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Roflumilast inhibits tumor growth and migration in STK11/LKB1 deficient pancreatic cancer.
Zhang S, Yun D, Yang H, Eckstein M, Elbait GD, Zhou Y, Lu Y, Yang H, Zhang J, Dörflein I, Britzen-Laurent N, Pfeffer S, Stemmler MP, Dahl A, Mukhopadhyay D, Chang D, He H, Zeng S, Lan B, Frey B, Hampel C, Lentsch E, Gollavilli PN, Büttner C, Ekici AB, Biankin A, Schneider-Stock R, Ceppi P, Grützmann R, Pilarsky C. Zhang S, et al. Cell Death Discov. 2024 Mar 9;10(1):124. doi: 10.1038/s41420-024-01890-y. Cell Death Discov. 2024. PMID: 38461159 Free PMC article.
Mechanistic analyses revealed that STK11 knockout influences blood vessel morphogenesis and is closely associated with the enhanced expression of phosphodiesterases (PDEs), especially PDE4D, PDE4B, and PDE10A. PDE4 inhibitor Roflumilast inhibited STK11-KO cell migration an …
Mechanistic analyses revealed that STK11 knockout influences blood vessel morphogenesis and is closely associated with the enhanced expressi …
Mechanism of Huanglian Zhimu Decoction in improving hepatic lipid deposition in type 2 diabetes based on lipidomics and transcriptomics.
Tu W, Tian X, Fu H, Xu F, Wang H, Wang Q, Lin X, Shu J, Lin S, Cao L, Wang L. Tu W, et al. J Ethnopharmacol. 2025 Sep 25;353(Pt A):120309. doi: 10.1016/j.jep.2025.120309. Epub 2025 Jul 18. J Ethnopharmacol. 2025. PMID: 40684822
To validate the pathway specificity, pharmacological inhibition experiments were performed using roflumilast, a selective PDE4D antagonist. Lastly, the chemical composition of HLZMD was characterized through ultra-performance liquid chromatography coupled with quadrupole t …
To validate the pathway specificity, pharmacological inhibition experiments were performed using roflumilast, a selective PDE4D antag …
Identification of a novel PDE4 inhibitor inspired by leoligin-derived lignans.
Coffey C, Perhal AF, Richter W, Chen Y, Linder T, Schwaiger S, Mihovilovic MD, Kirchmair J, Schnürch M, Dirsch VM. Coffey C, et al. Eur J Med Chem. 2026 Jan 15;302(Pt 1):118285. doi: 10.1016/j.ejmech.2025.118285. Epub 2025 Oct 20. Eur J Med Chem. 2026. PMID: 41124883 Free article.
PDE4s are widely expressed and play key roles in various physiologic paradigms, including immune responses, memory, cognition, and metabolism. Marketed PDE4 inhibitors, such as roflumilast and apremilast, treat chronic obstructive pulmonary disease and psoriasis. Identific …
PDE4s are widely expressed and play key roles in various physiologic paradigms, including immune responses, memory, cognition, and metabolis …
Acute administration of roflumilast enhances sensory gating in healthy young humans in a randomized trial.
Heckman PRA, Van Duinen MA, Blokland A, Uz T, Prickaerts J, Sambeth A. Heckman PRA, et al. Psychopharmacology (Berl). 2018 Jan;235(1):301-308. doi: 10.1007/s00213-017-4770-y. Epub 2017 Nov 3. Psychopharmacology (Berl). 2018. PMID: 29098341 Free PMC article. Clinical Trial.
METHODS: The current study investigated the effects of the PDE4 inhibitor roflumilast in a sensory gating paradigm in 20 healthy young human volunteers (age range 18-30 years). ...CONCLUSION: The PDE4 inhibitor roflumilast has a favorable side-effect profile at a co …
METHODS: The current study investigated the effects of the PDE4 inhibitor roflumilast in a sensory gating paradigm in 20 healthy youn …
An experimental medicine study of the phosphodiesterase-4 inhibitor, roflumilast, on working memory-related brain activity and episodic memory in schizophrenia patients.
Gilleen J, Farah Y, Davison C, Kerins S, Valdearenas L, Uz T, Lahu G, Tsai M, Ogrinc F, Reichenberg A, Williams SC, Mehta MA, Shergill SS. Gilleen J, et al. Psychopharmacology (Berl). 2021 May;238(5):1279-1289. doi: 10.1007/s00213-018-5134-y. Epub 2018 Dec 8. Psychopharmacology (Berl). 2021. PMID: 30536081 Free PMC article. Clinical Trial.
OBJECTIVES: Based on animal models, we investigated the potential for roflumilast, a selective inhibitor of phosphodiesterase type 4 (PDE4), to improve cognition, which may act by increasing intracellular cyclic adenosine monophosphate in brain regions underlying cognitive …
OBJECTIVES: Based on animal models, we investigated the potential for roflumilast, a selective inhibitor of phosphodiesterase type 4 …
Inhibition of Phosphodiesterase 4 Suppresses Neuronal Ferroptosis After Cerebral Ischemia/Reperfusion.
Chen K, Xu B, Long L, Wen H, Zhao Q, Tu X, Wang J, Xu J, Wang H. Chen K, et al. Mol Neurobiol. 2025 Mar;62(3):3376-3395. doi: 10.1007/s12035-024-04495-9. Epub 2024 Sep 17. Mol Neurobiol. 2025. PMID: 39287745
PDE4B knockdown also enhanced the levels of GSH, ferroportin (FPN), and ferritin heavy chain 1 (FTH1). Consistently, inhibition of PDE4 by roflumilast (Roflu) produced similar effects as PDE4B knockdown. Roflu also ameliorated the morphology and membrane potential of the m …
PDE4B knockdown also enhanced the levels of GSH, ferroportin (FPN), and ferritin heavy chain 1 (FTH1). Consistently, inhibition of PDE4 by …