Melatonin receptor ligands: a pharmaco‐chemical perspective

JA Boutin, PA Witt‐Enderby, C Sotriffer… - Journal of pineal …, 2020 - Wiley Online Library
Melatonin MT1 and MT2 receptor ligands have been vigorously explored for the last 4
decades. Inspection of approximately 80 publications in the field revealed that most …

Indole-based melatonin analogues: Synthetic approaches and biological activity

SY Wang, XC Shi, P Laborda - European Journal of Medicinal Chemistry, 2020 - Elsevier
Melatonin is a natural hormone primarily released by the pineal gland that regulates the
sleep-wake cycles. The diverse biological applications of melatonin, together with the need …

Melatonin receptor structures shed new light on melatonin research

E Cecon, L Liu, R Jockers - Journal of pineal research, 2019 - Wiley Online Library
The tryptophan derivative melatonin is an evolutionary old molecule that is involved in a
pleiotropy of physiological functions. In humans, age‐related decline of circulating melatonin …

Structural insights into melatonin receptors

B Stauch, LC Johansson, V Cherezov - The FEBS journal, 2020 - Wiley Online Library
The long‐anticipated high‐resolution structures of the human melatonin G protein‐coupled
receptors MT1 and MT2, involved in establishing and maintaining circadian rhythm, were …

Melatonin–vorinostat hybrid ligands show higher histone deacetylase and cancer cell growth inhibition than vorinostat

YY Helmi, N Papenkordt, G Rennar… - Archiv der …, 2023 - Wiley Online Library
Anticancer drug conjugates are an emerging approach for future cancer treatment. Here, we
report a series of hybrid ligands merging the neurohormone melatonin with the approved …

In silico drug discovery of melatonin receptor ligands with therapeutic potential

GM Elisi, L Scalvini, A Lodola, A Bedini… - Expert Opinion on …, 2022 - Taylor & Francis
Introduction The neurohormone melatonin (N-acetyl-5-methoxytryptamine) regulates
circadian rhythms exerting a variety of effects in the central nervous system and in periphery …

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

A Bedini, JA Boutin, C Legros… - Journal of Pineal …, 2024 - Wiley Online Library
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 …

Luminogenic HiBiT peptide-based NanoBRET ligand binding assays for melatonin receptors

F Gbahou, S Levin, IG Tikhonova… - ACS Pharmacology & …, 2022 - ACS Publications
The two human melatonin receptors MT1 and MT2, which belong to the G protein-coupled
receptor (GPCR) family, are important drug targets with approved indications for circadian …

Cancer Cells Show Higher Sensitivity to Melatonin-Tamoxifen Drug Conjugates than to Combination of Melatonin and Tamoxifen

MA Marzouk, S Greco, F Gbahou, J Küblbeck… - ACS …, 2024 - ACS Publications
Drug conjugates of tamoxifen and melatonin linked through the amide side chain of
melatonin (4a, 4b) were reported as promising agents for future treatment of breast cancer …

Synthesis and antitumor activity of daunorubicin conjugates with of 3, 4-methylendioxybenzaldehyde

AA Moiseeva, OI Artyushin, LV Anikina… - Bioorganic & Medicinal …, 2019 - Elsevier
The design of hybrid (chimeric) molecules containing two different pharmacophores
connected via a spacer (linker) is a promising approach to the functionalization of natural …