Ligand-dependent Activators

The LEDs of the ERa and the ER/1 share a similar overall architecture. Two separate transactivation domains (AF) mediate the transactivation of the ER an N-terminal hgand-independent activation fimction (AF-1) and a C-terminal ligand-dependent activation function (AF-2), which is located within the LED (Fig. 3). The surface of the AF-1 is composed of amino acids in helices 3,4, 5 and 12, and the binding of ligands alters the position of heHx... 

Extensive biophysical and molecular studies identified several regions in TRPM8 essential for ligand-dependent activation and channel modulation. Similar to TRPA1, some aspects of channel function depend on the concentration of intracellular Ca2+. For example, the activation of TRPM8 by icilin, a cooling agent more potent than menthol, is potently enhanced when intracellular Ca2+-levels are... 

Dilworth FJ, Fromental-Ramain C, Rem-boutsika E, Benecke A, Chambon P. 1999. Ligand-dependent activation of transcription in vitro by retinoic acid receptor alpha and retinoid X receptor alpha heterodimers that mimics transactivation by retinoids in vivo. Proc. Natl. Acad. Sci. USA 96 1995-2000... 

Voegel JJ, Heine MJ, Zechei C, Chambon P, Gronemeyer H. 1996. TIF2, apl60 kDa transcriptional mediator for the ligand-dependent activation function AF-2 of nuclear receptors. EMBO, J. 15 3667-75... 

Le Douarin B, Zechei C, Gamier JM, Lutz Y, Tora L, et al. 1995. The N-terminal part of TIF1, a putative mediator of the ligand-dependent activation function (AF-2) of nuclear receptors, is fused to B-raf in the oncogenic protein T18. EMBO J. 14 2020-33... 

Gradin, K., M.L. Whitelaw, R. Toftgard, L. Poellinger and A. Berghard. A tyrosine kinase-dependent pathway regulates ligand-dependent activation of the dioxin receptor in human keratinocytes. J. Biol. Chem. 269 23800-23807, 1994. 

Tzameli, I., Chua, S. S., Cheskis, B., and Moore, D. D. (2003) Complex effects of rexinoids on ligand dependent activation or inhibition of the xenobiotic receptor, CAR. Nucl. Recept. 1, 2. 

Ou, J., Tu, H., Shan, B., Luk, A., DeBose-Boyd, R.A., Bashmakov, Y, Goldstein, J.L., Brown, M.S. 2001. Unsaturated fatty acids inhibit transcription of the sterol regulatory element-binding protein-lc (SREBP-lc) gene by antagonizing ligand-dependent activation of the LXR. Proc. Natl. Acad. Sci. U.S.A. 98 6027-6032. 

Mitra AK, Sawada K, Tiwari P, Mui K, Gwin K, Lengyel E. Ligand-dependent activation of c-Met by fibronectin and a(5) (l)-integtin regulates ovarian cancer invasion and metastasis. Oncogene. 2011 30 1566-76. 

Ohshiro, T., Emori, Y. Saigo, K (2002). Ligand-dependent activation of breathless FGF receptor gene in Drosophila developing trachea.. Mechanisms of Development 114,3-11. 

Qian X, Karpova T, Sheppard AM et al (2004) E-cadherin-me-diated adhesion inhibits ligand-dependent activation of diverse receptor tyrosine kinases. EMBO J 23 1739-1748 Ra HJ, Parks WC (2007) Control of matrix metalloproteinase catalytic activity. Matrix Biol 26 587-596 Ramachandran GN, Kartha G (1954) Structure of collagen. Nature 174 (4423) 269-270... 

Zhang, Y. et al., CD40 ligand-dependent activation of cytotoxic T lymphocytes by adeno-associated virus vectors in vivo role of immature dendritic cells, /. Virol, 74,8003,2000. 

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