Linked Life Data

19408949

Source:http://linkedlifedata.com/resource/pubmed/id/19408949

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
2010-6-21
pubmed:abstractText
A combinatorial library of up to 65'536 peptide dendrimers (AcX(8)X(7))(8)(DapX(6)X(5))(4)(DapX(4)X(3))(2)DapX(2)X(1) (Dap = (S)-2,3-diaminopropionic acid branching point, X(8-1) = groups of four proteinogenic l-amino acids) was prepared on a photocleavable tentagel resin. The library was assayed for catalytic hydrolysis of the fluorogenic substrate 1-butyryloxy-pyrene-2,7,8-trisulfonate 1 and analogs by a simple procedure involving (a) photocleavage from the support in the absence of solvent, (b) spreading of the solid support beads on the surface of a silicagel plate impregnated with an aqueous buffered substrate solution, and (c) identification of hits as beads surrounded by a fluorescent halo indicative of catalysis and sequence determination in hits and nonhits by amino acid analysis of the beads. The experiment provides direct access to structure-activity relationships in the library and delivers active esterase dendrimers. Anionic glutamate residues in the outer dendrimer branches were found to inhibit catalysis by histidine residues at the dendrimer core. The "off-bead" in silica assay is simple to implement and transferable to other library and reaction types.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
1520-4774
pubmed:author
pubmed:issnType
Electronic
pubmed:volume
11
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
667-75
pubmed:meshHeading
pubmed:articleTitle
Identification of catalytic Peptide dendrimers by "off-bead" in silica high-throughput screening of combinatorial libraries.
pubmed:affiliation
Department of Chemistry and Biochemistry, University of Berne, Freiestrasse 3, Berne, Switzerland.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't