Targeting Sterol O-Acyltransferase/Acyl-CoA:Cholesterol Acyltransferase (ACAT): A Perspective on Small-Molecule Inhibitors and Their Therapeutic Potential

P Bhattacharjee, N Rutland, MR Iyer - Journal of Medicinal …, 2022 - ACS Publications
Sterol O-acyltransferase (SOAT) is a membrane-bound enzyme that aids the esterification of
cholesterol and fatty acids to cholesterol esters. SOAT has been studied extensively as a …

Chemical case studies from natural products of recent interest in the crop protection industry

G Späth, O Loiseleur - Natural Product Reports, 2024 - pubs.rsc.org
Covering: up to 2024 This review showcases selected natural products, which are of high
relevance to the craft of crop protection, including in its most recent aspects such as their …

Acyltransferase inhibitors: a patent review (2010–present)

T Ohshiro, H Tomoda - Expert Opinion on Therapeutic Patents, 2015 - Taylor & Francis
Introduction: Acyltransferase (AT) catalyzes the transfer of an acyl moiety from acyl-
coenzyme A (acyl-CoA) to an acceptor. ATs play important roles in the maintenance of …

Exploration of marine natural resources in Indonesia and development of efficient strategies for the production of microbial halogenated metabolites

H Yamazaki - Journal of natural medicines, 2022 - Springer
Nature is a prolific source of organic products with diverse scaffolds and biological activities.
The process of natural product discovery has gradually become more challenging, and …

Structure–Activity Relationships of the Antimalarial Agent Artemisinin 10. Synthesis and Antimalarial Activity of Enantiomers of rac-5β-Hydroxy-d-Secoartemisinin …

M Jahan, F Leon, FR Fronczek, KM Elokely, J Rimoldi… - Molecules, 2021 - mdpi.com
An efficient synthesis of rac-6-desmethyl-5β–hydroxy-d-secoartemisinin 2, a tricyclic analog
of R-(+)-artemisinin 1, was accomplished and the racemate was resolved into the (+)-2b and …

Discovery of selective ACAT2 antagonist via a combination strategy based on deep docking, pharmacophore modelling, and molecular dynamics simulation

Y Liu, F Ding, L Deng, S Zhang, L Wu… - Journal of Enzyme …, 2024 - Taylor & Francis
Acyl-CoA: cholesterol acyltransferase (ACAT), a pivotal enzyme in the absorption and
metabolism of cholesterol, is primarily responsible for intracellular esterification. ACAT …

Phenylpyropenes E and F: new meroterpenes from the marine-derived fungus Penicillium concentricum ZLQ-69

Z Ding, L Zhang, J Fu, Q Che, D Li, Q Gu… - The Journal of …, 2015 - nature.com
Two new meroterpenes, phenylpyropenes E (1) and F (2), together with seven known
phenylpyropenes (3–5) and pyripyropenes (6–9) were isolated from the marine-derived …

Identification of potential ACAT-2 selective inhibitors using pharmacophore, SVM and SVR from Chinese herbs

L Qiao, X Zhang, L Jiang, Y Zhang, G Li - Molecular diversity, 2016 - Springer
Acyl-coenzyme A cholesterol acyltransferase (ACAT) plays an important role in maintaining
cellular and organismal cholesterol homeostasis. Two types of ACAT isozymes with different …

Characterization of two acetyltransferase genes in the pyripyropene biosynthetic gene cluster from Penicillium coprobium

J Hu, A Furutani, K Yamamoto, K Oyama… - Biotechnology & …, 2014 - Taylor & Francis
Pyripyropenes potently and selectively inhibit acyl-CoA: cholesterol acyltransferase 2 (ACAT-
2). Among multiple isomers of pyripyropene (A to R), pyripyropene A (PyA) has insecticidal …

In vitro metabolism of pyripyropene A and ACAT inhibitory activity of its metabolites

D Matsuda, T Ohshiro, M Ohtawa, H Yamazaki… - The Journal of …, 2015 - nature.com
Abstract Pyripyropene A (PPPA, 1) of fungal origin, a selective inhibitor of acyl-CoA:
cholesterol acyltransferase 2 (ACAT2), proved orally active in atherogenic mouse models …