• Publications
  • Influence
Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor.
A class of high-affinity inhibitors is disclosed that selectively target and irreversibly inactivate the epidermal growth factor receptor tyrosine kinase through specific, covalent modification of aExpand
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Targeting GLUT1 and the Warburg Effect in Renal Cell Carcinoma by Chemical Synthetic Lethality
A screen identifies a drug that specifically kills glycolysis-dependent cancer cells by inhibiting glucose uptake. Cancer’s Achilles’ Heel A quick tug on a fuel line can stop a car dead in itsExpand
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Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling.
Recent genetic knock-in and pharmacological approaches have suggested that, of class IA PI3Ks (phosphatidylinositol 3-kinases), it is the p110alpha isoform (PIK3CA) that plays the predominant role inExpand
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A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types
Genetic alterations in PI3K (phosphoinositide 3-kinase) signalling are common in cancer and include deletions in PTEN (phosphatase and tensin homologue deleted on chromosome 10), amplifications ofExpand
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A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation.
Reactivation of silenced tumor suppressor genes by 5-azacytidine (Vidaza) and its congener 5-aza-2'-deoxycytidine (decitabine) has provided an alternate approach to cancer therapy. We have shownExpand
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Mechanism of Action and Preclinical Antitumor Activity of the Novel Hypoxia-Activated DNA Cross-Linking Agent PR-104
Purpose: Hypoxia is a characteristic of solid tumors and a potentially important therapeutic target. Here, we characterize the mechanism of action and preclinical antitumor activity of a novelExpand
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Prodrugs for Gene-Directed Enzyme-Prodrug Therapy (Suicide Gene Therapy)
  • W. Denny
  • Medicine, Biology
  • Journal of biomedicine & biotechnology
  • 19 March 2003
This review focuses on the prodrugs used in suicide gene therapy. These prodrugs need to satisfy a number of criteria. They must be efficient and selective substrates for the activating enzyme, andExpand
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Prodrug strategies in cancer therapy.
  • W. Denny
  • Medicine, Chemistry
  • European journal of medicinal chemistry
  • 1 August 2001
Systemic cytotoxic (anti-proliferative) anticancer drugs rely primarily for their therapeutic effect on cytokinetic differences between cancer and normal cells. One approach aimed at improving theExpand
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Tumor-activated Prodrugs—A New Approach to Cancer Therapy
  • W. Denny
  • Medicine
  • Cancer investigation
  • 1 January 2004
Systemic cytotoxic (antiproliferative) anticancer drugs rely primarily for their therapeutic effect on cytokinetic differences between cancer and normal cells. One approach aimed at improving theExpand
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Gemcitabine sensitization by checkpoint kinase 1 inhibition correlates with inhibition of a Rad51 DNA damage response in pancreatic cancer cells
The protein kinase checkpoint kinase 1 (Chk1) has been implicated as a key regulator of cell cycle progression and DNA repair, and inhibitors of Chk1 (e.g., UCN-01 and EXEL-9844) potentiate theExpand
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