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Identification of lead compounds for (99m)Tc and (18)F GPR91 radiotracers.


ABSTRACT: To develop the first radiotracer targeting GPR91, a cell membrane-bound receptor that modulates the cellular response to hyperglycemia and hypoxia, we designed and prepared a small series of compounds based on a published series of 1,8-naphthyridines with high affinity to GPR91. Our approach provides a mechanism to incorporate radioactive atoms ((99m)Tc and (18)F) into the GPR91 pharmacophore as the final synthetic step. Pharmacological assays confirmed lead compounds for (99m)Tc and (18)F GPR91 radiotracers within the series.

SUBMITTER: Klenc J 

PROVIDER: S-EPMC4433761 | biostudies-literature | 2015 Jun

REPOSITORIES: biostudies-literature

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Identification of lead compounds for (99m)Tc and (18)F GPR91 radiotracers.

Klenc Jeffrey J   Lipowska Malgorzata M   Taylor Andrew T AT  

Bioorganic & medicinal chemistry letters 20150411 11


To develop the first radiotracer targeting GPR91, a cell membrane-bound receptor that modulates the cellular response to hyperglycemia and hypoxia, we designed and prepared a small series of compounds based on a published series of 1,8-naphthyridines with high affinity to GPR91. Our approach provides a mechanism to incorporate radioactive atoms ((99m)Tc and (18)F) into the GPR91 pharmacophore as the final synthetic step. Pharmacological assays confirmed lead compounds for (99m)Tc and (18)F GPR91  ...[more]

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