Fatty acid amide hydrolase inhibition for treatment of amyotrophic lateral sclerosis
(2026) In JCI Insight- Abstract
Amyotrophic lateral sclerosis (ALS) is a devastating neurodegenerative disease caused by the selective loss of upper and lower motor neurons. There is a considerable variability in the disease progression of sporadic ALS, but the molecular basis for phenotypic heterogeneity remains largely unknown. ALS patients often manifest systemic metabolic abnormalities such as glucose intolerance and hypermetabolic state. We conducted reverse translational research to explore therapeutic targets in ALS based on the systemic metabolic alterations in patients and identified several metabolites associated with the disease progression, including metabolites involved in the expanded endocannabinoid system (ECS). In particular, the levels of N-acyl... (More)
Amyotrophic lateral sclerosis (ALS) is a devastating neurodegenerative disease caused by the selective loss of upper and lower motor neurons. There is a considerable variability in the disease progression of sporadic ALS, but the molecular basis for phenotypic heterogeneity remains largely unknown. ALS patients often manifest systemic metabolic abnormalities such as glucose intolerance and hypermetabolic state. We conducted reverse translational research to explore therapeutic targets in ALS based on the systemic metabolic alterations in patients and identified several metabolites associated with the disease progression, including metabolites involved in the expanded endocannabinoid system (ECS). In particular, the levels of N-acyl taurines (NATs) were correlated with the longitudinal change in the revised ALS functional rating scale and survival. Experiments with ALS cellular models, iPS cells derived from ALS patients and SOD1G93A transgenic mice revealed that PF-04457845, a fatty acid amide hydrolase inhibitor, upregulated the expanded ECS, particularly the levels of NATs and ameliorated motor neuron degeneration through the regulation of microglial environment, synapse plasticity, and neuronal development. These results collectively indicate that dysregulation of NATs is associated with ALS progression and PF-04457845 may represent a potential disease-modifying therapy for ALS.
(Less)
- author
- publishing date
- 2026-06-11
- type
- Contribution to journal
- publication status
- epub
- subject
- in
- JCI Insight
- publisher
- The American Society for Clinical Investigation
- external identifiers
-
- pmid:42275159
- ISSN
- 2379-3708
- DOI
- 10.1172/jci.insight.198842
- language
- English
- LU publication?
- no
- id
- 35ec5712-4a39-4525-93bc-25fb35f1648b
- date added to LUP
- 2026-06-15 11:36:26
- date last changed
- 2026-06-15 13:40:06
@article{35ec5712-4a39-4525-93bc-25fb35f1648b,
abstract = {{<p>Amyotrophic lateral sclerosis (ALS) is a devastating neurodegenerative disease caused by the selective loss of upper and lower motor neurons. There is a considerable variability in the disease progression of sporadic ALS, but the molecular basis for phenotypic heterogeneity remains largely unknown. ALS patients often manifest systemic metabolic abnormalities such as glucose intolerance and hypermetabolic state. We conducted reverse translational research to explore therapeutic targets in ALS based on the systemic metabolic alterations in patients and identified several metabolites associated with the disease progression, including metabolites involved in the expanded endocannabinoid system (ECS). In particular, the levels of N-acyl taurines (NATs) were correlated with the longitudinal change in the revised ALS functional rating scale and survival. Experiments with ALS cellular models, iPS cells derived from ALS patients and SOD1G93A transgenic mice revealed that PF-04457845, a fatty acid amide hydrolase inhibitor, upregulated the expanded ECS, particularly the levels of NATs and ameliorated motor neuron degeneration through the regulation of microglial environment, synapse plasticity, and neuronal development. These results collectively indicate that dysregulation of NATs is associated with ALS progression and PF-04457845 may represent a potential disease-modifying therapy for ALS.</p>}},
author = {{Ito, Daisuke and Iida, Madoka and Iguchi, Yohei and Hashizume, Atsushi and Yamada, Shinichiro and Kishimoto, Yoshiyuki and Komori, Shota and Obara, Kazuki and Nishisaki, Shuto and Yokoi, Satoshi and Shimamura, Teppei and Takemoto, Yuto and Nakatochi, Masahiro and Akashi, Tomohiro and Hinohara, Kunihiko and Lee-Okada, Hyeon-Cheol and Okada, Yohei and Niwa, Junichi and Sobue, Gen and Tanaka, Shinji and Takashina, Ken and Yokomizo, Takehiko and Katsuno, Masahisa}},
issn = {{2379-3708}},
language = {{eng}},
month = {{06}},
publisher = {{The American Society for Clinical Investigation}},
series = {{JCI Insight}},
title = {{Fatty acid amide hydrolase inhibition for treatment of amyotrophic lateral sclerosis}},
url = {{http://dx.doi.org/10.1172/jci.insight.198842}},
doi = {{10.1172/jci.insight.198842}},
year = {{2026}},
}
