Title
Biological evaluation of Tyr6 and Ser7 modified drosocin analogues
Author
de Visser, P.C.
van Hooft, P.A.V.
de Vries, A.-M.
de Jong, A.
van der Marel, G.A.
Overkleeft, H.S.
Noort, D.
TNO Defensie en Veiligheid
Publication year
2005
Abstract
An array of analogues of the cationic antimicrobial peptide drosocin was synthesized containing substitutions of Tyr6 and Ser7 in order to increase the proteolytic stability. Stabilizing the N-terminus with unnatural amino acids increased the serum stability of analogues by almost a factor 30 over an 8 h period. © 2005 Elsevier Ltd. All rights reserved.
Subject
Antibiotic agent
Amino acid substitution
Amino terminal sequence
Article
Controlled study
Drug screening
Drug stability
Drug synthesis
Nonhuman
Protein degradation
Amino Acid Sequence
Glycopeptides
Humans
Microbial Sensitivity Tests
Molecular Sequence Data
Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
Chemicals
Drosocin, 179048-25-0
Serine, 56-45-1, 6898-95-9
Tyrosine, 16870-43-2, 55520-40-6, 60-18-4
Drosocin, 149924-99-2
Glycopeptides
Serine, 56-45-1
Tyrosine, 55520-40-6
To reference this document use:
http://resolver.tudelft.nl/uuid:bd9b2348-4cfd-4098-9c3c-2c800408f0ce
DOI
https://doi.org/10.1016/j.bmcl.2005.03.074
TNO identifier
238547
ISSN
0960-894X
Source
Bioorganic and Medicinal Chemistry Letters, 15 (11), 2902-2905
Document type
article