PMID- 9624051
OWN - NLM
STAT- MEDLINE
DCOM- 19980702
LR  - 20190619
IS  - 0036-8075 (Print)
IS  - 0036-8075 (Linking)
VI  - 280
IP  - 5370
DP  - 1998 Jun 12
TI  - Hormone-dependent coactivator binding to a hydrophobic cleft on nuclear 
      receptors.
PG  - 1747-9
AB  - The ligand-binding domain of nuclear receptors contains a transcriptional 
      activation function (AF-2) that mediates hormone-dependent binding of coactivator 
      proteins. Scanning surface mutagenesis on the human thyroid hormone receptor was 
      performed to define the site that binds the coactivators, glucocorticoid 
      receptor-interacting protein 1 (GRIP1) and steroid receptor coactivator 1 
      (SRC-1). The residues involved encircle a small surface that contains a 
      hydrophobic cleft. Ligand activation of transcription involves formation of this 
      surface by folding the carboxyl-terminal alpha helix against a scaffold of three 
      other helices. These features may represent general ones for nuclear receptors.
FAU - Feng, W
AU  - Feng W
AD  - Metabolic Research Unit, Box 0540, University of California San Francisco, San 
      Francisco, CA 94143-0540, USA.
FAU - Ribeiro, R C
AU  - Ribeiro RC
FAU - Wagner, R L
AU  - Wagner RL
FAU - Nguyen, H
AU  - Nguyen H
FAU - Apriletti, J W
AU  - Apriletti JW
FAU - Fletterick, R J
AU  - Fletterick RJ
FAU - Baxter, J D
AU  - Baxter JD
FAU - Kushner, P J
AU  - Kushner PJ
FAU - West, B L
AU  - West BL
LA  - eng
GR  - DK09516/DK/NIDDK NIH HHS/United States
GR  - DK51281/DK/NIDDK NIH HHS/United States
GR  - P41-RR01081/RR/NCRR NIH HHS/United States
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - United States
TA  - Science
JT  - Science (New York, N.Y.)
JID - 0404511
RN  - 0 (Ligands)
RN  - 0 (NCOA2 protein, human)
RN  - 0 (Nuclear Receptor Coactivator 2)
RN  - 0 (Receptors, Retinoic Acid)
RN  - 0 (Receptors, Thyroid Hormone)
RN  - 0 (Recombinant Fusion Proteins)
RN  - 0 (Retinoid X Receptors)
RN  - 0 (Transcription Factors)
RN  - 06LU7C9H1V (Triiodothyronine)
RN  - EC 2.3.1.48 (Histone Acetyltransferases)
RN  - EC 2.3.1.48 (NCOA1 protein, human)
RN  - EC 2.3.1.48 (Nuclear Receptor Coactivator 1)
SB  - IM
MH  - HeLa Cells
MH  - Histone Acetyltransferases
MH  - Humans
MH  - Ligands
MH  - Models, Molecular
MH  - Mutagenesis, Site-Directed
MH  - Nuclear Receptor Coactivator 1
MH  - Nuclear Receptor Coactivator 2
MH  - Protein Conformation
MH  - Protein Folding
MH  - Protein Structure, Secondary
MH  - Receptors, Retinoic Acid/metabolism
MH  - Receptors, Thyroid Hormone/*chemistry/genetics/*metabolism
MH  - Recombinant Fusion Proteins/metabolism
MH  - Retinoid X Receptors
MH  - Transcription Factors/*metabolism
MH  - *Transcriptional Activation
MH  - Triiodothyronine/*metabolism/pharmacology
EDAT- 1998/06/20 00:00
MHDA- 1998/06/20 00:01
CRDT- 1998/06/20 00:00
PHST- 1998/06/20 00:00 [pubmed]
PHST- 1998/06/20 00:01 [medline]
PHST- 1998/06/20 00:00 [entrez]
AID - 10.1126/science.280.5370.1747 [doi]
PST - ppublish
SO  - Science. 1998 Jun 12;280(5370):1747-9. doi: 10.1126/science.280.5370.1747.