Design of a structure-activity relationship model of vitamin K epoxide reductase (VKORC1) inhibitors combining chemical synthesis of new compounds, enzymatic assays and molecular modelling

Publication date: 30 October 2023

Source: Bioorganic & Medicinal Chemistry, Volume 94

Author(s): Nolan Chatron, Manon Boulven, Adrien Montagut-Romans, Flavien Ponsot, Maïwenn Jacolot, Hervé Caruel, Etienne Benoît, Florence Popowycz, Virginie Lattard

Discovery of Novel Dual Bruton’s Tyrosine Kinase (BTK) and Janus Kinase 3 (JAK3) Inhibitors as A Promising Strategy for Rheumatoid Arthritis

Publication date: Available online 27 May 2023

Source: Bioorganic & Medicinal Chemistry

Author(s): Tingting Liang, Lifang Cen, Junjie Wang, Ming Cheng, Weibo Guo, Wenjie Wang, Chunqiu Yu, Haifeng Zhang, Yuan Wang, Zhongyan Hao, Jiaming Jin, Yaoyao Wu, Teng Jiang, Qihua Zhu, Yungen Xu

<em>In situ</em> Click Chemistry-based Discovery of 1,2,3-triazole-derived Diarylpyrimidines as Novel HIV-1 NNRTIs by Exploiting the Tolerant Region I in Binding Pocket

Publication date: Available online 23 September 2023

Source: Bioorganic & Medicinal Chemistry

Author(s): Yanying Sun, Da Feng, Zhenzhen Zhou, Tao Zhang, Erik De Clercq, Christophe Pannecouque, Dongwei Kang, Peng Zhan, Xinyong Liu

The mechanisms of multidrug resistance of breast cancer and research progress on related reversal agents

Publication date: Available online 30 September 2023

Source: Bioorganic & Medicinal Chemistry

Author(s): Shiwen Yu, Jinling Zheng, Yan Zhang, Dandan Meng, Yujue Wang, Xiaoyu Xu, Na Liang, Shayibai Shabiti, Xu Zhang, Zixi Wang, Zehua Yang, Pengbing Mi, Xing Zheng, Wenjun Li, Hongfei Chen

A novel genetically-encoded bicyclic peptide inhibitor of human urokinase-type plasminogen activator with better cross-reactivity toward the murine orthologue

Publication date: Available online 12 October 2023

Source: Bioorganic & Medicinal Chemistry

Author(s): Ylenia Mazzocato, Stefano Perin, Julia Morales-Sanfrutos, Zhanna Romanyuk, Stefano Pluda, Laura Acquasaliente, Giuseppe Borsato, Vincenzo De Filippis, Alessandro Scarso, Alessandro Angelini

Mass spectrometric assays monitoring the deubiquitinase activity of the SARS-CoV-2 papain-like protease inform on the basis of substrate selectivity and have utility for substrate identification

Publication date: Available online 12 October 2023

Source: Bioorganic & Medicinal Chemistry

Author(s): Lennart Brewitz, H.T. Henry Chan, Petra Lukacik, Claire Strain-Damerell, Martin A. Walsh, Fernanda Duarte, Christopher J. Schofield