Linked Life Data

7030914

Source:http://linkedlifedata.com/resource/pubmed/id/7030914

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
11
pubmed:dateCreated
1982-2-12
pubmed:abstractText
A series of leupeptin analogs R-L-leucyl-L-leucyl-L-argininal with variable N-terminal substituents has been synthesized using N alpha-tert-butyl-oxycarbonyl-NG-benzyloxycarbonyl-L-arginine-delta-lactam as the starting material. The modified leupeptins proved to be strong competitive inhibitors of the endoprotease acrosin from mammalian spermatozoa. Inhibition constants were found in the range of 4.7 X 10(-7)M (R = H) to 9.7 X 10(-9)M (R = tert-butyloxycarbonyl). N alpha-tert-butyloxycarbonyl leupeptin represents the strongest acrosin inhibitor synthesized so far. Two of the leupeptin derivatives (R = trifluoroacetyl, R = tert-butyloxycarbonyl) were more effective than the natural leupeptins from microbial sources (Ki = 5.9 X 10(-8)M). The potential use of synthetic leupeptins as antienzymatic contraceptives is discussed.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
0018-4888
pubmed:author
pubmed:issnType
Print
pubmed:volume
362
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1435-45
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1981
pubmed:articleTitle
Synthesis of leupeptins and inhibition of proteinases. I. Inhibition of acrosin and trypsin.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't