TY - JOUR
T1 - 2 α-(3-hydroxypropyl)- and 2 α-(3-hydroxypropoxy)-1 α,25-dihydroxyvitamin D3 accessible to vitamin D receptor mutant related to hereditary vitamin D-resistant rickets
AU - Kittaka, Atsushi
AU - Kurihara, Masaaki
AU - Peleg, Sara
AU - Suhara, Yoshitomo
AU - Takayama, Hiroaki
PY - 2003/3
Y1 - 2003/3
N2 - Hereditary vitamin D-resistant rickets (HVDRR) is a genetic disorder caused by mutations in the vitamin D receptor, which lead to resistance to 1 α,25-dihydroxyvitamin D3 [1 α,25(OH)2D 3]. We found that the A ring-modified analogues, 2 α-(3-hydroxypropyl)-and 2 α-(3-hydroxypropoxy)-1 α,25(OH) 2D3, (O1C3 and O2C3) can bind better than the natural hormone to the mutant VDR (R274A), which similar to the HVDRR mutant, R274L, had lost the hydrogen bond to the 1 α-hydroxyl group of 1 α,25(OH) 2D3.
AB - Hereditary vitamin D-resistant rickets (HVDRR) is a genetic disorder caused by mutations in the vitamin D receptor, which lead to resistance to 1 α,25-dihydroxyvitamin D3 [1 α,25(OH)2D 3]. We found that the A ring-modified analogues, 2 α-(3-hydroxypropyl)-and 2 α-(3-hydroxypropoxy)-1 α,25(OH) 2D3, (O1C3 and O2C3) can bind better than the natural hormone to the mutant VDR (R274A), which similar to the HVDRR mutant, R274L, had lost the hydrogen bond to the 1 α-hydroxyl group of 1 α,25(OH) 2D3.
KW - 2 α-substituted 1 α,25-dihydroxyvitamin D
KW - Docking study
KW - Mutant vitamin D receptor
KW - Potent ligand
KW - Rickets
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U2 - 10.1248/cpb.51.357
DO - 10.1248/cpb.51.357
M3 - Article
C2 - 12612432
AN - SCOPUS:0042398448
VL - 51
SP - 357
EP - 358
JO - Chemical and Pharmaceutical Bulletin
JF - Chemical and Pharmaceutical Bulletin
SN - 0009-2363
IS - 3
ER -