Adduct of 2-[18F]FDG and 2-nitroimidazole as a putative radiotracer for the detection of hypoxia with PET: synthesis, in vitro- and in vivo-characterization

Patt, Marianne; Sorger, Dietlind; Scheunemann, Matthias; Stöcklin, G.

doi:10.1016/s0969-8043(02)00186-0

Cited by 32 publications

(45 citation statements)

References 11 publications

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“…In clinical studies of patients with head and neck [190] and brain [191] tumors, it is suggested that FDG-PET may offer an indication of the extent of tumor hypoxia. However, the merit of FDG-PET relative to the use of bioreductive tracers such as the 2-nitroimidazoles is questionable, where FDG is not always retained in hypoxic tissue in mouse models [192][193][194][195] . Further evaluation of FDG-PET in relation to intrinsic and bioreductive markers of hypoxia, and response to radiotherapy or hypoxia-dependent drugs is needed to fully assess its application as a marker of hypoxia in the clinic.…”

Section: Fluorodeoxyglucose Positron Emission Tomographymentioning

confidence: 99%

Hypoxic Regulation of Glucose Transport, Anaerobic Metabolism and Angiogenesis in Cancer: Novel Pathways and Targets for Anticancer Therapeutics

2007

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Cancer cells require a steady source of metabolic energy in order to continue their uncontrolled growth and proliferation. Accelerated glycolysis is one of the biochemical characteristics of cancer cells. Recent work indicates that glucose transport and metabolism are essential for the posttreatment survival of tumor cells, leading to poor prognosis. Glycolytic breakdown of glucose is preceded by the transport of glucose across the cell membrane, a rate-limiting process mediated by facilitative glucose transporter proteins belonging to the facilitative glucose transporter/solute carrier GLUT/SLC2A family. Tumors frequently show overexpression of GLUTs, especially the hypoxia-responsive GLUT1 and GLUT3 proteins. There are also studies that have reported associations between GLUT expression and proliferative indices, whilst others suggest that GLUT expression may be of prognostic significance. In this article we revisit Warburg’s original hypothesis and review the recent clinical and basic research on the expression of GLUT family members in human cancers and in cell lines derived from human tumors. We also explore the links between hypoxia-induced genes, glucose transporters and angiogenic factors. Hypoxic tumors are significantly more malignant, metastatic, radio- and chemoresistant and have a poor prognosis. With the discovery the oxygen-sensitive transcription factor hypoxia-inducible factor (HIF-1) has come a new understanding of the molecular link between hypoxia and deregulated glucose metabolism. HIF-1 induces a number of genes integral to angiogenesis, e.g. vascular endothelial growth factor (VEGF), a process intimately involved with metastatic spread. This knowledge may enhance existing chemotherapeutic strategies so that treatment can be more rationally applied and personalized for cancer patients.

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Section: Fluorodeoxyglucose Positron Emission Tomographymentioning

confidence: 99%

Hypoxic Regulation of Glucose Transport, Anaerobic Metabolism and Angiogenesis in Cancer: Novel Pathways and Targets for Anticancer Therapeutics

2007

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“…However, a limited number of 18 F-labeled tracers are available originating from using [ 18 F]-FDG as a precursor[20][21][22][23][24]. As an effort to develop novel radiotracers for MPI studies, we here report rapid synthesis and initial preclinical…”

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confidence: 99%

Novel synthesis and initial preclinical evaluation of 18 F-[FDG] labeled rhodamine: a potential PET myocardial perfusion imaging agent

Al-Jammaz

Al‐Otaibi

AlHindas

et al. 2015

Nuclear Medicine and Biology

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“…However, 2-D-glucose-conjugated paclitaxel (Figure 4b) contains glucose in the α conformation, and this compound was demonstrated to be partially inhibited from entering cells upon treatment with GLUT-1 transporter inhibitor phloretin [53]. Substitutions of C1 oxygen for C1 nitrogen have also been reported in FDG analogs; these analogs have been shown to compete with D-glucose for cellular entry, suggesting their uptake is GLUT-mediated [81]. …”

Section: Mechanistic Considerations For the Design And Study Of Futurmentioning

confidence: 99%

Glucose conjugation for the specific targeting and treatment of cancer

2013

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Cancers of diverse origins exhibit marked glucose avidity and high rates of aerobic glycolysis. Increased understanding of this dysfunctional metabolism known as the Warburg effect has led to an interest in targeting it for cancer therapy. One promising strategy for such targeting is glycoconjugation, the linking of a drug to glucose or another sugar. This review summarizes the most salient examples of glycoconjugates, in which known cytotoxins or targeted anticancer therapeutics have been linked to glucose (or another glucose transporter substrate sugar) for improved cancer targeting and selectivity. Building on these examples, this review also provides a series of guidelines for the design and mechanistic evaluation of future glycoconjugates.

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Adduct of 2-[18F]FDG and 2-nitroimidazole as a putative radiotracer for the detection of hypoxia with PET: synthesis, in vitro- and in vivo-characterization

Cited by 32 publications

References 11 publications

Hypoxic Regulation of Glucose Transport, Anaerobic Metabolism and Angiogenesis in Cancer: Novel Pathways and Targets for Anticancer Therapeutics

Hypoxic Regulation of Glucose Transport, Anaerobic Metabolism and Angiogenesis in Cancer: Novel Pathways and Targets for Anticancer Therapeutics

Novel synthesis and initial preclinical evaluation of 18 F-[FDG] labeled rhodamine: a potential PET myocardial perfusion imaging agent

Glucose conjugation for the specific targeting and treatment of cancer

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