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Bioorganic and Medicinal Chemistry Letters
Volumn 24, Issue 1, 2014, Pages 199-203
Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor
Author keywords

CDK2; High throughput screening; Kinases; Modulator; Tumor
Indexed keywords

CYCLIN A; CYCLIN DEPENDENT KINASE 2; PHOSPHOTRANSFERASE INHIBITOR; QUINOLINE BASED KINASE INHIBITOR; QUINOLINE DERIVATIVE; UNCLASSIFIED DRUG; ADENOSINE TRIPHOSPHATE; CYCLIN DEPENDENT KINASE 2 INHIBITOR; MONOMER;
EID: 84891485898     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.11.041     Document Type: Article
Times cited : (20)
References (19)
  • 3
  • 16
    • 85172624274 scopus 로고    scopus 로고
    • ITC was used to obtain a full thermodynamic characterization of the binding affinity for several lead compounds. The procedure is similar to that reported by Mayhood and co-workers in Ref. 14. Briefly, human CDK2 was dialyzed in to 10 mM Hepes, 150 mM NaCl, 10% glycerol, 1 mM DTT, pH 7.5 overnight with 2 changes of buffer. Both protein and ligand samples were prepared in 2 ml volumes. To prepare the ligand solution 20 μl of a 10 mM compound stock (in DMSO) was added to 2 ml of buffer. The ITC runs were performed at 20 C using approximately 10-15 μM CDK2 and 100-150 μM compound and mixed at a rate of 350 rpm. Injection volumes varied from 15 to 18 μl and 360 s of data was recorded for each titration. When a clear baseline was not observed a blank titration was performed to subtract it from the raw data. The MicroCal MCS ITC and included software were used for performing the titrations and analysis.
    • ITC was used to obtain a full thermodynamic characterization of the binding affinity for several lead compounds. The procedure is similar to that reported by Mayhood and co-workers in Ref. 14. Briefly, human CDK2 was dialyzed in to 10 mM Hepes, 150 mM NaCl, 10% glycerol, 1 mM DTT, pH 7.5 overnight with 2 changes of buffer. Both protein and ligand samples were prepared in 2 ml volumes. To prepare the ligand solution 20 μl of a 10 mM compound stock (in DMSO) was added to 2 ml of buffer. The ITC runs were performed at 20 C using approximately 10-15 μM CDK2 and 100-150 μM compound and mixed at a rate of 350 rpm. Injection volumes varied from 15 to 18 μl and 360 s of data was recorded for each titration. When a clear baseline was not observed a blank titration was performed to subtract it from the raw data. The MicroCal MCS ITC and included software were used for performing the titrations and analysis.

* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.