus of some analogs. These GHRH analogs were prepared by solid-phase methodology and purified by HPLC. The evaluation of the activity of the analogs on GH release was carried out in vitro on rat pituitaries and in vivo in male rats. Receptor binding affinities were measured in vitro by the competitive binding analysis. The inhibitory activity of the analogs on tumor proliferation in vitro was tested in several human cancer cell lines such as HEC-1A endometrial adenocarcinoma, HCT-15 colorectal adenocarcinoma, and LNCaP prostatic carcinoma. For in vivo tests, various cell lines including PC-3 prostate cancer, HEC-1A endometrial adenocarcinoma, HT diffuse mixed beta cell lymphoma, and ACHN renal cell carcinoma cell lines were xenografted into nude mice and treated subcutaneously with GHRH antagonists at doses of 1-5 mu g/day. Analogs MIA-602, MIA-604, MIA-610, and MIA-640 showed the highest binding affinities, 30, 58, 48, and 73 times higher respectively, than GHRH (1-29) NH2. Treatment of LNCaP and HCT-15 cells with 5 mu M MIA-602 or MIA-690 decreased proliferation by 40%-80%. In accord with previous tests in various human cancer lines, analog MIA-602 showed high inhibitory activity in vivo on growth of PC-3 prostate cancer, HT-mixed beta cell lymphoma, HEC-1A endometrial adenocarcinoma and ACHN renal cell carcinoma. Thus, GHRH analogs of the Miami series powerfully suppress tumor growth, but have only a weak endocrine GH inhibitory activity. The suppression of tumor growth could be induced in part by the downregulation of GHRH receptors levels. Published by Elsevier Inc.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Peptides. - 89 (2017), p. 60-70. -
További szerzők:Cai, Ren-Zhi Kovács Magdolna Popovics Petra Szalontay Luca Cui, Tengjiao Sha, Wei Jászberényi Miklós Varga József XianYang, Zhang Block, Norman L. Rick Ferenc G. Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus) Schally, Andrew Victor
Internet cím:DOI
Intézményi repozitóriumban (DEA) tárolt változat
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