Receptor-interacting protein 140 is a repressor of the androgen receptor activity.: AR repression by RIP140

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HAL Id: inserm-00145497

https://www.hal.inserm.fr/inserm-00145497

Submitted on 11 May 2007

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To cite this version:

Sophie Carascossa, Jérôme Gobinet, Virginie Georget, Annick Lucas, Eric Badia, et al.. Receptor-interacting protein 140 is a repressor of the androgen receptor activity.: AR repression by RIP140. Molecular Endocrinology -Baltimore-, Endocrine Society, 2006, 20 (7), pp.1506-18. �10.1210/me.2005-0286�. �inserm-00145497�

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Control

IP: AR

IB:

α c-myc

IB:

α AR

AR AR + c-mycRIP140 Inpu t IP Inpu t IP Inpu t IP

1

2

3

4

5

6

c-mycRIP140 Inpu t IP

7

8

(3)

In

pu

t

G

ST

G

ST

-R

IP

(2

7-43

9)

G

ST

-R

IP

(4

28 -7

39 G

ST

-R

IP

(6

83 -1

15 AR

AR(1-501)

AR(618-919)

B

(4)

C

0 0,005

0,01

0,015

0,02

0,025

0,03

0,035

0,04

% input

promoter

enhancer

1h

6h

1h

6h

Ethanol

R1881 (10

-8

_{M )}

(5)

+ R1881

+ bicalutamide

CFP channel YFP channel overlay YFP channel

vehicle

+ R1881

CFP-AR(1-501) + YFP-RIP140

CFP channel YFP channel overlay

vehicle

CFP-AR (507-919) + YFP-RIP140

CFP channel YFP channel overlay

(6)

A

0 200 RIP140 (ng) 600 1000 2000 lu ci fe ra se ac ti v it y (% ) 0 20 40 60 80 100 120

C

RIP140 (800 ng) lucifer ase ac tiv it y (% ) 0 20 40 60 80 100 120 - wt (1-2 82) (1-4 80) (479 -115 8) (917 -115 8) RIP140(917-1158) (ng) 0 0 800 1200 1600 TIF2 (200 ng) - + + + + lucifer ase ac tiv it y (% ) 0 20 40 60 80 100 120 140 160

D

0 200 400 600 800 1000 1200 10 10 50 50 AR (ng) MEF wt -/- wt -/-lucif er as e activ it y (% )

B

(7)

lu ci fe ra se ac ti v it y (% ) 0 RIP140 (ng) 200 600 1000 2000 0 20 40 60 80 100 120 140

A

RIP140 (ng) TIF2 (200 ng) 0 -0 + 50 +

AR(507-919)

EtOH

R1881 (10

-9

_M)

lu ci fera se ac ti v ity (% ) 0 20 40 60 80 100 120

B

(8)

0

20

40

60

80

100

120

140

lu ci fera se acti v it y(% )

RIP140-wt (ng)

RIP140-PIDLS (ng)

RIP140-PINLS (ng)

RIP140-PILS (ng)

100 400 800

-

--

-

--

-

--

-

-100 400 800 100 400 800 100 400 800

EtOH

R1881 (10

-9

_M)

(9)

-RIP140 (ng)

0 800 1200 1600 2000 0 800 1200 1600 2000

TSA (50 nM)

RIP140 (ng)

0 800 1200 1600 2000 0 800 1200 1600 2000 0 20 40 60 80 100 120 140 0 20 40 60 80 100

TAT promoter

lu cife ra se ac ti v ity (% ) luci fe rase ac tiv it y (%

EtOH

R1881 (10

-9

_M)

Control

TSA (50 nM)

Control

B

(10)

0 1 2 3 4 5 Ctl 1h 3h 6h 12h Ratio RIP140 /3 6B 4

RIP140

36B4

1h 3h 6h 12h Ctl