Search

Your search keyword '"Kingsbury A"' showing total 78 results
Start Over Author "Kingsbury A" Journal chemischer informationsdienst
78 results on '"Kingsbury A"'

4. ChemInform Abstract: TRANSPORT OF ANTIMICROBIAL AGENTS USING PEPTIDE CARRIER SYSTEMS: ANTICANDIDAL ACTIVITY OF M-FLUOROPHENYLALANINE-PEPTIDE CONJUGATES

Author

Jeffrey C. Boehm, Sarah F. Grappel, Rajanikant J. Mehta, and William D. Kingsbury

Subjects
chemistry.chemical_classification, biology, Peptide, General Medicine, Tripeptide, Antimicrobial, biology.organism_classification, In vitro, Corpus albicans, chemistry, Biochemistry, Peptide transport, Antagonism, Candida albicans
Abstract

A series of di- and tripeptides containing D- and L-m-fluorophenylalanine was prepared and tested in vitro for the ability to inhibit the growth of the yeast Candida albicans. The results demonstrate that peptides containing L-m-fluorophenylalanine inhibited the growth of C. albicans with minimum inhibitory concentrations (MIC's) ranging from 0.5 to 63 micrograms/mL. The parent L-m-fluorophenylalanine and peptides containing D-m-fluorophenylalanine were inactive (MIC greater than 250 micrograms/mL) in these tests. 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.

Published
1984
Full Text
View/download PDF

27. ChemInform Abstract: A NOVEL PEPTIDE DELIVERY SYSTEM INVOLVING PEPTIDASE ACTIVATED PRODRUGS AS ANTIMICROBIAL AGENTS. SYNTHESIS AND BIOLOGICAL ACTIVITY OF PEPTIDYL DERIVATIVES OF 5-FLUOROURACIL

Author

Rajanikant J. Mehta, Charles Gilvarg, Sarah F. Grappel, William D. Kingsbury, and Jeffrey C. Boehm

Subjects
chemistry.chemical_classification, Carrier system, biology, Chemistry, Permease, Peptide, Biological activity, General Medicine, Prodrug, biology.organism_classification, Antimicrobial, Biochemistry, Peptide transport, Candida albicans
Abstract

As an approach to the development of antimicrobial agents, a novel peptide carrier system was designed, based on the chemical instability of alpha-substituted glycine analogues, with the explicit intent of actively transporting therapeutically useful compounds into microbial cells. Peptides containing 5-fluorouracil (5-FU) linked to the peptide backbone were selected to test the feasibility of this new delivery system. These peptide conjugates were designed such that they would be substrates for both the microbial peptide permeases and peptidases. After entry into cells, enzymatic hydrolysis of the peptide generates an unstable alpha-(5-FU)-glycine that spontaneously decomposes to release 5-FU. The 5-FU-peptide conjugates were tested for antifungal (Candida albicans) and antibacterial (Escherichia coli) activity and were found to have antimicrobial activities comparable to free 5-FU. Noninhibitory peptides antagonized the antimicrobial activities of the 5-FU-peptide conjugates but not of free 5-FU, a result consistent with peptide transport mediated entry of the peptide conjugates into cells. Further support for this conclusion was provided by the finding that biological activities were dependent upon peptide stereochemistry.

Published
1985
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results