Truncated Orexin Peptides: Structure–Activity Relationship Studies
نویسندگان
چکیده
منابع مشابه
Stapled truncated orexin peptides as orexin receptor agonists
The peptides orexin-A and -B, the endogenous agonists of the orexin receptors, have similar 19-amino-acid C-termini which retain full maximum response as truncated peptides with only marginally reduced potency, while further N-terminal truncations successively reduce the activity. The peptides have been suggested to bind in an α-helical conformation, and truncation beyond a certain critical len...
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In this study, we have compared the abilities of orexin-A and orexin-B and variants of orexin-A to activate different Ca(2+) responses (influx and release) in human OX(1) and OX(2) receptor- expressing Chinese hamster ovary cells. Responses mediated by activation of both receptor subtypes with either orexin-A or -B were primarily dependent on extracellular Ca(2+), suggesting similar activation ...
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Hypocretin/Orexin (H/O) neurons of the lateral hypothalamus are compelling modulator candidates for the chronobiology of neuroendocrine output and, as a consequence, hormone release from the anterior pituitary. Here we investigate the effects of H/O peptides upon tuberoinfundibular dopamine (TIDA) neurons - cells which control, via inhibition, the pituitary secretion of prolactin. In whole cell...
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Narcolepsy-cataplexy is a neurological disorder associated with the inability to maintain wakefulness and abnormal intrusions of rapid eye movement sleep-related phenomena into wakefulness such as cataplexy. The vast majority of narcoleptic-cataplectic individuals have low or undetectable levels of orexin (hypocretin) neuropeptides in the cerebrospinal fluid, likely due to specific loss of the ...
متن کاملOrexin and Orexin Receptors
“Reverse pharmacology”, i.e., ligand identification using cell lines expressing orphan receptors, combined with genetic engineering techniques, has increased our understanding of novel signaling systems in the body. Orexin is the first and most successful example of the factors to which such an approach was applied. Our group initially identified orexin A and orexin B as endogenous peptide liga...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2013
ISSN: 1948-5875,1948-5875
DOI: 10.1021/ml400333a