Development of a new sigma-2 receptor ligand for imaging and BNCT

2019 Fiscal Year Final Research Report

• Project/Area Number: 17K10355
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Radiation science
• Research Institution: Kanazawa University
• Principal Investigator: Kozaka Takashi 金沢大学, 学際科学実験センター, 助教 (50579836)
• Project Period (FY): 2017-04-01 – 2020-03-31
• Keywords: vesamicol

Outline of Final Research Achievements

For the purpose of the fusion of tumor image diagnosis and the boron neutron capture therapy, I had studied the development of the boron-containing imaging agent to have high affinity and selectivity to σ-2 receptor. Various new designed vesamicol relatives showed high affinity to σ receptor in in vitro screening. The boron-containing compound were performed the in vitro cellular uptake test using human malignant melanoma A375 cells, but the content of boron in all samples were 10 ng/mL. However, I found that new compounds having limonene frame showed 14 times more σ-2 receptor affinity than σ-1 receptor affinity.

Free Research Field

放射線化学

Academic Significance and Societal Importance of the Research Achievements

σ-2受容体は、乳がんや悪性黒色腫など多様な固形腫瘍細胞において高い発現が認められる上、増殖状態ではその発現が著しく増加していることが知られている。その機構はまだ不明な点が多いが、σ-2受容体アンタゴニストが抗がん作用を示すことも報告されている。今回開発したlimonene骨格を有する新規化合物は高いσ-2受容体選択性を示すことから、PETやSPECTによる腫瘍イメージング剤や抗がん剤のリード化合物として更なる研究を行う価値があると考えている。