TY - JOUR
T1 - Strategies towards in vivo imaging of active transglutaminase type 2 using positron emission tomography
AU - van der Wildt, Berend
AU - Lammertsma, Adriaan A.
AU - Drukarch, Benjamin
AU - Windhorst, Albert D.
PY - 2017/3/1
Y1 - 2017/3/1
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.
KW - Antibodies
KW - Irreversible TG2 inhibitors
KW - PET
KW - Reversible TG2 inhibitors
KW - Substrates
KW - Transglutaminase type 2
UR - http://www.scopus.com/inward/record.url?scp=84977142711&partnerID=8YFLogxK
U2 - https://doi.org/10.1007/s00726-016-2288-y
DO - https://doi.org/10.1007/s00726-016-2288-y
M3 - Article
C2 - 27380031
SN - 0939-4451
VL - 49
SP - 585
EP - 595
JO - Amino acids
JF - Amino acids
IS - 3
ER -