Negative regulation of two hyperproliferative keratinocyte differentiation markers by a retinoic acid receptor-specific retinoid: insight into the mechanism of retinoid action in psoriasis

Cell Growth Differ. 1996 Dec;7(12):1783-91.

Abstract

Retinoids down-regulate the expression of metalloproteinases, cytokines, and other genes involved in cell proliferation and inflammation. Tazarotene (AGN 190168), a retinoic acid receptor (RAR)-specific retinoid, is effective in the treatment of psoriasis, a hyperproliferative and inflammatory skin disease. Because negative regulation of genes appears to be important in the antiproliferative and antiinflammatory action of retinoids, we studied the down-regulation of genes in skin raft cultures by this antipsoriatic retinoid. By subtraction hybridization, we found that migration inhibitory factor-related protein (MRP-8) and skin-derived anti-leukoproteinase (SKALP) are down-regulated by AGN 190168. MRP-8 and SKALP are overexpressed in psoriatic lesions as compared to the normal epidermis, and they are markers of hyperproliferative keratinocyte differentiation. We also show that MRP-8 expression is retinoid inhibitable in cultured keratinocytes induced to differentiate with 10% serum or IFN-gamma, and that MRP-8 is inhibited by RAR but not by retinoid X receptor-specific retinoids in a dose-dependent manner. Finally, MRP-8, SKALP, and the previously characterized differentiation marker, transglutaminase I, are all down-regulated in vivo in psoriatic lesions after treatment with AGN 190168 in comparison to placebo. Taken together, these data suggest that these markers may be down-regulated by tazarotene in psoriasis through direct action on keratinocyte gene expression rather than by an overall tazarotene effect on lesional therapeutic status.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Antigens, Differentiation / genetics
  • Antineoplastic Agents / pharmacology
  • Biomarkers
  • Calcium-Binding Proteins / genetics
  • Calgranulin A
  • Cell Differentiation / physiology
  • Cells, Cultured / chemistry
  • Cells, Cultured / drug effects
  • Cells, Cultured / enzymology
  • DNA, Complementary / genetics
  • Dose-Response Relationship, Drug
  • Down-Regulation / physiology
  • Gene Expression Regulation, Enzymologic / drug effects
  • Gene Expression Regulation, Enzymologic / physiology
  • Glycogen Debranching Enzyme System / genetics
  • Humans
  • Interferon-gamma / pharmacology
  • Keratinocytes / chemistry
  • Keratinocytes / cytology*
  • Keratinocytes / enzymology
  • Male
  • Nicotinic Acids / pharmacology
  • Proteinase Inhibitory Proteins, Secretory
  • Proteins / genetics
  • Psoriasis / genetics
  • Psoriasis / metabolism
  • Psoriasis / pathology*
  • RNA, Messenger / metabolism
  • Receptors, Retinoic Acid / genetics*
  • Retinoids / pharmacology
  • Sensitivity and Specificity
  • Serine Proteinase Inhibitors / genetics
  • Skin / cytology
  • Teratogens / pharmacology

Substances

  • Antigens, Differentiation
  • Antineoplastic Agents
  • Biomarkers
  • Calcium-Binding Proteins
  • Calgranulin A
  • DNA, Complementary
  • Glycogen Debranching Enzyme System
  • Nicotinic Acids
  • Proteinase Inhibitory Proteins, Secretory
  • Proteins
  • RNA, Messenger
  • Receptors, Retinoic Acid
  • Retinoids
  • Serine Proteinase Inhibitors
  • Teratogens
  • tazarotene
  • Interferon-gamma
  • 4 alpha-glucanotransferase