Figure 5.
Figure 5 The three divergent LBP residues determine the RAR selectivity
of BMS641 and the isotype-dependent potential of BMS453. (A)
Partial proteolysis maps of in vitro-translated RARs in the
presence or absence of increasing concentrations of either
TTNPB, BMS453 or BMS641, as indicated. (B) Dose -response curves
to assess the binding affinity of BMS641 relative to TTNPB in
RAR pocket mutants. HeLa cells were co-transfected with
(RARE)3x-tk-luc and either RAR (closed
triangles), RAR (open
circles), RAR arrow
(RAR
(M[272]I,
A[397]V); open squares) or RAR arrow
(RAR
(I[263]M,
V[388]A); closed diamonds) and reporter gene transcription was
induced with 3 nM TTNPB (100%). (C) BMS453-induced luciferase
activity in HeLa cells co-transfected with (RARE)3x-tk-luc and
the indicated receptors.
The above figure is reprinted
from an Open Access publication published by Macmillan Publishers Ltd:
EMBO Rep
(2004,
5,
877-882)
copyright 2004.
selectivity
of BMS641 and the isotype-dependent potential of BMS453. (A)
Partial proteolysis maps of in vitro-translated RARs in the
presence or absence of increasing concentrations of either
TTNPB, BMS453 or BMS641, as indicated. (B) Dose -response curves
to assess the binding affinity of BMS641 relative to TTNPB in
RAR pocket mutants. HeLa cells were co-transfected with
(RARE)3x-tk-luc and either RAR 
(open
circles), RAR 
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