In breast cancer, cell culture, and/or xenograft models identified PIK3CA mutations as determinant of response to PI3K inhibition (O’Brien et al., 2010; Sanchez et al., 2011), dual PI3K/mTOR inhibition (Serra et al., 2008; Brachmann et al., 2009; Lehmann et al., 2011; Sanchez et al., 2011), mTOR kinase inhibition (Weigelt et al., 2011), allosteric mTOR inhibition (Sanchez et al., 2011; Weigelt et al., 2011), and AKT inhibition (She et al., 2008; Meuillet et al., 2010; Table 2). Here, PIK3CA is linked to breast cancer.