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NFkappaB selectivity of estrogen receptor ligands revealed by comparative crystallographic analyses.

Nettles KW, Bruning JB, Gil G, Nowak J, Sharma SK, Hahm JB, Kulp K, Hochberg RB, Zhou H, Katzenellenbogen JA, Katzenellenbogen BS, Kim Y, Joachmiak A, Greene GL
Nat Chem Biol 4 241-7 (2008)
Related entries: 2b23, 2qa6, 2qa8, 2qab, 2qgt, 2qgw, 2qr9, 2qse, 2qxm

Cited: 89 times
EuropePMC logo PMID: 18344977

Abstract

Our understanding of how steroid hormones regulate physiological functions has been significantly advanced by structural biology approaches. However, progress has been hampered by misfolding of the ligand binding domains in heterologous expression systems and by conformational flexibility that interferes with crystallization. Here, we show that protein folding problems that are common to steroid hormone receptors are circumvented by mutations that stabilize well-characterized conformations of the receptor. We use this approach to present the structure of an apo steroid receptor that reveals a ligand-accessible channel allowing soaking of preformed crystals. Furthermore, crystallization of different pharmacological classes of compounds allowed us to define the structural basis of NFkappaB-selective signaling through the estrogen receptor, thus revealing a unique conformation of the receptor that allows selective suppression of inflammatory gene expression. The ability to crystallize many receptor-ligand complexes with distinct pharmacophores allows one to define structural features of signaling specificity that would not be apparent in a single structure.

Reviews - 2qh6 mentioned but not cited (1)

  1. Versatility or promiscuity: the estrogen receptors, control of ligand selectivity and an update on subtype selective ligands. Ng HW, Perkins R, Tong W, Hong H. Int J Environ Res Public Health 11 8709-8742 (2014)

Articles - 2qh6 mentioned but not cited (6)

  1. NFkappaB selectivity of estrogen receptor ligands revealed by comparative crystallographic analyses. Nettles KW, Bruning JB, Gil G, Nowak J, Sharma SK, Hahm JB, Kulp K, Hochberg RB, Zhou H, Katzenellenbogen JA, Katzenellenbogen BS, Kim Y, Joachmiak A, Greene GL. Nat Chem Biol 4 241-247 (2008)
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  4. Identification and structure-activity relationships of a novel series of estrogen receptor ligands based on 7-thiabicyclo[2.2.1]hept-2-ene-7-oxide. Wang P, Min J, Nwachukwu JC, Cavett V, Carlson KE, Guo P, Zhu M, Zheng Y, Dong C, Katzenellenbogen JA, Nettles KW, Zhou HB. J Med Chem 55 2324-2341 (2012)
  5. Bicyclic core estrogens as full antagonists: synthesis, biological evaluation and structure-activity relationships of estrogen receptor ligands based on bridged oxabicyclic core arylsulfonamides. Zhu M, Zhang C, Nwachukwu JC, Srinivasan S, Cavett V, Zheng Y, Carlson KE, Dong C, Katzenellenbogen JA, Nettles KW, Zhou HB. Org Biomol Chem 10 8692-8700 (2012)
  6. Protein surface characterization using an invariant descriptor. Abu Deeb Z, Adjeroh DA, Jiang BH. Int J Biomed Imaging 2011 918978 (2011)


Reviews citing this publication (15)

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Articles citing this publication (67)

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