PMID- 28713886
OWN - NLM
STAT- PubMed-not-MEDLINE
DCOM- 20180216
LR  - 20180216
IS  - 1477-9234 (Electronic)
IS  - 1477-9226 (Linking)
VI  - 46
IP  - 29
DP  - 2017 Jul 25
TI  - A new tetrapodal 3-hydroxy-4-pyridinone ligand for complexation of (89)zirconium 
      for positron emission tomography (PET) imaging.
PG  - 9654-9663
LID - 10.1039/c7dt02196h [doi]
AB  - Zirconium-89 ((89)Zr) is an ideal radiometal isotope for antibody-based positron 
      emission tomography (immunoPET) as its physical half-life (3.27 days) is a good 
      match with the biological half-life of larger molecular weight targeting 
      molecules, such as antibodies (3-4 days), and its positron emission (BR = 100% 
      EC/beta(+), E(beta(+),avg) = 395.5 keV) is suited for high resolution PET imaging. 
      Concerns over the in vivo stability of the most commonly used (89)Zr-chelator, 
      desferrioxamine B (DFO), have spurred efforts into the development of alternative 
      (89)Zr-chelators that withstand the release of osteophilic (89)Zr(4+). Herein we 
      report the new chelator 
      1,3-propanediamine-N,N,N',N'-tetrakis[(2-(aminomethyl)-3-hydroxy-1,6-dimethyl-4(1H)-pyridinone)acetamide] 
      (THPN) based on four 3-hydroxy-4-pyridinone (3,4-HOPO) coordinating groups, as a 
      potentially superior chelator over DFO. THPN has been demonstrated to 
      quantitatively form a monometallic complex with Zr(4+) within 10 min at ambient 
      temperature at as low as 10(-6) M concentrations of the chelator. The resulting 
      complexes were studied in vitro and in vivo. The (89)Zr-THPN complex was stable 
      in serum and outperformed the (89)Zr-DFO complex in a direct transchelation 
      challenge. Healthy mice excreted (89)Zr-THPN rapidly without signs of 
      demetalation or residual organ uptake. This renders THPN as a promising 
      alternative to DFO and introduces the first octadentate 3,4-HOPO chelator to the 
      field.
FAU - Buchwalder, Christian
AU  - Buchwalder C
AUID- ORCID: 0000-0001-5577-8870
AD  - University of British Columbia, Faculty of Pharmaceutical Sciences, 2405 Wesbrook 
      Mall, Vancouver, BC V6T 1Z3, Canada. kathy.saatchi@ubc.ca urs.hafeli@ubc.ca.
FAU - Rodriguez-Rodriguez, Cristina
AU  - Rodriguez-Rodriguez C
AUID- ORCID: 0000-0002-3313-4422
AD  - University of British Columbia, Faculty of Pharmaceutical Sciences, 2405 Wesbrook 
      Mall, Vancouver, BC V6T 1Z3, Canada. kathy.saatchi@ubc.ca urs.hafeli@ubc.ca and 
      University of British Columbia, Department of Physics & Astronomy, 6224 
      Agricultural Road, Vancouver, BC V6T 1Z1, Canada and University of British 
      Columbia, Centre for Comparative Medicine, 4145 Wesbrook Mall, Vancouver, BC V6T 
      1W5, Canada.
FAU - Schaffer, Paul
AU  - Schaffer P
AUID- ORCID: 0000-0002-6392-8792
AD  - TRIUMF, Life Sciences Division, 4004 Wesbrook Mall, Vancouver, BC V6T 2A3, 
      Canada.
FAU - Karagiozov, Stoyan K
AU  - Karagiozov SK
AD  - University of British Columbia, Faculty of Pharmaceutical Sciences, 2405 Wesbrook 
      Mall, Vancouver, BC V6T 1Z3, Canada. kathy.saatchi@ubc.ca urs.hafeli@ubc.ca.
FAU - Saatchi, Katayoun
AU  - Saatchi K
AD  - University of British Columbia, Faculty of Pharmaceutical Sciences, 2405 Wesbrook 
      Mall, Vancouver, BC V6T 1Z3, Canada. kathy.saatchi@ubc.ca urs.hafeli@ubc.ca.
FAU - Hafeli, Urs O
AU  - Hafeli UO
AUID- ORCID: 0000-0003-0671-4509
AD  - University of British Columbia, Faculty of Pharmaceutical Sciences, 2405 Wesbrook 
      Mall, Vancouver, BC V6T 1Z3, Canada. kathy.saatchi@ubc.ca urs.hafeli@ubc.ca.
LA  - eng
PT  - Journal Article
PL  - England
TA  - Dalton Trans
JT  - Dalton transactions (Cambridge, England : 2003)
JID - 101176026
EDAT- 2017/07/18 06:00
MHDA- 2017/07/18 06:01
CRDT- 2017/07/18 06:00
PHST- 2017/07/18 06:00 [pubmed]
PHST- 2017/07/18 06:01 [medline]
PHST- 2017/07/18 06:00 [entrez]
AID - 10.1039/c7dt02196h [doi]
PST - ppublish
SO  - Dalton Trans. 2017 Jul 25;46(29):9654-9663. doi: 10.1039/c7dt02196h.