Efficacy and Mechanism of Action of 1α-hydroxy-24-ethyl-Cholecalciferol (1α[OH]D5) in Breast Cancer Prevention and Therapy

  • Erum A. Hussain
  • Rajeshwari R. Mehta
  • Rahul Ray
  • Tapas K. Das Gupta
  • Rajendra G. Mehta
Part of the Recent Results in Cancer Research book series (RECENTCANCER, volume 164)


It is now well established that the active metabolite of vitamin D3, 1α,25(OH)2D3, regulates cell growth and differentiation in various in vitrocancer models. However, its clinical use is precluded due to its hypercalcemicactivity in vivo. Hence, several less calcemic vitamin D analogs have been synthesizedand evaluated for their chemopreventive and therapeutic efficacy inexperimental carcinogenesis models. A novel analog of vitamin D3, 1α-hydroxy-24-ethyl-cholecalciferol (1α[OH]D5), has currently been under investigationin our laboratory for its application in breast cancer prevention andtherapy. 1α(OH)D5 had been shown to inhibit development of estrogen-andprogesterone-dependent ductal lesions as well as steroid hormone-independentalveolar lesions in a mammary gland organ culture (MMOC) model. Moreover, the inhibitory effect was more significant if 1α(OH)D5 was presentduring the promotional phase of the lesion development. The growth inhibitoryeffect of 1α(OH)D5 has also been manifested in several breast cancer celllines, including BT-474 and MCF-7. Breast cancer cell lines that responded to1a(OH)D5 treatment were vitamin D receptor positive (VDR+). Vitamin D receptor-negative (VDR_) cell lines, such as MDA-MB-231 and MDA-MB-435, did not show growth inhibition upon incubation with 1α(OH)D5.


Breast Cancer Mammary Gland Progesterone Receptor Breast Cancer Prevention Calcemic Activity 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


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Copyright information

© Springer-Verlag Berlin Heidelberg 2003

Authors and Affiliations

  • Erum A. Hussain
  • Rajeshwari R. Mehta
  • Rahul Ray
  • Tapas K. Das Gupta
  • Rajendra G. Mehta
    • 1
  1. 1.Department of Surgical OncologyUniversity of Illinois at ChicagoChicagoUSA

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