Tribuloside acts on the PDE/cAMP/PKA pathway to enhance melanogenesis, melanocyte dendricity and melanosome transport

Cao, Yan; Lv, Jinpeng; Tan, Yan; Chen, Ruolin; Jiang, Xiaoxue; Meng, Duo; Zou, Kun; Pan, Min; Tang, Liming

doi:10.1016/j.jep.2023.117673

Cited by 2 publications

(1 citation statement)

References 49 publications

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“…To identify increasingly effective PDE inhibitors, it is particularly important to choose appropriate screening methods. At present, the screening methods for PDE inhibitors mainly include 3 H adenine pre-labeling [6], enzyme-linked immunosorbent assay (ELISA) [7], fluorescence resonance energy transfer (FRET) [8], bioluminescence resonance energy transfer (BRET) [9], and PDE-Glo ™ determination [10]. The 3 H adenine pre-labeling method uses radioactive isotopes to label cAMP/cGMP, detect the number of remaining substrates, and determine enzyme activity [11].…”

Section: Introductionmentioning

confidence: 99%

The Construction and Application of a New Screening Method for Phosphodiesterase Inhibitors

Gao,

Wang,

Liu

et al. 2024

Biosensors

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Phosphodiesterases (PDEs), a superfamily of enzymes that hydrolyze cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), are recognized as a therapeutic target for various diseases. However, the current screening methods for PDE inhibitors usually experience problems due to complex operations and/or high costs, which are not conducive to drug development in respect of this target. In this study, a new method for screening PDE inhibitors based on GloSensor technology was successfully established and applied, resulting in the discovery of several novel compounds of different structural types with PDE inhibitory activity. Compared with traditional screening methods, this method is low-cost, capable of dynamically detecting changes in substrate concentration in live cells, and can be used to preliminarily determine the type of PDEs affected by the detected active compounds, making it more suitable for high-throughput screening for PDE inhibitors.

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Section: Introductionmentioning

confidence: 99%

The Construction and Application of a New Screening Method for Phosphodiesterase Inhibitors

Gao,

Wang,

Liu

et al. 2024

Biosensors

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Targeting Periplakin of Novel Benzenesulfonamides as Highly Selective Agonists for the Treatment of Vitiligo

Zhong,

Li,

Yan

et al. 2024

J. Med. Chem.

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Vitiligo is the most common cause of depigmentation worldwide, with immunosuppressive treatments often being inefficient and prone to recurrence, making it essential to identify new therapeutic targets. Periplakin (PPL) has been identified and confirmed as a key factor in vitiligo-related depigmentation. Based on this, a series of selective PPL agonists, specifically benzenesulfonamides, have been developed. Among these, compound I-3 exhibits superior efficacy compared to ruxolitinib, the only FDA-approved treatment for vitiligo. I-3 has been shown to increase cAMP levels by regulating PPL, which enhances MITF expression, a key transcription factor in melanin biosynthesis. Additionally, I-3 promotes melanin production by regulating tryptophan metabolism. In summary, PPL is a promising drug target, and I-3 has strong potential for future treatment of vitiligo due to its high selectivity and favorable druggability.

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Tribuloside acts on the PDE/cAMP/PKA pathway to enhance melanogenesis, melanocyte dendricity and melanosome transport

Cited by 2 publications

References 49 publications

The Construction and Application of a New Screening Method for Phosphodiesterase Inhibitors

The Construction and Application of a New Screening Method for Phosphodiesterase Inhibitors

Targeting Periplakin of Novel Benzenesulfonamides as Highly Selective Agonists for the Treatment of Vitiligo

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