Evaluation of the anti-angiogenic properties of the new selective alphaVbeta3 integrin antagonist RGDechiHCit(511 views) Santulli G, Basilicata MF, De Simone M, Del Giudice C, Anastasio A, Sorriento D, Saviano M, Del Gatto A, Trimarco B, Pedone C, Zaccaro L, Iaccarino G
J Transl Med (ISSN: 1479-5876electronic), 2011 Jan 13; 9: 7-7.
Keywords: Arginylglycylaspartic Acid, Cilengitide, Echistatin, Vitronectin Receptor, Angiogenesis Inhibitor, Cyclopeptide, Animal Cell, Animal Experiment, Animal Model, Animal Tissue, Antiangiogenic Activity, C57bl 6 Mouse, Cell Proliferation, Controlled Study, Drug Effect, Endothelium Cell, In Vitro Study, In Vivo Study, Nonhuman, Signal Transduction, Smooth Muscle Fiber, Vascular Smooth Muscle, Wistar Kyoto Rat, Wound Healing Impairment, C57bl Mouse, Cell Culture, Drug Antagonism, Drug Screening, Enzyme Specificity, Neoplasm, Pathology, Physiology, Vascularization, Drug Evaluation, Preclinical, Endothelial Cells, Integrin Alphavbeta3, Mice, Inbred C57bl, Myocytes, Neovascularization, Inbred Wky, Substrate Specificity, Pharmacology, Therapeutic Use, Blood Supply, Drug Therapy,
Affiliations: *** IBB - CNR ***
Department of Clinical Medicine, Cardiovascular and Immunologic Sciences, Federico II University of Naples, Italy
Department of Biological Sciences, Federico II University of Naples, Italy
Institute of Crystallography (Consiglio Nazionale delle Ricerche CNR), Bari, Italy
Institute of Biostructures and Bioimaging (Consiglio Nazionale delle Ricerche CNR), Naples, Italy
References: Santulli, G., Ciccarelli, M., Palumbo, G., Campanile, A., Galasso, G., Ziaco, B., Altobelli, G.G., D'Andrea, L.D., In vivo properties of the proangiogenic peptide QK (2009) J Transl Med, 7, p. 41. , 10.1186/1479-5876-7-41, 2702279, 1950532
Bonauer, A., Carmona, G., Iwasaki, M., Mione, M., Koyanagi, M., Fischer, A., Burchfield, J., Ohtani, K., MicroRNA-92a controls angiogenesis and functional recovery of ischemic tissues in mice (2009) Science, 324, pp. 1710-1713. , 10.1126/science.1174381, 19460962
Desgrosellier, J.S., Cheresh, D.A., Integrins in cancer: biological implications and therapeutic opportunities (2010) Nat Rev Cancer, 10, pp. 9-22. , 10.1038/nrc2748, 20029421
Hood, J.D., Frausto, R., Kiosses, W.B., Schwartz, M.A., Cheresh, D.A., Differential alphav integrin-mediated Ras-ERK signaling during two pathways of angiogenesis (2003) J Cell Biol, 162, pp. 933-943. , 10.1083/jcb.200304105, 2172815, 12952943
Takahashi, S., Moser, M., Montanez, E., Nakano, T., Seo, M., Backert, S., Inoue, I., Fassler, R., The fibronectin RGD motif is required for multiple angiogenic events during early embryonic development (2010) Arterioscler Thromb Vasc Biol, 30, pp. e1. , 10.1161/ATVBAHA.108.181164, 19713531
Castel, S., Pagan, R., Garcia, R., Casaroli-Marano, R.P., Reina, M., Mitjans, F., Piulats, J., Vilaro, S., Alpha v integrin antagonists induce the disassembly of focal contacts in melanoma cells (2000) Eur J Cell Biol, 79, pp. 502-512. , 10.1078/0171-9335-00067, 10961450
Soldi, R., Mitola, S., Strasly, M., Defilippi, P., Tarone, G., Bussolino, F., Role of alphavbeta3 integrin in the activation of vascular endothelial growth factor receptor-2 (1999) Embo J, 18, pp. 882-892. , 10.1093/emboj/18.4.882, 1171181, 10022831
Lu, H., Murtagh, J., Schwartz, E.L., The microtubule binding drug laulimalide inhibits vascular endothelial growth factor-induced human endothelial cell migration and is synergistic when combined with docetaxel (taxotere) (2006) Mol Pharmacol, 69, pp. 1207-1215. , 10.1124/mol.105.019075, 1462867, 16415178
Bayless, K.J., Salazar, R., Davis, G.E., RGD-dependent vacuolation and lumen formation observed during endothelial cell morphogenesis in three-dimensional fibrin matrices involves the alpha(v)beta(3) and alpha(5)beta(1) integrins (2000) Am J Pathol, 156, pp. 1673-1683. , 1876924, 10793078
Brooks, P.C., Stromblad, S., Sanders, L.C., von Schalscha, T.L., Aimes, R.T., Stetler-Stevenson, W.G., Quigley, J.P., Cheresh, D.A., Localization of matrix metalloproteinase MMP-2 to the surface of invasive cells by interaction with integrin alpha v beta 3 (1996) Cell, 85, pp. 683-693. , 10.1016/S0092-8674(00)81235-0, 8646777
Abumiya, T., Lucero, J., Heo, J.H., Tagaya, M., Koziol, J.A., Copeland, B.R., del Zoppo, G.J., Activated microvessels express vascular endothelial growth factor and integrin alpha(v)beta3 during focal cerebral ischemia (1999) J Cereb Blood Flow Metab, 19, pp. 1038-1050. , 10.1097/00004647-199909000-00012, 10478656
Mahabeleshwar, G.H., Feng, W., Reddy, K., Plow, E.F., Byzova, T.V., Mechanisms of integrin-vascular endothelial growth factor receptor cross-activation in angiogenesis (2007) Circ Res, 101, pp. 570-580. , 10.1161/CIRCRESAHA.107.155655, 2723825, 17641225
Xiong, J.P., Stehle, T., Zhang, R., Joachimiak, A., Frech, M., Goodman, S.L., Arnaout, M.A., Crystal structure of the extracellular segment of integrin alpha Vbeta3 in complex with an Arg-Gly-Asp ligand (2002) Science, 296, pp. 151-155. , 10.1126/science.1069040, 11884718
Aumailley, M., Gurrath, M., Muller, G., Calvete, J., Timpl, R., Kessler, H., Arg-Gly-Asp constrained within cyclic pentapeptides. Strong and selective inhibitors of cell adhesion to vitronectin and laminin fragment P1 (1991) FEBS Lett, 291, pp. 50-54. , 10.1016/0014-5793(91)81101-D, 1718779
Schottelius, M., Laufer, B., Kessler, H., Wester, H.J., Ligands for mapping alphavbeta3-integrin expression in vivo (2009) Acc Chem Res, 42, pp. 969-980. , 10.1021/ar800243b, 19489579
Eliceiri, B.P., Klemke, R., Stromblad, S., Cheresh, D.A., Integrin alphavbeta3 requirement for sustained mitogen-activated protein kinase activity during angiogenesis (1998) J Cell Biol, 140, pp. 1255-1263. , 10.1083/jcb.140.5.1255, 2132684, 9490736
Eskens, F.A., Dumez, H., Hoekstra, R., Perschl, A., Brindley, C., Bottcher, S., Wynendaele, W., van Oosterom, A.T., Phase I and pharmacokinetic study of continuous twice weekly intravenous administration of Cilengitide (EMD 121974), a novel inhibitor of the integrins alphavbeta3 and alphavbeta5 in patients with advanced solid tumours (2003) Eur J Cancer, 39, pp. 917-926. , 10.1016/S0959-8049(03)00057-1, 12706360
Dechantsreiter, M.A., Planker, E., Matha, B., Lohof, E., Holzemann, G., Jonczyk, A., Goodman, S.L., Kessler, H., N-Methylated cyclic RGD peptides as highly active and selective alpha(V)beta(3) integrin antagonists (1999) J Med Chem, 42, pp. 3033-3040. , 10.1021/jm970832g, 10447947
Del Gatto, A., Zaccaro, L., Grieco, P., Novellino, E., Zannetti, A., Del Vecchio, S., Iommelli, F., Saviano, M., Novel and selective alpha(v)beta3 receptor peptide antagonist: design, synthesis, and biological behavior (2006) J Med Chem, 49, pp. 3416-3420. , 10.1021/jm060233m, 16722662
Ciccarelli, M., Cipolletta, E., Santulli, G., Campanile, A., Pumiglia, K., Cervero, P., Pastore, L., Iaccarino, G., Endothelial beta2 adrenergic signaling to AKT: role of Gi and SRC (2007) Cell Signal, 19, pp. 1949-1955. , 10.1016/j.cellsig.2007.05.007, 17629454
Iaccarino, G., Ciccarelli, M., Sorriento, D., Cipolletta, E., Cerullo, V., Iovino, G.L., Paudice, A., Campanile, A., AKT participates in endothelial dysfunction in hypertension (2004) Circulation, 109, pp. 2587-2593. , 10.1161/01.CIR.0000129768.35536.FA, 15136501
Illario, M., Cavallo, A.L., Monaco, S., Di Vito, E., Mueller, F., Marzano, L.A., Troncone, G., Vitale, M., Fibronectin-induced proliferation in thyroid cells is mediated by alphavbeta3 integrin through Ras/Raf-1/MEK/ERK and calcium/CaMKII signals (2005) J Clin Endocrinol Metab, 90, pp. 2865-2873. , 10.1210/jc.2004-1520, 15687337
Iaccarino, G., Smithwick, L.A., Lefkowitz, R.J., Koch, W.J., Targeting Gbeta gamma signaling in arterial vascular smooth muscle proliferation: a novel strategy to limit restenosis (1999) Proc Natl Acad Sci USA, 96, pp. 3945-3950. , 10.1073/pnas.96.7.3945, 22400, 10097143
Sorriento, D., Ciccarelli, M., Santulli, G., Campanile, A., Altobelli, G.G., Cimini, V., Galasso, G., Pastore, L., The G-protein-coupled receptor kinase 5 inhibits NFkappaB transcriptional activity by inducing nuclear accumulation of IkappaB alpha (2008) Proc Natl Acad Sci USA, 105, pp. 17818-17823. , 10.1073/pnas.0804446105, 2584738, 19008357
Sorriento, D., Santulli, G., Fusco, A., Anastasio, A., Trimarco, B., Iaccarino, G., Intracardiac Injection of AdGRK5-NT Reduces Left Ventricular Hypertrophy by Inhibiting NF-{kappa}B-Dependent Hypertrophic Gene Expression (2010) Hypertension, 56, pp. 696-704. , 10.1161/HYPERTENSIONAHA.110.155960, 20660817
Santulli, G., Illario, M., Palumbo, G., Sorriento, D., Cipolletta, E., Trimarco, V., Del Giudice, C., Iaccarino, G., CaMK4 partecipates in the settings of the hypertensive phenotype: a human genome wide analysis supported by animal model (2009) Eur Heart J, 30 (SUPPL.1), p. 161
Astrof, S., Hynes, R.O., Fibronectins in vascular morphogenesis (2009) Angiogenesis, 12, pp. 165-175. , 10.1007/s10456-009-9136-6, 2716138, 19219555
Zaccaro, L., Del Gatto, A., Pedone, C., Saviano, M., Peptides for tumour therapy and diagnosis: current status and future directions (2009) Curr Med Chem, 16, pp. 780-795. , 10.2174/092986709787549307, 19275595
Verbisck, N.V., Costa, E.T., Costa, F.F., Cavalher, F.P., Costa, M.D., Muras, A., Paixao, V.A., Ierardi, D.F., ADAM23 negatively modulates alpha(v)beta(3) integrin activation during metastasis (2009) Cancer Res, 69, pp. 5546-5552. , 10.1158/0008-5472.CAN-08-2976, 19549921
Laitinen, I., Saraste, A., Weidl, E., Poethko, T., Weber, A.W., Nekolla, S.G., Leppanen, P., Walch, A., Evaluation of alphavbeta3 integrin-targeted positron emission tomography tracer 18F-galacto-RGD for imaging of vascular inflammation in atherosclerotic mice (2009) Circ Cardiovasc Imaging, 2, pp. 331-338. , 10.1161/CIRCIMAGING.108.846865, 19808614
Furundzija, V., Fritzsche, J., Kaufmann, J., Meyborg, H., Fleck, E., Kappert, K., Stawowy, P., IGF-1 increases macrophage motility via PKC/p38-dependent alphavbeta3-integrin inside-out signaling (2010) Biochem Biophys Res Commun, 394, pp. 786-791. , 10.1016/j.bbrc.2010.03.072, 20230795
Vanderslice, P., Woodside, D.G., Integrin antagonists as therapeutics for inflammatory diseases (2006) Expert Opin Investig Drugs, 15, pp. 1235-1255. , 10.1517/13543784.15.10.1235, 16989599
Tani, N., Higashiyama, S., Kawaguchi, N., Madarame, J., Ota, I., Ito, Y., Ohoka, Y., Matsuura, N., Expression level of integrin alpha 5 on tumour cells affects the rate of metastasis to the kidney (2003) Br J Cancer, 88, pp. 327-333. , 10.1038/sj.bjc.6600710, 2377056, 12610521
Santulli, R.J., Kinney, W.A., Ghosh, S., Decorte, B.L., Liu, L., Tuman, R.W., Zhou, Z., Clermont, A.C., Studies with an orally bioavailable alpha V integrin antagonist in animal models of ocular vasculopathy: retinal neovascularization in mice and retinal vascular permeability in diabetic rats (2008) J Pharmacol Exp Ther, 324, pp. 894-901. , 10.1124/jpet.107.131656, 18083913
Desgrosellier, J. S., Cheresh, D. A., Integrins in cancer: biological implications and therapeutic opportunities (2010) Nat Rev Cancer, 10, pp. 9-22. , 10. 1038/nrc2748, 20029421
Hood, J. D., Frausto, R., Kiosses, W. B., Schwartz, M. A., Cheresh, D. A., Differential alphav integrin-mediated Ras-ERK signaling during two pathways of angiogenesis (2003) J Cell Biol, 162, pp. 933-943. , 10. 1083/jcb. 200304105, 2172815, 12952943
Bayless, K. J., Salazar, R., Davis, G. E., RGD-dependent vacuolation and lumen formation observed during endothelial cell morphogenesis in three-dimensional fibrin matrices involves the alpha (v) beta (3) and alpha (5) beta (1) integrins (2000) Am J Pathol, 156, pp. 1673-1683. , 1876924, 10793078
Brooks, P. C., Stromblad, S., Sanders, L. C., von Schalscha, T. L., Aimes, R. T., Stetler-Stevenson, W. G., Quigley, J. P., Cheresh, D. A., Localization of matrix metalloproteinase MMP-2 to the surface of invasive cells by interaction with integrin alpha v beta 3 (1996) Cell, 85, pp. 683-693. , 10. 1016/S0092-8674 (00) 81235-0, 8646777
Mahabeleshwar, G. H., Feng, W., Reddy, K., Plow, E. F., Byzova, T. V., Mechanisms of integrin-vascular endothelial growth factor receptor cross-activation in angiogenesis (2007) Circ Res, 101, pp. 570-580. , 10. 1161/CIRCRESAHA. 107. 155655, 2723825, 17641225
Xiong, J. P., Stehle, T., Zhang, R., Joachimiak, A., Frech, M., Goodman, S. L., Arnaout, M. A., Crystal structure of the extracellular segment of integrin alpha Vbeta3 in complex with an Arg-Gly-Asp ligand (2002) Science, 296, pp. 151-155. , 10. 1126/science. 1069040, 11884718
Eliceiri, B. P., Klemke, R., Stromblad, S., Cheresh, D. A., Integrin alphavbeta3 requirement for sustained mitogen-activated protein kinase activity during angiogenesis (1998) J Cell Biol, 140, pp. 1255-1263. , 10. 1083/jcb. 140. 5. 1255, 2132684, 9490736
Eskens, F. A., Dumez, H., Hoekstra, R., Perschl, A., Brindley, C., Bottcher, S., Wynendaele, W., van Oosterom, A. T., Phase I and pharmacokinetic study of continuous twice weekly intravenous administration of Cilengitide (EMD 121974), a novel inhibitor of the integrins alphavbeta3 and alphavbeta5 in patients with advanced solid tumours (2003) Eur J Cancer, 39, pp. 917-926. , 10. 1016/S0959-8049 (03) 00057-1, 12706360
Dechantsreiter, M. A., Planker, E., Matha, B., Lohof, E., Holzemann, G., Jonczyk, A., Goodman, S. L., Kessler, H., N-Methylated cyclic RGD peptides as highly active and selective alpha (V) beta (3) integrin antagonists (1999) J Med Chem, 42, pp. 3033-3040. , 10. 1021/jm970832g, 10447947
Verbisck, N. V., Costa, E. T., Costa, F. F., Cavalher, F. P., Costa, M. D., Muras, A., Paixao, V. A., Ierardi, D. F., ADAM23 negatively modulates alpha (v) beta (3) integrin activation during metastasis (2009) Cancer Res, 69, pp. 5546-5552. , 10. 1158/0008-5472. CAN-08-2976, 19549921
Crawford, T. N., Alfaro, D. V., Kerrison, J. B., Jablon, E. P., Diabetic retinopathy and angiogenesis (2009) Curr Diabetes Rev, 5, pp. 8-13. , 10. 2174/157339909787314149, 19199892
Santulli, R. J., Kinney, W. A., Ghosh, S., Decorte, B. L., Liu, L., Tuman, R. W., Zhou, Z., Clermont, A. C., Studies with an orally bioavailable alpha V integrin antagonist in animal models of ocular vasculopathy: retinal neovascularization in mice and retinal vascular permeability in diabetic rats (2008) J Pharmacol Exp Ther, 324, pp. 894-901. , 10. 1124/jpet. 107. 131656, 18083913
Evaluation of the anti-angiogenic properties of the new selective alphaVbeta3 integrin antagonist RGDechiHCit