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首页> 外文会议>ASMS Conference on Mass Spectrometry and Allied Topics >Identifying Dynamical Profiles Associated with Toxicity of Rexinoid X Receptor Agonist by Hydrogen Deuterium Exchange Mass Spectrometry
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Identifying Dynamical Profiles Associated with Toxicity of Rexinoid X Receptor Agonist by Hydrogen Deuterium Exchange Mass Spectrometry

机译：用氢氘交换质谱法鉴定与戒指X受体激动剂的毒性相关的动态曲线

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RXR, a ligand dependent nuclear receptor is involved in many signaling pathways of transcription initiation that regulate cellular proliferation, differentiation, growth, and homeostasis. Due to RXR's unique involvement as a heterodimer partner it has become a target for therapeutics. We previously established that 9cUAB30 is a potent and selective agonist for the RXR's and have proven to be non-toxic. To probe the ligand binding pocket of RXR, methyl derivatives were synthesized and tested. Biological studies show that the four and seven methyl derivatives have increased potency and toxicity, due to activation of heterodimer pathways leading to severe hyperlipidemia. This work will establish the dynamics of key interactions between agonist and peptides/residues that may correlate with toxicity of some 9cUAB30 derivatives.
机译：RXR，一种配体依赖性核受体参与了调节细胞增殖，分化，生长和稳态的转录起始的许多信号传导途径。由于RXR独特的参与作为异二聚体合作伙伴，它已成为治疗剂的目标。我们以前认为9Cuab30是RXR的有效和选择性激动剂，并且已被证明是无毒的。为了探测RXR的配体结合袋，合成并测试甲基衍生物。生物学研究表明，由于导致严重的高脂血症的异二聚体途径的激活，四和7个甲基衍生物具有增加的效力和毒性。这项工作将建立激动剂和肽/残基之间的关键相互作用的动态，其可能与毒性相关的一些9Cuab30衍生物的毒性。

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