PMID- 33189949
OWN - NLM
STAT- MEDLINE
DCOM- 20210927
LR  - 20210927
IS  - 1872-9614 (Electronic)
IS  - 0969-8051 (Linking)
VI  - 90-91
DP  - 2020 Nov-Dec
TI  - Novel radiogallium-labeled pyridyl benzofuran derivative for detection of amylin 
      aggregates in pancreas.
PG  - 93-97
LID - S0969-8051(20)30283-3 [pii]
LID - 10.1016/j.nucmedbio.2020.10.003 [doi]
AB  - INTRODUCTION: The deposition of islet amyloid composed of amylin aggregates is 
      related to beta-cell mass dysfunction in type 2 diabetes mellitus (T2DM), and it may 
      be involved in the development and progression of T2DM. In this study, we newly 
      designed, synthesized, and evaluated a radiogallium-labeled pyridyl benzofuran 
      derivative ([(67/68)Ga]GPBF) as an amylin imaging probe. METHODS: An in vitro 
      competitive inhibition assay was performed to determine the binding affinity for 
      amylin aggregates. An in vitro autoradiographic study was carried out using 
      pancreatic sections from a T2DM patient. A biodistribution of [(67)Ga]GPBF in 
      normal mice was evaluated. Finally, we carried out ex vivo autoradiography using 
      mouse transplanted with amylin aggregates. RESULTS: GPBF exhibited binding 
      affinity for amylin aggregates in vitro. In addition, [(67)Ga]GPBF clearly 
      labeled islet amyloids in in vitro autoradiography of a T2DM pancreatic section. 
      In a biodistribution study using normal mice, [(67)Ga]GPBF showed initial uptake 
      into the pancreas, but non-specific accumulation in the liver, spleen, and 
      pancreas was also observed. Furthermore, an ex vivo autoradiogram demonstrated 
      that [(67)Ga]GPBF bound to amylin aggregates in the pancreas of the amylin 
      aggregate-transplanted mice. CONCLUSIONS: These results provide useful insights 
      into the development of radiogallium labeled probes that target amylin aggregates 
      in the T2DM pancreas.
CI  - Copyright (c) 2020 Elsevier Inc. All rights reserved.
FAU - Watanabe, Hiroyuki
AU  - Watanabe H
AD  - Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical 
      Sciences, Kyoto University, 46-29 Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 
      606-8501, Japan.. Electronic address: hwatanabe@pharm.kyoto-u.ac.jp.
FAU - Kawano, Kiyoshiro
AU  - Kawano K
AD  - Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical 
      Sciences, Kyoto University, 46-29 Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 
      606-8501, Japan.
FAU - Iikuni, Shimpei
AU  - Iikuni S
AD  - Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical 
      Sciences, Kyoto University, 46-29 Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 
      606-8501, Japan.
FAU - Shimizu, Yoichi
AU  - Shimizu Y
AD  - Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical 
      Sciences, Kyoto University, 46-29 Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 
      606-8501, Japan.
FAU - Ono, Masahiro
AU  - Ono M
AD  - Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical 
      Sciences, Kyoto University, 46-29 Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 
      606-8501, Japan.. Electronic address: ono@pharm.kyoto-u.ac.jp.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20201026
PL  - United States
TA  - Nucl Med Biol
JT  - Nuclear medicine and biology
JID - 9304420
RN  - 0 (Benzofurans)
RN  - 0 (Gallium Radioisotopes)
RN  - 0 (Islet Amyloid Polypeptide)
RN  - 0 (Protein Aggregates)
RN  - 0 (Pyridines)
RN  - 4LJK511Z86 (Gallium-67)
RN  - LK6946W774 (benzofuran)
RN  - NH9L3PP67S (pyridine)
SB  - IM
MH  - Animals
MH  - Autoradiography
MH  - Benzofurans/*chemistry
MH  - *Gallium Radioisotopes
MH  - Islet Amyloid Polypeptide/*chemistry
MH  - Isotope Labeling
MH  - Mice
MH  - Pancreas/diagnostic imaging/*metabolism
MH  - *Protein Aggregates
MH  - Pyridines/*chemistry
OTO - NOTNLM
OT  - (67/68)Ga
OT  - Amylin
OT  - Imaging
OT  - Pancreas
OT  - Type 2 diabetes mellitus
EDAT- 2020/11/16 06:00
MHDA- 2021/09/28 06:00
CRDT- 2020/11/15 20:26
PHST- 2020/08/04 00:00 [received]
PHST- 2020/09/28 00:00 [revised]
PHST- 2020/10/17 00:00 [accepted]
PHST- 2020/11/16 06:00 [pubmed]
PHST- 2021/09/28 06:00 [medline]
PHST- 2020/11/15 20:26 [entrez]
AID - S0969-8051(20)30283-3 [pii]
AID - 10.1016/j.nucmedbio.2020.10.003 [doi]
PST - ppublish
SO  - Nucl Med Biol. 2020 Nov-Dec;90-91:93-97. doi: 10.1016/j.nucmedbio.2020.10.003. 
      Epub 2020 Oct 26.