Clinical Applications of Positron Emission Tomography (PET) Imaging in Medicine: Oncology, Brain Diseases and Cardiology

Kitson, Sean L.; Cuccurullo, Vincenzo; Ciarmiello, Andrea; Salvo, Diana; Mansi, Luigi

doi:10.2174/1874471010902040224

Cited by 44 publications

(27 citation statements)

References 85 publications

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“…In addition, [ 18 F]FDG is also used as a standard radiotracer for PET neuro-imaging and diagnostics of cardiac and inflammatory diseases [16]. The role of [ 18 F]FDG in oncology is dependent on its affinity to accumulate inside the tumour cell where higher glucose metabolism takes place compared to normal surrounding cells [17].…”

Section: Discussionmentioning

confidence: 99%

Automated synthesis of [18F]fluorocholine using a modified GE TracerLab module

Sperandeo¹,

Ficola²,

Quartuccio³

et al. 2014

J Diagn Imaging Ther

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Section: Discussionmentioning

confidence: 99%

Automated synthesis of [18F]fluorocholine using a modified GE TracerLab module

Sperandeo¹,

Ficola²,

Quartuccio³

et al. 2014

J Diagn Imaging Ther

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“…This system consists of two scanning machines, namely the PET scanner and an X-ray computed tomography (CT) scanner. These modern medical modalities occupy a central role in the technological apex of nuclear medicine and provide a prominent role in theranostics [280].…”

Section: Pet Imagingmentioning

confidence: 99%

“…Subsequently, PET-FDG became an established imaging technique in the clinical assessment of many neoplasms, finding a role also in non-malignant diseases for example dementia, myocardial ischaemia, inflammation and infection [280] The fundamental aspect of PET imaging is the detection of radiation inside the human body. The radiation emitted is due to the decay of short-lived radionuclides.…”

Section: Pet Imagingmentioning

confidence: 99%

Squaryl Molecular Metaphors – Application to Rational Drug Design and Imaging Agents

Kitson¹

2017

J Diagn Imaging Ther

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Molecular Metaphors is the application of squaryl building blocks towards creative functional group chemistry to produce lead compounds and imaging agents. This strategy is applied to rational drug design and to various imaging agents that would normally contain conventional functional group chemistry. These, include carboxylic acids, α-amino acids, peptide bonds and phosphonates. Moreover, the squaryl metaphor is a precursor to complex organic molecules involving functional group interchange (FGI) and rearrangements. This article discusses the application of these metaphors in the area of neurochemistry, especially NMDA receptors. An important area of drug design is the inhibition of angiotensin II enzyme by the use of losartan. This commercial drug contains a tetrazole moiety that can be modified using the squaryl group to give a semisquarate derivative. These concepts can extend to the semisquarate of ibuprofen. Moreover, a discussion on peptidomimetics regarding the substitution of the peptide bond for squaramide allows for a change in the biological properties due to modification at the peptide bond. Furthermore, the topic on how squaryl metaphors can be exploited primarily by the central 1,3-hydroxyamide sequence to the generation of a novel class of HIV protease inhibitors. Also, squaryl metaphors can be used to develop potential inhibitors of glutathione and novel anti-migraine drugs. The discussion continues on the design of anticancer drugs: in particular, a novel class of metalloproteases, including phosphonates for semisquaramides, leading to squaryl nucleosides. This review concludes with the application of squaryl metaphors in the design of positron emission tomography (PET) and magnetic resonance imaging (MRI) agents towards theranostics. describe the ability of individual functional chemical groups to mimic other moieties [2,3]. KeywordsErlenmeyer rationalised these concepts and categorised isosteres into atoms, ions and molecules based on the valence level of electrons [4]. A further understanding by Friedman led to the term bioisosterism to include all atoms and molecules that fit the broadest definition of isosteres [5]. This approach was independent of whether the drug was an agonist or an antagonist towards biological activity.Moreover, Thornber applied the term bioisosterism to include subunits, groups or molecules that possess physicochemical properties of similar biological effects [6]. Finally, in 1991 Burger widened the definition of bioisosteres to include compounds or groups that possess similar molecular shapes and volumes independent of agonists or antagonists [7]. REVIEW ARTICLE Squaryl KitsonThese bioisosteres would require approximately the same distribution of electrons and give a high probability of generating comparable physical properties such as hydrophobicity [8]. Currently, bioisosterism is one of the most useful tools to the medicinal chemist in rational drug design and in particular regarding the carboxylic acid bioisosteres [9]. The carboxylic acid functional ...

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“…The most widely used radioligand thus far has been [ 11 C]-PK11195 [18], but interpretation of studies is limited by its relatively poor signal-to-noise ratio [23]. Table 2 Selected positron emission tomography radiotracers well characterized for pharmacodynamic studies (adapted from [43] Integration of data from PET target occupancy studies and functional MRI (fMRI) methods provides a novel strategy for directly relating information on drug-target interactions directly with a measure of functional effects in the brain. Recent studies illustrating this approach have related the extent of binding of an antagonist to its m-opioid target with modulation of fMRI reward responses to the administration of a palatable food stimulus [29] or a dopamine receptor occupancy to reward responses in a gambling task ( Figure 6).…”

Section: Figurementioning

confidence: 99%

Positron emission tomography molecular imaging for drug development

Matthews

Rabiner

Passchier

et al. 2012

Brit J Clinical Pharma

282

193

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Human in vivo molecular imaging with positron emission tomography (PET) enables a new kind of 'precision pharmacology' , able to address questions central to drug development. Biodistribution studies with drug molecules carrying positron-emitting radioisotopes can test whether a new chemical entity reaches a target tissue compartment (such as the brain) in sufficient amounts to be pharmacologically active. Competition studies, using a radioligand that binds to the target of therapeutic interest with adequate specificity, enable direct assessment of the relationship between drug plasma concentration and target occupancy. Tailored radiotracers can be used to measure relative rates of biological processes, while radioligands specific for tissue markers expected to change with treatment can provide specific pharmacodynamic information. Integrated application of PET and magnetic resonance imaging (MRI) methods allows molecular interactions to be related directly to anatomical or physiological changes in a tissue. Applications of imaging in early drug development can suggest approaches to patient stratification for a personalized medicine able to deliver higher value from a drug after approval. Although imaging experimental medicine adds complexity to early drug development and costs per patient are high, appropriate use can increase returns on R and D investment by improving early decision making to reduce new drug attrition in later stages. We urge that the potential value of a translational molecular imaging strategy be considered routinely and at the earliest stages of new drug development.

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Clinical Applications of Positron Emission Tomography (PET) Imaging in Medicine: Oncology, Brain Diseases and Cardiology

Cited by 44 publications

References 85 publications

Automated synthesis of [18F]fluorocholine using a modified GE TracerLab module

Automated synthesis of [18F]fluorocholine using a modified GE TracerLab module

Squaryl Molecular Metaphors – Application to Rational Drug Design and Imaging Agents

Positron emission tomography molecular imaging for drug development

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