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- W3136164482 endingPage "100808" @default.
- W3136164482 startingPage "100808" @default.
- W3136164482 abstract "Hemopressins ((x)-PVNFKLLSH) or peptide endocannabinoids (pepcans) can bind to cannabinoid receptors. RVD-hemopressin (pepcan-12) was shown to act as endogenous allosteric modulator of cannabinoid receptors, with opposite effects on CB1 and CB2, respectively. Moreover, the N-terminally elongated pepcan-23 was detected in different tissues and was postulated to be the pro-peptide of RVD-hemopressin. Currently, data about the pharmacokinetics, tissue distribution and stability of hemopressin-type peptides are lacking. Here we investigated the secondary structure and physiological role of pepcan-23 as precursor of RVD-hemopressin. We assessed the metabolic stability of these peptides, including hemopressin. Using LC-ESI-MS/MS, pepcan-23 was measured in mouse tissues and human whole blood (~50 pmol/mL) and in plasma was the most stable endogenous peptide containing the hemopressin sequence. Using peptide spiked human whole blood, mouse adrenal gland and liver homogenates demonstrate that pepcan-23 acts as endogenous pro-peptide of RVD-hemopressin. Furthermore, administered pepcan-23 converted to RVD-hemopressin in mice. In circular dichroism spectroscopy, pepcan-23 showed a helix-unordered-helix structure and efficiently formed complexes with divalent metal ions, in particular Cu(II) and Ni(II). Hemopressin and RVD-hemopressin were not bioavailable to the brain and showed poor stability in plasma, in agreement with their overall poor biodistribution. Acute hemopressin administration (100 mg/kg) did not modulate endogenous RVD-hemopressin/pepcan-23 levels or influence the endocannabinoid lipidome but increased 1-stearoyl-2-arachidonoyl-sn-glycerol. Overall, we show that pepcan-23 is a biological pro-peptide of RVD-hemopressin and divalent metal ions may regulate this process. Given the lack of metabolic stability of hemopressins, administration of pepcan-23 as pro-peptide may be suitable in pharmacological experiments as it is converted to RVD-hemopressin in vivo." @default.
- W3136164482 created "2021-03-29" @default.
- W3136164482 creator A5011170921 @default.
- W3136164482 creator A5018298410 @default.
- W3136164482 date "2021-05-01" @default.
- W3136164482 modified "2023-09-27" @default.
- W3136164482 title "Characterization of pepcan-23 as pro-peptide of RVD-hemopressin (pepcan-12) and stability of hemopressins in mice" @default.
- W3136164482 cites W1442915068 @default.
- W3136164482 cites W1488329806 @default.
- W3136164482 cites W1500227002 @default.
- W3136164482 cites W1517324664 @default.
- W3136164482 cites W1521241070 @default.
- W3136164482 cites W1583336701 @default.
- W3136164482 cites W1589105407 @default.
- W3136164482 cites W1794556151 @default.
- W3136164482 cites W1819429514 @default.
- W3136164482 cites W1963736429 @default.
- W3136164482 cites W1967961032 @default.
- W3136164482 cites W1968836935 @default.
- W3136164482 cites W1970902596 @default.
- W3136164482 cites W1974830797 @default.
- W3136164482 cites W1977573935 @default.
- W3136164482 cites W1989403800 @default.
- W3136164482 cites W1995267094 @default.
- W3136164482 cites W2004242436 @default.
- W3136164482 cites W2005281847 @default.
- W3136164482 cites W2005937298 @default.
- W3136164482 cites W2010631895 @default.
- W3136164482 cites W2016709120 @default.
- W3136164482 cites W2024322336 @default.
- W3136164482 cites W2026727321 @default.
- W3136164482 cites W2032049619 @default.
- W3136164482 cites W2035800834 @default.
- W3136164482 cites W2038376536 @default.
- W3136164482 cites W2038414558 @default.
- W3136164482 cites W2041826062 @default.
- W3136164482 cites W2049810522 @default.
- W3136164482 cites W2050828219 @default.
- W3136164482 cites W2052930399 @default.
- W3136164482 cites W2055865289 @default.
- W3136164482 cites W2060310074 @default.
- W3136164482 cites W2061543974 @default.
- W3136164482 cites W2062312968 @default.
- W3136164482 cites W2062694183 @default.
- W3136164482 cites W2066774737 @default.
- W3136164482 cites W2075894678 @default.
- W3136164482 cites W2084140416 @default.
- W3136164482 cites W2084242528 @default.
- W3136164482 cites W2088051811 @default.
- W3136164482 cites W2094077114 @default.
- W3136164482 cites W2094458603 @default.
- W3136164482 cites W2095450147 @default.
- W3136164482 cites W2097747770 @default.
- W3136164482 cites W2100694528 @default.
- W3136164482 cites W2107677733 @default.
- W3136164482 cites W2109158162 @default.
- W3136164482 cites W2115317881 @default.
- W3136164482 cites W2115822228 @default.
- W3136164482 cites W2121105634 @default.
- W3136164482 cites W2130229686 @default.
- W3136164482 cites W2139081697 @default.
- W3136164482 cites W2140260269 @default.
- W3136164482 cites W2142054355 @default.
- W3136164482 cites W2146678512 @default.
- W3136164482 cites W2160171025 @default.
- W3136164482 cites W2172140364 @default.
- W3136164482 cites W2187645930 @default.
- W3136164482 cites W2191832912 @default.
- W3136164482 cites W2300575185 @default.
- W3136164482 cites W2317528905 @default.
- W3136164482 cites W2318871426 @default.
- W3136164482 cites W2331946949 @default.
- W3136164482 cites W2332472138 @default.
- W3136164482 cites W2344689512 @default.
- W3136164482 cites W2411993703 @default.
- W3136164482 cites W2491354199 @default.
- W3136164482 cites W2545115907 @default.
- W3136164482 cites W2560967158 @default.
- W3136164482 cites W2582140652 @default.
- W3136164482 cites W2611792444 @default.
- W3136164482 cites W2620884371 @default.
- W3136164482 cites W2622896917 @default.
- W3136164482 cites W2717777254 @default.
- W3136164482 cites W2749469617 @default.
- W3136164482 cites W2793850056 @default.
- W3136164482 cites W2901547405 @default.
- W3136164482 cites W2936512562 @default.
- W3136164482 cites W2937351064 @default.
- W3136164482 cites W2990411841 @default.
- W3136164482 cites W3000486347 @default.
- W3136164482 cites W3003335660 @default.
- W3136164482 cites W3100301730 @default.
- W3136164482 cites W43967158 @default.
- W3136164482 doi "https://doi.org/10.1016/j.jbior.2021.100808" @default.
- W3136164482 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33799079" @default.
- W3136164482 hasPublicationYear "2021" @default.
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