Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:6.2.1.1 (
ACS
)
78,556
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
PD-132301, an inhibitor of sterol
O
-acyltransferase 1 (
SOAT1
; also known as acyl-coenzyme A:cholesterol acyltransferase-1, ACAT1), is under clinical investigation for numerous adrenal disorders. Radiolabeled
SOAT1
inhibitors could support drug discovery and help diagnose
SOAT1
-related disorders, such as atherosclerosis. We synthesized two radiolabeled
SOAT1
inhibitors, [
11
C]PD-132301 and fluorine analogue [
18
F]
1
. Rat biodistribution studies were conducted with both agents and, as the most selective tracer, [
11
C]PD-132301 was advanced to preclinical positron emission tomography studies in (atherosclerotic) ApoE
-/-
mice. The uptake of [
11
C]PD-132301 in
SOAT1
-rich tissue warrants further investigation into the compound as an atherosclerosis and adrenal imaging agent.
ACS
Med Chem Lett 2020 Jun 11
PMID:Synthesis and Evaluation of
11
C- and
18
F-Labeled SOAT1 Inhibitors as Macrophage Foam Cell Imaging Agents. 3255 Oct 15
