Examination of families of neuropeptides and their receptors can provide information about phyletic relationships and evolutionary processes. Within an individual a given signal molecule may serve many diverse functions, mediated via subtypes of the receptor which may be coupled to their transdu...
Neuropeptide Y (NPY-(1–36)) acts on Y1 and Y2 receptors at the sympathetic neuroeffector junction. Various truncated NPY analogs were tested in the isolated guinea-pig caval vein where NPY is a vasoconstrictor (Y1 receptors) and in isolated rat vas deferens, by monitoring the suppression of ele...
Balasubramaniam, A. Neuropeptide Y family of hormones: Receptor subtypes and antagonists. Peptides 18(3) 445–457, 1997.—Neuropeptide Y (NPY) is the most abundant peptide present in the mammalian central and peripheral nervous system. NPY exhibits a variety of potent central and peripheral effe...
Increased levels of neuropeptide Y correlate with severity of left ventricular hypertrophy in vivo. At cardiomyocyte level, hypertrophy is characterised by increased mass and altered phenotype. The aims were to determine the contributions of increased synthesis and reduced degradation of protein...
In the early 1970's the term "neuropeptide" was used for the first time by David de Wied for peptides related to peptide hormones but with non-endocrine biological activity in the brain. This early notion appreciated neuropeptides as a specific class of chemical signals produced by neurons,...
Neuropeptides and neurohormones are among the more diverse and functionally important classes of cell-to-cell signaling molecules involved in animal development and behavior. Less is known about the hormones and neuropeptides of the red flour beetle, Tribolium castaneum, than many other insects....
We substituted a truncated neuropeptide Y (NPY) analog, [Pro30, Tyr32, Leu34]NPY(28-36)NH2 also called BVD15, at various positions with DOTA (1,4,7,10-tetraazacyclododecane-1,4,7-10-tetraacetic acid) and evaluated the effect of the coupling position with the binding affinity for NPY Y1 receptors...
The distribution of neuropeptide Y (NPY)-immunoreactive neurons was studied in human frontal cerebral cortex from surgical biopsy speciments by immunohistochemical techniques. NPY-containing neurons were identified in all cortical sublayers except sublayer I. The stained neurons were of the mult...
The compact synthesis of a new ring fused benzo[b]thieno derivative with an embedded nine-membered ring system via ring closing metathesis methodology is described. The preparation of the novel 11H-benzo[b]thieno[2,3-c]pyrrolo[2,3-a]indol-11-one via palladium-mediated oxidative cyclisation of be...
Synthesis, molecular structure and cytotoxic activity of a series of 3-C, N, S, Se substituted benzo[b]selenophene derivatives on human fibrosarcoma HT-1080, mouse hepatoma MG-22A, and mouse fibroblasts 3T3 cell lines are described. The correlation between compound LD50 3T3 fibroblast cell line ...
A-π-D-π-A type conjugated small molecules (COOP-nHT-BDT (n=1–4)) with a benzo[1,2-b:4,5-b']dithiophene (BDT) as the electron-donating core, 2-cyano-3-octyloxy-3-oxo-1-propenyl (COOP) as the terminal electron-accepting unit, and two regioregular oligo(3-hexylthiophene) (nHT) as π-conjuga...
The thioredoxin-like activity of human follicle stimulating hormone (hFSH), hFSH-β-(83–88) peptide amide (hFSH-β-(83–88) which has a sequence similar to the thioredoxin active center (-His-Cys-Gly-Lys-Cys-Asp-)) and thioredoxin-(31–36)-peptide amide (TD-(31–36) which contains the redox-act...
New approaches to sterilizing male animals are needed to control captive and wild animal populations. We sought to develop a nonsurgical method of permanent sterilization for male animals by administering the gonadotoxicant melphalan conjugated to peptides derived from the β-chain of FSHβ. We ...
SummarySynthetic peptides corresponding to hFSH-beta-(33–53) and hFSH-beta-(81–95) each contain free sulfhydryl groups, inhibit binding of FSH to receptor and are partial agonists of estradiol synthesis in Sertoli cells. Recently, we have reported that sulfhydryl groups are important in FSH- r...
The cDNAs of FSH and LH β subunits were isolated from Atlantic croaker pituitary. The isolated genes in croaker showed 35–75% and 60–75% identities with FSH and LH β of other teleosts, and 41% and 45% with human FSH and LH β, respectively. The homology models of croaker FSH and LH β were c...
We have previously reported that synthetic peptide amides corresponding to subdomains of the human FSH β-subunit, hFSH-β-(33–53) and hFSH-β-(81–95), interact with the external domain of the FSH receptor in two in vitro model systems. Consistent with these in vitro observations, we found tha...
The majority of patients with advanced ovarian cancer will experience a relapse and ultimately die from refractory diseases. Targeted therapy shows promise for these patients. Novel therapeutic strategies should be developed on the basis of the molecular mechanisms involved in ovarian cancer and...
Topotecan was loaded into large unilamellar vesicles using nigericin-generated pH gradient or with triethylammonium (TA) ion gradient. Despite that in both loading methods, the encapsulated counter ion was 5-sulfosalicylate (5ssa), the resultant formulations exhibited distinct properties. In NaC...
BACKGROUND: Anaplastic lymphoma kinase (ALK) inhibitor crizotinib has proven to be effective in the treatment of ALK-mutated neuroblastoma, but crizotinib resistance was commonly observed in patients. We aimed to overcome crizotinib resistance by combining with the MEK inhibitor trametinib or lo...
Topotecan (TPT), a highly active anticancer camptothecin drug, would benefit from nanocarrier-mediated site-specific and intracellular delivery because of a labile lactone ring whose hydrolysis inactivates the drug, poor cellular uptake resulting from both lactone hydrolysis and a titratable phe...
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