Compounds that modulate the function of anti-apoptotic proteins such as Bcl-2 and Bcl-X.sub.L are identified. These compounds have the ability to convert the activity of Bcl-2-family member proteins from anti-apoptotic to pro-apoptotic. Methods for inducing apoptosis are described, together with methods for identifying molecules that induce apoptosis through interaction with Bcl-2-family members.