cAMP‐Specific Phosphodiesterases: Modulation, Inhibition, and Activation

Cameron, Ryan T.; Baillie, George S.

doi:10.1002/9781118185537.ch1

Cited by 4 publications

(4 citation statements)

References 170 publications

(222 reference statements)

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“…Rates of AEs reported with apremilast treatment decreased with longer-term ([52 weeks) exposure. Diarrhea and nausea, which are among the most common AEs associated with oral PDE4 inhibitors, 17 were predominantly mild or moderate in severity, occurred early, and resolved within the first month. Diarrhea induced by PDE4 inhibitors is thought to be secretory.…”

Section: Discussionmentioning

confidence: 99%

Long-term safety and tolerability of apremilast in patients with psoriasis: Pooled safety analysis for ≥156 weeks from 2 phase 3, randomized, controlled trials (ESTEEM 1 and 2)

Crowley

Thaçi

Joly

et al. 2017

Journal of the American Academy of Dermatology

151

126

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Section: Discussionmentioning

confidence: 99%

Long-term safety and tolerability of apremilast in patients with psoriasis: Pooled safety analysis for ≥156 weeks from 2 phase 3, randomized, controlled trials (ESTEEM 1 and 2)

Crowley

Thaçi

Joly

et al. 2017

Journal of the American Academy of Dermatology

151

126

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“…Various trials have reported diarrhea and nausea as one of the major adverse effects and patients don't need any routine laboratory investigations as no changes have been noticed. 13,38 In our study patients main side effects observed were nausea, headache, diarrhea. 14.2% had depression and psychiatric problems.…”

Section: Discussionmentioning

confidence: 55%

A comparative study of the efficacy and safety of oral apremilast versus oral methotrexate in patients with moderate to severe chronic plaque psoriasis

et al. 2018

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Background: Psoriasis is a chronic, inflammatory systemic disease. Methotrexate acts by inhibiting dihydrofolic reductase enzyme. Apremilast is an oral PDE4 inhibitor approved by US Food and Drug Administration for treatment of psoriasis.Methods: This is hospital based comparative study conducted from February 2018 to August 2018. Seventy patients above 18 years of age with chronic plaque psoriasis were divided into 35 patients in each group and were treated with oral Apremilast (30 mg twice daily) and oral methotrexate (15 mg per week in three divided doses with a 12-hour interval between doses and tab folic acid on methotrexate free days) and were evaluated every 4 weeks for a period of 16 weeks and followed-up at 24th week. Outcome was assessed on basis of psoriasis area-and-severity index score (PASI), psoriasis disability index (PDI) and clinical photographs.Results: % of improvement in Group-A patients (76.8%) after 16 weeks of treatment was relatively more (p<0.05) as compared to group B (71.5%). At the end of 16 weeks PASI score in methotrexate group was statistically significant (p<0.05) as compared to group B, PDI became 17.90±3.87 in group A and was statistically significant (p<0.05) as compared to group B which was 20.34±2.98. Side effects observed were comparatively less in group A patients.Conclusions: On comparing the two drugs, methotrexate was comparatively better tolerated and had better efficacy and safety. More studies are required to further prove the efficacy of Apremilast in treatment of psoriasis.

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“…Phosphodiesterase quenches the cAMP, so that the cellular concentration decreases when the E. gracilis cells are aligned with the gravity vector. The enzyme can be impaired by caffeine, theophylline, or IBM-X, which results in an increase in cellular cAMP [ 112 , 113 ]. Therefore, the application of these substances augments gravitaxis [ 114 ].…”

Section: Gravireceptor and Molecular Sensory Transduction Chain In ...mentioning

confidence: 99%

Euglena, a Gravitactic Flagellate of Multiple Usages

Häder

Hemmersbach

2022

Life

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Human exploration of space and other celestial bodies bears a multitude of challenges. The Earth-bound supply of material and food is restricted, and in situ resource utilisation (ISRU) is a prerequisite. Excellent candidates for delivering several services are unicellular algae, such as the space-approved flagellate Euglena gracilis. This review summarizes the main characteristics of this unicellular organism. Euglena has been exposed on various platforms that alter the impact of gravity to analyse its corresponding gravity-dependent physiological and molecular genetic responses. The sensory transduction chain of gravitaxis in E. gracilis has been identified. The molecular gravi-(mechano-)receptors are mechanosensory calcium channels (TRP channels). The inward gated calcium binds specifically to one of several calmodulins (CaM.2), which, in turn, activates an adenylyl cyclase. This enzyme uses ATP to produce cAMP, which induces protein kinase A, followed by the phosphorylation of a motor protein in the flagellum, initiating a course correction, and, finally, resulting in gravitaxis. During long space missions, a considerable amount of food, oxygen, and water has to be carried, and the exhaled carbon dioxide has to be removed. In this context, E. gracilis is an excellent candidate for biological life support systems, since it produces oxygen by photosynthesis, takes up carbon dioxide, and is even edible. Various species and mutants of Euglena are utilized as a producer of commercial food items, as well as a source of medicines, as it produces a number of vitamins, contains numerous trace elements, and synthesizes dietary proteins, lipids, and the reserve molecule paramylon. Euglena has anti-inflammatory, -oxidant, and -obesity properties.

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cAMP‐Specific Phosphodiesterases: Modulation, Inhibition, and Activation

Cited by 4 publications

References 170 publications

Long-term safety and tolerability of apremilast in patients with psoriasis: Pooled safety analysis for ≥156 weeks from 2 phase 3, randomized, controlled trials (ESTEEM 1 and 2)

Long-term safety and tolerability of apremilast in patients with psoriasis: Pooled safety analysis for ≥156 weeks from 2 phase 3, randomized, controlled trials (ESTEEM 1 and 2)

A comparative study of the efficacy and safety of oral apremilast versus oral methotrexate in patients with moderate to severe chronic plaque psoriasis

Euglena, a Gravitactic Flagellate of Multiple Usages

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