Zobrazeno 1 - 10
of 625
pro vyhledávání: '"Christophe, Pannecouque"'
Autor:
Yanying Sun, Zhenzhen Zhou, Zhongling Shi, Fabao Zhao, Minghui Xie, Zongji Zhuo, Erik De Clercq, Christophe Pannecouque, Dongwei Kang, Peng Zhan, Xinyong Liu
Publikováno v:
Acta Pharmaceutica Sinica B, Vol 14, Iss 7, Pp 3110-3124 (2024)
HIV-1 reverse transcriptase (RT) has received great attention as an attractive therapeutic target for acquired immune deficiency syndrome (AIDS), but the inevitable drug resistance and side effects have always been major challenges faced by non-nucle
Externí odkaz:
https://doaj.org/article/11cdd506ac7a43449abb83e409f2a953
Autor:
Zhao Wang, Heng Zhang, Zhen Gao, Zihao Sang, Erik De Clercq, Christophe Pannecouque, Dongwei Kang, Peng Zhan, Xinyong Liu
Publikováno v:
Acta Pharmaceutica Sinica B, Vol 14, Iss 3, Pp 1257-1282 (2024)
With our continuous endeavors in seeking potent anti-HIV-1 agents, we reported here the discovery, biological characterization, and druggability evaluation of a class of nonnucleoside reverse transcriptase inhibitors. To fully explore the chemical sp
Externí odkaz:
https://doaj.org/article/0233cd7e618049619eb07110425d4280
Publikováno v:
Acta Pharmaceutica Sinica B, Vol 13, Iss 12, Pp 4906-4917 (2023)
Following on our recently developed biphenyl-ATDP non-nucleoside reverse transcriptase inhibitor ZLM-66 (SI = 2019.80, S = 1.9 μg/mL), a series of novel heterocycle-substituted ATDP derivatives with significantly improved selectivity and solubility
Externí odkaz:
https://doaj.org/article/9fc6b09d87c44d3a900c1f299690c817
Autor:
Zongji Zhuo, Zhao Wang, Lanlan Jing, Tao Zhang, Anchao Ge, Zhenzhen Zhou, Ying Liu, Xin Li, Erik De Clercq, Christophe Pannecouque, Peng Zhan, Xinyong Liu, Dongwei Kang
Publikováno v:
International Journal of Molecular Sciences, Vol 25, Iss 16, p 9028 (2024)
Inspired by our previous work on the modification of diarylpyrimidine-typed non-nucleoside reverse transcriptase inhibitors (NNRTIs) and the reported crystallographic studies, a series of novel amino acids (analogues)-substituted thiophene[3,2-d]pyri
Externí odkaz:
https://doaj.org/article/6edd3910ff24434aa0d574a7696157ad
Publikováno v:
Acta Pharmaceutica Sinica B, Vol 13, Iss 7, Pp 3054-3066 (2023)
Considering the undesirable metabolic stability of our recently identified NNRTI 5 (t1/2 = 96 min) in human liver microsomes, we directed our efforts to improve its metabolic stability by introducing a new favorable hydroxymethyl side chain to the C-
Externí odkaz:
https://doaj.org/article/96af626d10184fe086ba06f1df9bc9ca
Autor:
Xuan-De Zhu, Angela Corona, Stefania Maloccu, Enzo Tramontano, Shuai Wang, Christophe Pannecouque, Erik De Clercq, Ge Meng, Fen-Er Chen
Publikováno v:
Molecules, Vol 29, Iss 9, p 2120 (2024)
Ribonuclease H (RNase H) was identified as an important target for HIV therapy. Currently, no RNase H inhibitors have reached clinical status. Herein, a series of novel thiazolone[3,2-a]pyrimidine-containing RNase H inhibitors were developed, based o
Externí odkaz:
https://doaj.org/article/4d4f54ff0ff54589865da65fa7714578
Autor:
Shenghua Gao, Letian Song, Yusen Cheng, Fabao Zhao, Dongwei Kang, Shu Song, Mianling Yang, Bing Ye, Wei Zhao, Yajie Tang, Erik De Clercq, Christophe Pannecouque, Peng Zhan, Xinyong Liu
Publikováno v:
Acta Pharmaceutica Sinica B, Vol 13, Iss 6, Pp 2747-2764 (2023)
Indolylarylsulfones (IASs) are classical HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with a unique scaffold and possess potent antiviral activity. To address the high cytotoxicity and improve safety profiles of IASs, we introduced
Externí odkaz:
https://doaj.org/article/8964cae7904a4512954b69a8af82c05c
Autor:
Xiangyi Jiang, Boshi Huang, Shawn Rumrill, David Pople, Waleed A. Zalloum, Dongwei Kang, Fabao Zhao, Xiangkai Ji, Zhen Gao, Lide Hu, Zhao Wang, Minghui Xie, Erik De Clercq, Francesc X. Ruiz, Eddy Arnold, Christophe Pannecouque, Xinyong Liu, Peng Zhan
Publikováno v:
Communications Chemistry, Vol 6, Iss 1, Pp 1-11 (2023)
Abstract HIV-1 reverse transcriptase is one of the most attractive targets for the treatment of AIDS. However, the rapid emergence of drug-resistant strains and unsatisfactory drug-like properties seriously limit the clinical application of HIV-1 non
Externí odkaz:
https://doaj.org/article/c38865deec50478fa334e921f6a1050d
Autor:
Xin Jin, Shuai Wang, Limin Zhao, Wenjuan Huang, Yinxiang Zhang, Christophe Pannecouque, Erik De Clercq, Ge Meng, Huri Piao, Fener Chen
Publikováno v:
Acta Pharmaceutica Sinica B, Vol 13, Iss 3, Pp 1192-1203 (2023)
Our recent studies for nonnucleoside reverse transcriptase inhibitors identified a highly potent compound JK-4b against WT HIV-1 (EC50 = 1.0 nmol/L), but the poor metabolic stability in human liver microsomes (t1/2 = 14.6 min) and insufficient select
Externí odkaz:
https://doaj.org/article/b86c2954f1994c90a07519bdfa82acd0
Autor:
Ngoc-Thao-Hien Le, Steven De Jonghe, Kristien Erven, Tom Vermeyen, Aliou M. Baldé, Wouter A. Herrebout, Johan Neyts, Christophe Pannecouque, Luc Pieters, Emmy Tuenter
Publikováno v:
Molecules, Vol 28, Iss 7, p 3222 (2023)
The Amaryllidaceae species are well-known as a rich source of bioactive compounds in nature. Although Hymenocallis littoralis has been studied for decades, its polar components were rarely explored. The current phytochemical investigation of Amarylli
Externí odkaz:
https://doaj.org/article/e5f432bc9e8c4b2da26b8e6b24bc94ff