Catalytic subunit of cyclic AMP-dependent protein kinase: Structure and dynamics of the active site cleft

The catalytic subunit of cyclic AMP dependent protein kinase serves as a st ructural template for the entire family of Ser, Thr, and Tyr specific prote in kinases. We review here the dynamics of the active catalytic subunit. Th ese dynamics correlate with an opening and closing of the active site cleft , and are considered to be a requirement for catalysis. The motions, descri bed by a set of several crystal structures, reveal a very fluid active site cleft. This active site cleft with its dynamic opening and closing is a pr ime target for protein kinase inhibitors. (C) 1999 Elsevier Science Inc. Al l rights reserved.