To the top

Page Manager: Webmaster
Last update: 9/11/2012 3:13 PM

Tell a friend about this page
Print version

Toward molecular imaging … - University of Gothenburg, Sweden Till startsida
Sitemap
To content Read more about how we use cookies on gu.se

Toward molecular imaging of the free fatty acid receptor 1

Journal article
Authors E. Hellstrom-Lindahl
O. Aberg
C. Ericsson
G. O'Mahony
P. Johnstrom
Stanko Skrtic
O. Eriksson
Published in Acta Diabetologica
Volume 54
Issue 7
Pages 663-668
ISSN 0940-5429
Publication year 2017
Published at Institute of Medicine
Pages 663-668
Language en
Links dx.doi.org/10.1007/s00592-017-0989-...
https://gup.ub.gu.se/file/207016
Keywords FFAR1, GPR40, Beta cell imaging, Islet imaging, Drug development, GLUCAGON-SECRETION, COUPLING REACTIONS, BETA-CELLS, GPR40, RADIOTRACERS, TAK-875, AGONIST, INSULIN, IODIDE
Subject categories Diabetology

Abstract

Molecular imaging of the free fatty acid receptor 1 (FFAR1) would be a valuable tool for drug development by enabling in vivo target engagement studies in human. It has also been suggested as a putative target for beta cell imaging, but the inherent lipophilicity of most FFAR1 binders produces high off-target binding, which has hampered progress in this area. The aim of this study was to generate a suitable lead compound for further PET labeling. In order to identify a lead compound for future PET labeling for quantitative imaging of FFAR1 in human, we evaluated tritiated small molecule FFAR1 binding probes ([H-3]AZ1, [H-3]AZ2 and [H-3]TAK-875) for their off-target binding, receptor density and affinity in human pancreatic tissue (islets and exocrine) and rodent insulinoma. [H-3]AZ1 showed improved specificity to FFAR1, with decreased off-target binding compared to [H-3]AZ2 and [H-3]TAK-875, while retaining high affinity in the nanomolar range. FFAR1 density in human islets was approximately 50% higher than in exocrine tissue. AZ1 is a suitable lead compound for PET labeling for molecular imaging of FFAR1 in humans, due to high affinity and reduced off-target binding.

Page Manager: Webmaster|Last update: 9/11/2012
Share:

The University of Gothenburg uses cookies to provide you with the best possible user experience. By continuing on this website, you approve of our use of cookies.  What are cookies?

Denna text är utskriven från följande webbsida:
http://www.gu.se/english/research/publication/?publicationId=255280
Utskriftsdatum: 2019-12-15