The active zone (AZ) is a specialized site for docking and fusion of synaptic vesicles in the nerve terminal. AZ-specific proteins include CAST, ELKS, RIMs, Munc13-1, Bassoon, and Piccolo. CAST interacts with these proteins, forming a large molecular complex at the AZ. Moreover, the direct interaction of CAST with RIM1 and Bassoon is involved in neurotransmitter release. Thus, CAST may play organizational and functional roles at the AZ. Furthermore, SAD kinase, a master kinase for axon/dendrite polarization in early synapse formation, has recently been identified as an AZ-associated kinase that directly phosphorylates RIM1. SAD regulates neurotransmitter release in a kinase activity-dependent manner. This chapter focuses on recent findings about the structure and function of the ELKS/CAST family and SAD, and discusses the roles of these proteins in neurotransmitter release. [ABSTRACT FROM AUTHOR]