Search Results - "Denny, William A."
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Nitroaromatic Hypoxia-Activated Prodrugs for Cancer Therapy
Published in Pharmaceuticals (Basel, Switzerland) (02-02-2022)“…The presence of "hypoxic" tissue (with O levels of <0.1 mmHg) in solid tumours, resulting in quiescent tumour cells distant from blood vessels, but capable of…”
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2
Cyclic Tetrapeptides from Nature and Design: A Review of Synthetic Methodologies, Structure, and Function
Published in Chemical reviews (11-09-2019)“…Small cyclic peptides possess a wide range of biological properties and unique structures that make them attractive to scientists working in a range of areas…”
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A Selective and Slowly Reversible Inhibitor of l‑Type Amino Acid Transporter 1 (LAT1) Potentiates Antiproliferative Drug Efficacy in Cancer Cells
Published in Journal of medicinal chemistry (23-06-2016)“…The l-type amino acid transporter 1 (LAT1) is a transmembrane protein carrying bulky and neutral amino acids into cells. LAT1 is overexpressed in several types…”
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4
Effect of wet milling process on the solid state of indomethacin and simvastatin
Published in International journal of pharmaceutics (01-10-2009)“…The aim of this study was to investigate the effect of wet milling on the solid state of indomethacin (IMC) and simvastatin (SIM). Wet milling was performed…”
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5
Targeting GLUT1 and the Warburg effect in renal cell carcinoma by chemical synthetic lethality
Published in Science translational medicine (03-08-2011)“…Identifying new targeted therapies that kill tumor cells while sparing normal tissue is a major challenge of cancer research. Using a high-throughput chemical…”
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6
Genotoxicity of non-covalent interactions: DNA intercalators
Published in Mutation Research-Fundamental and Molecular Mechanisms of Mutagenesis (01-10-2007)“…This review provides an update on the mutagenicity of intercalating chemicals, as carried out over the last 17 years. The most extensively studied DNA…”
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7
Inhibitors of Discoidin Domain Receptor (DDR) Kinases for Cancer and Inflammation
Published in Biomolecules (Basel, Switzerland) (10-11-2021)“…The discoidin domain receptor tyrosine kinases DDR1 and DDR2 are distinguished from other kinase enzymes by their extracellular domains, which interact with…”
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Inhibition of strigolactone receptors by N-phenylanthranilic acid derivatives: Structural and functional insights
Published in The Journal of biological chemistry (27-04-2018)“…The strigolactone (SL) family of plant hormones regulates a broad range of physiological processes affecting plant growth and development and also plays…”
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9
A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types
Published in Biochemical journal (15-08-2011)“…Genetic alterations in PI3K (phosphoinositide 3-kinase) signalling are common in cancer and include deletions in PTEN (phosphatase and tensin homologue deleted…”
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10
The Use of Heptamethine Cyanine Dyes as Drug-Conjugate Systems in the Treatment of Primary and Metastatic Brain Tumors
Published in Frontiers in oncology (01-06-2021)“…Effective cancer therapeutics for brain tumors must be able to cross the blood-brain barrier (BBB) to reach the tumor in adequate quantities and overcome the…”
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11
Systemic and Brain Pharmacokinetics of Perforin Inhibitor Prodrugs
Published in Molecular pharmaceutics (05-07-2016)“…We have recently reported that by converting a perforin inhibitor into an l-type amino acid transporter 1 (LAT1)-utilizing prodrug its cellular uptake can be…”
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12
Synergistic Activity of Nitroimidazole-Oxazolidinone Conjugates against Anaerobic Bacteria
Published in Molecules (Basel, Switzerland) (22-05-2020)“…The introductions of the bicyclic 4-nitroimidazole and the oxazolidinone classes of antimicrobial agents represented the most significant advancements in the…”
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13
Structure-Activity Relationships for the Anaesthetic and Analgaesic Properties of Aromatic Ring-Substituted Ketamine Esters
Published in Molecules (Basel, Switzerland) (26-06-2020)“…A series of benzene ring substituted ketamine -alkyl esters were prepared from the corresponding substituted norketamines. Few of the latter have been reported…”
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14
Synthetic Studies to Help Elucidate the Metabolism of the Preclinical Candidate TBAJ-876-A Less Toxic and More Potent Analogue of Bedaquiline
Published in Molecules (Basel, Switzerland) (20-03-2020)“…Bedaquiline is a novel drug approved in 2012 by the FDA for treatment of drug-resistant tuberculosis (TB). Although it shows high efficacy towards…”
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Pharmacokinetic/Pharmacodynamic Modeling Identifies SN30000 and SN29751 as Tirapazamine Analogues with Improved Tissue Penetration and Hypoxic Cell Killing in Tumors
Published in Clinical cancer research (15-10-2010)“…Tirapazamine (TPZ) has attractive features for targeting hypoxic cells in tumors but has limited clinical activity, in part because of poor extravascular…”
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16
Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling
Published in Biochemical journal (15-06-2007)“…Recent genetic knock-in and pharmacological approaches have suggested that, of class IA PI3Ks (phosphatidylinositol 3-kinases), it is the p110alpha isoform…”
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17
Mechanism of Action and Preclinical Antitumor Activity of the Novel Hypoxia-Activated DNA Cross-Linking Agent PR-104
Published in Clinical cancer research (01-07-2007)“…Purpose: Hypoxia is a characteristic of solid tumors and a potentially important therapeutic target. Here, we characterize the mechanism of action and…”
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18
Involvement of the tumour necrosis factor receptor system in glioblastoma cell death induced by palbociclib-heptamethine cyanine dye conjugate
Published in Cell communication and signaling (11-01-2024)“…Glioblastoma is the most common and aggressive primary brain tumour in adults. The development of anti-brain cancer agents are challenged by the blood-brain…”
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Transcriptional changes in response to ketamine ester-analogs SN 35210 and SN 35563 in the rat brain
Published in BMC genomics (11-04-2019)“…Ketamine ester analogs, SN 35210 and SN 35563, demonstrate different pharmacological profiles to ketamine in animal models. Both confer hypnosis with…”
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20
Evaluation of a crystalline nanosuspension: Polymorphism, process induced transformation and in vivo studies
Published in International journal of pharmaceutics (15-04-2011)“…The aim of this work was to evaluate a crystalline nanosuspension of an investigational anticancer compound, SN 30191. Solid forms of SN 30191 were prepared…”
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