| http://purl.uniprot.org/citations/30472117 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/30472117 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/30472117 | http://www.w3.org/2000/01/rdf-schema#comment | "Dysregulation of the cell cycle characterizes many cancer subtypes, providing a rationale for developing cyclin-dependent kinase (CDK) inhibitors. Potent CDK2 inhibitors might target certain cancers in which CCNE1 is amplified. However, current CDK2 inhibitors also inhibit CDK1, generating a toxicity liability. We have used biophysical measurements and X-ray crystallography to investigate the ATP-competitive inhibitor binding properties of cyclin-free and cyclin-bound CDK1 and CDK2. We show that these kinases can readily be distinguished by such inhibitors when cyclin-free, but not when cyclin-bound. The basis for this discrimination is unclear from either inspection or molecular dynamics simulation of ligand-bound CDKs, but is reflected in the contacts made between the kinase N- and C-lobes. We conclude that there is a subtle but profound difference between the conformational energy landscapes of cyclin-free CDK1 and CDK2. The unusual properties of CDK1 might be exploited to differentiate CDK1 from other CDKs in future cancer therapeutic design."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.org/dc/terms/identifier | "doi:10.1016/j.chembiol.2018.10.015"xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.org/dc/terms/identifier | "doi:10.1016/j.chembiol.2018.10.015"xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Endicott J.A."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Endicott J.A."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Martin M.P."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Martin M.P."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Noble M.E.M."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Noble M.E.M."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Wood D.J."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Wood D.J."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Wang L.Z."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Wang L.Z."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Korolchuk S."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Korolchuk S."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Tatum N.J."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/author | "Tatum N.J."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/date | "2019"xsd:gYear |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/date | "2019"xsd:gYear |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/name | "Cell Chem. Biol."xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/name | "Cell Chem Biol"xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/pages | "121-130.e5"xsd:string |
| http://purl.uniprot.org/citations/30472117 | http://purl.uniprot.org/core/pages | "121-130.e5"xsd:string |