Fig. 5
From: Dual protein kinase and nucleoside kinase modulators for rationally designed polypharmacology
Proposed model for masitinib activation. The binding of masitinib on a monophospho-nucleoside-bound enzyme conformation promotes the release of the enzymatic product of the reaction and the transition from the closed state to the open state, being the rate-limiting step for the reaction. After the binding of a fresh molecule of substrate, the enzyme returns to the closed conformation and catalyses the phosphorylation of the nucleoside
