RESUMO
Blocking the biological functions of scaffold proteins and aggregated proteins is a challenging goal. PROTAC proteolysis-targeting chimaera (PROTAC) technology may be the solution, considering its ability to selectively degrade target proteins. Recent progress in the PROTAC strategy include identification of the structure of the first ternary eutectic complex, extra-terminal domain-4-PROTAC-Von-Hippel-Lindau (BRD4-PROTAC-VHL), and PROTAC ARV-110 has entered clinical trials for the treatment of prostate cancer in 2019. These discoveries strongly proved the value of the PROTAC strategy. In this perspective, we summarized recent meaningful research of PROTAC, including the types of degradation proteins, preliminary biological data in vitro and in vivo, and new E3 ubiquitin ligases. Importantly, the molecular design, optimization strategy and clinical application of candidate molecules are highlighted in detail. Future perspectives for development of advanced PROTAC in medical fields have also been discussed systematically.
RESUMO
@#Nine compounds were isolated from the aerial part of Callicarpa kwangtungensis chun by various column chromatographic methods. Their structures were identified as pinnatifidanoid A(1), blumenol C(2), megastigman-5- ene-3β, 9R-diol(3), 3β-hydroxyurs-12-en-28-oic acid(4), kaji-ichigoside F1(5), 1, 4-terephthalic acid(6), syringic acid(7), vanillic acid(8), and 3, 5-dimethoxy-4-methylbenzyl alcohol(9)on the basis of spectral analysis. C13 nor-isoprenoids of 1-3, and compounds 5, 6 and 9, were isolated from the genus Callicarpa for the first time.