Open AccessJournal Article
Noninvasive Imaging of αvβ3 Integrin Expression Using 18F-labeled RGD-containing Glycopeptide and Positron Emission Tomography
Roland Haubner,Hans-Jürgen Wester,Wolfgang A. Weber,Christian Mang,Sibylle Ziegler,Simon L. Goodman,Reingard Senekowitsch-Schmidtke,Horst Kessler,Markus Schwaiger +8 more
TL;DR: First imaging results using a small animal positron emission tomograph suggest that this compound is suitable for noninvasive determination of the α v β 3 integrin status and therapy monitoring.
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Abstract: The alpha(v)beta3 integrin is an important cell adhesion receptor involved in tumor-induced angiogenesis and tumor metastasis. Here we describe the 18F-labeling of the RGD-containing glycopeptide cyclo(-Arg-Gly-Asp-D-Phe-Lys(sugar amino acid)-) with 4-nitrophenyl 2-[18F]fluoropropionate and the evaluation of this compound in vitro and in tumor mouse models. Binding assays with isolated immobilized alpha(v)beta3, alpha(v)beta5, and alpha(IIb)beta3 as well as in vivo studies using alpha(v)beta3-positive and -negative murine and xenotransplanted human tumors demonstrated receptor-specific binding of the radiolabeled glycopeptide yielding high tumor:background ratios (e.g., 120 min postinjection: tumor:blood, 27.5; tumor:muscle, 10.2). First imaging results using a small animal positron emission tomograph suggest that this compound is suitable for noninvasive determination of the alpha(v)beta3 integrin status and therapy monitoring.
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Citations
Be spoilt for choice with radiolabelled RGD peptides: preclinical evaluation of ⁶⁸Ga-TRAP(RGD)₃.
TL;DR: It is concluded that ⁶⁸Ga-TRAP(RGD)₃ could allow for imaging of low-level integrin expression in tissues which are not visible with the two competitors, and constitutes proof of concept for the favourable in vivo properties of TRAP-based ₸Ga radiopharmaceuticals.
96
Imaging of Tumor Angiogenesis: Functional or Targeted?
TL;DR: Both functional and targeted imaging techniques are reviewed for assessing tumor angiogenesis, a critical step in many pathologic processes, particularly cancer.
Synthesis of peptide radiopharmaceuticals for the therapy and diagnosis of tumor diseases.
TL;DR: The requirements to the design and synthesis of radiolabeled peptides for clinical applications are described, with a special emphasis on the synthesis of the building blocks required for the complexation of metallic radioisotopes.
93
Dual In Vivo Quantification of Integrin-targeted and Protease-activated Agents in Cancer Using Fluorescence Molecular Tomography (FMT)
Sylvie Kossodo,Maureen Pickarski,Shu-An Lin,Alexa Gleason,Renee C. Gaspar,Chiara Buono,Guojie Ho,Agnieszka Blusztajn,Garry Cuneo,Jun Zhang,Jayme Jensen,Richard Hargreaves,Paul J. Coleman,George D. Hartman,Milind Rajopadhye,Le Thi Duong,Cyrille Sur,Wael Yared,Jeffrey D. Peterson,Bohumil Bednar +19 more
TL;DR: NIRF-labeled integrin antagonists allow noninvasive molecular fluorescent imaging and quantification of tumors in vivo, improving and providing more refined approaches for cancer detection and treatment monitoring.
93
Targeted mast cell silencing protects against joint destruction and angiogenesis in experimental arthritis in mice
Manfred Kneilling,Lothar Hültner,Bernd J. Pichler,Reinhard Mailhammer,Lars Morawietz,Samuel Solomon,Martin Eichner,Joseph Sabatino,Tilo Biedermann,Veit Krenn,Wolfgang A. Weber,Harald Illges,Roland Haubner,Martin Röcken +13 more
TL;DR: It is shown that intraarticular and intraperitoneal mast cell engraftment fully restores susceptibility to antibody-induced arthritis, angiogenesis, and alphavbeta3 integrin activation in GPI antibody- induced arthritis.
92
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Detection of tumor angiogenesis in vivo by alphaVbeta3-targeted magnetic resonance imaging.
Dorothy A. Sipkins,David A. Cheresh,Mahmood R. Kazemi,Linda M. Nevin,Mark D. Bednarski,King C.P. Li +5 more
TL;DR: A novel approach to detecting angiogenesis in vivo using magnetic resonance imaging (MRI) and a paramagnetic contrast agent targeted to endothelial αvβ3 via the LM609 monoclonal antibody is described.
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Structural and Functional Aspects of RGD-Containing Cyclic Pentapeptides as Highly Potent and Selective Integrin αVβ3 Antagonists
Roland Haubner,Rainer Gratias,Beate Diefenbach,Simon Goodman,and Alfred Jonczyk,Horst Kessler +5 more
TL;DR: The design of low-molecular-mass αVβ3 antagonists by “spatial screening” led to the highly active peptides c( RGDFV) and c(RGDFV), and the influence of the amino acids in positions 4 and 5 flanking the RGD-sequence on the inhibition of vitronectin and fibrinogen binding to the isolated αV β3 and αIIbβ3 receptors was investigated.
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Arg‐Gly‐Asp constrained within cyclic pentapoptides Strong and selective inhibitors of cell adhesion to vitronectin and laminin fragment P1
TL;DR: NMR studies of the two most active cyclic peptides showed for both an all‐trans conformation with a βII′ and γ turn that Subtle conformational differences, however, exist between both peptides and may contribute to selectivity or inhibition.
597
•Journal Article
Radiolabeled αvβ3 Integrin Antagonists: A New Class of Tracers for Tumor Targeting
Roland Haubner,Hans-Jürgen Wester,Ute Reuning,Reingard Senekowitsch-Schmidtke,Beate Diefenbach,Horst Kessler,Gerhard Stöcklin,Markus Schwaiger +7 more
TL;DR: In vitro binding assays demonstrate that the introduction of tyrosine and subsequent iodination have no influence on the high affinity and selectivity for alpha(v)beta3, and the synthesis and biological evaluation of [125I]-3-iodo-D-Tyr4-cyclo(-Arg-Gly-Asp-D.Tyr-Val-) represents the first radiolabeled alpha( v) beta3 antagonist for the investigation of angiogenesis and metastasis
380
A comparative study of N.C.A. fluorine-18 labeling of proteins via acylation and photochemical conjugation.
TL;DR: Owing to competing O-acylation of Tyr residues, [18F]fluoropropionylated HSA was partially unstable under slightly basic conditions, and 18F]SFB seems to be the most suitable 18F-labeling agent for proteins, particularly for the labeling of antibodies.
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