Proteins of Bcl-2(B-cell lymphoma-2) family are key regulators of programmed cell death. Scientist found that some members of this family are over-expressed in malignant tumors and influence the sensitivity of tumor cells to chemotherapy and radiotherapy. This report reviews the recent progress of structures, functions and inhibition of Bcl-2 family proteins, especially the development of Bcl-2 inhibitors in past decades as anticancer agents.