Structure and functional characterization of the atypical human kinase haspin was written by Eswaran, Jeyanthy;Patnaik, Debasis;Filippakopoulos, Panagis;Wang, Fangwei;Stein, Ross L.;Murray, James W.;Higgins, Jonathan M. G.;Knapp, Stefan. And the article was included in Proceedings of the National Academy of Sciences of the United States of America in 2009.Reference of 24386-93-4 The following contents are mentioned in the article:
Protein kinase haspin/Gsg2 plays an important role in mitosis, where it specifically phosphorylates Thr-3 in histone H3 (H3T3). Its protein sequence is only weakly homologous to other protein kinases and lacks the highly conserved motifs normally required for kinase activity. Here, the authors report crystal structures of human haspin in complex with ATP and the inhibitor, 5-iodotubercidin. These structures reveal a constitutively active kinase conformation, stabilized by haspin-specific inserts. Haspin also has a highly atypical activation segment well adapted for specific recognition of the basic histone tail. Despite the lack of a DFG motif, ATP binding to haspin was similar to that in classical kinases; however, the ATP y-phosphate formed H-bonds with the conserved catalytic loop residues, Asp-649 and His-651, and a H651A haspin mutant was inactive, suggesting a direct role for the catalytic loop in ATP recognition. Enzyme kinetic data showed that haspin phosphorylates substrate peptides through a rapid equilibrium random mechanism. A detailed anal. of histone modifications in the neighborhood of H3T3 revealed that increasing methylation at Lys-4 (H3K4) strongly decreased substrate recognition, suggesting a key role of H3K4 methylation in the regulation of haspin activity. This study involved multiple reactions and reactants, such as (2R,3R,4S,5R)-2-(4-Amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol (cas: 24386-93-4Reference of 24386-93-4).
(2R,3R,4S,5R)-2-(4-Amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol (cas: 24386-93-4) belongs to tetrahydrofuran derivatives.Tetrahydrofuran has many industry uses as a solvent including in natural and synthetic resins, high polymers, fat oils, rubber, polymer. It is more basic than diethyl ether and forms stronger complexes with Li+, Mg2+, and boranes. It is a popular solvent for hydroboration reactions and for organometallic compounds such as organolithium and Grignard reagents.Reference of 24386-93-4
Referemce:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem