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Resource Category: Publications

A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove

Benny J Evison et al. Bioorg Med Chem. 2020 Mar 15;28(6):115344. doi: 10.1016/j.bmc.2020.115344. Epub 2020 Jan 31.

Investigation of stereoisomeric bisarylethenesulfonic acid esters for discovering potent and selective PTP1B inhibitors

Xie F, Yang F, Zhang Y, Xia Y, Liu W, Jiang F, Lam C, Qiao Y, Xie D, Li J, Fu L. Investigation of stereoisomeric bisarylethenesulfonic acid esters for discovering potent and selective PTP1B inhibitors. Eur J Med Chem. 2019

Discovery of trisubstituted nicotinonitrile derivatives as novel human GCN5 inhibitors through AlphaScreen-based high throughput screening

Tao H, et al. RSC Adv. 2019 Feb 8;9(9):4917-4924. doi: 10.1039/c8ra10074h.

Total Synthesis of Covalent Cysteine Protease Inhibitor N-Desmethyl Thalassospiramide C and Crystallographic Evidence for Its Mode of Action

Jeremy Fournier et al. Org Lett. 2019 Jan 18;21(2):508-512. doi: 10.1021/acs.orglett.8b03821. Epub 2019 Jan 10.

Design, synthesis and biological evaluation of novel 1-phenyl phenanthridin-6(5H)-one derivatives as anti-tumor agents targeting TOPK

Quan-Fang Hu et al. Eur J Med Chem. 2019 Jan 15;162:407-422. doi: 10.1016/j.ejmech.2018.11.007. Epub 2018 Nov 9.

Optimization of 5-arylidene barbiturates as potent, selective, reversible LSD1 inhibitors for the treatment of acute promyelocytic leukemia

Xu S, et al. Optimization of 5-arylidene barbiturates as potent, selective, reversible LSD1 inhibitors for the treatment of acute promyelocytic leukemia. Bioorg Med Chem. 2018 Sep 15;26(17):4871-4880. doi: 10.1016/j.bmc.2018.08.026. Epub 2018 Aug 22.

Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions

Tiansheng Wang et al. ACS Med Chem Lett. 2017 Nov 28;8(12):1224-1229. doi: 10.1021/acsmedchemlett.7b00239. eCollection 2017 Dec 14.

Identification of novel inhibitors of histone acetyltransferase hMOF through high throughput screening

Zhang R, et al. Eur J Med Chem. 2018 Sep 5;157:867-876. doi: 10.1016/j.ejmech.2018.08.026. Epub 2018 Aug 17.

The multimodal antidepressant vortioxetine may facilitate pyramidal cell firing by inhibition of 5-HT3 receptor expressing interneurons: An in vitro study in rat hippocampus slices

Dale E, Thomas D, Sager TN, Sanchez C. The multimodal antidepressant vortioxetine may facilitate pyramidal cell firing by inhibition of 5-HT3 receptor expressing interneurons: An in vitro study in rat hippocampus slices. Brain Res. 2018 Jun 15;1689:1-11. doi: 10.1016/j.brainres.2017.12.025. Epub

Discovery of 1,8-acridinedione derivatives as novel GCN5 inhibitors via high throughput screening

Han J, Chen Y, Xiong H, et al. Discovery of 1,8-acridinedione derivatives as novel GCN5 inhibitors via high throughput screening. Eur J Med Chem. 2018 May 10;151:740-751. doi: 10.1016/j.ejmech.2018.02.005. Epub 2018 Feb 14.
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