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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
25
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pubmed:dateCreated |
1978-1-27
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pubmed:abstractText |
The antitumor protein neocarzinostatin (NCS), isolated from Streptomyces carzinostaticus, is a single chain polypeptide with 109 amino acid residues. Complete acylation of the amino groups (alanine-1 and lysine-20) was observed when NCS was allowed to react with 3-(4-hydroxyphenyl)-propionic acid N-hydroxysuccinimide ester at pH 8.5. Since the ensuing bis[(alanine-1, lysine-20)-3-(4-hydroxyphenyl)]-propionamide NCS was fully active in antibacterial potency and in the inhibition of growth of leukemic (CCRF-CEM) cells in vitro, it appears that the two amino groups in the protein are not essential for biological activity. Radiolabeled NCS was prepared by using a tritiated or 125I-labeled acylating agent. Since the CD spectra of native and bis(alanine-1, lysine-20)-amino modified NCS were indistinguishable, there is presumably no change in the native conformation of the protein due to acylation. Reaction of NCS with ammonium chloride in the presence of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide at pH 4.75 converted all the 10 carboxyl groups into carboxamides and produced a protein derivative of basic character. This modification caused a change in the native conformation of the protein accompanied by a loss in biological inhibitory activities.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Dec
|
pubmed:issn |
0006-2960
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
13
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5573-8
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:144523-Amino Acids,
pubmed-meshheading:144523-Antibiotics, Antineoplastic,
pubmed-meshheading:144523-Biological Assay,
pubmed-meshheading:144523-Circular Dichroism,
pubmed-meshheading:144523-Potentiometry,
pubmed-meshheading:144523-Protein Conformation,
pubmed-meshheading:144523-Structure-Activity Relationship,
pubmed-meshheading:144523-Zinostatin
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pubmed:year |
1977
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pubmed:articleTitle |
Neocarzinostatin: effect of modification of side chain amino and carboxyl groups on chemical and biological properties.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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