Protein kinase-bisubstrate analog

Parang, K., Cole, P. A. Designing bisubstrate analog inhibitors for protein kinases. Pharmacol. Then 2002, 3, 145—157. 

The favorable results in the case of the insulin receptor tyrosine kinase prompted the application of the bisubstrate analog approach to a serine/ threonine kinase [44]. Protein kinase A was selected because it had been... 

Fig. 7.2-13 Synthetic scheme for the generation of a protein kinase A selective bisubstrate analog inhibitor based on a dissociative transition state.

Figure 12 Initial bisubstrate analog inhibitors for protein kinases.

Figure 13 Chemical structures of mechanism-based designed bisubstrate analog inhibitors of protein kinase.

Figure 14 Chemical structure of adenosine-5 -carboxylic acid-based bisubstrate analogs of protein kinase.

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