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Mammalian TIMELESS and Tipin are evolutionarily conserved replication fork-associated factors.
International Union of Basic and Clinical Pharmacology. LXXXVI. Orexin Receptor Function, Nomenclature and Pharmacology
- A. Gotter, A. Webber, P. Coleman, J. Renger, C. Winrow
- Biology, PsychologyPharmacological Reviews
- 1 July 2012
Combined genetic and pharmacological approaches indicate that orexin signaling may represent a confluence of sleep, feeding, and reward pathways and selective oX2 receptor antagonism takes advantage of these properties toward the development of novel insomnia therapeutics.
Constructing a Feedback Loop with Circadian Clock Molecules from the Silkmoth, Antheraea pernyi*
- D. C. Chang, H. McWatters, Julie A Williams, A. Gotter, J. Levine, S. Reppert
- BiologyJournal of Biological Chemistry
- 3 October 2003
A complete feedback loop, resembling that found in Drosophila, can be constructed from silkmoth CLOCK, BMAL, PERIOD, and TIMELESS, and the results suggest that the circadian autoinhibitory feedback loop discovered in Dosophila is likely to be widespread among insects.
Illuminating the Circadian Clock in Monarch Butterfly Migration
It is reported that constant light, which disrupts circadian clock function at both the behavioral and molecular levels in monarchs, also disrupts the time-compensated component of flight navigation and shown that ultraviolet light is important for flight navigation but is not required for photic entrainment of circadian rhythms.
Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors
The orexin (also known as hypocretin) G protein–coupled receptors (GPCRs) regulate sleep and other behavioral functions in mammals, and are therapeutic targets for sleep and wake disorders. The human…
In Vitro Characterization of T-Type Calcium Channel Antagonist TTA-A2 and In Vivo Effects on Arousal in Mice
The discovery of the potent and selective T-type channel antagonist TTA-A2 has enabled us to study the in vivo effects of pharmacological T-channel inhibition on arousal in mice, and it will help to explore the validity of these channels as potential drug targets for sleep-related and other neurological diseases.
Discovery of a Pharmacologically Active Antagonist of the Two‐Pore‐Domain Potassium Channel K2P9.1 (TASK‐3)
The discovery and lead optimization efforts for a novel series of TASK‐3 channel antagonists based on a 5,6,7,8‐tetrahydropyrido[4,3‐d]pyrimidine high‐throughput screening lead from which a subseries of potent and selective inhibitors were identified were described.
A time-less function for mouse Timeless
It is shown that mTim is essential for embryonic development, but does not have substantiated circadian function.
Pharmacological characterization of MK-6096 – A dual orexin receptor antagonist for insomnia
Antagonism of T-type calcium channels inhibits high-fat diet-induced weight gain in mice.
What is believed to be a previously unknown role for T-type calcium channels in the regulation of sleep and weight maintenance is identified and the potential for a novel therapeutic approach to treating obesity is suggested.