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Philip G Penketh Selected Research

laromustine (VNP40101M)

1/2018pH-dependent general base catalyzed activation rather than isocyanate liberation may explain the superior anticancer efficacy of laromustine compared to related 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazine prodrugs.
6/2013Expression of O6-Methylguanine-DNA Methyltransferase Examined by Alkyl-Transfer Assays, Methylation-Specific PCR and Western Blots in Tumors and Matched Normal Tissue.
3/2013Chloroethylating and methylating dual function antineoplastic agents display superior cytotoxicity against repair proficient tumor cells.
10/2012Design of a hypoxia-activated prodrug inhibitor of O6-alkylguanine-DNA alkyltransferase.
3/2012Preclinical evaluation of Laromustine for use in combination with radiation therapy in the treatment of solid tumors.
11/20114-nitrobenzyloxycarbonyl derivatives of O(6)-benzylguanine as hypoxia-activated prodrug inhibitors of O(6)-alkylguanine-DNA alkyltransferase (AGT), which produces resistance to agents targeting the O-6 position of DNA guanine.
6/2010Reductive activation of the prodrug 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-[[1-(4-nitrophenyl)ethoxy]carbonyl]hydrazine (KS119) selectively occurs in oxygen-deficient cells and overcomes O(6)-alkylguanine-DNA alkyltransferase mediated KS119 tumor cell resistance.
12/2008Development of an O(6)-alkylguanine-DNA alkyltransferase assay based on covalent transfer of the benzyl moiety from [benzene-3H]O(6)-benzylguanine to the protein.
10/2008Lethality to leukemia cell lines of DNA interstrand cross-links generated by Cloretazine derived alkylating species.
4/2006Mode of action of the chloroethylating and carbamoylating moieties of the prodrug cloretazine.
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Philip G Penketh Research Topics

Disease

24Neoplasms (Cancer)
01/2021 - 01/2005
8Hypoxia (Hypoxemia)
02/2013 - 06/2005
6Carcinoma (Carcinomatosis)
01/2016 - 11/2008
4Leukemia
01/2016 - 01/2005
2Ovarian Epithelial Carcinoma
03/2016 - 01/2016
2Fanconi Anemia (Fanconi's Anemia)
01/2016 - 03/2012
2Glioma (Gliomas)
05/2011 - 11/2008
2Acute Myeloid Leukemia (Acute Myelogenous Leukemia)
10/2008 - 01/2005

Drug/Important Bio-Agent (IBA)

14ProdrugsIBA
01/2021 - 01/2005
12laromustine (VNP40101M)IBA
01/2018 - 01/2005
10O(6)-Methylguanine-DNA MethyltransferaseIBA
05/2015 - 12/2008
8DNA (Deoxyribonucleic Acid)IBA
01/2016 - 04/2006
6Oxygen (Dioxygen)IBA
08/2012 - 11/2008
6hydrazine (hydrazine dihydrochloride)IBA
11/2011 - 01/2005
5Proteins (Proteins, Gene)FDA Link
05/2015 - 11/2011
5Carmustine (FIVB)FDA Link
08/2014 - 05/2005
5GuanineIBA
06/2013 - 12/2008
4Temozolomide (Temodar)FDA LinkGeneric
06/2013 - 12/2008
41,2- bis(methylsulfonyl)- 1- - (2- chloroethyl)- 2- ((1- (4- nitrophenyl)ethoxy)carbonyl)hydrazineIBA
10/2011 - 06/2005
3Antineoplastic Agents (Antineoplastics)IBA
01/2016 - 02/2013
3O(6)-benzylguanineIBA
02/2013 - 11/2011
3Alkyl and Aryl TransferasesIBA
02/2013 - 04/2006
3EnzymesIBA
11/2011 - 11/2008
2Carboplatin (JM8)FDA LinkGeneric
03/2016 - 01/2016
2Cisplatin (Platino)FDA LinkGeneric
03/2016 - 01/2016
2PlatinumIBA
03/2016 - 01/2016
23-aminopyridine-2-carboxaldehyde thiosemicarbazone (triapine)IBA
03/2016 - 01/2016
2Alkylating AgentsIBA
06/2013 - 11/2010
2Oxidoreductases (Dehydrogenase)IBA
11/2011 - 05/2011
2Cytotoxins (Cytolysins)IBA
10/2011 - 06/2005
1Etoposide (VP 16)FDA LinkGeneric
03/2016
1Doxorubicin (Adriamycin)FDA LinkGeneric
03/2016
1olaparibIBA
03/2016
1RNA (Ribonucleic Acid)IBA
01/2016
1Mitomycin (Mitomycin-C)FDA LinkGeneric
01/2016
1Paclitaxel (Taxol)FDA LinkGeneric
01/2016
1IsoenzymesIBA
08/2014
1MethyltransferasesIBA
06/2013
17-nitro-4-(phenylthio)benzofurazanIBA
10/2012
1Superoxides (Superoxide)IBA
10/2012
1Hydrogen Peroxide (Hydroperoxide)FDA LinkGeneric
10/2012
1DNA alkyltransferaseIBA
08/2012
1TransferasesIBA
03/2012
11,2- bis(methylsulfonyl)- 1- (2- chloroethyl)hydrazineIBA
06/2005
1Sulfhydryl Compounds (Thiols)IBA
06/2005
1AnnexinsIBA
01/2005
1methyl isocyanateIBA
01/2005

Therapy/Procedure

1Drug Therapy (Chemotherapy)
01/2016
1Radiotherapy
03/2012
1Therapeutics
03/2007