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Abstract 1919: Warfarin-dependent gamma-carboxylation regulates androgen receptor activity
The anti-coagulant warfarin prevents the gamma-carboxylation (gla) of target proteins by interfering with the vitamin K cycle through its inhibition of the vitamin K epoxide reductase (VKOR). Most known gla proteins are found in the blood clotting cascade, but we demonstrate using immunoprecipitation and mass spectrometry that the androgen receptor (AR) can also be gamma-carboxylated. This modification occurs at amino acid 2E and can be prevented by warfarin treatment. This residue has been found to be mutated in partial androgen insensitivity syndrome patients. Warfarin, likely through its ability to control carboxylation...
Source: Cancer Research - August 2, 2015 Category: Cancer & Oncology Authors: Tew, B. Y., Hong, T., Pal, S. K., Kalkum, M., Jones, J. Tags: Prevention Research Source Type: research

Abstract 37: Role and regulation of CYP24A1 in endometrial cancer
The cytochrome P450 enzyme, 24-hydroxylase, encoded by CYP24A1 is critical for the catabolism of 1,25(OH)2D3 (calcitriol). The unbalanced high levels of CYP24A1 seem to be a determinant of calcitriol resistance in tumors. We have previously shown that progesterone enhances calcitriol antitumor activity by upregulating vitamin D receptor expression and promoting apoptosis in endometrial cancer cells. In the present study, we evaluated CYP24A1 protein expression in normal and endometrial tumor tissues, assessed the effect of progesterone and calcitriol on CYP24A1 and its spliced variant expression in endometrial cancer cell ...
Source: Cancer Research - August 2, 2015 Category: Cancer & Oncology Authors: Bokhari, A. A., Lee, L. R., Dewayne, R., Hamilton, C. A., Maxwell, G. L., Rodriguez, G. C., Syed, V. Tags: Molecular and Cellular Biology Source Type: research

Abstract 1248: The Gemini vitamin D analogue BXL0124 inhibits Notch signaling via HES1, resulting in the reduction of CD44+/CD24-/low subpopulation and proliferation of MCF10DCIS cells
Activation of Notch signaling is correlated with poor prognosis and decreased survival of breast cancer patients. Recent studies reported that Notch signaling plays an important role for the maintenance of tumor-initiating cells in breast cancer. Using MCF10DCIS.com human breast cancer cells (MCF10DCIS), which contain tumor-initiating subpopulation (CD44+/CD24-/low), we demonstrated that the Gemini vitamin D analog, BXL0124, reduced the tumor-initiating subpopulation in vitro and repressed the growth of MCF10DCIS xenograft tumors in vivo. In the present study, we investigated Notch signaling in CD44+/CD24-/low and CD44+/CD...
Source: Cancer Research - September 30, 2014 Category: Cancer & Oncology Authors: So, J. Y., Salerno, D. M., Maehr, H., Uskokovic, M., Suh, N. Tags: Prevention Research Source Type: research

Abstract 4751: 25-hydroxyvitamin D3 induces vitamin D signaling independent of CYP27B1 in non-small cell lung cancer cells
Conclusions NSCLC cells expressing high levels of VDR display increased responsiveness to vitamin D metabolites. Although NSCLC cells express CYP27B1, our results demonstrate that the enzyme may not be required to achieve vitamin D signaling. Rather, 25(OH)D3 may act via the VDR to elicit an anti-tumor responses. The implication of these findings is that dietary supplementation to increase circulating 25(OH)D3 may be beneficial in a subset of NSCLC patients. Funding provided by NIH RO1 CA132844, training grant 5T32CA009072-37 and P30CA47904 Citation Format: Alissa R. Verone, Suzanne Shoemaker, Robert Parise, Jan H. Beumer,...
Source: Cancer Research - September 30, 2014 Category: Cancer & Oncology Authors: Verone, A. R., Shoemaker, S., Parise, R., Beumer, J. H., Hershberger, P. A. Tags: Endocrinology Source Type: research

CK2 Inhibitor Enhances Vitamin D-Mediated Antitumor Effects
Vitamin D has broad range of physiological functions and antitumor effects. 24-Hydroxylase, encoded by the CYP24A1 gene, is the key enzyme for degrading many forms of vitamin D including the most active form, 1,25D3. Inhibition of CYP24A1 enhances 1,25D3 antitumor activity. To isolate regulators of CYP24A1 expression in prostate cancer cells, we established a stable prostate cancer cell line PC3 with CYP24A1 promoter driving luciferase expression to screen a small molecular library for compounds that inhibit CYP24A1 promoter activity. From this screening, we identified, 4,5,6,7-tetrabromobenzimidazole (TBBz), a protein kin...
Source: Cancer Research - April 2, 2013 Category: Cancer & Oncology Authors: Luo, W., Yu, W.-D., Ma, Y., Chernov, M., Trump, D. L., Johnson, C. S. Tags: Therapeutics, Targets, and Chemical Biology Source Type: research