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MedKoo product information:
RC3095
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MedKoo Code#: 202430
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Name:
RC3095
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CAS#:
138147-78-1
Synonym:
RC3095; RC-3095; L-Leucinamide,
(3R)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carbonyl-L-glutaminyl-L-tryptophyl-L-alanyl-L-valylglycyl-L-histidyl-L-leucyl-.psi.(CH2-NH)-;
L-Histidinamide,
N2-[(2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-3-yl)carbonyl]-L-glutaminyl-L-tryptophyl-L-alanyl-L-valylglycyl-N-[1-[[[1-(aminocarbonyl)-3-methylbutyl]amino]methyl]-3-methylbutyl]-,
[1(R),6[S-(R*,R*)]]-; 1H-Pyrido[3,4-b]indole;
(D-Tpi6, Leu13 Ψ(CH2-NH)-Leu14)bombesin
(6-14),
(3R)-2,3,4,9-Tetrahydro-1H-pyrido[3,4-b]indole-3-carbonyl-L-glutaminyl-L-tryptophyl-L-alanyl-L-valylglycyl-L-histidyl-L-leucyl-Ψ(CH2-NH)-L-Leucinamide
trifluoroacetate salt.
Amino acid sequences: (D-TPI6, LEU13
y(CH2-NH)-LEU14)BOMBESIN (6-14).
IUPAC/Chemical name:
(S)-N1-((2S,5S,8S,14S,17S,20S)-14-((1H-imidazol-5-yl)methyl)-20-carbamoyl-1-(1H-indol-3-yl)-17-isobutyl-8-isopropyl-5,22-dimethyl-3,6,9,12,15-pentaoxo-4,7,10,13,16,19-hexaazatricosan-2-yl)-2-((R)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxamido)pentanediamide
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Chemical structure: |
Theoretical analysis
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Chemical Formula: C56H79N15O9
Exact Mass: 1105.61852
Molecular Weight: 1106.32
m/z: 1105.61852 (100.0%), 1106.62187 (60.6%),
1107.62523 (18.0%), 1106.61555 (5.5%), 1108.62858 (3.5%),
1107.61891 (3.4%), 1107.62276 (1.8%), 1108.62612 (1.1%).
Elemental Analysis: C, 60.80; H, 7.20;
N, 18.99; O, 13.02
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Availability and price:
This agent is not in stock, which may be available through custom synthesis. To inquire quotation and lead time or to ask questions, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
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Quality control
data:
Product will be shipped with
supporting analytical data.
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Information about this agent
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RC-3095 is a potent BB2 (GRP-preferring) bombesin
receptor antagonist.
Current developer:
AEterna Zentaris Inc。
1: Petronilho F, de Souza B, Vuolo F, Benetton
CA, Streck EL, Roesler R, Schwartsmann G, Dal-Pizzol F. Protective
effect of gastrin-releasing peptide receptor antagonist in carrageenan-induced
pleural inflammation in rats. Inflamm Res. 2010 Apr 3. [Epub ahead of
print] PubMed PMID: 20364359.
2: Cassol OJ Jr, Rezin GT, Petronilho FC, Scaini G, Gonçalves CL,
Ferreira GK, Roesler R, Schwartsmann G, Dal-Pizzol F, Streck EL. Effects
of N-acetylcysteine/deferoxamine, taurine and RC-3095 on respiratory
chain complexes and creatine kinase activities in rat brain after
sepsis. Neurochem Res. 2010 Apr;35(4):515-21. PubMed PMID: 20238483.
3: Valvassori SS, Moretti M, Kauer-Sant'Anna M, Roesler R, Petronilho F,
Schwartsmann G, Kapczinski F, Dal-Pizzol F, Quevedo J. Effects of a
gastrin-releasing peptide receptor antagonist on D-amphetamine-induced
oxidative stress in the rat brain. J Neural Transm. 2010
Mar;117(3):309-16. Epub 2010 Feb 4. PubMed PMID: 20131069.
4: Sotomayor S, Muńoz-Moreno L, Carmena MJ, Schally AV, Sánchez-Chapado
M, Prieto JC, Bajo AM. Regulation of HER expression and transactivation
in human prostate cancer cells by a targeted cytotoxic bombesin analog
(AN-215) and a bombesin antagonist (RC-3095). Int J Cancer. 2010 Jan 22.
[Epub ahead of print] PubMed PMID: 20099275.
5: Cassol OJ Jr, Rezin GT, Petronilho FC, Scaini G, Gonçalves CL,
Ferreira GK, Roesler R, Schwartsmann G, Dal-Pizzol F, Streck EL. Effects
of N-Acetylcysteine/Deferoxamine, Taurine and RC-3095 on Respiratory
Chain Complexes and Creatine Kinase Activities in Rat Brain After
Sepsis. Neurochem Res. 2009 Nov 13. [Epub ahead of print] PubMed PMID:
19911272.
6: Damin DC, Santos FS, Heck R, Rosito MA, Meurer L, Kliemann LM,
Roesler R, Schwartsmann G. Effects of the Gastrin-Releasing Peptide
Antagonist RC-3095 in a Rat Model of Ulcerative Colitis. Dig Dis Sci.
2009 Nov 6. [Epub ahead of print] PubMed PMID: 19894117.
7: Schmidt AL, de Farias CB, Abujamra AL, Kapczinski F, Schwartsmann G,
Brunetto AL, Roesler R. BDNF and PDE4, but not the GRPR, regulate
viability of human medulloblastoma cells. J Mol Neurosci. 2010
Mar;40(3):303-10. Epub 2009 Jul 30. PubMed PMID: 19642024.
8: de Farias CB, Stertz L, Lima RC, Kapczinski F, Schwartsmann G,
Roesler R. Reduced NGF secretion by HT-29 human colon cancer cells
treated with a GRPR antagonist. Protein Pept Lett. 2009;16(6):650-2.
PubMed PMID: 19519524.
9: Pereira DV, Steckert AV, Mina F, Petronilho F, Roesler R,
Schwartsmann G, Ritter C, Dal-Pizzol F. Effects of an antagonist of the
gastrin-releasing peptide receptor in an animal model of uveitis. Invest
Ophthalmol Vis Sci. 2009 Nov;50(11):5300-3. Epub 2009 Jun 10. PubMed
PMID: 19516017.
10: Petronilho F, Araújo JH, Steckert AV, Rezin GT, Ferreira GK, Roesler
R, Schwartsmann G, Dal-Pizzol F, Streck EL. Effect of a gastrin-releasing
peptide receptor antagonist and a proton pump inhibitor association in
an animal model of gastritis. Peptides. 2009 Aug;30(8):1460-5. Epub 2009
Jun 6. PubMed PMID: 19505518.
11: González N, Mantey SA, Pradhan TK, Sancho V, Moody TW, Coy DH,
Jensen RT. Characterization of putative GRP- and NMB-receptor
antagonist's interaction with human receptors. Peptides. 2009
Aug;30(8):1473-86. Epub 2009 May 20. PubMed PMID: 19463875; PubMed
Central PMCID: PMC2766550.
12: Abujamra AL, Almeida VR, Brunetto AL, Schwartsmann G, Roesler R. A
gastrin-releasing peptide receptor antagonist stimulates Neuro2a
neuroblastoma cell growth: prevention by a histone deacetylase
inhibitor. Cell Biol Int. 2009 Aug;33(8):899-903. Epub 2009 May 6.
PubMed PMID: 19426821.
13: de Oliveira MS, Cechim G, Braganhol E, Santos DG, Meurer L, de
Castro CG Jr, Brunetto AL, Schwartsmann G, Battastini AM, Lenz G,
Roesler R. Anti-proliferative effect of the gastrin-release peptide
receptor antagonist RC-3095 plus temozolomide in experimental
glioblastoma models. J Neurooncol. 2009 Jun;93(2):191-201. Epub 2009 Jan
8. Erratum in: J Neurooncol. 2009 Jun;93(2):203. Schwarstmann, Gilberto
[corrected to Schwartsmann, Gilberto]. PubMed PMID: 19129973.
14: Damin DC, Santos FS, Heck R, Schwartsmann G. Gastrin-releasing
peptide receptor: a potential target in treatment of IBD? J Clin
Gastroenterol. 2009 Mar;43(3):288. PubMed PMID: 18838920.
15: Oliveira PG, Brenol CV, Edelweiss MI, Brenol JC, Petronilho F,
Roesler R, Dal-Pizzol F, Schwartsmann G, Xavier RM. Effects of an
antagonist of the bombesin/gastrin-releasing peptide receptor on
complete Freund's adjuvant-induced arthritis in rats. Peptides. 2008
Oct;29(10):1726-31. Epub 2008 Jun 12. PubMed PMID: 18590783.
16: Mountney C, Anisman H, Merali Z. Effects of gastrin-releasing
peptide agonist and antagonist administered to the basolateral nucleus
of the amygdala on conditioned fear in the rat. Psychopharmacology (Berl).
2008 Sep;200(1):51-8. Epub 2008 Jun 18. PubMed PMID: 18563394.
17: Sakamoto H, Matsuda K, Zuloaga DG, Hongu H, Wada E, Wada K, Jordan
CL, Breedlove SM, Kawata M. Sexually dimorphic gastrin releasing peptide
system in the spinal cord controls male reproductive functions. Nat
Neurosci. 2008 Jun;11(6):634-6. Epub 2008 May 18. PubMed PMID: 18488022.
18: Flores DG, de Farias CB, Leites J, de Oliveira MS, Lima RC,
Tamajusuku AS, Di Leone LP, Meurer L, Brunetto AL, Schwartsmann G, Lenz
G, Roesler R. Gastrin-releasing peptide receptors regulate proliferation
of C6 Glioma cells through a phosphatidylinositol 3-kinase-dependent
mechanism. Curr Neurovasc Res. 2008 May;5(2):99-105. PubMed PMID:
18473825.
19: Luft T, Amaral OB, Schwartsmann G, Roesler R. Transient disruption
of fear-related memory by post-retrieval inactivation of gastrin-releasing
peptide or N-methyl-D-aspartate receptors in the hippocampus. Curr
Neurovasc Res. 2008 Feb;5(1):21-7. PubMed PMID: 18289018.
20: Cornelio DB, Dal-Pizzol F, Roesler R, Schwartsmann G. Targeting the
bombesin/gastrin-releasing peptide receptor to treat sepsis. Recent Pat
Antiinfect Drug Discov. 2007 Nov;2(3):178-81. Review. PubMed PMID:
18221174.
21: Petronilho F, Roesler R, Schwartsmann G, Dal Pizzol F. Gastrin-releasing
peptide receptor as a molecular target for inflammatory diseases.
Inflamm Allergy Drug Targets. 2007 Dec;6(4):197-200. Review. PubMed
PMID: 18220954.
22: Kauer-Sant'Anna M, Andreazza AC, Valvassori SS, Martins MR, Barbosa
LM, Schwartsmann G, Roesler R, Quevedo J, Kapczinski F. A gastrin-releasing
peptide receptor antagonist blocks D-amphetamine-induced hyperlocomotion
and increases hippocampal NGF and BDNF levels in rats. Peptides. 2007
Jul;28(7):1447-52. Epub 2007 Jun 16. PubMed PMID: 17629354.
23: Preissler T, Luft T, Kapczinski F, Quevedo J, Schwartsmann G,
Roesler R. Basic fibroblast growth factor prevents the memory impairment
induced by gastrin-releasing peptide receptor antagonism in area CA1 of
the rat hippocampus. Neurochem Res. 2007 Aug;32(8):1381-6. Epub 2007 Apr
4. PubMed PMID: 17406984.
24: Kang J, Ishola TA, Baregamian N, Mourot JM, Rychahou PG, Evers BM,
Chung DH. Bombesin induces angiogenesis and neuroblastoma growth. Cancer
Lett. 2007 Aug 18;253(2):273-81. Epub 2007 Mar 26. PubMed PMID:
17383815; PubMed Central PMCID: PMC2709810.
25: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods
Find Exp Clin Pharmacol. 2007 Jan-Feb;29(1):53-71. PubMed PMID:
17344945.
26: Presti-Torres J, de Lima MN, Scalco FS, Caldana F, Garcia VA,
Guimarăes MR, Schwartsmann G, Roesler R, Schröder N. Impairments of
social behavior and memory after neonatal gastrin-releasing peptide
receptor blockade in rats: Implications for an animal model of
neurodevelopmental disorders. Neuropharmacology. 2007 Mar;52(3):724-32.
Epub 2006 Nov 13. PubMed PMID: 17097693.
27: Luft T, Flores DG, Vianna MR, Schwartsmann G, Roesler R, Izquierdo
I. A role for hippocampal gastrin-releasing peptide receptors in
extinction of aversive memory. Neuroreport. 2006 Jun 26;17(9):935-9.
PubMed PMID: 16738491.
28: Dantas Ados S, Luft T, Henriques JA, Schwartsmann G, Roesler R.
Opposite effects of low and high doses of the gastrin-releasing peptide
receptor antagonist RC-3095 on memory consolidation in the hippocampus:
possible involvement of the GABAergic system. Peptides. 2006
Sep;27(9):2307-12. Epub 2006 May 2. PubMed PMID: 16650508.
29: Schwartsmann G, DiLeone LP, Horowitz M, Schunemann D, Cancella A,
Pereira AS, Richter M, Souza F, da Rocha AB, Souza FH, Pohlmann P, De
Nucci G. A phase I trial of the bombesin/gastrin-releasing peptide
(BN/GRP) antagonist RC3095 in patients with advanced solid malignancies.
Invest New Drugs. 2006 Sep;24(5):403-12. PubMed PMID: 16505950.
30: Dal-Pizzol F, Di Leone LP, Ritter C, Martins MR, Reinke A, Pens
Gelain D, Zanotto-Filho A, de Souza LF, Andrades M, Barbeiro DF, Bernard
EA, Cammarota M, Bevilaqua LR, Soriano FG, Cláudio J, Moreira F, Roesler
R, Schwartsmann G. Gastrin-releasing peptide receptor antagonist effects
on an animal model of sepsis. Am J Respir Crit Care Med. 2006 Jan
1;173(1):84-90. Epub 2005 Sep 28. PubMed PMID: 16192447.
31: Martins MR, Reinke A, Valvassori SS, Machado RA, Quevedo J,
Schwartsmann G, Roesler R. Non-associative learning and anxiety in rats
treated with a single systemic administration of the gastrin-releasing
peptide receptor antagonist RC-3095. Peptides. 2005 Dec;26(12):2525-9.
Epub 2005 Jul 14. PubMed PMID: 16023260.
32: Stangelberger A, Schally AV, Letsch M, Szepeshazi K, Nagy A, Halmos
G, Kanashiro CA, Corey E, Vessella R. Targeted chemotherapy with
cytotoxic bombesin analogue AN-215 inhibits growth of experimental human
prostate cancers. Int J Cancer. 2006 Jan 1;118(1):222-9. PubMed PMID:
16003723.
33: Schwartsmann G, Di Leone LP, Dal Pizzol F, Roesler R. MAPK pathway
activation in colorectal cancer: a therapeutic opportunity for GRP
receptor antagonists. Lancet Oncol. 2005 Jul;6(7):444-5. PubMed PMID:
15992692.
34: Heuser M, Schlott T, Schally AV, Kahler E, Schliephake R, Laabs SO,
Hemmerlein B. Expression of gastrin releasing Peptide receptor in renal
cell carcinomas: a potential function for the regulation of
neoangiogenesis and microvascular perfusion. J Urol. 2005
Jun;173(6):2154-9. PubMed PMID: 15879878.
35: Venturella R, Lessa D, Luft T, Roozendaal B, Schwartsmann G, Roesler
R. Dexamethasone reverses the memory impairment induced by antagonism of
hippocampal gastrin-releasing peptide receptors. Peptides. 2005
May;26(5):821-5. Epub 2005 Jan 18. PubMed PMID: 15808912.
36: Engel JB, Keller G, Schally AV, Halmos G, Hammann B, Nagy A.
Effective inhibition of experimental human ovarian cancers with a
targeted cytotoxic bombesin analogue AN-215. Clin Cancer Res. 2005 Mar
15;11(6):2408-15. PubMed PMID: 15788692.
37: Pereira AS, DiLeone L, Souza FH, Lilla S, Richter M, Schwartsmann G,
De Nucci G. Quantification of the bombesin/gastrin releasing peptide
antagonist RC-3095 by liquid chromatography-tandem mass spectrometry. J
Chromatogr B Analyt Technol Biomed Life Sci. 2005 Feb 25;816(1-2):321-6.
PubMed PMID: 15664365.
38: Meller CA, Henriques JA, Schwartsmann G, Roesler R. The bombesin/gastrin
releasing peptide receptor antagonist RC-3095 blocks apomorphine but not
MK-801-induced stereotypy in mice. Peptides. 2004 Apr;25(4):585-8.
PubMed PMID: 15165713.
39: Roesler R, Lessa D, Venturella R, Vianna MR, Luft T, Henriques JA,
Izquierdo I, Schwartsmann G. Bombesin/gastrin-releasing peptide
receptors in the basolateral amygdala regulate memory consolidation. Eur
J Neurosci. 2004 Feb;19(4):1041-5. PubMed PMID: 15009151.
40: Roesler R, Kopschina MI, Rosa RM, Henriques JA, Souza DO,
Schwartsmann G. RC-3095, a bombesin/gastrin-releasing peptide receptor
antagonist, impairs aversive but not recognition memory in rats. Eur J
Pharmacol. 2004 Feb 13;486(1):35-41. PubMed PMID: 14751406.
41: Bajo AM, Schally AV, Groot K, Szepeshazi K. Bombesin antagonists
inhibit proangiogenic factors in human experimental breast cancers. Br J
Cancer. 2004 Jan 12;90(1):245-52. PubMed PMID: 14710236; PubMed Central
PMCID: PMC2395331.
42: Heuser M, Gralla O, Nustede R, Post S. [Significance of regulatory
peptide GRP for microcirculation of the small intestine after
ischemia/reperfusion]. Langenbecks Arch Chir Suppl Kongressbd. 1998;115(Suppl
I):105-7. German. PubMed PMID: 14518222.
43: Roesler R, Meller CA, Kopschina MI, Souza DO, Henriques JA,
Schwartsmann G. Intrahippocampal infusion of the bombesin/gastrin-releasing
peptide antagonist RC-3095 impairs inhibitory avoidance retention.
Peptides. 2003 Jul;24(7):1069-74. PubMed PMID: 14499286.
44: Bajo AM, Schally AV, Krupa M, Hebert F, Groot K, Szepeshazi K.
Bombesin antagonists inhibit growth of MDA-MB-435 estrogen-independent
breast cancers and decrease the expression of the ErbB-2/HER-2
oncoprotein and c-jun and c-fos oncogenes. Proc Natl Acad Sci U S A.
2002 Mar 19;99(6):3836-41. Epub 2002 Mar 12. PubMed PMID: 11891317;
PubMed Central PMCID: PMC122610.
45: Chatzistamou I, Schally AV, Szepeshazi K, Groot K, Hebert F,
Arencibia JM. Inhibition of growth of ES-2 human ovarian cancers by
bombesin antagonist RC-3095, and luteinizing hormone-releasing hormone
antagonist Cetrorelix. Cancer Lett. 2001 Sep 28;171(1):37-45. PubMed
PMID: 11485826.
46: Chatzistamou I, Schally AV, Sun B, Armatis P, Szepeshazi K.
Inhibition of growth of OV-1063 human epithelial ovarian cancers and c-
jun and c- fos oncogene expression by bombesin antagonists. Br J Cancer.
2000 Oct;83(7):906-13. PubMed PMID: 10970693; PubMed Central PMCID:
PMC2374679.
47: Heuser M, Pfaar O, Gralla O, Gröne HJ, Nustede R, Post S. Impact of
gastrin-releasing peptide on intestinal microcirculation after
ischemia-reperfusion in rats. Digestion. 2000;61(3):172-80. PubMed PMID:
10773722.
48: Kahán Z, Sun B, Schally AV, Arencibia JM, Cai RZ, Groot K, Halmos G.
Inhibition of growth of MDA-MB-468 estrogen-independent human breast
carcinoma by bombesin/gastrin-releasing peptide antagonists RC-3095 and
RC-3940-II. Cancer. 2000 Mar 15;88(6):1384-92. PubMed PMID: 10717621.
49: Kiaris H, Schally AV, Sun B, Armatis P, Groot K. Inhibition of
growth of human malignant glioblastoma in nude mice by antagonists of
bombesin/gastrin-releasing peptide. Oncogene. 1999 Nov
25;18(50):7168-73. PubMed PMID: 10597318.
50: Szepesházi K, Halmos G, Schally AV, Arencibia JM, Groot K,
Vadillo-Buenfil M, Rodriguez-Martin E. Growth inhibition of experimental
pancreatic cancers and sustained reduction in epidermal growth factor
receptors during therapy with hormonal peptide analogs. J Cancer Res
Clin Oncol. 1999 Aug-Sep;125(8-9):444-52. PubMed PMID: 10480336.
51: Alvaro-Alonso I, Muńoz-Acedo G, Rodríguez-Martín E, Schally AV,
Arilla E. Bombesin induces a reduction of somatostatin inhibition of
adenylyl cyclase activity, Gi function, and somatostatin receptors in
rat exocrine pancreas. Peptides. 1999;20(6):723-30. PubMed PMID:
10477127.
52: Koppán M, Halmos G, Arencibia JM, Lamharzi N, Schally AV. Bombesin/gastrin-releasing
peptide antagonists RC-3095 and RC-3940-II inhibit tumor growth and
decrease the levels and mRNA expression of epidermal growth factor
receptors in H-69 small cell lung carcinoma. Cancer. 1998 Oct
1;83(7):1335-43. PubMed PMID: 9762934.
53: Miyazaki M, Lamharzi N, Schally AV, Halmos G, Szepeshazi K, Groot K,
Cai RZ. Inhibition of growth of MDA-MB-231 human breast cancer
xenografts in nude mice by bombesin/gastrin-releasing peptide (GRP)
antagonists RC-3940-II and RC-3095. Eur J Cancer. 1998 Apr;34(5):710-7.
PubMed PMID: 9713279.
54: Szepeshazi K, Schally AV, Halmos G, Lamharzi N, Groot K, Horvath JE.
A single in vivo administration of bombesin antagonist RC-3095 reduces
the levels and mRNA expression of epidermal growth factor receptors in
MXT mouse mammary cancers. Proc Natl Acad Sci U S A. 1997 Sep
30;94(20):10913-8. PubMed PMID: 9380734; PubMed Central PMCID: PMC23529.
55: Halmos G, Schally AV. Reduction in receptors for bombesin and
epidermal growth factor in xenografts of human small-cell lung cancer
after treatment with bombesin antagonist RC-3095. Proc Natl Acad Sci U S
A. 1997 Feb 4;94(3):956-60. PubMed PMID: 9023364; PubMed Central PMCID:
PMC19621.
56: Konety BR, Getzenberg RH. Novel therapies for advanced prostate
cancer. Semin Urol Oncol. 1997 Feb;15(1):33-42. Review. PubMed PMID:
9050138.
57: Wang QJ, Knezetic JA, Schally AV, Pour PM, Adrian TE. Bombesin may
stimulate proliferation of human pancreatic cancer cells through an
autocrine pathway. Int J Cancer. 1996 Nov 15;68(4):528-34. PubMed PMID:
8945626.
58: Kozacko MF, Mang TS, Schally AV, Priore RL, Liebow C. Bombesin
antagonist prevents CO2 laser-induced promotion of oral cancer. Proc
Natl Acad Sci U S A. 1996 Apr 2;93(7):2953-7. PubMed PMID: 8610149;
PubMed Central PMCID: PMC39741.
59: Qin Y, Ertl T, Cai RZ, Horvŕth JE, Groot K, Schally AV. Antagonists
of bombesin/gastrin-releasing peptide inhibit growth of SW-1990 human
pancreatic adenocarcinoma and production of cyclic AMP. Int J Cancer.
1995 Oct 9;63(2):257-62. PubMed PMID: 7591214.
60: Groot K, Horvŕth JE, Cai RZ, Schally AV. Development of a
radioimmunoassay for a pseudononapeptide bombesin/GRP antagonist with
antitumor activity. Int J Pept Protein Res. 1995 Jun;45(6):561-6. PubMed
PMID: 7558587.
61: Pinski J, Schally AV, Halmos G, Szepeshazi K, Groot K. Somatostatin
analogues and bombesin/gastrin-releasing peptide antagonist RC-3095
inhibit the growth of human glioblastomas in vitro and in vivo. Cancer
Res. 1994 Nov 15;54(22):5895-901. PubMed PMID: 7954420.
62: Pinski J, Schally AV, Halmos G, Szepeshazi K, Groot K, O'Byrne K,
Cai RZ. Effects of somatostatin analogue RC-160 and bombesin/gastrin-releasing
peptide antagonists on the growth of human small-cell and non-small-cell
lung carcinomas in nude mice. Br J Cancer. 1994 Nov;70(5):886-92. PubMed
PMID: 7947094; PubMed Central PMCID: PMC2033546.
63: Szepshazi K, Halmos G, Groot K, Schally AV. Combination treatment of
nitrosamine-induced pancreatic cancers in hamsters with analogs of LH-RH
and a bombesin/GRP antagonist. Int J Pancreatol. 1994
Oct-Dec;16(2-3):141-9. PubMed PMID: 7868940.
64: Halmos G, Pinski J, Szoke B, Schally AV. Characterization of
bombesin/gastrin-releasing peptide receptors in membranes of MKN45 human
gastric cancer. Cancer Lett. 1994 Sep 30;85(1):111-8. PubMed PMID:
7923093.
65: Reile H, Armatis PE, Schally AV. Characterization of high-affinity
receptors for bombesin/gastrin releasing peptide on the human prostate
cancer cell lines PC-3 and DU-145: internalization of receptor bound
125I-(Tyr4) bombesin by tumor cells. Prostate. 1994 Jul;25(1):29-38.
PubMed PMID: 8022709.
66: Pinski J, Halmos G, Yano T, Szepeshazi K, Qin Y, Ertl T, Schally AV.
Inhibition of growth of MKN45 human gastric-carcinoma xenografts in nude
mice by treatment with bombesin/gastrin-releasing-peptide antagonist
(RC-3095) and somatostatin analogue RC-160. Int J Cancer. 1994 May
15;57(4):574-80. PubMed PMID: 7910153.
67: Liebow C, Crean DH, Lee MT, Kamer AR, Mang TS, Schally AV.
Synergistic effects of bombesin and epidermal growth factor on cancers.
Proc Natl Acad Sci U S A. 1994 Apr 26;91(9):3804-8. PubMed PMID:
8170991; PubMed Central PMCID: PMC43670.
68: Qin Y, Ertl T, Cai RZ, Halmos G, Schally AV. Inhibitory effect of
bombesin receptor antagonist RC-3095 on the growth of human pancreatic
cancer cells in vivo and in vitro. Cancer Res. 1994 Feb
15;54(4):1035-41. PubMed PMID: 8313359.
69: Yano T, Pinski J, Szepeshazi K, Halmos G, Radulovic S, Groot K,
Schally AV. Inhibitory effect of bombesin/gastrin-releasing peptide
antagonist RC-3095 and luteinizing hormone-releasing hormone antagonist
SB-75 on the growth of MCF-7 MIII human breast cancer xenografts in
athymic nude mice. Cancer. 1994 Feb 15;73(4):1229-38. PubMed PMID:
8313327.
70: Qin Y, Halmos G, Cai RZ, Szoke B, Ertl T, Schally AV. Bombesin
antagonists inhibit in vitro and in vivo growth of human gastric cancer
and binding of bombesin to its receptors. J Cancer Res Clin Oncol.
1994;120(9):519-28. PubMed PMID: 8045917.
71: Radulovic S, Schally AV, Reile H, Halmos G, Szepeshazi K, Groot K,
Milovanovic S, Miller G, Yano T. Inhibitory effects of antagonists of
bombesin/gastrin releasing peptide (GRP) and somatostatin analog
(RC-160) on growth of HT-29 human colon cancers in nude mice. Acta Oncol.
1994;33(6):693-701. PubMed PMID: 7946450.
72: Pinski J, Reile H, Halmos G, Groot K, Schally AV. Inhibitory effects
of somatostatin analogue RC-160 and bombesin/gastrin-releasing peptide
antagonist RC-3095 on the growth of the androgen-independent Dunning
R-3327-AT-1 rat prostate cancer. Cancer Res. 1994 Jan 1;54(1):169-74.
PubMed PMID: 7903203.
73: Shirahige Y, Cai RZ, Szepeshazi K, Halmos G, Pinski J, Groot K,
Schally AV. Inhibitory effect of bombesin/gastrin-releasing peptide
(GRP) antagonists RC-3950-II and RC-3095 on MCF-7 MIII human breast
cancer xenografts in nude mice. Biomed Pharmacother. 1994;48(10):465-72.
PubMed PMID: 7858155.
74: Pinski J, Schally AV, Halmos G, Szepeshazi K. Effect of somatostatin
analog RC-160 and bombesin/gastrin releasing peptide antagonist RC-3095
on growth of PC-3 human prostate-cancer xenografts in nude mice. Int J
Cancer. 1993 Dec 2;55(6):963-7. PubMed PMID: 7902829.
75: Pinski J, Halmos G, Szepeshazi K, Schally AV. Antagonists of
bombesin/gastrin-releasing peptides as adjuncts to agonists of
luteinizing hormone-releasing hormone in the treatment of experimental
prostate cancer. Cancer. 1993 Dec 1;72(11):3263-70. PubMed PMID:
8242552.
76: Crean DH, Liebow C, Penetrante RB, Mang TS. Evaluation of porfimer
sodium fluorescence for measuring tissue transformation. Cancer. 1993
Nov 15;72(10):3068-77. PubMed PMID: 8106141.
77: Pinski J, Halmos G, Schally AV. Somatostatin analog RC-160 and
bombesin/gastrin-releasing peptide antagonist RC-3095 inhibit the growth
of androgen-independent DU-145 human prostate cancer line in nude mice.
Cancer Lett. 1993 Jul 30;71(1-3):189-96. PubMed PMID: 8103419.
78: Szepeshazi K, Schally AV, Groot K, Halmos G. Effect of bombesin,
gastrin-releasing peptide (GRP)(14-27) and bombesin/GRP receptor
antagonist RC-3095 on growth of nitrosamine-induced pancreatic cancers
in hamsters. Int J Cancer. 1993 May 8;54(2):282-9. PubMed PMID: 8387464.
79: Konturek SJ, Tasler J, Bilski J, Cieszkowski M, Cai RZ, Schally AV.
Antagonism of receptors for gastrin, cholecystokinin and GRP/bombesin in
postprandial stimulation of exocrine pancreas in dogs. J Physiol
Pharmacol. 1993 Mar;44(1):43-53. PubMed PMID: 8390873.
80: Liebow C, Crean DH, Schally AV, Mang TS. Peptide analogues alter the
progression of premalignant lesions, as measured by Photofrin
fluorescence. Proc Natl Acad Sci U S A. 1993 Mar 1;90(5):1897-901.
PubMed PMID: 8095335; PubMed Central PMCID: PMC45987.
81: Radulovic S, Comaru-Schally AM, Milovanovic S, Schally AV.
Somatostatin analogue RC-160 and LH-RH antagonist SB-75 inhibit growth
of MIA PaCa-2 human pancreatic cancer xenografts in nude mice. Pancreas.
1993 Jan;8(1):88-97. PubMed PMID: 8093555.
82: Szepeshazi K, Schally AV, Halmos G, Groot K, Radulovic S. Growth
inhibition of estrogen-dependent and estrogen-independent MXT mammary
cancers in mice by the bombesin and gastrin-releasing peptide antagonist
RC-3095. J Natl Cancer Inst. 1992 Dec 16;84(24):1915-22. PubMed PMID:
1460673.
83: Pinski J, Yano T, Schally AV. Inhibitory effects of the new bombesin
receptor antagonist RC-3095 on the luteinizing hormone release in rats.
Neuroendocrinology. 1992 Dec;56(6):831-7. PubMed PMID: 1369591.
84: Pinski J, Yano T, Rekasi Z, Cai RZ, Radulovic S, Schally AV. High
potency of a new bombesin antagonist (RC-3095) in inhibiting serum
gastrin levels; comparison of different routes of administration. Regul
Pept. 1992 Oct 13;41(3):185-93. PubMed PMID: 1438988.
85: Pinski J, Yano T, Groot K, Cai RZ, Radulovic S, Schally AV.
Endocrine effects of new bombesin/gastrin-releasing peptide antagonists
in rats. Am J Physiol. 1992 Oct;263(4 Pt 1):E712-7. PubMed PMID:
1415689.
86: Yano T, Pinski J, Groot K, Schally AV. Stimulation by bombesin and
inhibition by bombesin/gastrin-releasing peptide antagonist RC-3095 of
growth of human breast cancer cell lines. Cancer Res. 1992 Aug
15;52(16):4545-7. PubMed PMID: 1643647.
87: Jaworek J, Konturek PK, Konturek SJ, Cai RZ, Schally AV. Actions of
novel bombesin receptor antagonists on pancreatic secretion in rats. Eur
J Pharmacol. 1992 Apr 22;214(2-3):239-45. PubMed PMID: 1381317.
88: Milovanovic SR, Radulovic S, Groot K, Schally AV. Inhibition of
growth of PC-82 human prostate cancer line xenografts in nude mice by
bombesin antagonist RC-3095 or combination of agonist
[D-Trp6]-luteinizing hormone-releasing hormone and somatostatin analog
RC-160. Prostate. 1992;20(4):269-80. PubMed PMID: 1376910.
89: Radulovic S, Cai RZ, Serfozo P, Groot K, Redding TW, Pinski J,
Schally AV. Biological effects and receptor binding affinities of new
pseudononapeptide bombesin/GRP receptor antagonists with N-terminal D-Trp
or D-Tpi. Int J Pept Protein Res. 1991 Dec;38(6):593-600. PubMed PMID:
1726427.
90: Radulovic S, Miller G, Schally AV. Inhibition of growth of HT-29
human colon cancer xenografts in nude mice by treatment with bombesin/gastrin
releasing peptide antagonist (RC-3095). Cancer Res. 1991 Nov
1;51(21):6006-9. PubMed PMID: 1682040.
91: Szepeshazi K, Schally AV, Cai RZ, Radulovic S, Milovanovic S, Szoke
B. Inhibitory effect of bombesin/gastrin-releasing peptide antagonist
RC-3095 and high dose of somatostatin analogue RC-160 on
nitrosamine-induced pancreatic cancers in hamsters. Cancer Res. 1991 Nov
1;51(21):5980-6. PubMed PMID: 1682039.
92: Dembiński A, Warzecha Z, Konturek SJ, Banas M, Cai RZ, Schally AV.
The effect of antagonist of receptors for gastrin, cholecystokinin and
bombesin on growth of gastroduodenal mucosa and pancreas. J Physiol
Pharmacol. 1991 Sep;42(3):263-77. PubMed PMID: 1665365.
93: Dembiński A, Warzecha Z, Konturek SJ, Cai RZ, Schally AV. The
effects of antagonists of receptors for gastrin, cholecystokinin and
bombesin on growth of gastroduodenal mucosa and pancreas. J Physiol
Pharmacol. 1991 Jun;42(2):195-209. PubMed PMID: 1664265.
94: Konturek SJ, Dembinski A, Warzecha Z, Jaworek J, Konturek PK, Cai
RZ, Schally AV. Antagonism of receptors for bombesin, gastrin and
cholecystokinin in pancreatic secretion and growth. Digestion.
1991;48(2):89-97. PubMed PMID: 1714408.
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