Vitamin D receptor (VDR) regulation of voltage-gated chloride channels by ligands preferring a VDR-alternative pocket (VDR-AP).
作者： Antonio Barrientos-Duran , Ning Chen , Helen L. Henry , Anthony W. Norman , Danusa Menegaz
DOI: 10.1210/ME.2010-0442
关键词:
摘要: We have postulated that the vitamin D receptor (VDR) contains two overlapping ligand binding sites, a genomic pocket and an alternative (AP), mediate regulation of gene transcription rapid responses, respectively. Flexible VDR + docking calculations predict major blood metabolite, 25(OH)-vitamin D3 (25D3), curcumin (CM) bind more selectively to VDR-AP when compared with seco-steroid hormone 1α,25(OH)2-vitamin (1,25D3). In wild-type-transfected COS-1 cells TM4 Sertoli cells, 1,25D3, 25D3, CM each trigger voltage-gated, outwardly rectifying chloride channel (ORCC) currents can be blocked by antagonist 1β,25(OH)2-vitamin (4,4′-diisothiocyanatostilbene-2,2′-disulfonic acid). mutational analysis in transfected demonstrate DNA-binding domain is not, but hinge domains are, required for 1,25D3 25D3 activate ORCC. Dose-response studies demon...
oup.com
endojournals.org参考文章(51)
Helen L. Henry, A. W. Norman, Encyclopedia of hormones Academic Press. ,(2003)
Ava Masoumi, Ben Goldenson, Senait Ghirmai, Hripsime Avagyan, Justin Zaghi, Ken Abel, Xueying Zheng, Araceli Espinosa-Jeffrey, Michelle Mahanian, Phillip T. Liu, Martin Hewison, Matthew Mizwicki, John Cashman, Milan Fiala, 1alpha,25-dihydroxyvitamin D3 interacts with curcuminoids to stimulate amyloid-beta clearance by macrophages of Alzheimer's disease patients. Journal of Alzheimer's Disease. ,vol. 17, pp. 703- 717 ,(2009) , 10.3233/JAD-2009-1080
A.W. Norman, R Bouillon, M.C. Farach-Carson, J.E. Bishop, L.X. Zhou, I Nemere, J Zhao, K.R. Muralidharan, W.H. Okamura, Demonstration that 1 beta,25-dihydroxyvitamin D3 is an antagonist of the nongenomic but not genomic biological responses and biological profile of the three A-ring diastereomers of 1 alpha,25-dihydroxyvitamin D3. Journal of Biological Chemistry. ,vol. 268, pp. 20022- 20030 ,(1993) , 10.1016/S0021-9258(20)80689-9
Anthony W. Norman, Seiichi Ishizuka, William H. Okamura, Ligands for the vitamin D endocrine system: different shapes function as agonists and antagonists for genomic and rapid response receptors or as a ligand for the plasma vitamin D binding protein. The Journal of Steroid Biochemistry and Molecular Biology. ,vol. 76, pp. 49- 59 ,(2001) , 10.1016/S0960-0760(00)00145-X
Mathew T. Mizwicki, Craig. M. Bula, June E. Bishop, Anthony W. Norman, A perspective on how the Vitamin D sterol/Vitamin D receptor (VDR) conformational ensemble model can potentially be used to understand the structure–function results of A-ring modified Vitamin D sterols The Journal of Steroid Biochemistry and Molecular Biology. ,vol. 97, pp. 69- 82 ,(2005) , 10.1016/J.JSBMB.2005.06.025
Céline Auzanneau, Caroline Norez, Sabrina Noël, Chantal Jougla, Frédéric Becq, Clarisse Vandebrouck, Pharmacological profile of inhibition of the chloride channels activated by extracellular acid in cultured rat Sertoli cells. Reproduction Nutrition Development. ,vol. 46, pp. 241- 255 ,(2006) , 10.1051/RND:2006013
Anthony W. Norman, June E. Bishop, Elaine D. Collins, Eun-Gyoung Seo, Donald P. Satchell, Murray C. Dormanen, Susana B. Zanello, Mary C. Farach-Carson, Roger Bouillon, William H. Okamura, Differing shapes of 1α,25-dihydroxyvitamin D3 function as ligands for the D-binding protein, nuclear receptor and membrane receptor: A status report The Journal of Steroid Biochemistry and Molecular Biology. ,vol. 56, pp. 13- 22 ,(1996) , 10.1016/0960-0760(95)00219-7
Anthony W Norman, Christopher J Olivera, Fátima R Mena Barreto Silva, June E Bishop, A specific binding protein/receptor for 1α,25-dihydroxyvitamin D3 is present in an intestinal caveolae membrane fraction Biochemical and Biophysical Research Communications. ,vol. 298, pp. 414- 419 ,(2002) , 10.1016/S0006-291X(02)02482-8
Guisheng Zhao, Robert U. Simpson, Membrane localization, Caveolin-3 association and rapid actions of vitamin D receptor in cardiac myocytes. Steroids. ,vol. 75, pp. 555- 559 ,(2010) , 10.1016/J.STEROIDS.2009.12.001
Anthony W. Norman, Mathew T. Mizwicki, Derek P. G. Norman, Steroid-hormone rapid actions, membrane receptors and a conformational ensemble model. Nature Reviews Drug Discovery. ,vol. 3, pp. 27- 41 ,(2004) , 10.1038/NRD1283