PMID- 29560490
OWN - NLM
STAT- MEDLINE
DCOM- 20190311
LR  - 20190311
IS  - 1477-0539 (Electronic)
IS  - 1477-0520 (Linking)
VI  - 16
IP  - 14
DP  - 2018 Apr 4
TI  - Effects of 2-substitution on 14-epi-19-nortachysterol-mediated biological events: 
      based on synthesis and X-ray co-crystallographic analysis with the human vitamin 
      D receptor.
PG  - 2448-2455
LID - 10.1039/C8OB00158H [doi]
AB  - Both 2alpha- and 2beta-hydroxypropyl substituted 
      14-epi-1alpha,25-dihydroxy-19-nortachysterols were synthesized to study the human 
      vitamin D receptor (hVDR) binding affinity, binding configurations, and 
      interactions with amino acid residues in the ligand binding domain of hVDR by 
      X-ray co-crystallographic analysis. In conjunction with our previous results on 
      14-epi-19-nortachysterol, 2-methylidene-, 2alpha-methyl-, 2beta-methyl, and 
      2alpha-hydroxypropoxy-14-epi-19-nortachysterol, we propose a variety of effects of 
      substitution at the C2 position in the 14-epi-19-nortachysterol skeleton on 
      biological activities.
FAU - Sawada, Daisuke
AU  - Sawada D
AD  - Faculty of Pharmaceutical Sciences, Teikyo University, Kaga, Itabashi, Tokyo 
      173-8605, Japan. akittaka@pharm.teikyo-u.ac.jp.
FAU - Kakuda, Shinji
AU  - Kakuda S
AD  - Teijin Institute for Bio-medical Research, Teijin Pharma Ltd, Hino, Tokyo 
      191-8512, Japan.
FAU - Takeuchi, Akiko
AU  - Takeuchi A
AD  - Teijin Institute for Bio-medical Research, Teijin Pharma Ltd, Hino, Tokyo 
      191-8512, Japan.
FAU - Kawagoe, Fumihiro
AU  - Kawagoe F
AD  - Faculty of Pharmaceutical Sciences, Teikyo University, Kaga, Itabashi, Tokyo 
      173-8605, Japan. akittaka@pharm.teikyo-u.ac.jp.
FAU - Takimoto-Kamimura, Midori
AU  - Takimoto-Kamimura M
AD  - Teijin Institute for Bio-medical Research, Teijin Pharma Ltd, Hino, Tokyo 
      191-8512, Japan.
FAU - Kittaka, Atsushi
AU  - Kittaka A
AUID- ORCID: 0000-0003-3091-2476
AD  - Faculty of Pharmaceutical Sciences, Teikyo University, Kaga, Itabashi, Tokyo 
      173-8605, Japan. akittaka@pharm.teikyo-u.ac.jp.
LA  - eng
PT  - Journal Article
PL  - England
TA  - Org Biomol Chem
JT  - Organic & biomolecular chemistry
JID - 101154995
RN  - 0 (Ligands)
RN  - 0 (Receptors, Calcitriol)
RN  - 0 (VDR protein, human)
RN  - 1C6V77QF41 (Cholecalciferol)
RN  - HDA46400N5 (previtamin D(3))
SB  - IM
MH  - Binding Sites
MH  - Cholecalciferol/*analogs & derivatives/chemical synthesis/chemistry
MH  - Crystallography, X-Ray
MH  - Humans
MH  - Ligands
MH  - Molecular Structure
MH  - Receptors, Calcitriol/*chemistry
EDAT- 2018/03/22 06:00
MHDA- 2019/03/12 06:00
CRDT- 2018/03/22 06:00
PHST- 2018/03/22 06:00 [pubmed]
PHST- 2019/03/12 06:00 [medline]
PHST- 2018/03/22 06:00 [entrez]
AID - 10.1039/C8OB00158H [doi]
PST - ppublish
SO  - Org Biomol Chem. 2018 Apr 4;16(14):2448-2455. doi: 10.1039/C8OB00158H.