Inhibition of T and B lymphocyte proliferation by rapamycin

Immunology. 1991 Apr;72(4):544-9.


The immunosuppressive macrolide rapamycin shows marked structural similarity to FK-506, and like FK-506 inhibits the activation of cultured T and B lymphocytes at concentrations as low as 10(-10) M. However, rapamycin blocks T-lymphocyte proliferation at a much later stage than FK-506. It also inhibits human, porcine and murine T- and B-lymphocyte activation by all pathways tested, including pathways which are insensitive to FK-506, such as interleukin-2 (IL-2)-mediated proliferation of IL-2-dependent T-cell lines, activation of human peripheral blood T lymphocytes by phorbol ester and anti-CD28 and activation of murine B lymphocytes by bacterial lipopolysaccharide. Thus these two macrolides that bind competitively to the same major intracellular receptor protein inhibit T- and B-lymphocyte activation by quite distinct mechanisms.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / pharmacology*
  • B-Lymphocytes / immunology*
  • Cell Division / drug effects
  • Cells, Cultured
  • Cyclosporins / pharmacology
  • Drug Interactions / immunology
  • Immunosuppressive Agents / pharmacology*
  • Lymphocyte Activation / drug effects*
  • Male
  • Mice
  • Mice, Inbred CBA
  • Mitogens / immunology
  • Polyenes / pharmacology*
  • Sirolimus
  • Swine
  • T-Lymphocytes / immunology*
  • Tacrolimus


  • Anti-Bacterial Agents
  • Cyclosporins
  • Immunosuppressive Agents
  • Mitogens
  • Polyenes
  • Sirolimus
  • Tacrolimus