Systemic leukocyte-directed siRNA delivery revealing cyclin D1 as an anti-inflammatory target

Science. 2008 Feb 1;319(5863):627-30. doi: 10.1126/science.1149859.

Abstract

Cyclin D1 (CyD1) is a pivotal cell cycle-regulatory molecule and a well-studied therapeutic target for cancer. Although CyD1 is also strongly up-regulated at sites of inflammation, its exact roles in this context remain uncharacterized. To address this question, we developed a strategy for selectively silencing CyD1 in leukocytes in vivo. Targeted stabilized nanoparticles (tsNPs) were loaded with CyD1-small interfering RNA (siRNA). Antibodies to beta(7) integrin (beta(7) I) were then used to target specific leukocyte subsets involved in gut inflammation. Systemic application of beta(7) I-tsNPs silenced CyD1 in leukocytes and reversed experimentally induced colitis in mice by suppressing leukocyte proliferation and T helper cell 1 cytokine expression. This study reveals CyD1 to be a potential anti-inflammatory target, and suggests that the application of similar modes of targeting by siRNA may be feasible in other therapeutic settings.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibodies
  • Cell Proliferation
  • Colitis / drug therapy*
  • Colitis / metabolism
  • Colitis / pathology
  • Colon / pathology
  • Cyclin D
  • Cyclins / genetics*
  • Cyclins / physiology
  • Cytokines / metabolism
  • Drug Carriers*
  • Genes, bcl-1*
  • Hyaluronic Acid
  • Inflammatory Bowel Diseases / drug therapy
  • Inflammatory Bowel Diseases / immunology
  • Inflammatory Bowel Diseases / pathology
  • Integrin beta Chains / immunology
  • Leukocytes / cytology
  • Leukocytes / drug effects*
  • Leukocytes / immunology
  • Leukocytes / metabolism
  • Liposomes
  • Mice
  • Nanoparticles
  • Protamines
  • RNA Interference*
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • RNA, Small Interfering / administration & dosage*
  • RNA, Small Interfering / chemistry
  • RNA, Small Interfering / metabolism
  • T-Lymphocytes, Helper-Inducer / immunology

Substances

  • Antibodies
  • Cyclin D
  • Cyclins
  • Cytokines
  • Drug Carriers
  • Integrin beta Chains
  • Liposomes
  • Protamines
  • RNA, Messenger
  • RNA, Small Interfering
  • integrin beta7
  • Hyaluronic Acid