http://purl.uniprot.org/citations/25313996 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
http://purl.uniprot.org/citations/25313996 | http://www.w3.org/2000/01/rdf-schema#comment | "An affinity-based mass spectrometry screening technology was used to identify novel binders to both nonphosphorylated and phosphorylated ERK2. Screening of inactive ERK2 identified a pyrrolidine analogue 1 that bound to both nonphosphorylated and phosphorylated ERK2 and inhibited ERK2 kinase activity. Chemical optimization identified compound 4 as a novel, potent, and highly selective ERK1,2 inhibitor which not only demonstrated inhibition of phosphorylation of ERK substrate p90RSK but also demonstrated inhibition of ERK1,2 phosphorylation on the activation loop. X-ray cocrystallography revealed that upon binding of compound 4 to ERK2, Tyr34 undergoes a rotation (flip) along with a shift in the poly-Gly rich loop to create a new binding pocket into which 4 can bind. This new binding mode represents a novel mechanism by which high affinity ATP-competitive compounds may achieve excellent kinase selectivity."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.org/dc/terms/identifier | "doi:10.1021/jm500847m"xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Deng Y."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Jin W."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Nan Y."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Xiao L."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Wang T."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Zhu H.Y."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Carr D."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Cooper A."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Dayananth P."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Windsor W.T."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Kirschmeier P."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Chuang C.C."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "English J.M."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Samatar A.A."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Annis D.A."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Shipps G.W. Jr."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/author | "Hruza A.W."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/date | "2014"xsd:gYear |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/name | "J Med Chem"xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/pages | "8817-8826"xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/title | "Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase."xsd:string |
http://purl.uniprot.org/citations/25313996 | http://purl.uniprot.org/core/volume | "57"xsd:string |