Matches in SemOpenAlex for { <https://semopenalex.org/work/W1488961103> ?p ?o ?g. }
Showing items 1 to 49 of
49
with 100 items per page.
- W1488961103 abstract "The incidence of malignant melanoma has increased rapidly during the last decades, and the prognosis for disseminated melanoma is poor. The melanoma cells produce melanin, and therefore the melanogenesis may serve as a target for treatment of melanotic melanoma; thioureyelenes such as thiourea and 2-thiouracil, e.g., are known to be incorporated into melanin solely during its synthesis.By in vitro screening, using spectrophotometry, inductively coupled plasma-atomic emission spectroscopy (ICP-AES) and HPLC, 22 substances, mainly thioureylenes, were studied in order to find candidates suitable for melanoma targeting, and to investigate the mechanisms of the incorporation into melanin.The results suggest that the incorporation occurs by binding to intermediates of the melanin synthetic pathway, i.e. dopaquinone and indolequinones. Substances that most effectively suppressed the early part of the synthetic pathway (dopachrome formation) were found also to be inhibitors of the essential enzyme tyrosinase. Mercaptobenzothiazole (MBT) showed the highest incorporation in the early part of the synthesis, whereas dithiouracil interacted with the later part of the synthesis. It was found that thiourea is incorporated into melanin by covalent binding to dopaquinone in 6-position via the sulfur ligand. Incorporation by binding to indolequinones could not be demonstrated.Both thiourea and MBT were accumulated and retained in melanotic melanoma transplanted to mice (shown by whole-body autoradiography) although MBT is a strong tyrosinase inhibitor. Incorporation of thiourea changed the properties of the melanin, such as the solubility and the colour, to a more pheomelanin-like pigment. The incorporation of thiourea may affect the protective role of melanin in the body. The binding to pheomelanin was found to be lower than the binding to eumelanin, though a high pheomelanin-related uptake of chloroquine was seen in the skin of yellow mice in vivo. The binding to thiourea-melanin was even lower. This indicates that the toxicological implications of the binding are applicable to persons with a high content of pheomelanin in the skin and hair.The thioureylenes may also be used as markers of the effects of radiation therapy of melanotic melanoma, since a changed uptake was seen in the tumours after irradiation." @default.
- W1488961103 created "2016-06-24" @default.
- W1488961103 creator A5084053815 @default.
- W1488961103 date "1998-01-01" @default.
- W1488961103 modified "2023-09-23" @default.
- W1488961103 title "Melanogenesis as the basis for melanoma targeting" @default.
- W1488961103 hasPublicationYear "1998" @default.
- W1488961103 type Work @default.
- W1488961103 sameAs 1488961103 @default.
- W1488961103 citedByCount "0" @default.
- W1488961103 crossrefType "journal-article" @default.
- W1488961103 hasAuthorship W1488961103A5084053815 @default.
- W1488961103 hasConcept C107538193 @default.
- W1488961103 hasConcept C178790620 @default.
- W1488961103 hasConcept C181199279 @default.
- W1488961103 hasConcept C185592680 @default.
- W1488961103 hasConcept C202751555 @default.
- W1488961103 hasConcept C2777658100 @default.
- W1488961103 hasConcept C2780538656 @default.
- W1488961103 hasConcept C502942594 @default.
- W1488961103 hasConcept C55493867 @default.
- W1488961103 hasConcept C86803240 @default.
- W1488961103 hasConcept C87554066 @default.
- W1488961103 hasConceptScore W1488961103C107538193 @default.
- W1488961103 hasConceptScore W1488961103C178790620 @default.
- W1488961103 hasConceptScore W1488961103C181199279 @default.
- W1488961103 hasConceptScore W1488961103C185592680 @default.
- W1488961103 hasConceptScore W1488961103C202751555 @default.
- W1488961103 hasConceptScore W1488961103C2777658100 @default.
- W1488961103 hasConceptScore W1488961103C2780538656 @default.
- W1488961103 hasConceptScore W1488961103C502942594 @default.
- W1488961103 hasConceptScore W1488961103C55493867 @default.
- W1488961103 hasConceptScore W1488961103C86803240 @default.
- W1488961103 hasConceptScore W1488961103C87554066 @default.
- W1488961103 hasLocation W14889611031 @default.
- W1488961103 hasOpenAccess W1488961103 @default.
- W1488961103 hasPrimaryLocation W14889611031 @default.
- W1488961103 hasRelatedWork W126506303 @default.
- W1488961103 hasRelatedWork W1511722047 @default.
- W1488961103 hasRelatedWork W1512812876 @default.
- W1488961103 hasRelatedWork W1977247923 @default.
- W1488961103 hasRelatedWork W2032815887 @default.
- W1488961103 hasRelatedWork W2062123462 @default.
- W1488961103 hasRelatedWork W2331255735 @default.
- W1488961103 hasVolume "188" @default.
- W1488961103 isParatext "false" @default.
- W1488961103 isRetracted "false" @default.
- W1488961103 magId "1488961103" @default.
- W1488961103 workType "article" @default.