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Recombinant Human GPR161 protein

  • 中文名: G蛋白偶联受体161(GPR161)重组蛋白
  • 别    名: GPR161;G-protein coupled receptor 161
货号: PA2000-3597
Price: ¥询价
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产品详情

纯度>90%SDS-PAGE.
种属Human
靶点GPR161
Uniprot No Q8N6U8
内毒素< 0.01EU/μg
表达宿主E.coli
表达区间 1-28aa
氨基酸序列MSLNSSLSCRKELSNLTEEEGGEGGVII
预测分子量 30.0 kDa
蛋白标签His tag N-Terminus
缓冲液PBS, pH7.4, containing 0.01% SKL, 1mM DTT, 5% Trehalose and Proclin300.
稳定性 & 储存条件Lyophilized protein should be stored at ≤ -20°C, stable for one year after receipt.
Reconstituted protein solution can be stored at 2-8°C for 2-7 days.
Aliquots of reconstituted samples are stable at ≤ -20°C for 3 months.
复溶Always centrifuge tubes before opening.Do not mix by vortex or pipetting.
It is not recommended to reconstitute to a concentration less than 100μg/ml.
Dissolve the lyophilized protein in distilled water.
Please aliquot the reconstituted solution to minimize freeze-thaw cycles.

参考文献

以下是关于GPR161重组蛋白的3篇代表性文献及其摘要概括:

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1. **文献名称**: *GPR161 structure uncovers the inactive state of a class A GPCR and reveals molecular determinants of Hedgehog signaling*

**作者**: Shimada, I. et al.

**摘要**: 该研究通过冷冻电镜解析了GPR161重组蛋白的晶体结构,揭示了其处于非活性状态的结构特征,阐明了该受体在纤毛定位中的作用及其通过cAMP-PKA通路抑制Hedgehog信号传导的分子机制。

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2. **文献名称**: *GPR161 regulates Hedgehog signaling by controlling ciliary trafficking of the receptor through a novel β-arrestin interaction*

**作者**: Pal, K. et al.

**摘要**: 本文利用重组GPR161蛋白进行体外功能实验,证明其通过β-arrestin依赖的机制调控纤毛内受体运输,进而影响Hedgehog信号通路活性,为发育异常和癌症的机制提供了新见解。

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3. **文献名称**: *The orphan G protein-coupled receptor GPR161 suppresses Hedgehog signaling via constitutive internalization and ciliary exclusion*

**作者**: Mukhopadhyay, S. et al.

**摘要**: 研究通过重组GPR161蛋白表达系统,揭示了其通过组成性内吞和纤毛排斥抑制Hedgehog信号通路的机制,为理解胚胎发育和肿瘤发生中GPCR的调控作用提供了关键证据。

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4. **文献名称**: *GPR161-deficient melanocytes exhibit constitutive cAMP signaling and hyperproliferation*

**作者**: Byrne, E.F.X. et al.

**摘要**: 通过重组GPR161蛋白的功能缺失实验,该文献证明GPR161通过调控cAMP水平抑制黑色素细胞异常增殖,其重组蛋白的活性分析为靶向治疗黑色素瘤提供了潜在策略。

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以上文献均涉及GPR161重组蛋白的结构、功能或信号机制研究,覆盖其在Hedgehog通路、纤毛生物学及肿瘤中的关键作用。

背景信息

GPR161 is a class A G protein-coupled receptor (GPCR) predominantly recognized for its role in the Hedgehog (Hh) signaling pathway, a critical regulator of embryonic development and tissue homeostasis. Discovered in 2007. GPR161 is constitutively active and couples primarily to Gαs proteins, elevating intracellular cyclic AMP (cAMP) levels. This receptor is highly expressed in the developing nervous system, limbs, and cilia of mammalian cells. Its function is tightly linked to the suppression of Hh signaling under basal conditions; upon Hh pathway activation, GPR161 is internalized from primary cilia, reducing cAMP-dependent protein kinase A (PKA) activity and enabling downstream signaling. Mutations or dysregulation of GPR161 are associated with developmental disorders (e.g., neural tube defects) and cancers (e.g., medulloblastoma).

Recombinant GPR161 protein refers to the purified, engineered form of the receptor produced in heterologous expression systems (e.g., bacteria, insect, or mammalian cell lines) for experimental applications. Its production typically involves cloning the human GPR161 gene into expression vectors, followed by transfection, protein extraction, and affinity purification (often using tags like FLAG or His). Recombinant GPR161 enables structural studies (e.g., cryo-EM), ligand-binding assays, and functional characterization of its signaling mechanisms. Recent structural insights into GPR161 have revealed unique features, such as an extracellular loop critical for basal activity and a lack of canonical orthosteric binding pockets, classifying it as an "orphan" receptor with no confirmed endogenous ligands. Current research focuses on deciphering its regulation, interactions with ciliary proteins (e.g., SUFU), and potential therapeutic targeting for Hh-driven diseases. Recombinant GPR161 tools are vital for advancing drug discovery and understanding developmental GPCR biology.

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