Targeting NEDD8-activating enzyme for cancer therapy: developments, clinical trials, challenges and future research directions

Autor: Dong-Jun Fu, Ting Wang

Publikováno v: Journal of Hematology & Oncology, Vol 16, Iss 1, Pp 1-25 (2023)

Abstract NEDDylation, a post-translational modification through three-step enzymatic cascades, plays crucial roles in the regulation of diverse biological processes. NEDD8-activating enzyme (NAE) as the only activation enzyme in the NEDDylation modif

Externí odkaz: https://doaj.org/article/a8a37cb35e4444f19344ede43e995b2c

Novel piperidine derivatives as colchicine binding site inhibitors induce apoptosis and inhibit epithelial-mesenchymal transition against prostate cancer PC3 cells

Autor: Dong-Jun Fu, Si-Meng Liu, Jia-Jia Yang, Jun Li

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 1403-1413 (2020)

Tubulin polymerisation inhibitors that target colchicine binding site were powerful anticancer agents. Although along the years many colchicine binding site inhibitors (CBSIs) have been reported, few piperidine derivatives were identified as CBSIs. I

Externí odkaz: https://doaj.org/article/34d3593dc05442e68d162cd24ed493cd

Design and Antiproliferative Evaluation of Novel Sulfanilamide Derivatives as Potential Tubulin Polymerization Inhibitors

Autor: Dong-Jun Fu, Ji-Feng Liu, Ruo-Han Zhao, Jia-Huan Li, Sai-Yang Zhang, Yan-Bing Zhang

Publikováno v: Molecules, Vol 22, Iss 9, p 1470 (2017)

A series of sulfanilamide-1,2,3-triazole hybrids were designed by a molecular hybridization strategy and evaluated for antiproliferative activity against three selected cancer cell lines (MGC-803, MCF-7 and PC-3). The detailed structure-activity rela

Externí odkaz: https://doaj.org/article/6522f56becfd477da1f4c166d1d93690

Synthesis of S-2-phenylchromane Derivatives and Evaluation of the Antiproliferative Properties as Apoptosis Inducers in Cancer Cell Lines

Autor: Jun Li, Dong-Jun Fu, Yunfeng Zhang, Jiale Ma, Yujie Pei, Zeyuan Xie

Publikováno v: Anti-Cancer Agents in Medicinal Chemistry. 23

Background: Cancer remains one of the major health issues globally, where chemotherapy forms the main treatment mode for different types of cancers. Due to cancer cell ability to develop resistance, decreased clinical effectiveness of anticancer drug

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1d8132797c8d075f2d698b709352a0ba
https://doi.org/10.2174/1871520623666230420100254

Antiproliferative benzothiazoles incorporating a trimethoxyphenyl scaffold as novel colchicine site tubulin polymerisation inhibitors

Autor: Jia-Jia Yang, Fu-Hao Li, Dong-Jun Fu, Jun Li, Si-Meng Liu

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 1050-1059 (2020)
Journal of Enzyme Inhibition and Medicinal Chemistry

Tubulin polymerisation inhibitors exhibited an important role in the treatment of patients with prostate cancer. Herein, we reported the medicinal chemistry efforts leading to a new series of benzothiazoles by a bioisosterism approach. Biological tes

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58ba2778e824f894decf0e9c91c4b1b2
https://doi.org/10.1080/14756366.2020.1753721