HPPE(化合物236)是一款口服活性强效Bach1抑制剂,属于特定的非亲电性生理性抑制剂。Bach1是cap'n'collar型碱性区亮氨酸拉链因子家族(CNC-bZip)的转录因子,可调控线粒体代谢并降低葡萄糖利用率;而HPPE通过结合Bach1蛋白的血红素结合位点,解除Bach1介导的抑制作用,适用于银屑病、多发性硬化症及慢性阻塞性肺疾病(COPD)的相关研究。
[1] Ahuja M, Ammal Kaidery N, Attucks OC, McDade E, Hushpulian DM, Gaisin A, Gaisina I, Ahn YH, Nikulin S, Poloznikov A, Gazaryan I, Yamamoto M, Matsumoto M, Igarashi K, Sharma SM, Thomas B. Bach1 derepression is neuroprotective in a mouse model of Parkinson's disease. Proc Natl Acad Sci U S A. 2021 Nov 9;118(45):e2111643118. doi: 10.1073/pnas.2111643118. Erratum in: Proc Natl Acad Sci U S A. 2021 Dec 28;118(52):e2120610118. doi: 10.1073/pnas.2120610118. Erratum in: Proc Natl Acad Sci U S A. 2024 Jul 2;121(27):e2411303121. doi: 10.1073/pnas.2411303121. PMID: 34737234; PMCID: PMC8694049.[2]Freeman R, Bollong MJ. HPPE Activates NRF2 Signaling by Liberating Heavy Metal Stores. Chembiochem. 2025 Feb 16;26(4):e202400529. doi: 10.1002/cbic.202400529. Epub 2024 Oct 29. PMID: 39240245; PMCID: PMC11948088.





