Modulating Innate and Adaptive Immunity by (R)-Roscovitine: Potential Therapeutic Opportunity in Cystic Fibrosis

(R)-Roscovitine, a pharmacological inhibitor of kinases, is currently in phase II clinical trial as a drug candidate for the treatment of cancers, Cushing's disease and rheumatoid arthritis. We here review the data that support the investigation of (R)-roscovitine as a potential therapeutic agent for the treatment of cystic fibrosis (CF). (R)-Roscovitine displays four independent properties that may favorably combine against CF: (1) it partially protects F508del-CFTR from proteolytic degradation and favors its trafficking to the plasma membrane; (2) by increasing membrane targeting of the TRPC6 ion channel, it rescues acidification in phagolysosomes of CF alveolar macrophages (which show abnormally high pH)…

• AB
  American Breast Cancer Foundation
• LD
  Laboratoire d'Excellence Inflamex

  Award: ANR-11-IDEX-0005-02
• AN
  Agence Nationale de la Recherche

  Awards: ANR-11-IDEX-0005-02, 11-IDEX-0005-02, IDEX-0005, ANR-11-IDEX, ANR-11-IDEX-0005
• CD
  Chancellerie des Universités de Paris
• NI
  National Institutes of Health

  Award: RO1 GM36823