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Last update 08 May 2025

ACAT1

Last update 08 May 2025

Basic Info

Synonyms

ACAT, ACAT1, acetoacetyl Coenzyme A thiolase

+ [7]

Introduction

This is one of the enzymes that catalyzes the last step of the mitochondrial beta-oxidation pathway, an aerobic process breaking down fatty acids into acetyl-CoA (PubMed:1715688, PubMed:7728148, PubMed:9744475). Using free coenzyme A/CoA, catalyzes the thiolytic cleavage of medium- to long-chain 3-oxoacyl-CoAs into acetyl-CoA and a fatty acyl-CoA shortened by two carbon atoms (PubMed:1715688, PubMed:7728148, PubMed:9744475). The activity of the enzyme is reversible and it can also catalyze the condensation of two acetyl-CoA molecules into acetoacetyl-CoA (PubMed:17371050). Thereby, it plays a major role in ketone body metabolism (PubMed:1715688, PubMed:17371050, PubMed:7728148, PubMed:9744475).

Drugs associated with ACAT1

447C88

Target

ACAT1

Mechanism

ACAT1 inhibitors

Active Org.-

Originator Org.

GSK Plc

Active Indication-

Inactive Indication

Hyperlipidemias

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

FR-129169

Target

ACAT1

Mechanism

ACAT1 inhibitors

Active Org.-

Originator Org.

Astellas Pharma, Inc.

Active Indication-

Inactive Indication

Hypercholesterolemia

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

PD-13201-2

Target

ACAT1

Mechanism

ACAT1 inhibitors

Active Org.-

Originator Org.

Parke-Davis & Co. Ltd.

Active Indication-

Inactive Indication

Atherosclerosis [+1]

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with ACAT1

NCT00078026

/ TerminatedPhase 1/2

A Phase I/II Randomized Study of the Short-Term Effects of APOMINE vs Placebo in Postmenopausal Women With Osteoporosis or Low Bone Mass

Osteoporosis affects millions of postmenopausal women in the USA. The current approved treatments are all drugs that prevent bone loss and possibly result in small gains in bone mass. Another possible treatment consists of drugs that increase bone formation. There are currently two drugs that stimulate bone formation, sodium fluoride and human parathyroid hormone (hPTH). Neither of these two drugs has been approved by the FDA. APOMINE has shown significant bone formation in animal studies. In this study we plan to test whether APOMINE is able to stimulate new bone formation in women with osteoporosis or low bone mass.

Start Date01 Aug 2003

Sponsor / Collaborator

Genzyme Corp.

NCT00004049

/ CompletedPhase 1

A Phase I and Pharmacokinetic Study of SR-45023A Administered Once Every 7 Days

RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die.
PURPOSE: Phase I trial to study the effectiveness of SR-45023A in treating patients who have locally advanced or metastatic solid tumors that have not responded to previous treatment.

Start Date01 Apr 1999

Sponsor / Collaborator

Genzyme Corp.

NCT00003822

/ CompletedPhase 1

A Phase I and Pharmacokinetic Study of SR-45023A During a 14-Day Treatment Schedule

Start Date01 Aug 1998

Sponsor / Collaborator

Genzyme Corp.

100 Clinical Results associated with ACAT1

100 Translational Medicine associated with ACAT1

0 Patents (Medical) associated with ACAT1

879

Literatures (Medical) associated with ACAT1

01 Sep 2025·Journal of Pharmaceutical and Biomedical Analysis

Interspecies comparison on the O-methylation metabolism of LJR003, a novel immunomodulator targeting acetyl-CoA acetyltransferase 1

Article

Author: Chen, Xiaoguang ; Liu, Xiaoyu ; Sheng, Li ; Zhao, Yanshi ; Chang, Yongchun ; Zhang, Weilin ; Chen, Jieyi ; Luo, Lijun ; Ji, Ming

Catechol structures are essential for drug activity and can undergo meta- or para-methylation, which affects their pharmacological properties. The regioselectivity and species differences in O-methylation metabolism significantly influence drug efficacy and toxicity, requiring further study. LJR003, an immunomodulator with a catechol structure, targets acetyl-CoA acetyltransferase 1 (ACAT1), a potential target for cancer immunotherapy. This study investigated the activity, methylation regioselectivity, and species differences of LJR003 and its methylated metabolites. Pharmacokinetic studies were conducted in rats, mice, and dogs, and methylation regioselectivity was analyzed in liver, kidney, and erythrocytes from these species and humans after LJR003 incubation. Results showed that meta-methylated LJR003 had weaker ACAT1 inhibitory activity and higher systemic exposure than LJR003 in rats, mice, and dogs. Erythrocytes exhibited the lowest methylation activity in vitro, while liver catalytic efficiency in rats, mice, and dogs was at least twice that of the kidney. In humans, liver and kidney showed similar catalytic activity. LJR003 favored meta-methylation in mice, dogs, and humans in vitro, with consistent in vivo results in mice and dogs. Rats displayed a unique metabolic pattern, suggesting species-specific differences. In conclusion, LJR003 is predicted to undergo meta-methylation in humans, contributing to its pharmacological effects alongside the parent compound. These findings improve understanding of methylation metabolism and provide insights for developing catechol-based drugs, emphasizing the importance of species-specific metabolic pathways in drug development.

01 Jun 2025·Metabolic Engineering Communications

Production of borneol, camphor, and bornyl acetate using engineered Saccharomyces cerevisiae

Article

Author: Kondo, Akihiko ; Tominaga, Masahiro ; Ogawa, Hiro ; Kawakami, Kazuma ; Ishii, Jun ; Nakamura, Tomomi

Microbial production of bicyclic monoterpenes is of great interest because their production primarily utilizes non-sustainable resources. Here, we report an engineered Saccharomyces cerevisiae yeast that produces bicyclic monoterpenes, including borneol, camphor, and bornyl acetate. The engineered yeast expresses a bornyl pyrophosphatase synthase from Salvia officinalis fused with mutated farnesyl pyrophosphate synthase from S. cerevisiae and two mevalonate pathway enzymes (an acetoacetyl-CoA thiolase/hydroxymethylglutaryl-CoA [HMG-CoA] reductase and an HMG-CoA synthase) from Enterococcus faecalis. The yeast produced up to 23.0 mg/L of borneol in shake-flask fermentation. By additionally expressing borneol dehydrogenase from Pseudomonas sp. TCU-HL1 or bornyl acetyltransferase from Wurfbainia villosa, the engineered yeast produced 23.5 mg/L of camphor and 21.1 mg/L of bornyl acetate, respectively. This is the first report of heterologous production of camphor and bornyl acetate.

01 Jun 2025·Biochemistry and Biophysics Reports

Intrinsic Alu affects for RNA splicing in a minigene model

Article

Author: Imanaka, Bunta ; Kimoto, Yuma ; Nakama, Mina

Alu elements are commonly located in the introns of primate genomes and, once transcribed, can alter splicing patterns. The insertion of an antisense Alu element into intron 9 was shown to enhance exon 10 skipping in a previously developed ACAT1 minigene model including exon 9-exon 11. This study investigates two intrinsic original Alus' role located in the intron in ACAT1 sequence using the same minigene splicing system. The deletion of intrinsic full AluSx originally located in intron 10 resulted in intron 10 retention, whereas the partial AluJb or antisense AluSx in the same intron was not sufficient for this process. Even normal splicing transcript wasn't shown without intrinsic full AluSx. Exon skipping was induced under the condition in which the intronic splice out prior to. Also, exon skipping was required with two close Alu elements with inverse orientations such as head-to-head and tail-to-tail in our minigene model. Intron retention seems to have been affected by shortening of introns or deletion of Alu's splicing regulatory elements. Either way, Alus are associated with human gene expression incorporating themself and adopting in the human genome splicing system.

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