A number of mycobacterial macromolecules have been shown to target biological processes within host macrophages; however, the exact mechanism for the majority of these host-pathogen interactions is poorly understood. The following review summarizes current knowledge and expands on a subset of mycobacterial effectors for which a cognate substrate, cellular partner or signaling pathway have been experimentally identified within the human host. (c) 2012 Institut Pasteur. Published by Elsevier Masson SAS. All rights reserved.