scholarly journals PET imaging of αvβ3 integrin expression in tumours with 68Ga-labelled mono-, di- and tetrameric RGD peptides

2010 ◽  
Vol 38 (1) ◽  
pp. 128-137 ◽  
Author(s):  
Ingrid Dijkgraaf ◽  
Cheng-Bin Yim ◽  
Gerben M. Franssen ◽  
Robert C. Schuit ◽  
Gert Luurtsema ◽  
...  
Keyword(s):  
Pet Imaging ◽  
Αvβ3 Integrin ◽  
Integrin Expression ◽  
Rgd Peptides

scholarly journals There is a world beyond αvβ3-integrin: Multimeric ligands for imaging of the integrin subtypes αvβ6, αvβ8, αvβ3, and α5β1 by positron emission tomography

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Katja Steiger ◽  
Neil Gerard Quigley ◽  
Tanja Groll ◽  
Frauke Richter ◽  
Maximilian Alexander Zierke ◽  
...  
Keyword(s):  
Pet Imaging ◽  
Αvβ3 Integrin ◽  
Rgd Peptides ◽  
Rgd Sequence ◽  
Positron Emission ◽  
German Research ◽  
Integrin Ligands ◽  
Αvβ6 Integrin ◽  
Gallium 68 ◽  
Clinical Potential

Abstract Background In the context of nuclear medicine and theranostics, integrin-related research and development was, for most of the time, focused predominantly on 'RGD peptides' and the subtype αvβ3-integrin. However, there are no less than 24 known integrins, and peptides without the RGD sequence as well as non-peptidic ligands play an equally important role as selective integrin ligands. On the other hand, multimerization is a well-established method to increase the avidity of binding structures, but multimeric radiopharmaceuticals have not made their way into clinics yet. In this review, we describe how these aspects have been interwoven in the framework of the German Research Foundation's multi-group interdisciplinary funding scheme CRC 824, yielding a series of potent PET imaging agents for selective imaging of various integrin subtypes. Results The gallium-68 chelator TRAP was utilized to elaborate symmetrical trimers of various peptidic and non-peptidic integrin ligands. Preclinical data suggested a high potential of the resulting Ga-68-tracers for PET-imaging of the integrins α5β1, αvβ8, αvβ6, and αvβ3. For the first three, we provide some additional immunohistochemistry data in human cancers, which suggest several future clinical applications. Finally, application of αvβ3- and αvβ6-integrin tracers in pancreatic carcinoma patients revealed that unlike αvβ3-targeted PET, αvβ6-integrin PET is not characterized by off-target uptake and thus, enables a substantially improved imaging of this type of cancer. Conclusions Novel radiopharmaceuticals targeting a number of different integrins, above all, αvβ6, have proven their clinical potential and will play an increasingly important role in future theranostics.

68Ga- and 111In-labelled DOTA-RGD peptides for imaging of αvβ3 integrin expression

2008 ◽  
Vol 35 (8) ◽  
pp. 1507-1515 ◽  
Author(s):  
Clemens Decristoforo ◽  
Ignacio Hernandez Gonzalez ◽  
Janette Carlsen ◽  
Marco Rupprich ◽  
Marc Huisman ◽  
...  
Keyword(s):  
Αvβ3 Integrin ◽  
Integrin Expression ◽  
Rgd Peptides

scholarly journals 18F-Labeled Galacto and PEGylated RGD Dimers for PET Imaging of αvβ3 Integrin Expression

2009 ◽  
Vol 12 (5) ◽  
pp. 530-538 ◽  
Author(s):  
Shuanglong Liu ◽  
Zhaofei Liu ◽  
Kai Chen ◽  
Yongjun Yan ◽  
Petra Watzlowik ◽  
...  
Keyword(s):  
Pet Imaging ◽  
Αvβ3 Integrin ◽  
Integrin Expression

scholarly journals Absence of the αvβ3 Integrin Dictates the Time-Course of Angiogenesis in the Hypoxic Central Nervous System: Accelerated Endothelial Proliferation Correlates with Compensatory Increases in α5β1 Integrin Expression

2010 ◽  
Vol 30 (5) ◽  
pp. 1031-1043 ◽  
Author(s):  
Longxuan Li ◽  
Jennifer V Welser ◽  
Richard Milner
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Time Course ◽  
Αvβ3 Integrin ◽  
Integrin Expression ◽  
Brain Endothelial Cells ◽  
Endothelial Proliferation ◽  
Β3 Integrin ◽  
Α5β1 Integrin

Cerebral angiogenesis is an important adaptive response to hypoxia. As the αvβ3 integrin is induced on angiogenic vessels in the ischemic central nervous system (CNS), and the suggested angiogenic role for this integrin in other systems, it is important to determine whether the αvβ3 integrin is an important mediator of cerebral angiogenesis. αvβ3 integrin expression was examined in a model of cerebral hypoxia, in which mice were subject to hypoxia (8% O2) for 0, 4, 7, or 14 days. Immunofluorescence and western blot analysis revealed that in the hypoxic CNS, αvβ3 integrin was strongly induced on angiogenic brain endothelial cells (BEC), along with its ligand vitronectin. In the hypoxia model, β3 integrin-null mice showed no obvious defect in cerebral angiogenesis. However, early in the angiogenic process, BEC in these mice showed an increased mitotic index that correlated closely with increased α5 integrin expression. In vitro experiments confirmed α5 integrin upregulation on β3 integrin-null BEC, which also correlated with increased BEC proliferation on fibronectin. These studies confirm hypoxic induction of αvβ3 integrin on angiogenic vessels, but suggest distinct roles for the BEC integrins αvβ3 and α5β1 in cerebral angiogenesis, with αvβ3 having a nonessential role, and α5β1 promoting BEC proliferation.

Nitric Oxide Induces Angiogenesis and Upregulates αvβ3 Integrin Expression on Endothelial Cells

2000 ◽  
Vol 60 (3) ◽  
pp. 269-280 ◽  
Author(s):  
Paul C. Lee ◽  
Melina R. Kibbe ◽  
Matthew J. Schuchert ◽  
Donna B. Stolz ◽  
Simon C. Watkins ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Endothelial Cells ◽  
Αvβ3 Integrin ◽  
Integrin Expression

A developmental analysis of oligodendroglial integrins in primary cells: changes in alpha v-associated beta subunits during differentiation

Development ◽  
1994 ◽  
Vol 120 (12) ◽  
pp. 3497-3506 ◽  
Author(s):  
R. Milner ◽  
C. Ffrench-Constant
Keyword(s):  
Progenitor Cell ◽  
Beta Subunits ◽  
Integrin Expression ◽  
Primary Cells ◽  
Developmentally Regulated ◽  
Rgd Peptides ◽  
Rational Explanation ◽  
Oligodendrocyte Precursor ◽  
Alpha V Beta 3 ◽  
Developmental Analysis

We have examined the expression of integrins on primary oligodendroglial cells during the differentiation of the proliferative oligodendrocyte precursor (O-2A progenitor) cell to the postmitotic oligodendrocyte. Cells of the oligodendrocyte lineage expressed a limited repertoire of integrins: alpha 6 beta 1 and alpha v integrins including alpha v beta 1, alpha v beta 3 and alpha v beta 5, as well as a potentially novel integrin alpha v beta 80 kDa. Integrin expression was developmentally regulated; during differentiation alpha v beta 1 was reduced and alpha v beta 5 upregulated. These results suggest that laminin and vitronectin are important extracellular matrix ligands for oligodendrocytes, and provide a rational explanation for previous observations that RGD peptides inhibit the expression of myelin-specific genes. They also suggest a simple model by which switching of integrin beta subunits might regulate differentiation. As chimeric beta 1 integrins with a beta 5 cytoplasmic domain support proliferation less well than normal beta 1 integrins (Pasqualini and Hemler (1994), J. Cell Biol. 125, 447–460) the switch from alpha v beta 1 to alpha v beta 5 might play a key instructive role in the cessation of proliferation and subsequent differentiation.

Leukaemia inhibitory factor increases αvβ3 integrin expression in cultured mouse blastocysts

2020 ◽  
pp. NULL
Author(s):  
Ali Hosseini ◽  
Nassim Ghorbanmehr ◽  
Mojtaba Rezazadeh Valojerdi ◽  
Mehrdad Bakhtiyari ◽  
Bahar Movaghar
Keyword(s):  
Inhibitory Factor ◽  
Leukaemia Inhibitory Factor ◽  
Αvβ3 Integrin ◽  
Integrin Expression
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