Show simple item record

dc.contributor.authorCummings, Jeffrey
dc.contributor.authorRitchie, Alison
dc.contributor.authorButler, John
dc.contributor.authorWard, Timothy H
dc.contributor.authorLangdon, Simon
dc.date.accessioned2009-09-23T11:45:22Z
dc.date.available2009-09-23T11:45:22Z
dc.date.issued2009-09-23T11:45:22Z
dc.identifier.citationActivity profile of the novel aziridinylbenzoquinones MeDZQ and RH1 in human tumour xenografts., 23 (5A):3979-83 Anticancer Res.en
dc.identifier.issn0250-7005
dc.identifier.pmid14666706
dc.identifier.urihttp://hdl.handle.net/10541/82315
dc.description.abstractBACKGROUND: RH1 and MeDZQ represent novel aziridinylbenzoquinones that can be activated by DT-diaphorase to form unique DNA lesions. RH1 is due to enter a phase 1 clinical trial in the United Kingdom in the summer of 2003, where pharmacodynamic monitoring of DT-diaphorase will be performed. MATERIALS AND METHODS: The antitumour efficacy of RH1 and MeDZQ has been studied in 4 human xenografts (3 non-small cell lung cancer and 1 colon cancer), and compared to the level of constitutive DT-Diaphorase activity measured by the DCPIP assay. RESULTS: The 4 xenografts exhibited a wide range of DT-diaphorase activity (4.8-303 nmol/min/mg). Greater antitumour activity was recorded in the xenografts expressing high levels of DT-diaphorase (e.g. NX002, DT-diaphorase activity, 303 +/- 52 nmol/min/mg, T/C to MeDZQ, 33.3% and to RH1, 43.4%). CONCLUSION: These data add in vivo support to a role for DT-Diaphorase in the antitumour activity of RH1.
dc.language.isoenen
dc.subjectLung Canceren
dc.subjectXenograft Model Antitumour Assaysen
dc.subjectColonic Canceren
dc.subject.meshAnimals
dc.subject.meshAntineoplastic Agents
dc.subject.meshAziridines
dc.subject.meshBenzoquinones
dc.subject.meshCarcinoma, Non-Small-Cell Lung
dc.subject.meshColonic Neoplasms
dc.subject.meshDose-Response Relationship, Drug
dc.subject.meshFemale
dc.subject.meshHumans
dc.subject.meshLung Neoplasms
dc.subject.meshMice
dc.subject.meshMice, Nude
dc.subject.meshNAD(P)H Dehydrogenase (Quinone)
dc.subject.meshTransplantation, Heterologous
dc.subject.meshXenograft Model Antitumor Assays
dc.titleActivity profile of the novel aziridinylbenzoquinones MeDZQ and RH1 in human tumour xenografts.en
dc.typeArticleen
dc.contributor.departmentCancer Research UK, Edinburgh Medical Oncology Unit, Western General Hospital, Edinburgh, EH4 2XR, U.K. jcummings@picr.man.ac.uken
dc.identifier.journalAnticancer Researchen
html.description.abstractBACKGROUND: RH1 and MeDZQ represent novel aziridinylbenzoquinones that can be activated by DT-diaphorase to form unique DNA lesions. RH1 is due to enter a phase 1 clinical trial in the United Kingdom in the summer of 2003, where pharmacodynamic monitoring of DT-diaphorase will be performed. MATERIALS AND METHODS: The antitumour efficacy of RH1 and MeDZQ has been studied in 4 human xenografts (3 non-small cell lung cancer and 1 colon cancer), and compared to the level of constitutive DT-Diaphorase activity measured by the DCPIP assay. RESULTS: The 4 xenografts exhibited a wide range of DT-diaphorase activity (4.8-303 nmol/min/mg). Greater antitumour activity was recorded in the xenografts expressing high levels of DT-diaphorase (e.g. NX002, DT-diaphorase activity, 303 +/- 52 nmol/min/mg, T/C to MeDZQ, 33.3% and to RH1, 43.4%). CONCLUSION: These data add in vivo support to a role for DT-Diaphorase in the antitumour activity of RH1.


This item appears in the following Collection(s)

Show simple item record