PMID- 16848739
OWN - NLM
STAT- MEDLINE
DCOM- 20070221
LR  - 20190907
IS  - 1568-0266 (Print)
IS  - 1568-0266 (Linking)
VI  - 6
IP  - 12
DP  - 2006
TI  - Ligand recognition by vitamin D receptor: total alanine scanning mutational 
      analysis of the residues lining the ligand binding pocket of vitamin D receptor.
PG  - 1255-65
AB  - We performed total alanine scanning mutational analysis (ASMA) of the residues 
      lining the ligand binding pocket (LBP) of the human vitamin D receptor (hVDR) to 
      investigate allosteric effects of ligands in the function of nuclear receptors 
      (NRs). This was accomplished for the first time in the NR superfamily. The 
      effects of ligand structure were also examined in this system (termed 2D-ASMA) 
      using 8 representative VDR ligands. The results clearly revealed the role and 
      importance of all amino acid residues lining the LBP and the relationships 
      between ligand binding and transcriptional potency. 2D-ASMA indicated 
      ligand-specific ligand-protein interactions, which are essential in determining 
      the transactivation potency of the ligand. Taking the results as a whole, we 
      suggest a ligand-mediated allosteric network, which allows transmission of 
      information from ligands to the interfaces of the VDR in association with protein 
      cofactors and was shown to be linked to a part of the network identified by 
      statistical coupling analysis (SCA).
FAU - Yamada, Sachiko
AU  - Yamada S
AD  - Department of Biochemistry, Nihon University School of Medicine, 
      Oyaguchi-kamicho, Itabashi-ku, Tokyo 173-8610, Japan. yamada.vd@image.ocn.ne.jp
FAU - Yamamoto, Keiko
AU  - Yamamoto K
LA  - eng
PT  - Journal Article
PL  - United Arab Emirates
TA  - Curr Top Med Chem
JT  - Current topics in medicinal chemistry
JID - 101119673
RN  - 0 (Ligands)
RN  - 0 (Receptors, Calcitriol)
RN  - OF5P57N2ZX (Alanine)
SB  - IM
MH  - Alanine/*genetics
MH  - Amino Acid Sequence
MH  - Binding Sites
MH  - Ligands
MH  - Mutagenesis/*genetics
MH  - Protein Binding
MH  - Receptors, Calcitriol/agonists/*chemistry/genetics/*metabolism
MH  - Structure-Activity Relationship
EDAT- 2006/07/20 09:00
MHDA- 2007/02/22 09:00
CRDT- 2006/07/20 09:00
PHST- 2006/07/20 09:00 [pubmed]
PHST- 2007/02/22 09:00 [medline]
PHST- 2006/07/20 09:00 [entrez]
AID - 10.2174/156802606777864881 [doi]
PST - ppublish
SO  - Curr Top Med Chem. 2006;6(12):1255-65. doi: 10.2174/156802606777864881.