Biological studies of radiolabeled glucose analogues iodinated in positions 3, 4 or 6

Perret, Pascale; Ghezzi, Cathérine; Ogier, Lionel; Abbadi, Medhi; Morin, Christophe; Mathieu, Jean‐Paul; Fagret, Daniel

doi:10.1016/j.nucmedbio.2003.08.009

Cited by 12 publications

(3 citation statements)

References 21 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Primary adipocyte glucose uptake and size measurement was performed as previously described ( 7 ), except for the use of tracer amounts of 3 H-2-deoxyglucose (50 nmol/L; catalog #NET549250UC; PerkinElmer) diluted in 5 µmol/L glucose. Glucose uptake using a higher concentration of 2-deoxyglucose has been shown to be linear for up to 30 min in primary adipocytes ( 18 ). Briefly, dissociated adipocytes from female mice were treated with insulin for 20 min prior to the addition of 3 H-2-deoxyglucose.…”

Section: Methodsmentioning

confidence: 99%

Disruption of Adipose Rab10-Dependent Insulin Signaling Causes Hepatic Insulin Resistance

et al. 2016

View full text Add to dashboard Cite

Insulin controls glucose uptake into adipose and muscle cells by regulating the amount of GLUT4 in the plasma membrane. The effect of insulin is to promote the translocation of intracellular GLUT4 to the plasma membrane. The small Rab GTPase, Rab10, is required for insulin-stimulated GLUT4 translocation in cultured 3T3-L1 adipocytes. Here we demonstrate that both insulin-stimulated glucose uptake and GLUT4 translocation to the plasma membrane are reduced by about half in adipocytes from adipose-specific Rab10 knockout (KO) mice. These data demonstrate that the full effect of insulin on adipose glucose uptake is the integrated effect of Rab10-dependent and Rab10-independent pathways, establishing a divergence in insulin signal transduction to the regulation of GLUT4 trafficking. In adipose-specific Rab10 KO female mice, the partial inhibition of stimulated glucose uptake in adipocytes induces insulin resistance independent of diet challenge. During euglycemic-hyperinsulinemic clamp, there is no suppression of hepatic glucose production despite normal insulin suppression of plasma free fatty acids. The impact of incomplete disruption of stimulated adipocyte GLUT4 translocation on whole-body glucose homeostasis is driven by a near complete failure of insulin to suppress hepatic glucose production rather than a significant inhibition in muscle glucose uptake. These data underscore the physiological significance of the precise control of insulin-regulated trafficking in adipocytes.

show abstract

Section: Methodsmentioning

confidence: 99%

Disruption of Adipose Rab10-Dependent Insulin Signaling Causes Hepatic Insulin Resistance

et al. 2016

View full text Add to dashboard Cite

show abstract

“…Unfortunately, in vivo studies showed 123 I-FIM has a rapid blood clearance and high stomach and thyroid uptake, indicating its rapid deiodination after injection [49]. In addition, iodination of glucose isomers in positions 3, 4, and 6 were investigated, and none of them exhibited the similar biological features of 2-deoxy-D-glucose [50]. The iodinated glucose analogues have not been found to be metabolic markers for in vivo studies.…”

Section: Preclinical Development Of Glucose-based Radiopharmaceutimentioning

confidence: 99%

Nuclear Imaging of Glucose Metabolism: Beyond ¹⁸F-FDG

Han

Wang

Chen

et al. 2019

Contrast Media & Molecular Imaging

View full text Add to dashboard Cite

Glucose homeostasis plays a key role in numerous fundamental aspects of life, and its dysregulation is associated with many important diseases such as cancer. The atypical glucose metabolic phenomenon, known as the Warburg effect, has been recognized as a hallmark of cancer and serves as a promising target for tumor specific imaging. At present, 2-deoxy-2-[18F]fluoro-glucose (18F-FDG)-based positron emission tomography/computed tomography (PET/CT) represented the state-of-the-art radionuclide imaging technique for this purpose. The powerful impact of 18F-FDG has prompted intensive research efforts into other glucose-based radiopharmaceuticals for positron emission tomography (PET) and single-photon emission computed tomography (SPECT) imaging. Currently, glucose and its analogues have been labeled with various radionuclides such as 99mTc, 111In, 18F, 68Ga, and 64Cu and have been successfully investigated for tumor metabolic imaging in many preclinical studies. Moreover, 99mTc-ECDG has advanced into its early clinical trials and brings a new era of tumor imaging beyond 18F-FDG. In this review, preclinical and early clinical development of glucose-based radiopharmaceuticals for tumor metabolic imaging will be summarized.

show abstract

“…234 While [ 18 F]-2-fluoro-2-deoxy-D-glucose (FDG) has been developed for applications in localization of tumor and metastatic tissue, 235 the development of a glucose analogue labeled with a g-emitter for SPECT and readily available for routine use is of considerable clinical interest. [236][237][238][239] Glucose has been functionalized at the C-1 and C-3 positions for coordination to the { 9m Tc(CO) 3 } + by Alberto and Schibli, 237,240 as shown in Fig. 28.…”

Section: Carbohydratesmentioning

confidence: 99%

Single amino acid chelates (SAAC): a strategy for the design of technetium and rhenium radiopharmaceuticals

Bartholomä

Valliant

Maresca³

et al. 2009

Chem. Commun.

179

142

View full text Add to dashboard Cite

Radiolabeled biomolecules can be used to visualize a variety of diseases through interaction with specific cell receptors. A key step is the introduction of a molecular entity that allows facile labeling with the medically useful radionuclide (99m)Tc without significant alteration of the structure and function of the biomolecule. One strategy focuses on the design of single amino acid chelates (SAACs), novel bifunctional chelators constructed from derivatized amino acids or amino acid analogues. The chelating terminus of the SAAC has been designed for effective coordination to the {(99m)Tc(CO)(3)}(+) core, while the other terminus allows incorporation into any position along a peptide sequence or into a variety of biomolecules. In applications to peptidic materials, the approach affords significant flexibility in the choice of donors for (99m)Tc coordination combined with the considerable advantages of routine solid phase synthetic techniques. The methodology allows libraries of peptide-based (99m)Tc(i) and (186,188)Re(i) radiopharmaceuticals to prepared using conventional automated peptides synthesis. Other biomolecules, including nucleosides, carbohydrates, folic acid and vitamin B12 are also readily modified using analogous methods. The approach also allows the preparation of isostructural (99m)Tc and Re complexes for the correlation of in vivo and in vitro imaging studies.

show abstract

Biological studies of radiolabeled glucose analogues iodinated in positions 3, 4 or 6

Cited by 12 publications

References 21 publications

Disruption of Adipose Rab10-Dependent Insulin Signaling Causes Hepatic Insulin Resistance

Disruption of Adipose Rab10-Dependent Insulin Signaling Causes Hepatic Insulin Resistance

Nuclear Imaging of Glucose Metabolism: Beyond ¹⁸F-FDG

Single amino acid chelates (SAAC): a strategy for the design of technetium and rhenium radiopharmaceuticals

Contact Info

Product

Resources

About

Biological studies of radiolabeled glucose analogues iodinated in positions 3, 4 or 6

Cited by 12 publications

References 21 publications

Disruption of Adipose Rab10-Dependent Insulin Signaling Causes Hepatic Insulin Resistance

Disruption of Adipose Rab10-Dependent Insulin Signaling Causes Hepatic Insulin Resistance

Nuclear Imaging of Glucose Metabolism: Beyond 18F-FDG

Single amino acid chelates (SAAC): a strategy for the design of technetium and rhenium radiopharmaceuticals

Contact Info

Product

Resources

About

Nuclear Imaging of Glucose Metabolism: Beyond ¹⁸F-FDG