RAR beta ligand-binding domain bound to an SRC-1 co-activator peptide: purification, crystallization and preliminary X-ray diffraction analysis

Kammerer S; Germain P; Flaig RPeluso-Iltis CMitschler ARochel NGronemeyer HMoras D

首页> 外文期刊>Acta crystallographica.Section D. Biological crystallography >RAR beta ligand-binding domain bound to an SRC-1 co-activator peptide: purification, crystallization and preliminary X-ray diffraction analysis

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RAR beta ligand-binding domain bound to an SRC-1 co-activator peptide: purification, crystallization and preliminary X-ray diffraction analysis

机译：RARβ配体结合域绑定到一个SRC-1co-activator肽:净化,结晶和初步的x射线衍射分析

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Retinoids have demonstrated therapeutic efficacy in the treatment of acute promyelocytic leukaemia and in the chemoprevention of a large number of cancers. As the cellular signalling pathway of retinoids can be transduced by the three retinoic acid receptor (RAR) isotypes alpha, beta and gamma, the side effects of these treatments induced efforts to generate isotype-selective ligands. Despite knowledge of the crystal structures of RARalpha and RARgamma ligand-binding domains (LBDs), the rational design of such ligands has been hampered by the absence of RARbeta LBD structural data. Here, a strategy used to express a large-scale soluble fraction of the human RARbeta LBD suitable for biophysical analysis is reported, as well as a procedure for crystallizing it bound to a synthetic retinoid (TTNPB) with or without a co-activator peptide (SRC-1). Preliminary X-ray analysis revealed that both complexes crystallized in the orthorhombic space group P2(1)2(1)2(1). The unit-cell parameters are a=47.81, b=58.52, c=92.83 Angstrom for the TTNPB-hRARbeta LBD crystal and a=58.14, b=84.07, c=102.37Angstrom when the SRC-1 peptide is also bound.

机译：类维生素a显示了治疗效果治疗急性早幼粒细胞白血病在大量的化学预防癌症。类维生素a可以传导三视黄酸受体(RAR)同形像α,β和γ,这些疗法的副作用诱导生成isotype-selective的努力配体。结构rarα和RARgamma配体结合域(精神的小黑裙),理性设计这样的配体一直受阻缺乏RARbeta小黑裙结构数据。策略用来表达一个大规模的可溶性一部分的人类RARbeta小黑裙适合生物物理分析报告,以及结晶的过程它绑定到一个合成维生素a (TTNPB)有或没有co-activator肽(SRC-1)。分析表明,两种复合物斜方晶系的空间组的结晶P2(1) 2(1) 2(1)。b = 58.52 = 47.81, c = 92.83埃TTNPB-hRARbeta小黑裙晶体和一个= 58.14,b = 84.07,c = 102.37埃SRC-1肽也绑定。

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《Acta crystallographica.Section D. Biological crystallography》 |2004年第11期|2048-2050|共3页
作者
Kammerer S; Germain P; Flaig RPeluso-Iltis CMitschler ARochel NGronemeyer HMoras D;
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IGBMC, Dept Struct Biol & Gen, F-67404 Illkirch Graffenstaden, France;

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正文语种英语
中图分类化学;
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Tretinoin; crystal structure; RetinoidsAgonistRetinoic Acid Receptor alphaBinding Sitesretinoic acid receptor betaBoundPeptidesX-ray diffraction analysisNuclear receptorsBreast Cancer;

机译：结构;RetinoidsAgonistRetinoic酸受体alphaBinding Sitesretinoic酸受体betaBoundPeptidesX-ray衍射analysisNuclear receptorsBreast癌症;

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RAR beta ligand-binding domain bound to an SRC-1 co-activator peptide: purification, crystallization and preliminary X-ray diffraction analysis

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