Shergalis, Andrea Xue, Ding Gharbia, Fatma Z Driks, Hannah Shrestha, Binita Tanweer, Amina Cromer, Kirin Ljungman, Mats Neamati, Nouri
Published in
Journal of medicinal chemistry
Disulfide bond formation is a critical post-translational modification of newly synthesized polypeptides in the oxidizing environment of the endoplasmic reticulum and is mediated by protein disulfide isomerase (PDIA1). In this study, we report a series of α-aminobenzylphenol analogues as potent PDI inhibitors. The lead compound, AS15, is a covalent...
Choudhry, Namrta Zhao, Xin Xu, Dan Zanin, Mark Chen, Weisan Yang, Zifeng Chen, Jianxin
Published in
Journal of medicinal chemistry
The coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has led to more than 20 million people infected worldwide with an average mortality rate of 3.6%. This virus poses major challenges to public health, as it not only is highly contagious but also can be transmitted by asymptomatic infected ...
Dang, Xiawei Zhang, Lihong Franco, Antonietta Li, Jiajia Rocha, Agostinho G Devanathan, Sriram Dolle, Roland E Bernstein, Peter R Dorn, Gerald W 2nd
Published in
Journal of medicinal chemistry
Shuto, Satoshi Suzuki, Takayoshi
Published in
Journal of medicinal chemistry
Walloch, Philipp Henke, Björn Häuer, Susan Bergmann, Bärbel Spielmann, Tobias Beitz, Eric
Published in
Journal of medicinal chemistry
The spreading of malaria parasites, Plasmodium falciparum, with resistance to all known drugs calls for novel classes of inhibitors with new modes of action. Recently, we discovered and validated the plasmodial l-lactate transporter, PfFNT, as a novel antimalarial drug target. However, treatment of parasites with a screening hit from the malaria bo...
Hu, Shuai Sechi, Mario Singh, Pankaj Kumar Dai, Lipeng McCann, Sean Sun, Duxin Ljungman, Mats Neamati, Nouri
Published in
Journal of medicinal chemistry
Redox modulators have been developed as an attractive approach to treat cancer. Herein, we report the synthesis, identification, and biological evaluation of a quinazolinedione reactive oxygen species (ROS) inducer, QD394, with significant cytotoxicity in pancreatic cancer cells. QD394 shows a transcriptomic profile remarkably similar to napabucasi...
Poulie, Christian B M Liu, Na Jensen, Anders A Bunch, Lennart
Published in
Journal of medicinal chemistry
We report the synthesis of the first series of heterobivalent ligands targeting the putative heteromeric 5-HT2A/mGlu2 receptor complex, based on the 5-HT2A antagonist MDL-100,907 and the mGlu2 ago-PAM JNJ-42491293. The functional properties of monovalent and heterobivalent ligands were characterized in 5-HT2A-, mGlu2/Gqo5-, 5-HT2A/mGlu2-, and 5-HT2...
Sang, Peng Shi, Yan Lu, Junhao Chen, Lihong Yang, Leixiang Borcherds, Wade Abdulkadir, Sami Li, Qi Daughdrill, Gary Chen, Jiandong
...
Published in
Journal of medicinal chemistry
Lear, Sam Pflimlin, Elsa Zhou, Zhihong Huang, David Weng, Sharon Nguyen-Tran, Van Joseph, Sean B Roller, Shane Peterson, Scott Li, Jing
...
Published in
Journal of medicinal chemistry
Bariatric surgery results in increased intestinal secretion of hormones GLP-1 and anorexigenic PYY, which is believed to contribute to the clinical efficacy associated with the procedure. This observation raises the question whether combination treatment with gut hormone analogs might recapitulate the efficacy and mitigate the significant risks ass...
Yan, Wei Lakkaniga, Naga Rajiv Carlomagno, Francesca Santoro, Massimo McDonald, Neil Q Lv, Fengping Gunaganti, Naresh Frett, Brendan Li, Hong-Yu
Published in
Journal of medicinal chemistry
