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Literature summary for 2.7.11.22 extracted from

  • Talapati, S.; Nataraj, V.; Pothuganti, M.; Gore, S.; Ramachandra, M.; Antony, T.; More, S.; Krishnamurthy, N.
    Structure of cyclin-dependent kinase 2 (CDK2) in complex with the specific and potent inhibitor CVT-313 (2020), Acta Crystallogr. Sect. F, 76, 350-356 .
    View publication on PubMedView publication on EuropePMC
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Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli BL21 (DE3) Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
hanging-drop vapor-diffusion method at 18°C, the crystal structure of CDK2 bound to 2-[2-hydroxyethyl-[6-[(4-methoxyphenyl)methylamino]-9-propan-2-ylpurin-2-yl]amino]ethanol (CVT-313) is determined to a resolution of 1.74 A Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2,2'-[(6-([(4-methoxyphenyl)methyl]-amino)-9-(1-methylethyl)-9H-purin-2-yl)imino]bis(ethanol) i.e. CVT-313, specific and potent inhibitor. Inhibits the growth of human lung carcinoma cell line A549 in a dose-dependent manner, with an IC50 of 0.0012 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P24941
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
CDK2
-
 Homo sapiens
cyclin-dependent kinase 2
-
 Homo sapiens

Temperature Stability [°C]

Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
45
-
 melting temperature (Tm). The Tm shifts are 6.8°C and 10.2°C at 10 mM and 100 mM CVT-313 Homo sapiens