Source:http://linkedlifedata.com/resource/pubmed/id/11306297
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
|
pubmed:dateCreated |
2001-4-18
|
pubmed:abstractText |
A chemical-genetic method for the generation of target-specific protein kinase inhibitors has been developed recently. This strategy utilizes a functionally silent active-site mutation to sensitize a target kinase to inhibition by a small molecule that does not inhibit wild-type kinases. Tyrosine and serine/threonine kinases are equally amenable to the drug-sensitization approach, which has been used to generate selective inhibitors of mutant Src-family kinases, Abl-family kinases, cyclin-dependent kinases, mitogen-activated kinases, p21-activated kinases and Ca(2+)/calmodulin-dependent kinases. The designed inhibitors are specific for the sensitized kinase in a cellular background where the wild-type kinase has been inactivated. By these means, kinase-sensitization has been used systematically to generate and analyze conditional alleles of several yeast protein kinases in vivo.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Carrier Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Intracellular Signaling Peptides...,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/protein kinase modulator
|
pubmed:status |
MEDLINE
|
pubmed:month |
Apr
|
pubmed:issn |
0962-8924
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
11
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
167-72
|
pubmed:dateRevised |
2009-11-19
|
pubmed:meshHeading |
pubmed-meshheading:11306297-Animals,
pubmed-meshheading:11306297-Carrier Proteins,
pubmed-meshheading:11306297-Drug Delivery Systems,
pubmed-meshheading:11306297-Drug Design,
pubmed-meshheading:11306297-Gene Therapy,
pubmed-meshheading:11306297-Humans,
pubmed-meshheading:11306297-Intracellular Signaling Peptides and Proteins,
pubmed-meshheading:11306297-Mutagenesis,
pubmed-meshheading:11306297-Protein Kinases
|
pubmed:year |
2001
|
pubmed:articleTitle |
Magic bullets for protein kinases.
|
pubmed:affiliation |
Skaggs Institute for Chemical Biology, Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037, USA.
|
pubmed:publicationType |
Journal Article,
Review
|