Strategies towards in vivo imaging of active transglutaminase type 2 using positron emission tomography

Berend van der Wildt; Adriaan A. Lammertsma; Benjamin Drukarch; Albert D. Windhorst

doi:10.1007/s00726-016-2288-y

Strategies towards in vivo imaging of active transglutaminase type 2 using positron emission tomography

Berend van der Wildt^*
, Adriaan A. Lammertsma
, Benjamin Drukarch
, Albert D. Windhorst

^*Corresponding author for this work

Research output: Contribution to journal › Article › Academic › peer-review

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Abstract

Transglutaminase type 2 (TG2) is increasingly linked to the pathogenesis of several diseases, such as celiac disease, cancer, and fibrotic and neurodegenerative diseases. In parallel with becoming an attractive target for therapy, interest in the development of compounds for in vivo imaging of TG2 is rising. Such imaging biomarkers might assist in clarifying the role of TG2 in pathology and in monitoring TG2 inhibition in vivo and thus assist in drug development. In this review, the latest results together with various strategies in TG2 PET tracer development are discussed, including radiolabelling of irreversible and reversible active-site inhibitors, as well as allosteric inhibitors, acyl-donor and acyl-acceptor substrates, and anti-TG2 monoclonal antibodies.

Original language	English
Pages (from-to)	585-595
Number of pages	11
Journal	Amino acids
Volume	49
Issue number	3
DOIs	https://doi.org/10.1007/s00726-016-2288-y
Publication status	Published - 1 Mar 2017

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Antibodies
Irreversible TG2 inhibitors
PET
Reversible TG2 inhibitors
Substrates
Transglutaminase type 2

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abstract = "Transglutaminase type 2 (TG2) is increasingly linked to the pathogenesis of several diseases, such as celiac disease, cancer, and fibrotic and neurodegenerative diseases. In parallel with becoming an attractive target for therapy, interest in the development of compounds for in vivo imaging of TG2 is rising. Such imaging biomarkers might assist in clarifying the role of TG2 in pathology and in monitoring TG2 inhibition in vivo and thus assist in drug development. In this review, the latest results together with various strategies in TG2 PET tracer development are discussed, including radiolabelling of irreversible and reversible active-site inhibitors, as well as allosteric inhibitors, acyl-donor and acyl-acceptor substrates, and anti-TG2 monoclonal antibodies.",

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AU - van der Wildt, Berend

AU - Lammertsma, Adriaan A.

AU - Drukarch, Benjamin

AU - Windhorst, Albert D.

PY - 2017/3/1

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N2 - Transglutaminase type 2 (TG2) is increasingly linked to the pathogenesis of several diseases, such as celiac disease, cancer, and fibrotic and neurodegenerative diseases. In parallel with becoming an attractive target for therapy, interest in the development of compounds for in vivo imaging of TG2 is rising. Such imaging biomarkers might assist in clarifying the role of TG2 in pathology and in monitoring TG2 inhibition in vivo and thus assist in drug development. In this review, the latest results together with various strategies in TG2 PET tracer development are discussed, including radiolabelling of irreversible and reversible active-site inhibitors, as well as allosteric inhibitors, acyl-donor and acyl-acceptor substrates, and anti-TG2 monoclonal antibodies.

AB - Transglutaminase type 2 (TG2) is increasingly linked to the pathogenesis of several diseases, such as celiac disease, cancer, and fibrotic and neurodegenerative diseases. In parallel with becoming an attractive target for therapy, interest in the development of compounds for in vivo imaging of TG2 is rising. Such imaging biomarkers might assist in clarifying the role of TG2 in pathology and in monitoring TG2 inhibition in vivo and thus assist in drug development. In this review, the latest results together with various strategies in TG2 PET tracer development are discussed, including radiolabelling of irreversible and reversible active-site inhibitors, as well as allosteric inhibitors, acyl-donor and acyl-acceptor substrates, and anti-TG2 monoclonal antibodies.

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KW - Substrates

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Strategies towards in vivo imaging of active transglutaminase type 2 using positron emission tomography

Abstract

UN SDGs

Keywords

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