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dc.contributor.authorFechner, Gregory
dc.contributor.authorJacobs, J.
dc.contributor.authorParsons, P.
dc.date.accessioned2017-05-03T13:46:12Z
dc.date.available2017-05-03T13:46:12Z
dc.date.issued1994
dc.identifier.issn0006291X
dc.identifier.doi10.1006/bbrc.1994.1755
dc.identifier.urihttp://hdl.handle.net/10072/27831
dc.description.abstractHistamine displayed specific and saturable binding to membrane fractions of the human melanoma cell line MM96E (Kd = 72.4 nM and Bmax = 487 fmol/mg protein). There was weak competition with isothioureas that inhibit tyrosinase in intact cells: dimaprit (an H2 agonist) nordimaprit and S-[2-(N,N-diisopropyl)ethyl] isothiourea (DINOR). Under culture conditions, rapid, pH-dependent hydrolysis of the isothiureas occurred, with cleavage to urea and a thiol which spontaneously oxidised to the disulphide. The H3 agonist imetit, which also inhibited tyrosinase, behaved similarly. The disulphide breakdown product of DINOR but not the thiol inhibited tyrosinase activity in intact MM96E cells to a similar extent as DINOR itself. Isothioureas with more bulky substituents, however, were stable in culture and did not inhibit tyrosinase. The results show that (a) certain histaminergic drugs exert effects via a disulphide hydrolysis product independently of the histamine H2 receptor, and (b) ߭aminoethyldisulphides are depigmenting agents.
dc.description.peerreviewedYes
dc.description.publicationstatusYes
dc.languageEnglish
dc.language.isoeng
dc.publisherAcademic Press
dc.publisher.placeUSA
dc.relation.ispartofpagefrom687
dc.relation.ispartofpageto693
dc.relation.ispartofjournalBiochemical and Biophysical Research Communications
dc.relation.ispartofvolume201
dc.subject.fieldofresearchInformation and Computing Sciences
dc.subject.fieldofresearchMedicinal and Biomolecular Chemistry
dc.subject.fieldofresearchBiochemistry and Cell Biology
dc.subject.fieldofresearchMedical Biochemistry and Metabolomics
dc.subject.fieldofresearchcode08
dc.subject.fieldofresearchcode0304
dc.subject.fieldofresearchcode0601
dc.subject.fieldofresearchcode1101
dc.titleDimaprit analogues inhibit tyrosinase via a disulphide breakdown product independently of the histamine (H2) receptor.
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.date.issued2015-05-15T04:41:09Z
gro.hasfulltextNo Full Text
gro.griffith.authorFechner, Gregory A.


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