W
William D. Kingsbury
Researcher at Smith, Kline & French
Publications - 17
Citations - 795
William D. Kingsbury is an academic researcher from Smith, Kline & French. The author has contributed to research in topics: Peptide & Peptide transport. The author has an hindex of 9, co-authored 17 publications receiving 782 citations.
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Journal ArticleDOI
Modification of the hydroxy lactone ring of camptothecin: inhibition of mammalian topoisomerase I and biological activity.
Robert P. Hertzberg,Mary Jo Caranfa,Kenneth G. Holden,Dalia R. Jakas,Gregory Gallagher,Michael R. Mattern,Shau Ming Mong,J O Bartus,Randall K. Johnson,William D. Kingsbury +9 more
TL;DR: The present findings, as well as other reports that the hydroxy lactone ring of camptothecin is critical for antitumor activity in vivo, correlate with the structure-activity relationships at the level of topoisomerase I and support the hypothesis that antitumors activity is related to inhibition of this target enzyme.
Journal ArticleDOI
A novel peptide delivery system involving peptidase activated prodrugs as antimicrobial agents. Synthesis and biological activity of peptidyl derivatives of 5-fluorouracil
TL;DR: Support for this conclusion was provided by the finding that biological activities were dependent upon peptide stereochemistry, and noninhibitory peptides antagonized the antimicrobial activities of the 5-FU-peptide conjugates but not of free5-FU.
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Synthesis of Water-Soluble (Aminoalkyl)camptothecin Analogues: Inhibition of Topoisomerase I and Antitumor Activity.
William D. Kingsbury,Jeffrey C. Boehm,D. R. Jakas,K. G. Holden,S. M. Hech,G. Gallagher,M. J. Caranfa,Francis L. McCabe,Leo F. Faucette,Randall K. Johnson,R. P. Hertzberg +10 more
TL;DR: 9-[(dimethylamino)methyl]-10-hydroxycamptothecin (4, SK&F 104864) for development as an antitumor agent demonstrated broad-spectrum activity in preclinical tumor models and is currently undergoing Phase I clinical trials in cancer patients.
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Transport of antimicrobial agents using peptide carrier systems: anticandidal activity of m-fluorophenylalanine--peptide conjugates.
TL;DR: The results of competitive antagonism studies support peptide transport mediated entry of the inhibitory peptides, followed by release of L-m-fluorophenylalanine inside the cell.
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Portage of various compounds into bacteria by attachment to glycine residues in peptides
TL;DR: Synthetic di- and oligopeptides that contain nucleophilic moieties attached to the alpha carbon of a glycine residue are described that have broad applicability to the study of microbial physiology and the development of an additional class of antimicrobial agents.