Search Results
Search for other papers by Aprajita S Yadav in
Google Scholar
PubMed
Search for other papers by Nina Isoherranen in
Google Scholar
PubMed
Division of Metabolism, Endocrinology and Nutrition, Department of Medicine, University of Washington, Seattle, Washington, USA
Search for other papers by Katya B Rubinow in
Google Scholar
PubMed
interventional strategies to mitigate body weight gain and its sequelae ( Blüher 2019 ). Vitamin A or retinol is a fat-soluble vitamin with long recognized roles in vision, growth, reproduction, and immunity. An expanding body of evidence further implicates
Pathology Laboratory and Molecular Biology Laboratory, Istituto Auxologico Italiano, Via Zucchi, 18-Cusano Milanino, Milano, Italy
Dept of Obstetrics and Gynecology, Clinica Macedonio Melloni, University of Milano, Milano, Italy
BioXell S.p.A, Milano, Italy
Search for other papers by P Viganò in
Google Scholar
PubMed
Pathology Laboratory and Molecular Biology Laboratory, Istituto Auxologico Italiano, Via Zucchi, 18-Cusano Milanino, Milano, Italy
Dept of Obstetrics and Gynecology, Clinica Macedonio Melloni, University of Milano, Milano, Italy
BioXell S.p.A, Milano, Italy
Search for other papers by D Lattuada in
Google Scholar
PubMed
Pathology Laboratory and Molecular Biology Laboratory, Istituto Auxologico Italiano, Via Zucchi, 18-Cusano Milanino, Milano, Italy
Dept of Obstetrics and Gynecology, Clinica Macedonio Melloni, University of Milano, Milano, Italy
BioXell S.p.A, Milano, Italy
Search for other papers by S Mangioni in
Google Scholar
PubMed
Pathology Laboratory and Molecular Biology Laboratory, Istituto Auxologico Italiano, Via Zucchi, 18-Cusano Milanino, Milano, Italy
Dept of Obstetrics and Gynecology, Clinica Macedonio Melloni, University of Milano, Milano, Italy
BioXell S.p.A, Milano, Italy
Search for other papers by L Ermellino in
Google Scholar
PubMed
Pathology Laboratory and Molecular Biology Laboratory, Istituto Auxologico Italiano, Via Zucchi, 18-Cusano Milanino, Milano, Italy
Dept of Obstetrics and Gynecology, Clinica Macedonio Melloni, University of Milano, Milano, Italy
BioXell S.p.A, Milano, Italy
Search for other papers by M Vignali in
Google Scholar
PubMed
Pathology Laboratory and Molecular Biology Laboratory, Istituto Auxologico Italiano, Via Zucchi, 18-Cusano Milanino, Milano, Italy
Dept of Obstetrics and Gynecology, Clinica Macedonio Melloni, University of Milano, Milano, Italy
BioXell S.p.A, Milano, Italy
Search for other papers by E Caporizzo in
Google Scholar
PubMed
Pathology Laboratory and Molecular Biology Laboratory, Istituto Auxologico Italiano, Via Zucchi, 18-Cusano Milanino, Milano, Italy
Dept of Obstetrics and Gynecology, Clinica Macedonio Melloni, University of Milano, Milano, Italy
BioXell S.p.A, Milano, Italy
Search for other papers by P Panina-Bordignon in
Google Scholar
PubMed
Pathology Laboratory and Molecular Biology Laboratory, Istituto Auxologico Italiano, Via Zucchi, 18-Cusano Milanino, Milano, Italy
Dept of Obstetrics and Gynecology, Clinica Macedonio Melloni, University of Milano, Milano, Italy
BioXell S.p.A, Milano, Italy
Search for other papers by M Besozzi in
Google Scholar
PubMed
Pathology Laboratory and Molecular Biology Laboratory, Istituto Auxologico Italiano, Via Zucchi, 18-Cusano Milanino, Milano, Italy
Dept of Obstetrics and Gynecology, Clinica Macedonio Melloni, University of Milano, Milano, Italy
BioXell S.p.A, Milano, Italy
Search for other papers by A M Di Blasio in
Google Scholar
PubMed
Introduction Vitamin D is a major regulator of mineral ion homeostasis by facilitating calcium and phosphate uptake in the gut and by modulating bone cell development and action ( Kumar 1980 , Jones et al. 1998 ). However, the
Search for other papers by T Ichikawa in
Google Scholar
PubMed
Search for other papers by K Horie-Inoue in
Google Scholar
PubMed
Search for other papers by K Ikeda in
Google Scholar
PubMed
Search for other papers by B Blumberg in
Google Scholar
PubMed
Division of Gene Regulation and Signal Transduction, Research Center for Genomic Medicine, Saitama Medical University, Hidaka-shi, Saitama 350-1241, Japan Department of Developmental and Cell Biology, University of California, Irvine, California 92697-2300, USA Department of Geriatric Medicine, Graduate School of Medicine, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8655, Japan
Search for other papers by S Inoue in
Google Scholar
PubMed
Introduction Vitamin Ks are fat-soluble 2-methyl-1,4-naphthoquinone-related compounds, including natural phylloquinone (K 1 ) and menaquinones (K 2 ). Vitamins K 1 and K 2 differ only in the substituent group. Vitamin K 1 possesses a phytyl group
Department of Pathology,
National Centre for Laboratory Animal Sciences, National Institute of Nutrition, Jamai-Osmania PO, Hyderabad-500 007, Andhra Pradesh, India
Search for other papers by S M Jeyakumar in
Google Scholar
PubMed
Department of Pathology,
National Centre for Laboratory Animal Sciences, National Institute of Nutrition, Jamai-Osmania PO, Hyderabad-500 007, Andhra Pradesh, India
Search for other papers by A Vajreswari in
Google Scholar
PubMed
Department of Pathology,
National Centre for Laboratory Animal Sciences, National Institute of Nutrition, Jamai-Osmania PO, Hyderabad-500 007, Andhra Pradesh, India
Search for other papers by B Sesikeran in
Google Scholar
PubMed
Department of Pathology,
National Centre for Laboratory Animal Sciences, National Institute of Nutrition, Jamai-Osmania PO, Hyderabad-500 007, Andhra Pradesh, India
Search for other papers by N V Giridharan in
Google Scholar
PubMed
continuous recruitment of newer cells and elimination of adipocytes by apoptosis under normal physiological conditions as well as disease conditions. Vitamin A, an important micronutrient, has an unusually wide range of vital physiological actions in
Search for other papers by Maria K Tsoumpra in
Google Scholar
PubMed
Search for other papers by Shun Sawatsubashi in
Google Scholar
PubMed
Search for other papers by Michihiro Imamura in
Google Scholar
PubMed
Search for other papers by Seiji Fukumoto in
Google Scholar
PubMed
Search for other papers by Shin’ichi Takeda in
Google Scholar
PubMed
Search for other papers by Toshio Matsumoto in
Google Scholar
PubMed
Search for other papers by Yoshitsugu Aoki in
Google Scholar
PubMed
Introduction The biologically active metabolite of vitamin D, 1,25-dihydroxyvitamin D 3 (VD3), is a calcium regulating hormone that exerts its tissue-specific biological actions through binding to its intracellular vitamin D receptor (VDR
Search for other papers by R F Chun in
Google Scholar
PubMed
Search for other papers by M Gacad in
Google Scholar
PubMed
Search for other papers by L Nguyen in
Google Scholar
PubMed
Search for other papers by M Hewison in
Google Scholar
PubMed
Search for other papers by J S Adams in
Google Scholar
PubMed
and vitamin D receptors; VDRs), it seems unlikely that the process of binding a specific ligand will depend simply on localized concentration gradients. Whereas the mechanisms that define the intracellular localization and movement of receptor proteins
Search for other papers by Vincent Giguère in
Google Scholar
PubMed
from organs and biological fluids that had profound effects on reproduction, development, and general maintenance of a healthy organism. Coincidently, the chemical structure of vitamin A and the steroid hormones estradiol and progesterone were resolved
Search for other papers by M J Campbell in
Google Scholar
PubMed
Search for other papers by E Elstner in
Google Scholar
PubMed
Search for other papers by S Holden in
Google Scholar
PubMed
Search for other papers by M Uskokovic in
Google Scholar
PubMed
Search for other papers by H P Koeffler in
Google Scholar
PubMed
ABSTRACT
We have synthesized and studied the ability of a series of seven novel 1α,25(OH)2 vitamin D3 analogues to inhibit clonal growth of prostate cancer cells (LNCaP, PC-3 and DU-145). Addition of double and triple bonds to the C/D ring (C-16) and side chain (C-22 and C-23) as well as lengthening of the side chain were important for enhanced activity against LNCaP and PC-3. Reorientation of the side chain in the 20-epi configuration resulted in analogues that were extremely potent only against LNCaP (ED50 ≈ 5 × 10−11 m). Compounds with six fluorines on the end of the side chain were very active against both PC-3 and LNCaP (ED50 ≈ 2 × 10−8 m). DU-145 cells were relatively resistant to compounds with all of these modifications, but removal of C-19 (e.g. 1,25(OH)2-16-ene-23-yne-26,27-F6-19-nor-D3) resulted in an analogue that was inhibitory against all three prostate cell lines. Further analysis showed that pulse exposure (3 days, 10−7 m) to this analogue was enough to inhibit clonal growth of PC-3 cells by 50%. The same exposure also induced cell cycle arrest of all three cell lines, accompanied by upregulated protein expression of the cyclin-dependent kinase inhibitor (CDKI) known as p21 waf1 in all three cell lines, and the CDKI known as p27 kip1 in LNCaP cells. Associated with upregulation of these CDKIs, partial differentiation occurred as measured by increased expression of both prostate-specific antigen by LNCaP cells and E-cadherin, a cell adhesion protein that may act as a putative tumour suppressor (LNCaP and PC-3 cells). In summary, this is the first report of a potent series of 19-nor-vitamin D3 analogues with the ability to inhibit proliferation of LNCaP, PC-3 and DU-145 prostate cancer cell lines. These compounds may mediate their potent anti-proliferative activities through a cell cycle arrest pathway.
Search for other papers by Andrea Hanel in
Google Scholar
PubMed
Search for other papers by Henna-Riikka Malmberg in
Google Scholar
PubMed
Search for other papers by Carsten Carlberg in
Google Scholar
PubMed
Introduction The micronutrient vitamin D 3 is known best as a key regulator of calcium homeostasis, which is essential for proper bone formation ( van de Peppel & van Leeuwen 2014 , Carmeliet et al . 2015 ). Interestingly, the nuclear
Search for other papers by Lorraine J Gudas in
Google Scholar
PubMed
Introduction and focus Vitamin A (all-trans retinol, ROL), a lipid-soluble micronutrient, is absolutely required for mammalian life. Without vitamin A, mammals develop many clinical pathologies, from xerophthalmia (dryness and inflammation of
