Huang Li, Jung Katherine, Chen Chin Ho
Department of Surgery, Duke University Medical Center, Durham, NC 27710, USA.
Biomolecules. 2014 Oct 14;4(4):931-9. doi: 10.3390/biom4040931.
The 26S proteasome is a cellular proteolytic complex containing 19S regulatory particles and the 20S core proteasome. It was reported that the small molecule b-AP15 targets the proteasome by inhibiting deubiquitination of the 19S regulatory particles of the proteasome complex. An investigation of b-AP15 on the 20S proteasome core suggested that this compound can also inhibit the 20S proteasome with a potency equivalent to that found to inhibit the 19S regulatory particles.
26S蛋白酶体是一种细胞内的蛋白水解复合物，包含19S调节颗粒和20S核心蛋白酶体。据报道，小分子b-AP15通过抑制蛋白酶体复合物19S调节颗粒的去泛素化作用来靶向蛋白酶体。对b-AP15作用于20S蛋白酶体核心的研究表明，该化合物还能抑制20S蛋白酶体，其效力与抑制19S调节颗粒时相当。
