William D. Kingsbury

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.

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.

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.

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.

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.