A new perspective of probe development for imaging pancreatic beta cell in vivo

Neo, Claire Wen Ying; Ciaramicoli, Larissa Miasiro; Soetedjo, Andreas Alvin Purnomo; Teo, Adrian Kee Keong; Kang, Nam‐Young

doi:10.1016/j.semcdb.2020.01.009

Cited by 6 publications

(1 citation statement)

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“…During the last decade, several putative beta cell-specific probes have been identified, including monoclonal antibodies (mAbs) [ 42 , 43 ], short or fragments of antibodies [ 44 , 45 ], peptides [ 46 , 47 , 48 ], small molecules such as metabolites [ 49 , 50 , 51 ], and ion-binding probes [ 52 , 53 ]. The different existing tracers have been recently and comprehensively reviewed [ 54 ] and will not be further discussed here. Amongst this variety of probes, only three families of radiotracers are currently undergoing clinical evaluation in humans: 18 F-dihydro-tetrabenazine (DTBZ) for imaging of vesicular monoamine transporter 2 (VMAT2) [ 49 , 55 ], 11 C-hydroxytryptophan (HTP) as a marker for the serotonergic system [ 50 ], and 111 In- and 68 Ga-labeled exendin-4 and derivatives targeting the GLP-1 receptor [ 46 ].…”

Section: Bcm Probes Presently Under Clinical Investigationmentioning

confidence: 99%

Beta Cell Imaging—From Pre-Clinical Validation to First in Man Testing

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et al. 2020

IJMS

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There are presently no reliable ways to quantify human pancreatic beta cell mass (BCM) in vivo, which prevents an accurate understanding of the progressive beta cell loss in diabetes or following islet transplantation. Furthermore, the lack of beta cell imaging hampers the evaluation of the impact of new drugs aiming to prevent beta cell loss or to restore BCM in diabetes. We presently discuss the potential value of BCM determination as a cornerstone for individualized therapies in diabetes, describe the presently available probes for human BCM evaluation, and discuss our approach for the discovery of novel beta cell biomarkers, based on the determination of specific splice variants present in human beta cells. This has already led to the identification of DPP6 and FXYD2ga as two promising targets for human BCM imaging, and is followed by a discussion of potential safety issues, the role for radiochemistry in the improvement of BCM imaging, and concludes with an overview of the different steps from pre-clinical validation to a first-in-man trial for novel tracers.

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