日期:
2020 年 — 2026 年
2020
2021
2022
2023
2024
2025
2026
影响因子:

Discovery of Two Highly Selective Structurally Orthogonal Chemical Probes for Activin Receptor-like Kinases 1 and 2

发现两种针对激活素受体样激酶 1 和 2 的高选择性结构正交化学探针

Václav Němec, Marek Remeš, Petr Beňovský, Michael C Böck, Eliška Šranková, Jong Fu Wong, Julien Cros, Eleanor Williams, Lap Hang Tse, David Smil, Deeba Ensan, Methvin B Isaac, Rima Al-Awar, Regina Gomolková, Vlad-Constantin Ursachi, Bohumil Fafílek, Zuzana Kahounová, Ráchel Víchová, Ondřej Vacek, Be

A non-traditional crystal-based compound screening method targeting the ATP binding site of Plasmodium falciparum GRP78 for identification of novel nucleoside analogues

一种针对恶性疟原虫 GRP78 的 ATP 结合位点的非传统基于晶体的化合物筛选方法,用于鉴定新型核苷类似物

Alexander Mrozek, Tetyana Antoshchenko, Yun Chen, Carlos Zepeda-Velázquez, David Smil, Nirbhay Kumar, Hua Lu, Hee-Won Park

Probing the SAM Binding Site of SARS-CoV-2 Nsp14 In Vitro Using SAM Competitive Inhibitors Guides Developing Selective Bisubstrate Inhibitors

使用 SAM 竞争性抑制剂体外探测 SARS-CoV-2 Nsp14 的 SAM 结合位点,指导开发选择性双底物抑制剂

Kanchan Devkota, Matthieu Schapira, Sumera Perveen, Aliakbar Khalili Yazdi, Fengling Li, Irene Chau, Pegah Ghiabi, Taraneh Hajian, Peter Loppnau, Albina Bolotokova, Karla J F Satchell, Ke Wang, Deyao Li, Jing Liu, David Smil, Minkui Luo, Jian Jin, Paul V Fish, Peter J Brown, Masoud Vedadi

Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma

利用开放科学药物发现模型开发中枢神经系统渗透性 ALK2 抑制剂,用于治疗弥漫性内在性脑桥胶质瘤

David Smil, Jong Fu Wong, Eleanor P Williams, Roslin J Adamson, Alison Howarth, David A McLeod, Ahmed Mamai, Soyoung Kim, Brian J Wilson, Taira Kiyota, Ahmed Aman, Julie Owen, Gennady Poda, Kurumi Y Horiuchi, Ekaterina Kuznetsova, Haiching Ma, J Nicole Hamblin, Sue Cramp, Owen G Roberts, Aled M Edwa

A chemical biology toolbox to study protein methyltransferases and epigenetic signaling

研究蛋白质甲基转移酶和表观遗传信号传导的化学生物学工具箱

Sebastian Scheer, Suzanne Ackloo, Tiago S Medina, Matthieu Schapira, Fengling Li, Jennifer A Ward, Andrew M Lewis, Jeffrey P Northrop, Paul L Richardson, H Ümit Kaniskan, Yudao Shen, Jing Liu, David Smil, David McLeod, Carlos A Zepeda-Velazquez, Minkui Luo, Jian Jin, Dalia Barsyte-Lovejoy, Kilian V

Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6

发现一种强效、选择性且具有细胞活性的蛋白质精氨酸甲基转移酶 4 和蛋白质精氨酸甲基转移酶 6 双重抑制剂

Yudao Shen #, Magdalena M Szewczyk #, Mohammad S Eram #, David Smil, H Ümit Kaniskan, Renato Ferreira de Freitas, Guillermo Senisterra, Fengling Li, Matthieu Schapira, Peter J Brown, Cheryl H Arrowsmith, Dalia Barsyte-Lovejoy, Jing Liu, Masoud Vedadi, Jian Jin

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia

C/EBPα N 端白血病中 Wdr5-MLL 相互作用的药理学靶向

Florian Grebien #, Masoud Vedadi #, Matthäus Getlik #, Roberto Giambruno, Amit Grover, Roberto Avellino, Anna Skucha, Sarah Vittori, Ekaterina Kuznetsova, David Smil, Dalia Barsyte-Lovejoy, Fengling Li, Gennadiy Poda, Matthieu Schapira, Hong Wu, Aiping Dong, Guillermo Senisterra, Alexey Stukalov, Ki

A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3)

一种强效、选择性且具有细胞活性的蛋白质精氨酸甲基转移酶 3 (PRMT3) 变构抑制剂

H Ümit Kaniskan, Magdalena M Szewczyk, Zhengtian Yu, Mohammad S Eram, Xiaobao Yang, Keith Schmidt, Xiao Luo, Miao Dai, Feng He, Irene Zang, Ying Lin, Steven Kennedy, Fengling Li, Elena Dobrovetsky, Aiping Dong, David Smil, Sun-Joon Min, Melissa Landon, Jennifer Lin-Jones, Xi-Ping Huang, Bryan L Roth

Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors

利用 PRMT3 的变构结合位点可产生强效且选择性的抑制剂

Feng Liu, Fengling Li, Anqi Ma, Elena Dobrovetsky, Aiping Dong, Cen Gao, Ilia Korboukh, Jing Liu, David Smil, Peter J Brown, Stephen V Frye, Cheryl H Arrowsmith, Matthieu Schapira, Masoud Vedadi, Jian Jin

Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5

小分子通过破坏与 WDR5 的相互作用来抑制 MLL 活性

Guillermo Senisterra, Hong Wu, Abdellah Allali-Hassani, Gregory A Wasney, Dalia Barsyte-Lovejoy, Ludmila Dombrovski, Aiping Dong, Kong T Nguyen, David Smil, Yuri Bolshan, Taraneh Hajian, Hao He, Alma Seitova, Irene Chau, Fengling Li, Gennadiy Poda, Jean-François Couture, Peter J Brown, Rima Al-Awar,