Light exposure at night can disrupt the circadian timing of cellular processes and is associated with a broad range of health disorders. To spectrally engineer lighting which minimizes circadian disruption at night it is necessary to define the precise spectral sensitivity of the human circadian system. Prior attempts have used short monochromatic light exposures in dark-adapted human subjects, or dark-adapted isolated retina or melanopsin. However, humans spend virtually all their awake hours in a fully light-adapted state. Here we review the evidence for a narrow blue circadian sensitivity curve for light-adapted humans derived from experiments using spectral filtering of light sources, and comparisons of light sources with diverse spectral power distributions. This light-adapted Circadian Potency function permits the development of circadian-protective light for nocturnal use and circadian-entraining light for daytime use.
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ACS Chem Neurosci
January 2025
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Jagtvej 160, 2100 Copenhagen, Denmark.
The serotonin 7 receptor (5-HTR) regulates various processes in the central nervous system, including mood, learning, and circadian rhythm control, among others. Receptor activation can lead to activation of the Gα protein and a subsequent increase of intracellular cyclic adenosine monophosphate (cAMP). Receptor interaction with inverse agonists results in a decrease of basal cAMP levels and therefore a downstream effect of reduced neuronal excitability and neurotransmission.
View Article and Find Full Text PDFCureus
December 2024
School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, IND.
Aim Traditional Ayurvedic herbo-mineral medicines have proven their potential in managing COVID-19. Cell-based assays of the Svarnvir-IV tablet demonstrated the virucidal activity against SARS-CoV-2 and its therapeutic action, along with safety in cytotoxicity, has been proved. In the present study, in vivo, safety profile and compositional analysis of the Svarnvir-IV tablet were performed.
View Article and Find Full Text PDFJ Mammary Gland Biol Neoplasia
November 2024
Department of Developmental Biology and Genetics, Institut Curie, INSERM U934, CNRS UMR3215, Sorbonne University, Paris, France.
Following previous editions, the fifteenth annual workshop of the European Network for Breast Development and Cancer (ENBDC) on Methods in Mammary Gland Biology and Breast Cancer was held from the 2nd to the 4th of May in Weggis, Switzerland. Over the course of this meeting, participants followed and discussed presentations from a roster of internationally renowned invited speakers and selected abstracts, complemented with two poster sessions covering exciting unpublished results. The sessions covered projects on normal mammary gland development, breast cancer evolution and metastasis, as well as epigenetic and metabolic regulation of breast cancer.
View Article and Find Full Text PDFBackground: It has been reported that circadian clock components, Brain and Muscle ARNT-Like 1 (BMAL1) and Circadian Locomotor Output Cycles Kaput (CLOCK), are uniquely essential for glioblastoma (GBM) stem cell (GSC) biology and survival. Consequently, we developed a novel Cryptochrome (CRY) activator SHP1705, which inhibits BMAL1-CLOCK transcriptional activity.
Methods: We analyzed buffy coats isolated from Phase 1 clinical trial subjects' blood to assess any changes to circadian, housekeeping, and blood transcriptome-based biomarkers following SHP1705 treatment.
Bioorg Med Chem Lett
November 2024
Department of Chemistry, University of Nebraska at Kearney, Kearney, NE 69949, USA. Electronic address:
Arylalkylamine N-acetyltransferase (AANAT) catalyzes the rate-limiting step in melatonin synthesis and is a potential target for disorders involving melatonin overproduction, such as seasonal affective disorder. Previously described AANAT inhibitor bromoacetyltryptamine (BAT) and benzothiophenes analogs were reported to react with CoASH to form potent bisubstrate inhibitors through AANAT's alkyltransferase function, which is secondary to its role as an acetyltransferase. We replaced the bromoacetyl group in BAT with various Michael acceptors to mitigate possible off-target activity of its bromoacetyl group.
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