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团队简介/TEAM INTRODUCTION

本课题组于2016年建立,目前包括教授1名、副研究员1名、讲师1名、科研助理1名、博士后4名及在读研究生12名。课题组专注于研究重大疾病相关的靶标蛋白,重点研究“类核受体”转录因子——bHLH-PAS(basic helix-loop-helix-PER-ARNT-SIM)家族。该家族与很多人类疾病密切相关,而且普遍含有小分子配体结合口袋,因此是继核受体之后第二个可作为潜在药物靶标的转录因子家族。一方面综合利用多种实验方法,研究这些蛋白的结构和功能,并揭示蛋白和配体的相互作用,以及配体...

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科研团队/TEAM INTRODUCTION
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武大雷
武大雷

山东大学微生物改造技术全国重点实验室副主任,先后入选山东省“青年泰山学者”、“省杰青基金”和教育部高层次青年人才项目(“新药创制”岗位),学术兼职包括中国药理学会专委会委员和《药学学报》青年编委等。课题组主要针对转录因子靶标从事结构与分子药理学研究和靶向分子发现,也从事生物合成相关酶的结构解析和催化机理研究,成果发表于Nature、Nature Chemical Biology、Nature Communications、PNAS、JACS、JMC等期刊...

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2022-02-07 |

Transcription factors (TFs) specifically bind to DNA, recruit cofactor proteins and modulate target gene expression, rendering them essential roles in the regulation of numerous biological processes. Meanwhile, mutated or dysregulated TFs are involved in a variety of human diseases. As multiple signaling pathways ultimately converge at TFs, targeting these TFs directly may prove to be more specific and cause fewer side effects, than targeting the upfront conventional targets in these pathways. All these features together endue TFs with great potential and high selectivity as therapeutic dru...

Hypoxia-inducible factors (HIFs) are α/β heterodimeric transcription factors modulating cellular responses to the low oxygen condition. Among three HIF-α isoforms, HIF-3α is the least studied to date. Here we show that oleoylethanolamide (OEA), a physiological lipid known to regulate food intake and metabolism, binds selectively to HIF-3α. Through crystallographic analysis of HIF-3 α/β heterodimer in both apo and OEA-bound forms, hydrogen-deuterium exchange mass spectrometry (HDX-MS), molecular dynamics (MD) simulations, and biochemical and cell-based assays, we unveil the molecular ...

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