Figure 1.
Mer kinase inhibitor design. (A) General structure of pyrazolopyrimidine template designed for Mer kinase inhibition. R1, R2, and R3 represent substituents that can be synthetically varied to optimize the biological properties of this template. (B) X-ray cocrystal structure (PDB 3TCP) of UNC569 and the Mer kinase catalytic domain illustrating the binding mode and location of R1, R2, and R3 in the enzyme active site. (C) Structure and inhibitory properties of UNC1062 versus the TAM family kinases.