title: A melanocortin receptor 1 and 5 antagonist inhibits sebaceous gland differentiation and the production of sebum-specific lipids.
abstract: BACKGROUND
  The melanocortin receptor-5 (MC5R) is present in human sebaceous glands, where it is expressed in differentiated sebocytes only. The targeted disruption of MC5R in mice resulted in reduced sebaceous lipid production and a severe defect in water repulsion.
  
  
  OBJECTIVE
  To investigate the physiological function of MC5R in human sebaceous glands.
  
  
  METHODS
  A novel MC1R and MC5R antagonist (JNJ-10229570) was used to treat primary human sebaceous cells or human skins grafted onto severe combined immunodeficient (SCID) mice. Transcription profiling, lipid analyses, and histological and immunohistochemical staining were used to analyze the effect of MC5R inhibition on sebaceous gland differentiation and sebum production.
  
  
  RESULTS
  JNJ-10229570 dose dependently inhibited the production of sebaceous lipids in cultured primary human sebocytes. Topical treatment with JNJ-10229570 of human skins transplanted onto SCID mice resulted in a marked decrease in sebum-specific lipid production, sebaceous gland's size and the expression of the sebaceous differentiation marker epithelial-membrane antigen (EMA). Treatment with flutamide, a known inhibitor of sebum production, gave similar results, validating the human skin/SCID mouse experimental system for sebaceous secretion studies.
  
  
  CONCLUSIONS
  Our data suggest that antagonists of MC1R and MC5R could be effective sebum suppressive agents and might have a potential for the treatment of acne and other sebaceous gland pathologies.
authors: The Johnson & Johnson Skin Research Center, Consumer Product Worldwide, a Unit of Johnson & Johnson Consumer Companies, Inc. 199 Grandview Rd., Skillman, NJ 08558, USA.
authors: Magdalena
authors: M
authors: Eisinger
authors: Wen-Hwa
authors: WH
authors: Li
authors: Michael
authors: M
authors: Anthonavage
authors: Apostolos
authors: A
authors: Pappas
authors: Li
authors: L
authors: Zhang
authors: Dianne
authors: D
authors: Rossetti
authors: Qiuling
authors: Q
authors: Huang
authors: Miri
authors: M
authors: Seiberg