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1.

001-es BibID:BIBFORM033631
035-os BibID:WOS:000088208700022 PMID:10891548
Első szerző:Halmos Gábor (gyógyszerész, receptorfarmakológus, experimentális onkológus)
Cím:Down-regulation and change in subcellular distribution of receptors for luteinizing hormone-releasing hormone in OV-1063 human epithelial ovarian cancers during therapy with LH-RH antagonist Cetrorelix / Gábor Halmos, Andrew V. Schally, Zsuzsanna Kahan
Dátum:2000
Megjegyzések:The inhibition of growth of various hormone-dependent cancers by analogs of luteinizing hormone-releasing hormone (LH-RH) may be exerted in port through receptors for LH-RN present on tumor cells, but the direct mode of action of LH-RH agonists and antagonists is still not completely understood. The aim of this study was to investigate the effects of agonist [D-Trp(6)]LH-RH and antagonist Cetrorelix, administered s.c, at a dose of 100 mu g/day for 3 weeks on the binding characteristics and subcellular localization of receptors for LH-RH in OV-1063 human epithelial ovarian cancers xenografted into nude mice. Using radioligand binding studies, following in vitro desaturation, we demonstrated the presence of specific, high affinity binding sites for LH-RH in both cell membrane and nuclear fraction of OV-1063 tumors. Treatment with Cetrorelix, but not [D-Trp(6)]LH-RH, caused about 60% reduction (p<0.01) in tumor volume and weight. [D-Trp(6)]LH-RH decreased the number of LH-RN receptors on OV-1063 tumor membranes by 44% after 14 days (p<0.01), and the concentration of receptors remained at that level on day 21. The maximal binding capacity of receptors for LH-RH in the nuclei was significantly higher (p<0.05) after 3 weeks of treatment with [D-Trp(6)]LH-RH, Cetrorelix decreased the concentration of membrane receptors for LH-RH by 53% (p<0.01) after 14 days and the levels on day 21 were even lower, showing a 70% reduction (p<0.01). In contrast, the number of LH-RN binding sites in the nuclear pellet was significantly increased (p<0.01) by Cetrorelix at that time. Our results demonstrate for the first time that the down-regulation of LH-RN receptors on the cell membranes of OV-1063 human ovarian cancers after therapy with antagonist Cetrorelix or agonist [D-Trp(6)]LH-RH is associated with an increase in receptor concentration in the nuclei. These phenomena could be related to the internalization and subcellular translocation of receptors in these tumor cells.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
külföldön készült közlemény
Megjelenés:International Journal of Oncology. - 17 : 2 (2000), p. 367-373. -
További szerzők:Schally, Andrew Victor Kahán Zsuzsa
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2.

001-es BibID:BIBFORM033548
035-os BibID:WOS:000239132600020 PMID:16820890
Első szerző:Halmos Gábor (gyógyszerész, receptorfarmakológus, experimentális onkológus)
Cím:Characterization of receptors for growth hormone-releasing hormone in human osteosarcomas and Ewing's sarcomas / Gabor Halmos, Andrew V. Schally, Andrea L. F. Bernardino, Jozsef L. Varga
Dátum:2006
Megjegyzések:Antagonists of growth hormone-releasing hormone (GH-RH) inhibit growth of various human can s including osteosarcomas and Ewing's sarcomas, xenografted into nude mice or cultured in vitro. The antiproliferative effect of GH-RH antagonists could be mediated. in part. through the splice variants (SVs) of receptors for GH-RH which have been found in several human cancers and cancer cell lines. In this study we investigated the expression of SVs of GH-RH receptors and the binding, characteristics of these receptor isoforms in MNNG/HOS human osteosarcoma and SK-ES-1 human Ewing's sarcoma grown in nude mice. RT-PCR revealed the presence of mRNA for SVs of GH-RH receptors in both human malignant bone cancer models. Using ligand competition assays with I-125-labeled GH-RH antacyonist JV-1-42. we demonstrated in MNNG/HOS and SK-ES-I tumors the presence of specific high affinity binding sites for GH-RH (K-d=5.83 nM and K-d=2.76 nM) with a maximal binding capacity (B-max) of 552.1 fmol/mg protein and 371.9 fmol/mg protein, respectively. We also investigated the effect of GH-RH antagonist JV-1-38. administered s.c. at a dose of 20 mu g, twice daily for 4 weeks on the gene expression, affinity and concentration of receptors for GH-RH in MNNG/HOS human osteosarcomas xenografted into nude mice. Treatment with JV-1-38 did not affect the expression and binding characteristics of GH-RH receptors. High affinity binding of JV-1-38 to GH-RH receptors on MNNG/HOS tumors was characterized by an IC50 value of 1.04 nM. The presence of GH-RH receptors in human bone tumors provides a rationale for new approaches to the therapy of this malignancy based on GH-RH antagonists.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
egyetemen (Magyarországon) készült közlemény
Megjelenés:International journal of oncology 29 : 2 (2006), p. 463-469. -
További szerzők:Schally, Andrew Victor Bernardino, Andrea L. F. Varga József L.
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
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3.

001-es BibID:BIBFORM033812
035-os BibID:PMID:21533457 WOS:A1997WW11900001
Első szerző:Jungwirth, Andreas
Cím:Regression of rat Dunning R-3327-H prostate carcinoma by treatment with targeted cytotoxic analog of luteinizing hormone-releasing hormone AN-207 containing 2-pyrrolinodoxorubicin / Andreas Jungwirth, Andrew V. Schally, Attila Nagy, Jacek Pinski, Kate Groot, Georg Galvan, Karoly Szepeshazi, Gabor Halmos
Dátum:1997
Megjegyzések:The effects of AN-207, a new targeted cytotoxic analog of LH-RH, were evalued in rats bearing hormone-dependent Dunning R-3327-H prostate carcinomas. AN-207 consists of the agonist [D-Lys(6)]LH-RH linked to 2-pyrrolino-doxorubicin, an intensely potent derivative of doxorubicin. In the first experiment, 2-pyrrolinodoxorubicin was administered at a concentration of 50 nmol/kg, as a single drug (AN-201) and as an unconjugated mixture with [D-Lys(6)]LH-RH or conjugated to the carrier [D-Lys(6)]LH-RH (AN-207). Following the second administration of radical AN-201 alone or mixed with the carrier, all rats died with signs of general toxicity, but all animals treated with the conjugate AN-207, survived. After 5 weeks of treatment with a total dose of 150 nmol/kg AN-207, the tumors regressed from an initial volume of 8.35 +/- 1.7 cm(3) to 4.47 +/- 0.8 cm(3), while tumors in the control group measured 17.84 +/- 2.2 cm(3). The therapy with AN-207 also significantly reduced tumor weight and tumor burden. In the second experiment, we compared the efficacy and toxicity of 3 injections of 25 nmol/kg AN-201 or 25 nmol/kg and 50 nmol/kg AN-207. The initial tumor volume in all groups was between 3.9 and 4.5 cm(3). After 5 weeks of therapy, the tumors of rats treated with 50 nmol/kg AN-207 regressed to 2.3 +/- 0.51 cm(3), whereas 25 nmol/kg AN-201 was still toxic in contrast to 25 nmol/kg AN-207, while the reduction in final tumor volume was similar (6.76 +/- 1.4 cm(3) and 6.74 +/- 1 cm(3), respectively), as compared to 15.6 +/- 2.2 cm(3) for untreated animals. High capacity LH-RH receptors were found in the membranes of untreated Dunning tumor specimens, but after treatment with AN-207, they could no longer be detected. This is the first demonstration that the new targeted cytotoxic LH-RH analog AN-207 is an effective antitumor agent. Our work indicates that the cytotoxic analog AN-207 is much less toxic than the antineoplastic radical (AN-201) incorporated, and significantly more active in inhibiting tumor growth. Further development of approaches based on targeted cytotoxic analog AN-207 may lead to major improvements in current palliative therapy of prostate cancer.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
külföldön készült közlemény
Megjelenés:International journal of oncology. - 10 : 5 (1997), p. 877-884. -
További szerzők:Schally, Andrew Victor Nagy Attila Pinski, Jacek Groot, Kate Galvan, Georg Szepesházi Károly Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus)
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
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4.

001-es BibID:BIBFORM033713
Első szerző:Kanashiro, Celia A.
Cím:Inhibition of experimental U-118MG glioblastoma by targeted cytotoxic analogs of bombesin and somatostatin is associated with a suppression of angiogenic and antiapoptotic mechanisms / Celia A. Kanashiro, Andrew V. Schally, Attila Nagy, Gabor Halmos
Dátum:2005
Megjegyzések:Human gliomas express receptors for bombesin and somatostatin that can be used for targeted chemotherapy. In the present study, the efficacy and the mechanism of action of cytotoxic bombesin analog AN-215, and cytotoxic somatostatin analog AN-238 were investigated in U-118MG human glioblastomas xenografted into nude mice. The expression of vascular endothelial growth factor (VEGF) and the apoptotic markers Bcl-2 and Bax was analyzed by Western blotting. The toxicity was evaluated by measuring leukocyte levels and body weights. Treatment with AN-215 or AN-238 reduced tumor growth by approximately 50%, and diminished the levels of VEGF by 45 and 75%, respectively. The relative ratio of Bcl-2 to Bax proteins was decreased by approximately 90%, indicating a net apoptotic gain and efficacy of treatment. Specific receptors for bombesin and somatostatin were found in U-118MG tumors. Our results suggest that targeted cytotoxic analogs, AN-215 and AN-238, could be useful for the treatment of human glioblastomas.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
külföldön készült közlemény
Megjelenés:International Journal of Oncology. - 27 : 1 (2005), p. 169-174. -
További szerzők:Schally, Andrew Victor Nagy Attila Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus)
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
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5.

001-es BibID:BIBFORM033545
035-os BibID:WOS:000237824800020 PMID:16685451
Első szerző:Keller, Gunhild
Cím:Effective therapy of experimental human malignant melanomas with a targeted cytotoxic somatostatin analogue without induction of multi-drug resistance proteins / Gunhild Keller, Andrew V. Schally, Attila Nagy, Benjamin Baker, Gabor Halmos, Jorg B. Engel
Dátum:2006
Megjegyzések:Malignant melanomas are characterized by a high intrinsic resistance to chemotherapy. Multiple drug resistance (MDR) can be mediated by transport proteins such as MDR-1, multidrug resistance-associated protein (MRP) or lung resistance protein (LRP). The cytotoxic analogue of somatostatin AN-238 consisting of 2-pyrrolinodoxorubicin (AN-201) linked to a somatostatin analogue RC-121 binds to receptors for somatostatin and is targeted to tumors expressing these receptors. We evaluated the expression of somatostatin receptors on human malignant melanoma tumor lines MRI-H255 and MRI-H187 and examined the effects of the targeted analogue AN-238 and its cytotoxic radical AN-201 on growth of these tumors in nude mice. We also studied the effects of AN-238 and AN-201 on the expression of MDR-1, MRP-1 and LRP by real-time PCR. AN-238 inhibited the growth of MRI-H255 and MRI-H187 tumors while AN-201 was ineffective. Blockade of somatostatin receptors by somatostatin analogue RC-121 abolished the effects of AN-238. Targeted therapy with AN-238 did not produce an induction of mRNA of MDR-1, MRP-1 or LRP. Our findings show that targeted chemotherapy with cytotoxic somatostatin analogue AN-238 inhibits the growth of malignant melanomas. AN-238 could provide a novel treatment approach for advanced malignant melanomas.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
külföldön készült közlemény
Megjelenés:International journal of oncology. - 28 : 6 (2006), p. 1507-1513. -
További szerzők:Schally, Andrew Victor Nagy Attila Baker, Benjamin Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus) Engel, Jörg B.
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
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6.

001-es BibID:BIBFORM033754
035-os BibID:PMID:9683774 WOS:000075371900002
Első szerző:Lamharzi, Najib
Cím:Decrease in the level and mRNA expression of LH-RH and EGF receptors after treatment with LH-RH antagonist cetrorelix in DU-145 prostate tumor xenografts in nude mice / Najib Lamharzi, Gábor Halmos, Andreas Jungwirth, Andrew V. Schally
Dátum:1998
Megjegyzések:Using radioligand binding, RT-PCR, and Southern blot analyses, we evaluated whether agonist [D-Trp6]LH-RH and antagonist Cetrorelix could affect the levels of receptors for LH-RH and EGF and expression of mRNA for these receptors in DU-145 human androgen-independent prostate cancers xenografted into nude mice. Radioligand binding studies showed the presence of specific high affinity receptors for LH-RH and EGF in DU-145 prostate tumors. Cetrorelix, but not [D-Trp6]LH-RH significantly inhibited tumor growth. The concentration of LH-RH receptors was reduced by 22% (p<0. 05) and 67% (p<0.01) after 4 weeks of treatment with [D-Trp6]LH-RH and Cetrorelix respectively. The concentration of EGF receptors fell by 48% (p<0.05) in the [D-Trp6]LH-RH group, whereas Cetrorelix led to a 66% reduction (p<0.01). The expression of LH-RH and EGF receptor mRNA was investigated by RT-PCR analysis followed by Southern blotting. Densitometric analysis of the developed bands showed that the antagonist Cetrorelix decreased the expression of LH-RH receptor mRNA by 55% (p<0.01) compared to control group while the 20% reduction after treatment with the LH-RH agonist was non-significant. Treatment with [D-Trp6]LH-RH and Cetrorelix also reduced the expression of EGF receptor mRNA by 35% and 68% respectively (both, p<0.01) compared to control group. In conclusion, these data demonstrate that growth inhibition of DU-145 prostate tumors induced by prolonged administration of LH-RH antagonist Cetrorelix is accompanied by a marked decrease in the concentration of LH-RH and EGF receptors as well as in their mRNA levels.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
külföldön készült közlemény
Megjelenés:International journal of oncology. - 13 : 3 (1998), p. 429-435. -
További szerzők:Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus) Jungwirth, Andreas Schally, Andrew Victor
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
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7.

001-es BibID:BIBFORM033816
035-os BibID:PMID:21541617 WOS:A1996VU54900002
Első szerző:Pinski, Jacek
Cím:Inhibition of growth of human small cell and non-small cell lung carcinomas by antagonists of growth hormone-releasing hormone (GH-RH) / Jacek Pinski, Andrew V. Schally, Andreas Jungwirth, Kate Groot, Gábor Halmos, Patricia Armatis, Márta Zarandi, Manuel Vadillo-Buenfil
Dátum:1996
Megjegyzések:Insulin-like growth factors-I and-II (IGF-I and IGF-II) may be involved in the proliferation of human lung carcinomas. The purpose of this study was to investigate the effects of two potent antagonists of growth hormone-releasing hormone (GH-RH), MZ-4-71 and MZ-5-156 on the growth of the H69 human small cell lung cancer (SCLC) and H157 non-SCLC (NSCLC) lines transplanted into nude mice or cultured in vitro. Nude mice bearing H69 and H157 tumors were treated for 3-5 weeks with MZ-4-71 or MZ-5-156 injected s.c. twice a day at a dose of 20 mu g/animal. Growth of H69 and H157 tumors in nude mice was significantly inhibited by MZ-4-71 and MZ-5-156 as shown by a reduction in tumor volume and weight. In animals bearing H157 NSCLC, treatment with MZ-4-71 decreased IGF-I and IGF-II levels in tumor tissue. Levels of IGF-I, but not of IGF-II in serum and liver tissue of H157 tumor-bearing nude mice treated with MZ-4-71 were decreased. High affinity binding sites for ICF-I were demonstrated on membranes of H69 and H157 tumors. In cell cultures, the proliferation rate of H69 SCLC cells was suppressed by 10(-7)-10(-5) M MZ-4-71, but H157 NSCLC line was only inhibited by 10(-5) M antagonist. Our findings demonstrate that the GHRH antagonists MZ-4-71 and MZ-5-156 can inhibit the growth of SCLC and NSCLC. This new approach to the management of lung cancer merits further investigation.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
külföldön készült közlemény
Megjelenés:International journal of oncology. - 9 : 6 (1996), p. 1099-1105. -
További szerzők:Schally, Andrew Victor Jungwirth, Andreas Groot, Kate Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus) Armatis, Patricia Zarándi Márta Vadillo-Buenfil, Manuel
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
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8.

001-es BibID:BIBFORM033718
Első szerző:Plonowski, Artur
Cím:Effective treatment of experimental DU-145 prostate cancers with targeted cytotoxic somatostatin analog AN-238 / Artur Plonowski, Andrew V. Schally, Attila Nagy, Baodong Sun, Gabor Halmos
Dátum:2002
Megjegyzések:We evaluated the effectiveness of targeted cytotoxic analog of somatostatin (SST) AN-238, consisting of 2-pyrrolinodoxorubicin (AN-201) linked covalently to SST octapeptide carrier RC-121 in DU-145 human androgen-independent prostate cancers xenografted into nude mice. We also investigated the expression of mRNAs for SST receptor subtypes 2A and 5 (sst2A and sst5) in DU-145 tumors. After 8 weeks of treatment, AN-238 practically arrested the proliferation of DU-145 cancers. The tumor volume in nude mice that received 4 injections of AN-238 at the dose of 150 nmol/kg was 63.4+/-6.7 mm3, nearly 4 times smaller than that in controls which measured 249.1+/-36.3 mm3 (p<0.001). Treatment with AN-238 lowered tumor weight by 68% (p<0.01) compared with the control group and extended the tumor volume doubling time to 184.1+/-69.4 days, versus 32.1+/-6.6 days in controls (p<0.05). No toxicity-related deaths occurred during treatment with AN-238. Cytotoxic radical AN-201 administered alone or in an unconjugated mixture with carrier RC-121 inhibited the growth of DU-145 tumors only after the third and fourth injection and was toxic. The expression of mRNA for sst2A and sst5 was detected in all specimens of control DU-145 tumors and in tumors treated with AN-238. The present study demonstrates the high efficacy of SST-receptor-targeted chemotherapy in a model of human androgen-independent prostatic carcinoma.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
külföldön készült közlemény
Megjelenés:International Journal of Oncology. - 20 : 2 (2002), p. 397-402. -
További szerzők:Schally, Andrew Victor Nagy Attila Sun, Baodong Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus)
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
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9.

001-es BibID:BIBFORM011475
Első szerző:Rózsa Bernadett (molekuláris biológus)
Cím:Expression of mRNA for human type-I LHRH receptor transcript forms in human benign prostatic hyperplasia / Rózsa B., Juhász A., Treszl A., Tóth G., Flaskó T., Dezsö B., Block N. L., Schally A. V., Halmos G.
Dátum:2009
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:International Journal of Oncology. - 35 : 5 (2009), p. 1053-1059. -
További szerzők:Juhász Alíz (1977-) (molekuláris biológus) Treszl Andrea (1974-) (molekuláris biológus) Tóth György (1965-) (urológus) Flaskó Tibor (1960-) (urológus) Dezső Balázs (1951-) (pathológus) Block, Norman L. Schally, Andrew Victor Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus)
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
DOI
Borító:

10.

001-es BibID:BIBFORM033851
035-os BibID:PMID:21559676 WOS:A1994PL93100006
Első szerző:Shirahige, Yutaka
Cím:Treatment with luteinizing-hormone-releasing hormone antagonist sb-75 decreases levels of epidermal growth-factor receptor and its messenger-RNA in ov-1063 human epithelial ovarian-cancer xenografts in nude-mice / Yutaka Shirahige, Curtiss B. Cook, Jacek Pinski, Gabor Halmos, Radha Nair, Andrew V. Schally
Dátum:1994
Megjegyzések:The aim of this study was to investigate the effect of administration of LH-RH antagonist SB-75 and agonist [D-Trp(6)]LH-RH on receptors for epidermal growth factor (EGF) in OV-1063 human epithelial ovarian cancer. Female athymic nude mice bearing xenografts of OV-1063 human epithelial ovarian cancer were treated for 3 weeks with the modern LH-releasing hormone (LH-RH) antagonist [Ac-DNal(2)(1), D-Phe(4Cl)(2), D-Pal(3)(3), D-Cit(6), D-Ala(10)] LH-RH (SB-75, Cetrorelix), the agonist [D-Trp(6)]LH-RH, or bombesin/gastrin-releasing peptide antagonist RC-3095. SB-75 and [D-Trp(6)] LH-RH were injected s.c. at doses of 100 mu g/day, and RC-3095 was injected at a dose of 40 mu g/day. Tumor growth, as measured by percentage change in tumor volume, was significantly inhibited by the treatment with SB-75, but not by [D-Trp(6)] LH-RH or RC-3095. Treatment with SB-75 greatly decreased the levels of mRNA for EGF receptor and reduced the number of EGF binding sites on tumor membranes. Effects of SB-75 on EGF receptors might be related to inhibition of tumor growth. Our findings support the view that LH-RH antagonists such as SB-75 could be considered for possible hormonal therapy of epithelial ovarian cancer.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
külföldön készült közlemény
Megjelenés:International journal of oncology. - 5 : 5 (1994), p. 1031-1035. -
További szerzők:Cook, Curtiss B. Pinski, Jacek Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus) Nair, Radha Schally, Andrew Victor
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
Borító:

11.

001-es BibID:BIBFORM033825
035-os BibID:WOS:A1996VC50000002 PMID:21541526
Első szerző:Szepesházi Károly
Cím:Effects of new bombesin antagonists given singly or in combination with a somatostatin analog on nitrosamine-induced pancreatic cancers in hamsters / Károly Szepeshazi, Andrew V. Schally, Ren-Zhi Cai, Gábor Halmos, Kate Groot
Dátum:1996
Megjegyzések:In three experiments, hamsters with N-nitroso-bis(2-oxopropyl)amine-induced pancreatic cancers were treated for two months with bombesin/GRP antagonists RC-3095 [D-Tpi(6),Leu(13)psi(CH2NH)Leu(14)-bombesin(6-14)], RC-3910-II [D-Tpi(6),Leu(13)psi(CH2N)Tac(14)-bombesin(6-14)], RC-3940-II [Hca(6),Leu(13)psi(CH2N)Tac(14)-bombesin(6-14)], RC-3950-II [D-Phe(6),Leu(13)psi(CH2N)Tac(14)-bombesin(6-14)], somatostatin analog RC-160 (D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Trp-NH2), or the combination of RC-3095 with RC160. All peptides inhibited pancreatic cancers to various degrees, reducing the number of tumorous animals, lowering the weight of tumorous pancreata by 40-55% and decreasing AgNOR numbers which are indicators of cell proliferation rate. Combination therapy with RC-3095 and RC-160 did not inhibit tumors better than single peptides. Among new bombesin/GRP antagonists, RC-3940-II had the strongest inhibitory effect. RC-3950-II and RC-3095 caused similar inhibition, but RC-3910-II was less effective. Tumor inhibitory activity of the bombesin/GRP antagonists was correlated with their binding affinities to bombesin receptors on tumor cells. RC-3940-II caused 50% inhibition of specific binding of [I-125-Tyr(4)]bombesin to tumor cell membranes at 0.96 nM concentration, while the IC50 for RC-3950-II was 5.27 nM and 12.94 nM for RC-3095. Our findings suggest that in addition to RC-3095, other bombesin/GRP antagonists such as RC-3950-II and especially RC-3940-II could be further developed for therapy of human pancreatic cancer.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
külföldön készült közlemény
Megjelenés:International journal of oncology. - 9 : 3 (1996), p. 397-403. -
További szerzők:Schally, Andrew Victor Cai, Ren-Zhi Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus) Groot, Kate
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
Borító:

12.

001-es BibID:BIBFORM002246
Első szerző:Szepesházi Károly
Cím:LH-RH receptors in human colorectal cancers : unexpected molecular targets for experimental therapy / Szepeshazi K., Schally A. V., Halmos G.
Dátum:2007
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:International Journal of Oncology. - 30 : 6 (2007), p. 1485-1492. -
További szerzők:Schally, Andrew Victor Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus)
Internet cím:elektronikus változat
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