Why Are We Still Cloning Melatonin Receptors? A Commentary

Gautier, Célia; Théret, Isabelle; Lizzo, Giulia; Ferry, Gilles; Guenin, Sophie-Pénélope

doi:10.1007/978-1-0716-2593-4_29

Cited by 7 publications

(9 citation statements)

References 50 publications

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“…Recent studies have confirmed that melatonin and its indolic and kynurenic derivatives downstream the pathway of melanogenesis, causing a drop in the cyclic adenosine monophosphate (cAMP) level and the microphthalmia-associated transcription factor (MITF) and causing the resultant collapse in tyrosinase (TYR) activity and melanin content. These findings can be a breakthrough for the future studies on pigmentation in melanoma therapies [122,142,[196][197][198][199]. Since the inhibition of melanogenesis in advanced melanomas can serve as an adjuvant strategy in the systemic therapy of melanoma [200], melatonin as a mitochondrial protector with anti-inflammatory properties and direct antioxidants should be explored in topical and transepidermal delivery, especially in skin damage after UVR exposition.…”

Section: Melanoma: a Tumor Of Melanocyte Originmentioning

confidence: 95%

Melatonin/Sericin Wound Healing Patches: Implications for Melanoma Therapy

Adamiak,

Gaida,

Schäfer

et al. 2024

IJMS

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Melatonin and sericin exhibit antioxidant properties and may be useful in topical wound healing patches by maintaining redox balance, cell integrity, and regulating the inflammatory response. In human skin, melatonin suppresses damage caused by ultraviolet radiation (UVR) which involves numerous mechanisms associated with reactive oxygen species/reactive nitrogen species (ROS/RNS) generation and enhancing apoptosis. Sericin is a protein mainly composed of glycine, serine, aspartic acid, and threonine amino acids removed from the silkworm cocoon (particularly Bombyx mori and other species). It is of interest because of its biodegradability, anti-oxidative, and anti-bacterial properties. Sericin inhibits tyrosinase activity and promotes cell proliferation that can be supportive and useful in melanoma treatment. In recent years, wound healing patches containing sericin and melatonin individually have attracted significant attention by the scientific community. In this review, we summarize the state of innovation of such patches during 2021–2023. To date, melatonin/sericin-polymer patches for application in post-operational wound healing treatment has been only sparingly investigated and it is an imperative to consider these materials as a promising approach targeting for skin tissue engineering or regenerative dermatology.

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Section: Melanoma: a Tumor Of Melanocyte Originmentioning

confidence: 95%

Melatonin/Sericin Wound Healing Patches: Implications for Melanoma Therapy

Adamiak,

Gaida,

Schäfer

et al. 2024

IJMS

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“…Nowadays, functional MTRs have been cloned from various species, such as human, rat, mouse, sheep, rabbit, hamster, chicken, fish, xenopus, platypus etc. 15,16 Most recent alignment of sequences from 300 vertebrates revealed the likely existence of four ancestral vertebrate MTR subtypes named Mel1a, Mel1b, Mel1c and Mel1d, with Mel1d being closely related to Mel1a and Mel1c to Mel1b. 17 While Mel1d was lost in mammals and birds, Mel1c evolved into GPR50 in eutherian mammals and lost its high-affinity melatonin binding property, 18,19 most likely because of altered structural features in the 2nd extracellular loop (ECL2) important for melatonin binding.…”

Section: Mtrs Discovery and Classificationmentioning

confidence: 99%

“…Nowadays, functional MTRs have been cloned from various species, such as human, rat, mouse, sheep, rabbit, hamster, chicken, fish, xenopus, platypus etc 15,16 . Most recent alignment of sequences from 300 vertebrates revealed the likely existence of four ancestral vertebrate MTR subtypes named Mel1a, Mel1b, Mel1c and Mel1d, with Mel1d being closely related to Mel1a and Mel1c to Mel1b 17 .…”

Section: Mtrs Discovery and Classificationmentioning

confidence: 99%

Melatonin receptor structure and signaling

Okamoto,

Cecon,

Nureki

et al. 2024

Journal of Pineal Research

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Melatonin (5‐methoxy‐N‐acetyltryptamine) binds with high affinity and specificity to membrane receptors. Several receptor subtypes exist in different species, of which the mammalian MT1 and MT2 receptors are the best‐characterized. They are members of the G protein‐coupled receptor superfamily, preferentially coupling to Gi/o proteins but also to other G proteins in a cell‐context‐depending manner. In this review, experts on melatonin receptors will summarize the current state of the field. We briefly report on the discovery and classification of melatonin receptors, then focus on the molecular structure of human MT1 and MT2 receptors and highlight the importance of molecular simulations to identify new ligands and to understand the structural dynamics of these receptors. We then describe the state‐of‐the‐art of the intracellular signaling pathways activated by melatonin receptors and their complexes. Brief statements on the molecular toolbox available for melatonin receptor studies and future perspectives will round‐up this review.

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“…Physiological melatonin acts through two G proteincoupled receptors, MT 1 and MT 2 in mammals. It is worth mentioning that other targets of melatonin have been described over the years, including NQO2 (MT 3 ), 6 and other proteins the list of which can be found in the exhaustive review from Liu et al 7 Other melatonin receptors might exist in several animal species, such as insects, and fishes, 8 as well as in plants 9,10 (see below). The role and characteristics of those other receptors is poorly described from a pharmacological point of view.…”

Section: Melatonin Receptorsmentioning

confidence: 99%

“…The general theory was that the more thermostable a protein was, the more likely it was to crystalize "easily," 46 once purified to homogeneity. 47,48 Our studies were still in their infancy 8 when the crystallization was beautifully reported by Stevens group 17,18 and served the purpose of discovering new ligands. 49…”

Section: Tools: the Gene And The Proteinmentioning

confidence: 99%

Industrial and academic approaches to the search for alternative melatonin receptor ligands: An historical survey

Bedini,

Boutin,

Legros

et al. 2024

Journal of Pineal Research

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The search for melatonin receptor agonists formed the main part of melatonin medicinal chemistry programs for the last three decades. In this short review, we summarize the two main aspects of these programs: the development of all the necessary tools to characterize the newly synthesized ligands at the two melatonin receptors MT1 and MT2, and the medicinal chemist's approaches to find chemically diverse ligands at these receptors. Both strategies are described. It turns out that the main source of tools were industrial laboratories, while the medicinal chemistry was mainly carried out in academia. Such complete accounts are interesting, as they delineate the spirits in which the teams were working demonstrating their strength and innovative character. Most of the programs were focused on nonselective agonists and few of them reached the market. In contrast, discovery of MT1‐selective agonists and melatonergic antagonists with proven in vivo activity and MT1 or MT2‐selectivity is still in its infancy, despite the considerable interest that subtype selective compounds may bring in the domain, as the physiological respective roles of the two subtypes of melatonin receptors, is still poorly understood. Poly‐pharmacology applications and multitarget ligands have also been considered.

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Why Are We Still Cloning Melatonin Receptors? A Commentary

Cited by 7 publications

References 50 publications

Melatonin/Sericin Wound Healing Patches: Implications for Melanoma Therapy

Melatonin/Sericin Wound Healing Patches: Implications for Melanoma Therapy

Melatonin receptor structure and signaling

Industrial and academic approaches to the search for alternative melatonin receptor ligands: An historical survey

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