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| integrin alphavbeta3SummarySummary: An integrin that binds to a variety of plasma and extracellular matrix proteins containing the conserved RGD amino acid sequence and modulates cell adhesion. Integrin alphavbeta3 is highly expressed in OSTEOCLASTS where it may play role in BONE RESORPTION. It is also abundant in vascular smooth muscle and endothelial cells, and in some tumor cells, where it is involved in angiogenesis and cell migration. Although often referred to as the vitronectin receptor there is more than one receptor for vitronectin (RECEPTORS, VITRONECTIN). Top Publications
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Publications
Biological and molecular properties of a new alpha(v)beta3/alpha(v)beta5 integrin antagonistLaura Belvisi
Organic and Industrial Chemistry Department, Centre for Biomolecular Interdisciplinary Studies and Industrial Applications, University of Milan, Italy
Mol Cancer Ther 4:1670-80. 2005..Taken together, these observations indicate that ST1646 represents a dual alpha(v)beta3/alpha(v)beta5 integrin antagonist with interesting biochemical and biological features to be tested in cancer therapy...
Expression of podocalyxin enhances the adherence, migration, and intercellular communication of cellsSusana Larrucea
Department of Physiopathology, Centro de Investigaciones Biologicas CSIC, Spain
Exp Cell Res 314:2004-15. 2008..To conclude, we present evidence indicating that human PODXL enhances the adherence of cells to immobilized ligands and to vascular endothelial cells through a mechanism(s) dependent on the activity of integrins...
Long exposure of non-cytotoxic concentrations of methylselenol suppresses the invasive potential of B16F10 melanomaAeyung Kim
Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon, Korea
Oncol Rep 20:557-65. 2008..5, 5 and 10 microM plus 0.02 U/ml METase, methioninase) induced a substantial decrease in the expression of integrin alphavbeta3, the FN receptor and adhesion ability to vitronectin (VN) and fibronectin (FN) in B16F10 melanoma cells...
Crystal structure of the complete integrin alphaVbeta3 ectodomain plus an alpha/beta transmembrane fragmentJian Ping Xiong
Program in Leukocyte Biology and Inflammation, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA
J Cell Biol 186:589-600. 2009....
Pegylated Arg-Gly-Asp peptide: 64Cu labeling and PET imaging of brain tumor alphavbeta3-integrin expressionXiaoyuan Chen
PET Imaging Science Center, Keck School of Medicine, University of Southern California, Los Angeles, California 90033, USA
J Nucl Med 45:1776-83. 2004..In addition, the same ligand labeled with therapeutic radionuclides may be applicable for integrin-targeted internal radiotherapy...
microPET imaging of glioma integrin {alpha}v{beta}3 expression using (64)Cu-labeled tetrameric RGD peptideYun Wu
Molecular Imaging Program at Stanford (MIPS, Department of Radiology and Bio-X Program, Stanford University, Stanford, California 94305, USA
J Nucl Med 46:1707-18. 2005..0164 mSv/MBq. CONCLUSION: The high integrin and avidity and favorable biokinetics make (64)Cu-DOTA-E{E[c(RGDfK)](2)}(2) a promising agent for peptide receptor radionuclide imaging and therapy of integrin-positive tumors...
Noninvasive visualization of the activated alphavbeta3 integrin in cancer patients by positron emission tomography and [18F]Galacto-RGDRoland Haubner
Nuklearmedizinische Klinik und Poliklinik, Technische Universitat Munchen, Germany
PLoS Med 2:e70. 2005The integrin alphavbeta3 plays an important role in angiogenesis and tumor cell metastasis, and is currently being evaluated as a target for new therapeutic approaches...
Integrin alphavbeta3 is a coreceptor for human cytomegalovirusXin Wang
Lineberger Comprehensive Cancer Center, CB 7295, Lineberger Building, School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, USA
Nat Med 11:515-21. 2005..Here we show that HCMV also uses integrin alphavbeta3 as a coreceptor...
Integrin activation dynamics between the RGD-binding site and the headpiece hingeEileen Puklin-Faucher
Department of Materials, Laboratory of Biologically Oriented Materials, ETH, Zurich CH 8049, Switzerland
J Biol Chem 284:36557-68. 2009..become strengthened under force), as well as earlier evidence that Ca(2+) at the ADMIDAS results in lower binding affinity, these simulations provide a common structural model for the dynamic process by which integrins become activated...
Cooperation between integrin alphavbeta3 and VEGFR2 in angiogenesisPayaningal R Somanath
Joseph J Jacobs Center for Thrombosis and Vascular Biology, Department of Molecular Cardiology, NB50, Lerner Research Institute, The Cleveland Clinic, 9500 Euclid Avenue, Cleveland, OH 44195, USA
Angiogenesis 12:177-85. 2009..On endothelial cells, an interaction between integrin alphavbeta3 and VEGFR2 seems to be particularly important process during vascularization...
(68)Ga-labeled cyclic RGD dimers with Gly3 and PEG4 linkers: promising agents for tumor integrin alphavbeta3 PET imagingZhaofei Liu
Department of Radiology, Biophysics and Bio X, Stanford University, Stanford, CA 94305, USA
Eur J Nucl Med Mol Imaging 36:947-57. 2009....
Integrin alphaVbeta3 contains a cell surface receptor site for thyroid hormone that is linked to activation of mitogen-activated protein kinase and induction of angiogenesisJoel J Bergh
Ordway Research Institute, 150 New Scotland Avenue, Albany, New York 12208, USA
Endocrinology 146:2864-71. 2005..These findings suggest that T(4) binds to alpha(V)beta(3) near the RGD recognition site and show that hormone-binding to alpha(V)beta(3) has physiological consequences...
Anti-angiogenic cancer therapy based on integrin alphavbeta3 antagonismWeibo Cai
Molecular Imaging Program at Stanford, Department of Radiology and Bio-X Program, Stanford University School of Medicine, Stanford, CA 94305-5484, USA
Anticancer Agents Med Chem 6:407-28. 2006..b>Integrin alphavbeta3 is highly expressed on activated endothelial cells and tumor cells but is not present in resting ..
In vivo near-infrared fluorescence imaging of integrin alphavbeta3 in brain tumor xenograftsXiaoyuan Chen
PET Imaging Science Center, University of Southern California Keck School of Medicine, Los Angeles, California, USA
Cancer Res 64:8009-14. 2004....
Synthesis, characterization, and biological evaluation of integrin alphavbeta3-targeted PAMAM dendrimersC Andrew Boswell
Radioimmune and Inorganic Chemistry Section, Radiation Oncology Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland 20892 1088, USA
Mol Pharm 5:527-39. 2008..30+/-0.03) at 2 h postinjection...
Biodistribution and pharmacokinetics of the alphavbeta3-selective tracer 18F-galacto-RGD in cancer patientsAmbros J Beer
Department of Nuclear Medicine, , Germany
J Nucl Med 46:1333-41. 2005..Consequently, this tracer offers a new strategy for noninvasive monitoring of molecular processes and may supply helpful information for planning and controlling of therapeutic approaches targeting the alpha(v)beta(3) integrin...
Multimodality imaging of tumor integrin alphavbeta3 expressionXiaoyuan Chen
Molecular Imaging Program at Stanford, MIPS, Department of Radiology, Stanford University, CA 94305, USA
Mini Rev Med Chem 6:227-34. 2006..This review highlights some recent advances in multimodality imaging of tumor integrin expression with emphasis on positron emission tomography (PET)...
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 tumoursF A L M Eskens
Erasmus Medical Center, Department of Medical Oncology, PO Box 2040, 3000 CA Rotterdam, The Netherlands
Eur J Cancer 39:917-26. 2003..Cilengitide can be safely administered using a continuous twice-weekly infusion regimen. As DLT was not reached, future trials should explore Cilengitide at different doses...
L-Thyroxine vs. 3,5,3'-triiodo-L-thyronine and cell proliferation: activation of mitogen-activated protein kinase and phosphatidylinositol 3-kinaseHung Yun Lin
Ordway Research Institute, Albany, NY 12208, USA
Am J Physiol Cell Physiol 296:C980-91. 2009..T(3) action here is inhibited by tetrac alone, but the effect of T(4) is blocked by both tetrac and the RGD peptide...
Near-infrared fluorescent RGD peptides for optical imaging of integrin alphavbeta3 expression in living miceZhen Cheng
Molecular Imaging Program at Stanford (MIPS, Department of Radiology and Bio-X Program, Stanford University, California 94305-5344, USA
Bioconjug Chem 16:1433-41. 2005..The multmerization of RGD peptide results in moderate improvement of imaging characteristics of the tetramer, compared to that of the monomer and dimeric counterparts...
Quantitative PET imaging of tumor integrin alphavbeta3 expression with 18F-FRGD2Xianzhong Zhang
Molecular Imaging Program at Stanford, MIPS, and Bio X Program, Department of Radiology, Stanford University, California 94305 5484, USA
J Nucl Med 47:113-21. 2006..We labeled the dimeric RGD peptide E[c(RGDyK)](2) with (18)F and evaluated its tumor-targeting efficacy and pharmacokinetics of (18)F-FB-E[c(RGDyK)](2) ((18)F-FRGD2)...
Plasminogen activator inhibitor-1 regulates integrin alphavbeta3 expression and autocrine transforming growth factor beta signalingBenjamin S Pedroja
Department of Ophthalmology, Mount Sinai School of Medicine, New York, New York 10029, USA
J Biol Chem 284:20708-17. 2009..PAI-1 induces the internalization of urokinase plasminogen activator/receptor and integrin alphavbeta3 from the cell surface...
Src phosphorylates Tyr284 in TGF-beta type II receptor and regulates TGF-beta stimulation of p38 MAPK during breast cancer cell proliferation and invasionAmy J Galliher
Department of Pharmacology, University of Colorado Health Sciences Center, 12801 East 17th Avenue, Aurora, CO 80045, USA
Cancer Res 67:3752-8. 2007....
Tumor targeting with radiolabeled alpha(v)beta(3) integrin binding peptides in a nude mouse modelMarcel L Janssen
Department of Nuclear Medicine, University Medical Center Nijmegen, The Netherlands
Cancer Res 62:6146-51. 2002..Injection of (90)Y-DOTA-E-[c(RGDfK)](2) induced a significant delay in tumor growth. Potentially, these peptides can be used for peptide receptor radionuclide imaging as well as therapy...
Improved targeting of the alpha(v)beta (3) integrin by multimerisation of RGD peptidesIngrid Dijkgraaf
Department of Nuclear Medicine, Radboud University Nijmegen Medical Centre, P O Box 9101, 6500 HB, Nijmegen, The Netherlands
Eur J Nucl Med Mol Imaging 34:267-73. 2007..In this study the alpha(v)beta(3) binding characteristics of an (111)In-labelled monomeric, dimeric and tetrameric RGD analogue were compared...
Acting via a cell surface receptor, thyroid hormone is a growth factor for glioma cellsFaith B Davis
Ordway Research Institute, Inc, Albany, NY 12208, USA
Cancer Res 66:7270-5. 2006..the thyroid hormone L-thyroxine (T4) stimulates growth of cancer cells via a plasma membrane receptor on integrin alphaVbeta3. The contribution of this recently described receptor for thyroid hormone and receptor-based stimulation of ..
Translational implications of nongenomic actions of thyroid hormone initiated at its integrin receptorPaul J Davis
Signal Transduction Laboratory, Ordway Research Institute, Albany, NY 12208, USA
Am J Physiol Endocrinol Metab 297:E1238-46. 2009A thyroid hormone receptor on integrin alphavbeta3 that mediates cell surface-initiated nongenomic actions of thyroid hormone on tumor cell proliferation and on angiogenesis has been described...
JWA regulates melanoma metastasis by integrin alphaVbeta3 signalingJ Bai
Department of Molecular Cell Biology and Toxicology, Cancer Center, School of Public Health, Nanjing Medical University, Nanjing, People s Republic of China
Oncogene 29:1227-37. 2010..These findings suggest that JWA suppresses melanoma metastasis and may serve a potential therapeutic target for human melanoma...
Click chemistry for (18)F-labeling of RGD peptides and microPET imaging of tumor integrin alphavbeta3 expressionZi Bo Li
The Molecular Imaging Program at Stanford MIPS, Department of Radiology and Bio X Program, Stanford University School of Medicine, Stanford, CA, USA
Bioconjug Chem 18:1987-94. 2007..This new (18)F labeling method based on click reaction may also be useful for radiolabeling of other biomolecules with azide groups in high yield...
Mechanisms of integrin-vascular endothelial growth factor receptor cross-activation in angiogenesisGanapati H Mahabeleshwar
Department of Molecular Cardiology, The Cleveland Clinic, 9500 Euclid Ave, Cleveland, OH 44195, USA
Circ Res 101:570-80. 2007....
Ultrasonic analysis of peptide- and antibody-targeted microbubble contrast agents for molecular imaging of alphavbeta3-expressing cellsPaul A Dayton
Department of Biomedical Engineering, UC Davis, CA 95616, USA
Mol Imaging 3:125-34. 2004....
Optical imaging of integrin alphavbeta3 expression with near-infrared fluorescent RGD dimer with tetra(ethylene glycol) linkersZhaofei Liu
Molecular Imaging Program at Stanford, Department of Radiology, Stanford University School of Medicine, Stanford, CA, USA
Mol Imaging 9:21-9. 2010b>Integrin alphavbeta3 plays great roles in tumor angiogenesis, invasion, and metastasis...
microPET of tumor integrin alphavbeta3 expression using 18F-labeled PEGylated tetrameric RGD peptide (18F-FPRGD4)Zhanhong Wu
The Molecular Imaging Program at Stanford MIPS, Department of Radiology and Bio X Program, Stanford University School of Medicine, 1201 Welch Road, Stanford, CA 94305, USA
J Nucl Med 48:1536-44. 2007..Here we report an example of (18)F-labeled tetrameric RGD peptide for PET of alpha(v)beta(3) expression in both xenograft and spontaneous tumor models...
Comparison of a monomeric and dimeric radiolabeled RGD-peptide for tumor targetingMarcel Janssen
Department of Nuclear Medicine and Obstetrics and Gynecology, University Medical Center Nijmegen, PO Box 9101, 6500 HB Nijmegen, The Netherlands
Cancer Biother Radiopharm 17:641-6. 2002..Furthermore, kidney retention of the dimeric peptide was higher than that of the monomeric peptide...
Improved tumor targeting of radiolabeled RGD peptides using rapid dose fractionationMarcel Janssen
Department of Nuclear Medicine, University Medical Center Nijmegen, The Netherlands
Cancer Biother Radiopharm 19:399-404. 2004..In conclusion, dose fractionation resulted in higher radiation doses. However, therapeutic efficacy of the radiolabeled peptide was not significantly improved by dose fractionation...
Micro-PET imaging of alphavbeta3-integrin expression with 18F-labeled dimeric RGD peptideXiaoyuan Chen
University of Southern California, Los Angeles, USA
Mol Imaging 3:96-104. 2004..5 +/- 0.8. The synergistic effect of polyvalency and improved pharmacokinetics may be responsible for the superior imaging characteristics of [18F]FB-E[c(RGDyK)]2...
Rigidity sensing at the leading edge through alphavbeta3 integrins and RPTPalphaGuoying Jiang
Department of Biological Sciences, Columbia University, New York, New York 11027, USA
Biophys J 90:1804-9. 2006..We suggest that RPTPalpha and alphavbeta3 at the leading edge are critical elements for sensing FN matrix rigidity possibly through SFK activation at the edge and downstream signaling...
Integrin alphaVbeta3 Binds to the RGD motif of glycoprotein B of Kaposi's sarcoma-associated herpesvirus and functions as an RGD-dependent entry receptorH Jacques Garrigues
Department of Pathobiology, Box 357238, University of Washington, Seattle, WA 98195, USA
J Virol 82:1570-80. 2008..Our studies demonstrate that alpha(V)beta(3) is a cellular receptor mediating both the cell adhesion and entry of KSHV into target cells through binding the virion-associated gB(RGD)...
Expression of integrin alphavbeta3 in gliomas correlates with tumor grade and is not restricted to tumor vasculatureOliver Schnell
Department of Neurosurgery, Klinikum Grosshadern, Ludwig Maximilians Universitat Munchen, Munich, Germany
Brain Pathol 18:378-86. 2008....
Imaging of integrin alphavbeta3 expressionAmbros J Beer
Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universitat Munchen, Munich, Germany
Cancer Metastasis Rev 27:631-44. 2008The integrin alphavbeta3 plays an important role in angiogenesis and tumor metastasis. It is expressed on activated endothelial cells as well as some tumor cells...
Activation of tumor cell integrin alphavbeta3 controls angiogenesis and metastatic growth in the brainMihaela Lorger
Department of Molecular and Experimental Medicine, The Scripps Research Institute, MEM 150, La Jolla, CA 92037, USA
Proc Natl Acad Sci U S A 106:10666-71. 2009..Targeting this molecular mechanism could prove valuable for the inhibition of brain metastasis...
Resveratrol is pro-apoptotic and thyroid hormone is anti-apoptotic in glioma cells: both actions are integrin and ERK mediatedHung Yun Lin
Signal Transduction Laboratory, Ordway Research Institute, 150 New Scotland Avenue, Albany, NY 12208, USA
Carcinogenesis 29:62-9. 2008The stilbene resveratrol (RV) initiates p53-dependent apoptosis via plasma membrane integrin alphaVbeta3 in human cancer cells. A thyroid hormone (L-thyroxine, T(4)) membrane receptor also exists on alphaVbeta3...
Alphavbeta3 and alphavbeta5 integrins control glioma cell response to ionising radiation through ILK and RhoBSylvie Monferran
Institut Claudius Regaud, INSERMU563, Department of Oncogenesis, Signalling and Therapeutic Innovation, France
Int J Cancer 123:357-64. 2008....
Stromal cell-derived factor-1 increase alphavbeta3 integrin expression and invasion in human chondrosarcoma cellsTzu Hsiu Lai
Graduate Institute of Basic Medical Science, China Medical University, Taichung, Taiwan
J Cell Physiol 218:334-42. 2009..Taken together, our results indicate that lung derived-SDF-1alpha enhances the invasiveness of chondrosarcoma cells by increasing alphavbeta3 integrin expression through the CXCR4/ERK/NF-kappaB signal transduction pathway...
Imaging tumor angiogenesis with contrast ultrasound and microbubbles targeted to alpha(v)beta3Dilantha B Ellegala
Department of Neurosurgery, University of Virginia School of Medicine, Charlottesville, USA
Circulation 108:336-41. 2003..This technique, when coupled with changes in blood volume and velocity, may provide insights into the biology of tumor angiogenesis and be used for diagnostic applications...
MR molecular imaging and fluorescence microscopy for identification of activated tumor endothelium using a bimodal lipidic nanoparticleWillem J M Mulder
Biomedical NMR, Department of Biomedical Engineering, Eindhoven University of Technology, MB Eindhoven, The Netherlands
FASEB J 19:2008-10. 2005....
Improving tumor-targeting capability and pharmacokinetics of (99m)Tc-labeled cyclic RGD dimers with PEG(4) linkersLijun Wang
School of Health Sciences, Purdue University, Indiana 47907, USA
Mol Pharm 6:231-45. 2009..Thus, (99m)Tc-3PEG(4)-dimer is a very promising radiotracer for the early detection of integrin alpha(v)beta(3)-positive tumors, and may have the potential for noninvasive monitoring of tumor growth or treatment efficacy...
Radiolabeled multimeric cyclic RGD peptides as integrin alphavbeta3 targeted radiotracers for tumor imagingShuang Liu
School of Health Sciences, Purdue University, Civil Engineering Building Room 1275, 550 Stadium Mall Drive, West Lafayette, Indiana 47907, USA
Mol Pharm 3:472-87. 2006b>Integrin alphavbeta3 plays a significant role in tumor angiogenesis and is a receptor for the extracellular matrix proteins with the exposed arginine-glycine-aspartic (RGD) tripeptide sequence...
Neuronal Thy-1 induces astrocyte adhesion by engaging syndecan-4 in a cooperative interaction with alphavbeta3 integrin that activates PKCalpha and RhoAAna Maria Avalos
Laboratory of Cellular Communication, University of Chile, Santiago 8380453, Chile
J Cell Sci 122:3462-71. 2009..These observations are likely to be of widespread biological relevance because Thy-1-integrin binding is reportedly relevant to melanoma invasion, monocyte transmigration through endothelial cells and host defense mechanisms...
Differential alphav integrin-mediated Ras-ERK signaling during two pathways of angiogenesisJohn D Hood
Department of Immunology, The Scripps Research Institute, La Jolla, CA 92037, USA
J Cell Biol 162:933-43. 2003..VEGF-mediated Ras and c-Raf activity on the chick chorioallantoic membrane, whereas blockade of FAK or integrin alphavbeta3 had no effect on bFGF-mediated Ras activity, but did suppress c-Raf activation...
Synthesis and biological evaluation of potent alphavbeta3-integrin receptor antagonistsIngrid Dijkgraaf
Department of Nuclear Medicine, Radboud University Nijmegen Medical Center, Nijmegen, The Netherlands
Nucl Med Biol 33:953-61. 2006..Due to the selective expression of alpha(v)beta(3) integrin in tumors, radiolabeled RGD peptides and peptidomimetics are attractive candidates for tumor targeting...
99mTc-labeled cyclic RGDfK dimer: initial evaluation for SPECT imaging of glioma integrin alphavbeta3 expressionBing Jia
Medical Isotopes Research Center, Peking University, Beijing 100083, China
Bioconjug Chem 17:1069-76. 2006..Among the three radiotracers evaluated in this study, [(99m)Tc(SQ168)(tricine)(TPPTS)] has the best imaging quality and is a promising candidate for more preclinical evaluations in the future...
Clustering of alpha(5)beta(1) integrins determines adhesion strength whereas alpha(v)beta(3) and talin enable mechanotransductionPere Roca-Cusachs
Department of Biological Sciences, Columbia University, 1212 Amsterdam Avenue, New York, NY 10027, USA
Proc Natl Acad Sci U S A 106:16245-50. 2009....
MicroPET imaging of integrin αvβ3 expressing tumors using 89Zr-RGD peptidesOrit Jacobson
Laboratory of Molecular Imaging and Nanomedicine LOMIN, National Institute of Biomedical Imaging and Bioengineering NIBIB, National Institutes of Health NIH, Bethesda, MD 20892, USA
Mol Imaging Biol 13:1224-33. 2011..4 h), using the chelator desferrioxamine-p-SCN (Df) for imaging tumor integrin α(v)β(3)...
Regulation of macrophage foam cell formation by alphaVbeta3 integrin: potential role in human atherosclerosisAlexander S Antonov
Department of Pathology, BF 231, Medical College of Georgia, 1120 15th Street, Augusta, GA 30912, USA
Am J Pathol 165:247-58. 2004..b>Integrin alphaVbeta3 plays a role in the differentiation of several cell types, but its involvement in the transition of ..
Absence of the alpha v beta 3 integrin dictates the time-course of angiogenesis in the hypoxic central nervous system: accelerated endothelial proliferation correlates with compensatory increases in alpha 5 beta 1 integrin expressionLongxuan Li
Department of Molecular and Experimental Medicine, The Scripps Research Institute, La Jolla, California 92037, USA
J Cereb Blood Flow Metab 30:1031-43. 2010....
Structural insights into how the MIDAS ion stabilizes integrin binding to an RGD peptide under forceDavid Craig
Center of Nanotechnology and Department of Bioengineering, University of Washington, Seattle, WA 98195, USA
Structure 12:2049-58. 2004..The functional role of single water molecules tightly coordinated to the MIDAS ion might reflect a general strategy for the stabilization of protein-protein adhesion against cell-derived forces through divalent cations...
Microvessel vascular smooth muscle cells contribute to collagen type I deposition through ERK1/2 MAP kinase, alphavbeta3-integrin, and TGF-beta1 in response to ANG II and high glucoseSouad Belmadani
Dept of Physiology, Hypertension and Renal Center of Excellence, Tulane Univ, School of Medicine, Health Sciences Center, New Orleans, Louisana, USA
Am J Physiol Heart Circ Physiol 295:H69-76. 2008..This pathway could be a potential target for overcoming small artery complications in diabetes and hypertension...
Pilot pharmacokinetic and dosimetric studies of (18)F-FPPRGD2: a PET radiopharmaceutical agent for imaging α(v)β(3) integrin levelsErik S Mittra
Molecular Imaging Program, Department of Radiology, Division of Nuclear Medicine, Stanford Hospital and Clinics, 300 Pasteur Dr, Room H2200, Stanford, CA 94305 5281, USA
Radiology 260:182-91. 2011....
Synthesis and biological evaluation of a (99m)Tc-labelled cyclic RGD peptide for imaging the alphavbeta3 expressionR Haubner
Nuklearmedizinische Klinik, Technische Universitat Munchen, Ismaningerstr 22, 81675 Munchen, Germany
Nuklearmedizin 43:26-32. 2004..The alphavbeta3 integrin is involved in tumour induced angiogenesis and tumour metastasis. We describe the synthesis and evaluation of a (99m)Tc-labelled RGD analogue for the visualisation of alphavbeta3 integrin expression...
Evaluation of copper-64 labeled AmBaSar conjugated cyclic RGD peptide for improved microPET imaging of integrin alphavbeta3 expressionHancheng Cai
Molecular Imaging Center, Keck School of Medicine, University of Southern California, Los Angeles, CA 90033, USA
Bioconjug Chem 21:1417-24. 2010..The AmBaSar chelator will also have general applications for (64)Cu labeling of various bioactive molecules in high radiochemical yield and high in vivo stability...
Direct electrophilic radiofluorination of a cyclic RGD peptide for in vivo alpha(v)beta3 integrin related tumor imagingMikako Ogawa
Department of Biofunctional Research, National Institute for Longevity Sciences, Gengo, Morioka-cho, Obu 474-8522, Japan
Nucl Med Biol 30:1-9. 2003..In tumor-bearing mice, the labeled peptides accumulated at the tumor with a high tumor to blood ratio. These findings suggest that an assessment of tumor characteristics may be obtained by using these (18)F-labeled peptides...
Derivation of a compartmental model for quantifying 64Cu-DOTA-RGD kinetics in tumor-bearing miceGregory Z Ferl
Department of Molecular and Medical Pharmacology, David Geffen School of Medicine at UCLA, University of California, Los Angeles, California 90095 6948, USA
J Nucl Med 50:250-8. 2009..To better understand the PET signal obtained with radiolabeled RGD peptides, we have constructed a compartmental model that can describe the time-activity curves in tumors after an intravenous injection...
Role of the integrin alphaVbeta3 in mediating increased smooth muscle cell responsiveness to IGF-I in response to hyperglycemic stressDavid R Clemmons
Department of Medicine, Division of Endocrinology, University of North Carolina at Chapel Hill, School of Medicine, Chapel Hill, NC 27599, USA
Growth Horm IGF Res 17:265-70. 2007..SMC secrete increased concentrations of thrombospondin, vitronectin and osteopontin, ligands for the integrin alphaVbeta3. Activation of alphaVbeta3 stimulates recruitment of a tyrosine phosphatase, SHP-2...
Identification and functions of the plasma membrane receptor for thyroid hormone analoguesHung Yun Lin
Signal Transduction Laboratory, Ordway Research Institute, Albany, New York 12208, USA
Discov Med 11:337-47. 2011..Thus, the receptor described on integrin αvβ3 for T(4) and T(3), the function of which is materially affected by tetrac and nanotetrac, provides insight into tumor cell biology and vascular biology...
The microtubule binding drug laulimalide inhibits vascular endothelial growth factor-induced human endothelial cell migration and is synergistic when combined with docetaxel (taxotere)Haiyan Lu
Department of Oncology, Albert Einstein College of Medicine, Montefiore Medical Center, 111 East 210th Street, Bronx, NY 10467, USA
Mol Pharmacol 69:1207-15. 2006..These complementary actions could account for their synergistic effects on HUVEC...
Integrin alphavbeta3, requirement for VEGFR2-mediated activation of SAPK2/p38 and for Hsp90-dependent phosphorylation of focal adhesion kinase in endothelial cells activated by VEGFBénédicte Masson-Gadais
Centre de recherche en cancérologie de l Université Laval, L Hôtel Dieu de Québec, 9 rue McMahon, Quebec, G1R 2J6, Canada
Cell Stress Chaperones 8:37-52. 2003..We conclude that a necessary cross talk should occur between VEGFR2 and the integrin alphavbeta3, to transduce the VEGF signals to SAPK2/p38 and FAK and that Hsp90 is instrumental in the building up of ..
PKD1/PKCmu promotes alphavbeta3 integrin recycling and delivery to nascent focal adhesionsAlison J Woods
Department of Biochemistry, University of Leicester, Leicester, UK
EMBO J 23:2531-43. 2004..These data indicate that PKD1 influences cell migration by directing vesicular transport of the alphavbeta3 integrin heterodimer...
Improving tumor uptake and excretion kinetics of 99mTc-labeled cyclic arginine-glycine-aspartic (RGD) dimers with triglycine linkersJiyun Shi
School of Health Sciences, Purdue University, 550 Stadium Mall Drive, Indiana 47907, USA
J Med Chem 51:7980-90. 2008..Complex 8 is a very promising radiotracer for the early detection of integrin alpha(v)beta(3)-positive tumors and may have the potential for noninvasive monitoring of tumor growth or shrinkage during antiangiogenic treatment...
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosisJohn H Hutchinson
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
J Med Chem 46:4790-8. 2003..These products proved useful in the identification of active metabolites generated by either in vitro or in vivo metabolism...
Extracellular matrix-bound vascular endothelial growth factor promotes endothelial cell adhesion, migration, and survival through integrin ligationHelen Hutchings
GDR CNRS 1927-Angiogenese and UMR CNRS 5089, Institut de Pharmacologie et Biologie Structurale, Toulouse, France
FASEB J 17:1520-2. 2003..We have thus determined a new VEGF receptor-independent role for immobilized VEGF in supporting cell adhesion and survival through interactions with integrins...
A novel adaptation of the integrin PSI domain revealed from its crystal structureJian Ping Xiong
Structural Biology Program, Leukocyte Biology and Inflammation Program, Renal Unit
J Biol Chem 279:40252-4. 2004..This architecture may be relevant to the evolution of integrins and should help refine the current models of integrin activation...
Integrin receptor imaging of breast cancer: a proof-of-concept study to evaluate 99mTc-NC100692Tore Bach-Gansmo
Rikshospitalet Radiumhospitalet Medical Center, Oslo, Norway
J Nucl Med 47:1434-9. 2006..The agent is a small peptide with high affinity for integrin receptors that are upregulated and expressed preferentially on proliferating endothelial cells...
Specific targeting of tumor angiogenesis by RGD-conjugated ultrasmall superparamagnetic iron oxide particles using a clinical 1.5-T magnetic resonance scannerChunfu Zhang
Junior Group Molecular Imaging, German Cancer Research Center, Im Neuenheimer Feld 280, 69120 Heidelberg, Germany
Cancer Res 67:1555-62. 2007..Furthermore, these molecular MR imaging probes are capable of distinguishing tumors differing in the degree of alpha(v)beta(3) integrin expression and in their angiogenesis profile even when using a clinical 1.5-T MR scanner...
ADAM23 negatively modulates alpha(v)beta(3) integrin activation during metastasisNewton V Verbisck
Laboratory of Molecular Biology and Genomics, Ludwig Institute for Cancer Research, Sao Paulo SP, Brazil
Cancer Res 69:5546-52. 2009..Our results strongly support a functional role of ADAM23 during metastatic progression by negatively modulating alpha(v)beta(3) integrin activation...
Integrin alpha v beta 3 antagonist Cilengitide enhances efficacy of radiotherapy in endothelial cell and non-small-cell lung cancer modelsJeffrey M Albert
Department of Radiation Oncology, Vanderbilt Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, TN, USA
Int J Radiat Oncol Biol Phys 65:1536-43. 2006....
A novel alpha(v)beta (3)-blocking disintegrin containing the RGD motive, DisBa-01, inhibits bFGF-induced angiogenesis and melanoma metastasisOscar H P Ramos
Dep Ciências Fisiológicas, Universidade Federal de Sao Carlos, Sao Carlos, SP, Brasil
Clin Exp Metastasis 25:53-64. 2008..We conclude that DisBa-01 is a potent new inhibitor of alpha(v)beta(3)-dependent adherence mechanisms involved in neo-vascularization and tumor metastasis processes...
Key interactions in integrin ectodomain responsible for global conformational change detected by elastic network normal-mode analysisAtsushi Matsumoto
Quantum Bioinformatics Team, Center for Computational Science and Engineering, Japan Atomic Energy Agency, 8 1 Umemidai, Kizugawa, Kyoto 619 0215, Japan
Biophys J 95:2895-908. 2008..This conservation pattern suggests that the molecular mechanism of the conformational change relying on the interactions found in integrin alpha(V)beta(3) is unique to the limited types of integrins...
[Expression of integrin alphavbeta3, tissue factor, and vascular endothelial growth factor in experimental choroidal neovascularization]Renhong Tang
Department of Ophthalmology, Third Xiangya Hospital, Central South University, Changsha 410013, China
Zhong Nan Da Xue Xue Bao Yi Xue Ban 34:762-7. 2009To study the expression of vascular endothelial growth factor (VEGF), integrin alphavbeta3, and tissue factor (TF) in choroidal neovascularization (CNV).
IGF-1 increases macrophage motility via PKC/p38-dependent alphavbeta3-integrin inside-out signalingVesna Furundzija
Department of Medicine Cardiology, Deutsches Herzzentrum Berlin, Augustenburger Platz 1, D 13353 Berlin, Germany
Biochem Biophys Res Commun 394:786-91. 2010..The aim of this study was to investigate the impact of IGF-1 on macrophage migration, its signaling pathways and the involvement of integrins and/or matrix metalloproteinases (MMPs)...
Role of integrin alphavbeta3 in substrate-dependent apoptosis of human intestinal carcinoma cellsG E Morozevich
Institute of Biomedical Chemistry, Russian Academy of Medical Sciences, Moscow, 119992, Russia
Biochemistry (Mosc) 68:416-23. 2003..Caco-2 cell population, the anoikis-negative cells demonstrated markedly decreased levels of expression of integrin alphavbeta3 on the cell surface and of transcription of the alphav subunit gene...
Discrete functional motifs reside within the cytoplasmic tail of alphaV integrin subunitThomas A Haas
Department of Anatomy and Cell Biology and Molecular Design Research Group, College of Medicine, University of Saskatchewan, Saskatoon, Canada
Thromb Haemost 99:96-107. 2008....
Radiotracer-based strategies to image angiogenesisR H Haubner
Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universitat Munchen, Munich, Germany
Q J Nucl Med 47:189-99. 2003..Nevertheless, translation of these approaches into clinical settings allowing visualisation of tumour-induced angiogenesis in patients needs still to be demonstrated...
Anti-angiogenic effects of non-peptide integrin alphavbeta3 specific antagonist on laser-induced choroidal neovascularization in miceShigeru Honda
Department of Surgery, Division of Ophthalmology, Kobe University Graduate School of Medicine, Chuo Ku, Kobe 650 0017, Japan
Graefes Arch Clin Exp Ophthalmol 247:515-22. 2009To evaluate the anti-angiogenic effects of integrin alphavbeta3 specific antagonist BS-1417 on laser-induced choroidal neovascularization (CNV) in mice.
The direct binding of insulin-like growth factor-1 (IGF-1) to integrin alphavbeta3 is involved in IGF-1 signalingJun Saegusa
Department of Dermatology, University of California Davis School of Medicine, Sacramento, CA 95817, USA
J Biol Chem 284:24106-14. 2009It has been proposed that ligand occupancy of integrin alphavbeta3 with extracellular matrix ligands (e.g. vitronectin) plays a critical role in insulin-like growth factor-1 (IGF-1) signaling...
Simultaneous integrin alphavbeta3 and glycoprotein IIb/IIIa inhibition causes reduction in infarct size in a model of acute coronary thrombosis and primary angioplastyTadamichi Sakuma
Cardiovascular Division, Medical Center, University of Virginia, Charlottesville, 22908-0158, USA
Cardiovasc Res 66:552-61. 2005..These results may have important implications in the treatment of acute coronary syndromes...
A bidirectional "alpha(v)beta(3) integrin-ERK1/ERK2 MAPK" connection regulates the proliferation of breast cancer cellsLuciano Vellon
Department of Medicine, Breast Cancer Translational Research Laboratory, Evanston Northwestern Healthcare Research Institute, Evanston, Illinois 60201, USA
Mol Carcinog 45:795-804. 2006..Collectively, these results strongly suggest the existence of a bidirectional molecular connection alpha(v)beta(3)-ERK1/ERK2 MAPK that would regulate breast cancer cells survival and proliferation...
Zoledronate inhibits alphavbeta3 and alphavbeta5 integrin cell surface expression in endothelial cellsA Bellahcene
Metastasis Research Laboratory, Center of Experimental Cancer Research, University of Liege, 4000 Liege, Belgium
Endothelium 14:123-30. 2007..This effect is likely to contribute to the previously demonstrated antiangiogenic effect of zoledronate. Whether this mechanism of action also applies to metastatic tumor cells is under investigation...
Engineering conditionally replication-competent adenoviral vectors carrying the cytosine deaminase gene increases the infectivity and therapeutic effect for breast cancer gene therapyY Liu
Sidney Kimmel Cancer Center, San Diego, CA 92121, USA
Cancer Gene Ther 13:346-56. 2006....
The lipoxygenase inhibitor, baicalein, modulates cell adhesion and migration by up-regulation of integrins and vinculin in rat heart endothelial cellsY C S Hsieh
Graduate Institute of Chinese Pharmaceutical Sciences, China Medical University, Taichung, Taiwan, ROC
Br J Pharmacol 151:1235-45. 2007..We reported previously that baicalein strongly inhibited proliferation of rat heart endothelial cells and here we assess effects on migration and adhesion of these cells...
Efficient targeting of adenoviral vectors to integrin positive vascular cells utilizing a CAR-cyclic RGD linker proteinY D Krom
Department of Human Genetics, Leiden University Medical Center, Leiden, The Netherlands
Biochem Biophys Res Commun 338:847-54. 2005..In conclusion, CAR-cRGD is a versatile and highly efficient construct to target Ad vectors to both transformed and primary VSMC and EC...
Alphavbeta3 integrin and cofilin modulate K1735 melanoma cell invasionDongmin Dang
Department of Orofacial Sciences, University of California at San Francisco, Box 0512, San Francisco, CA 94143 0512, USA
Exp Cell Res 312:468-77. 2006..Interestingly, the invasion of M2Tbeta3 cells could be sustained by overexpression of cofilin A3. These results suggest that the integrin alphavbeta3 and cofilin together regulate K1735 melanoma cell invasion.
Non-cytotoxic cobra cardiotoxin A5 binds to alpha(v)beta3 integrin and inhibits bone resorption. Identification of cardiotoxins as non-RGD integrin-binding proteins of the Ly-6 familyPo Long Wu
Institute of Bioinformatics and Structural Biology, National Tsing Hua University, Hsinchu 30043, Taiwan
J Biol Chem 281:7937-45. 2006..These results identify CTX A5 as a non-RGD integrin-binding protein with therapeutic potential as an integrin antagonist...
The CXC-chemokine CXCL4 interacts with integrins implicated in angiogenesisSallouha Aidoudi
INSERM, U920, Talence, France
PLoS ONE 3:e2657. 2008..Soluble CXCL4, in turn, inhibits integrin-dependent endothelial cell adhesion and migration. As a whole, our study identifies integrins as novel receptors for CXCL4 that may contribute to its antiangiogenic effect...
The contributions of integrin affinity and integrin-cytoskeletal engagement in endothelial and smooth muscle cell adhesion to vitronectinSteingrimur Stefansson
Department of Physiology and Center for Vascular and Inflammatory Diseases, University of Maryland School of Medicine, Baltimore, Maryland 21201, USA
J Biol Chem 282:15679-89. 2007..Finally, we show that cell adhesion in the presence of PAI-1 leads to colocalization of PAI-1 with the integrins alphavbeta3 and alphavbeta5 at the cell-matrix interface...
Multivalent effects of RGD peptides obtained by nanoparticle displayXavier Montet
Department of Radiology, Geneva Hospital, Geneva, Switzerland, and Department of Angiography and Interventional Radiology, Vienna Medical University, Vienna, Austria
J Med Chem 49:6087-93. 2006..Based on the multivalent enhancement of affinity and extension of blood half-life, multivalent RGD nanoparticle-sized materials should be potent inhibitors of the alpha(V)beta(3) function on endothelial cells in vivo...
Integrin alpha3beta1, a novel receptor for alpha3(IV) noncollagenous domain and a trans-dominant Inhibitor for integrin alphavbeta3Corina M Borza
Division of Nephrology, Department of Medicine, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA
J Biol Chem 281:20932-9. 2006..These biological functions are attributed to the binding of alpha3NC1 to integrin alphavbeta3. However, in some tumor cells that express integrin alphavbeta3, the alpha3NC1 domain does not inhibit ..
Novel and selective alpha(v)beta3 receptor peptide antagonist: design, synthesis, and biological behaviorAnnarita Del Gatto
Institute of Biostructures and Bioimaging, CNR, Department of Biological Sciences, University of Naples Federico II, and C. I. R. Pe. B, Via Mezzocannone 16, 80134 Naples, Italy
J Med Chem 49:3416-20. 2006..Cell adhesion assays have demonstrated that the peptide is a potent and selective antagonist of the alpha(v)beta3 receptor...
A conjugate of camptothecin and a somatostatin analog against prostate cancer cell invasion via a possible signaling pathway involving PI3K/Akt, alphaVbeta3/alphaVbeta5 and MMP-2/-9Li chun Sun
Peptide Research Laboratories, Department of Medicine, Tulane Health Sciences Center, Tulane University School of Medicine, New Orleans, LA 70112 2699, USA
Cancer Lett 246:157-66. 2007..to various extracellular matrix components, mainly to vitronectin, the ligand of cell surface receptors integrin alphaVbeta3 and alphaVbeta5...
Phenotypic and functional differences between human liver cancer endothelial cells and liver sinusoidal endothelial cellsLian Qiu Wu
Institute of Clinical Medical Sciences, China Japan Friendship Hospital, Beijing, PR China
J Vasc Res 45:78-86. 2008..The phenotypic and functional characteristics of microvascular endothelial cells derived from human liver cancer (HLCEC) were analyzed in vitro and compared with those of human liver sinusoidal endothelial cells (LSEC)...
Cell surface overexpression of alphavbeta5 integrin impedes alphavbeta3-mediated migration of the human ovarian adenocarcinoma cell line IGROV1Sylvie Maubant
GRECAN, Université de Caen Basse Normandie and Centre de Lutte Contre le Cancer François Baclesse, Avenue du General Harris, 14076 Caen Cedex 05, France
Cell Biol Int 31:109-18. 2007..Finally, the response to cisplatin was not significantly modified in beta5 transfectants when compared to IGROV1 parental cells...
Research Grants
- Brain tumor angiogenesis: Integrin ceramide signalingAnat Erdreich Epstein; Fiscal Year: 2007..Important questions stemming from this are: 1) Is RGDfV-induced ceramide required for integrin alphavbeta3/beta3-mediated apoptosis; 2) Do integrins alphavbeta3/beta5 control p53 activity via their regulatory ..
- Activation of alpha5beta3 integrin on blood and endothelial cellsTatiana Byzova; Fiscal Year: 2007..The central hypothesis of this proposal is that cellular interaction of integrin alphavbeta3 with matrix ligands is tightly controlled and depends on the activation state of the receptor...
- Tissue Factor, Flow, and Platelet Adhesion/Aggregation on Activated EndotheliumERIC FRANKLIN GRABOWSKI; Fiscal Year: 2010..Our studies promise to clarify the potential of treatments for HUS directed at blocking the above adhesive molecules and vessel wall tissue factor. ..
- TUMOR CELL ADHESIVE GLYCOPROTEINS AND METASTASISKENNETH HONN; Fiscal Year: 1993..e., alpha-II-b-beta-3 and alpha- v-beta-3 ) to cellular functions correlated with high metastatic potential...
- CONTROL OF PERICELLULAR PLASMIN BY MATRIX VITRONECTINPAULA MC KEOWN LONGO; Fiscal Year: 1993..These studies will contribute towards the understanding of processes such as angiogenesis and tumor invasion...
- MATRIX PROTEIN/INTEGRIN MEDIATED OSTEOCLAST REGULATIONKeith Hruska; Fiscal Year: 1999..It is suggested that the results of the proposed studies will represent significant advances in the cell biology of the osteoclast and provide important leads for pharmacologic product development. ..
- PROTECTIVE ROLE OF APOPTOSIS IN ASBESTOS PLEURAL INJURYV Broaddus; Fiscal Year: 2001..These studies should provide important information about the mechanisms by which asbestos induces apoptosis in mesothelial cells and the role of asbestos-induced apoptosis in asbestos-induced pathology. ..
- ROLE OF JAM-1 IN CELL ADHESION AND MIGRATIONUlhas Naik; Fiscal Year: 2003..This JAM-1 induced endothelial cell migration is specific to integrin alphaVbeta3, the vitronectin receptor...
- REGULATION OF CELL MIGRATION IN VASCULAR REMODELINGEric Howard; Fiscal Year: 2002..Understanding this mechanism will be important in defining the biochemical events that occur during vascular remodeling in both normal and disease processes. ..
- L1 CAM AND MELANOMA PROGRESSION AND ANGIOGENESISAnthony Montgomery; Fiscal Year: 2002..tested, it will be determined whether L1 is angiogenic by virtue of its ability to interact with the integrin alphavbeta3 expressed on host vasculature...
