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Discovery of Novel Non-nucleoside DOT1LR231Q Inhibitors with Improved Pharmacokinetic Properties and Anti-lung Cancer Efficacy J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Zehui Tan, Ning Guo, Shuyu Liu, Jiandong Li, Yu Chen, Jianming Cui, Hongrui Lei, Nan Jiang, Lihui Wang, Xin Zhai
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Structure–Activity Relationship of Inositol Thiophosphate Analogs as Allosteric Activators of Clostridioides difficile Toxin B J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Rebecca Cummer, Félix Grosjean, Raphaël Bolteau, Seyed Ehsan Vasegh, Simon Veyron, Liam Keogh, Jean-François Trempe, Bastien Castagner
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Influence of Trp-Cage on the Function and Stability of GLP-1R Agonist Exenatide Derivatives J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Dániel Horváth, Pál Stráner, Nóra Taricska, Zsolt Fazekas, Dóra K. Menyhárd, András Perczel
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Identifying Artifacts from Large Library Docking J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Yujin Wu, Fangyu Liu, Isabella Glenn, Karla Fonseca-Valencia, Lu Paris, Yuyue Xiong, Steven V. Jerome, Charles L. Brooks, III, Brian K. Shoichet
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Can Machine Learning Overcome the 95% Failure Rate and Reality that Only 30% of Approved Cancer Drugs Meaningfully Extend Patient Survival? J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Duxin Sun, Christian Macedonia, Zhigang Chen, Sriram Chandrasekaran, Kayvan Najarian, Simon Zhou, Tim Cernak, Vicki L. Ellingrod, H. V. Jagadish, Bernard Marini, Manjunath Pai, Angela Violi, Jason C. Rech, Shaomeng Wang, Yan Li, Brian Athey, Gilbert S. Omenn
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A Lysosome-Targeting hNEU1 Inhibitor Treats Myocardial Infarction: A Potential Therapeutic Breakthrough J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Wen Zhou, Wanxiang Yang, Ping Jiang, Shaohua Gou
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Structure, Function, and Activity of Small Molecule and Peptide Inhibitors of Protein Arginine Methyltransferase 1 J. Med. Chem. (IF 6.8) Pub Date : 2024-09-09 Thordur Hendrickson-Rebizant, Sadhana R. N. Sudhakar, Michael J. Rowley, Adam Frankel, James R. Davie, Ted M. Lakowski
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The “Doorstop Pocket” In Thioredoxin Reductases─An Unexpected Druggable Regulator of the Catalytic Machinery J. Med. Chem. (IF 6.8) Pub Date : 2024-09-09 Matteo Ardini, Sammy Y. Aboagye, Valentina Z. Petukhova, Irida Kastrati, Rodolfo Ippoliti, Gregory R. J. Thatcher, Pavel A. Petukhov, David L. Williams, Francesco Angelucci
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Photoinduction of Ferroptosis and cGAS-STING Activation by a H2S-Responsive Iridium(III) Complex for Cancer-Specific Therapy J. Med. Chem. (IF 6.8) Pub Date : 2024-09-09 Yi Li, Ben Liu, Yue Zheng, Meng Hu, Liu-Yi Liu, Cai-Rong Li, Wei Zhang, Yu-Xiao Lai, Zong-Wan Mao
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Discovery of Thiophene Derivatives as Potent, Orally Bioavailable, and Blood–Brain Barrier-Permeable Ebola Virus Entry Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-09-09 Marcos Morales-Tenorio, Fátima Lasala, Alfonso Garcia-Rubia, Elnaz Aledavood, Michelle Heung, Catherine Olal, Beatriz Escudero-Pérez, Covadonga Alonso, Ana Martínez, César Muñoz-Fontela, Rafael Delgado, Carmen Gil
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Merging Natural Product Structures with Pharmaceutical Leads: Unnatural Enantiomers of Estranes as Glucocorticoid Receptor Modulators That Suppress TNF-α and IL-6 Release J. Med. Chem. (IF 6.8) Pub Date : 2024-09-06 Joshua M. Nicholson, Dexi Yang, Thomas Koelblen, Eric L. Hu, Christopher C. Coss, Thomas P. Burris, Xiao Hu, Glenn C. Micalizio
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A Photoactivatable Version of Ivabradine Enables Light-Induced Block of HCN Current In Vivo J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Alessandro Porro, Edoardo Armano, Federico Brandalise, Rebecca Appiani, Monica Beltrame, Andrea Saponaro, Clelia Dallanoce, Koichi Nakajo, Kaei Ryu, Roberta Leone, Gerhard Thiel, Marco Pallavicini, Anna Moroni, Cristiano Bolchi
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Developing a Palladium(II) Agent to Overcome Multidrug Resistance and Metastasis of Liver Tumor by Targeted Multiacting on Tumor Cell, Inactivating Cancer-Associated Fibroblast and Activating Immune Response J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Ming Jiang, Wenjuan Li, Jinzhe Liang, Min Pang, Shanhe Li, Gang Xu, Minghui Zhu, Hong Liang, Zhenlei Zhang, Feng Yang
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Development of Tailless Homologue Receptor (TLX) Agonist Chemical Tools J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Emily C. Hank, Minh Sai, Till Kasch, Isabelle Meijer, Julian A. Marschner, Daniel Merk
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Structure Tailoring of Hemicyanine Dyes for In Vivo Shortwave Infrared Imaging J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Jiaming Guo, Yiling Zhu, Yuqian Qu, Longfei Zhang, Mingxi Fang, Zihan Xu, Tianbao Wang, Yufei Qin, Yihan Xu, Yuying Li, Yimin Chen, Hualong Fu, Xiayu Liu, Yajun Liu, Cheng Liu, Yuan Gao, Mengchao Cui, Kaixiang Zhou
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Antimicrobial Resistance: An Ultimate Challenge for 21st Century Scientists, Healthcare Professionals, and Policymakers to Save Future Generations J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Vazahyil Hari Krishnaprasad, Sanjay Kumar
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Natural Product-Inspired Discovery of Naphthoquinone-Furo-Piperidine Derivatives as Novel STAT3 Inhibitors for the Treatment of Triple-Negative Breast Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-09-03 Chengcheng Fan, Shengying Lou, Chenjun Shen, Jialing Liao, Hao Ni, Siyu Chen, Zhihui Zhu, Xueping Hu, Wei Xie, Huajun Zhao, Sunliang Cui
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Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents against Drug-Resistant Pathogens J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Haijia Lu, Xiaowan Han, Di Qin, Li Sheng, Chen Du, Bin Wang, Hongyi Zhao, Yu Lu, Yishuang Liu, Hai-Yu Hu, Ya Liu, Dongfeng Zhang
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Discovery and Evaluation of TLR-Targeted Immune Agonists J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Natalia Chernyak, Bhagyashree Bhagwat, Saraswathi Naravula, Ying Chen, Nicolas Solban, Fan Zhang, Esther Kofman, Fahimeh Raoufi, Xibei Dang, Jianming Bao, Daniela Tomazela, Marc Baily, Bernhard Geierstanger, John A. Flygare, Jin-Hwan Han, Aarron Willingham, W. Michael Seganish
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Transferrin-Modified Carprofen Platinum(IV) Nanoparticles as Antimetastasis Agents with Tumor Targeting, Inflammation Inhibition, Epithelial–Mesenchymal Transition Suppression, and Immune Activation Properties J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Ming Zhang, Yan Chen, Shuaiqi Feng, Yanqin He, Zhifang Liu, Ning Zhang, Qingpeng Wang
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Structure Activity of β-Amidomethyl Vinyl Sulfones as Covalent Inhibitors of Chikungunya nsP2 Cysteine Protease with Antialphavirus Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Anirban Ghoshal, Kesatebrhan Haile Asressu, Mohammad Anwar Hossain, Peter J. Brown, Meganathan Nandakumar, Anand Vala, Eric M. Merten, John D. Sears, Isabella Law, Jane E. Burdick, Noah L. Morales, Sumera Perveen, Kenneth H. Pearce, Konstantin I. Popov, Nathaniel J. Moorman, Mark T. Heise, Timothy M. Willson
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Photostable Iridium(III) Cyclometallated Complex is an Efficient Photosensitizer for Killing Multiple Cancer Cell Lines and 3D Models under Low Doses of Visible Light J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Callum Jones, Marta Martinez-Alonso, Hannah Gagg, Liam Kirby, Julia A. Weinstein, Helen E. Bryant
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The New Frontier: Merging Molecular Glue Degrader and Antibody–Drug Conjugate Modalities To Overcome Strategic Challenges J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Yam B. Poudel, Ruchita R. Thakore, Eugene P. Chekler
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Discovery of a Highly Potent and Selective Inhibitor Targeting Protein Lysine Methyltransferase NSD2 J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Jianwei Wei, Qiongyu Shi, Bang Li, Hong Yang, Li Liu, Ruilin Zhou, Zongbo Feng, Zhenjiao Yang, Jinhong Zhan, Xiao-Feng Xiong, Xun Huang, Yuanxiang Wang
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A Glycyrrhizin Derivative with a More Potent Inhibitory Activity against High-Mobility Group Box 1 Efficiently Discovered by Chemical Synthesis Inspired by the Bioconversion Products of an Endophytic Fungus Isolated from Licorice J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Aoi Machida, Kengo Banshoya, Akiho Miyamaru, Tamaki Eto, Shoji Maehara, Yuhzo Hieda, Toshiyuki Hata, Masatoshi Ohnishi
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Re-Evaluating PIN1 as a Therapeutic Target in Oncology Using Neutral Inhibitors and PROTACs J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Chuan Liu, Zhonghui Chen, Tao Chen, Hongmei Song, Jianbo Shen, Xiaoxi Yuan, Shuai Xia, Qian Liu, Qiuxia Chen, Qiang Tian, Xiaoyun Meng, Zhu Han, Xiaofei Dong, Yu Yang, Longying Cai, Xuemin Cheng, Yangyang Jia, Guansai Liu, Jin Li, Junyou Ge, Dengfeng Dou
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Heat Shock Protein 90 Interactome-Mediated Proteolysis Targeting Chimera (HIM-PROTAC) Degrading Glutathione Peroxidase 4 to Trigger Ferroptosis J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Jinyun Dong, Furong Ma, Maohua Cai, Fei Cao, Haobin Li, Hui Liang, Yulong Li, Guangyu Ding, Juan Li, Xiangdong Cheng, Jiang-Jiang Qin
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Rational Design, Synthesis, and Structure–Activity Relationship of a Novel Isoquinolinone-Based Series of HBV Capsid Assembly Modulators Leading to the Identification of Clinical Candidate AB-836 J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Andrew G. Cole, Steven G. Kultgen, Nagraj Mani, Kristi Yi Fan, Andrzej Ardzinski, Kim Stever, Bruce D. Dorsey, Eugen F. Mesaros, Emily P. Thi, Ingrid Graves, Sunny Tang, Troy O. Harasym, Amy C. H. Lee, Andrea Olland, Robert K. Suto, Michael J. Sofia
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Discovery and Optimization of N-Heteroaryl Indazole LRRK2 Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Kaitlyn M. Logan, Will Kaplan, Vladimir Simov, Hua Zhou, Derun Li, Luis Torres, Gregori J. Morriello, John J. Acton, Barbara Pio, Yi-Heng Chen, Mitchell H. Keylor, Rebecca Johnson, Solomon D. Kattar, Ryan Chau, Xin Yan, Michael Ardolino, Cayetana Zarate, Karin M. Otte, Rachel L. Palte, Tina Xiong, Spencer E. McMinn, Shishi Lin, Santhosh F. Neelamkavil, Ping Liu, Jing Su, Laxminarayan G. Hegde, Janice
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A Cyclometalated Iridium(III) Complex Exerts High Anticancer Efficacy via Fatty Acid Beta-Oxidation Inhibition and Sphingolipid Metabolism Reprogramming J. Med. Chem. (IF 6.8) Pub Date : 2024-09-03 Cuiyan Lin, Huiling Wang, Keyu Chen, Shuangqiang Liu, Zhichen Mao, Zuyu Mo, Rizhen Huang, Ye Zhang, Wei Xie, Jianhua Wei, Junfei Jin
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Pyrazolone-Based Zn(II) Complexes Display Antitumor Effects in Mutant p53-Carrying Cancer Cells J. Med. Chem. (IF 6.8) Pub Date : 2024-09-02 Sonila Xhafa, Corrado Di Nicola, Alessia Tombesi, Riccardo Pettinari, Claudio Pettinari, Francesca Scarpelli, Alessandra Crispini, Massimo La Deda, Angela Candreva, Alessia Garufi, Gabriella D’Orazi, Agustín Galindo, Fabio Marchetti
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Structural Optimization and Structure–Activity Relationship of 1H-Pyrazole-4-carboxylic Acid Derivatives as DNA 6mA Demethylase ALKBH1 Inhibitors and Their Antigastric Cancer Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-09-03 Feng Li, Liang Xiong, Jian Zhang, Yinping Guo, Ke Xu, Zijie Xiong, Yuyang Wang, Shanmian Ji, Aiping Tong, Linli Li, Shengyong Yang
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Structure-Based Design and Development of Phosphine Oxides as a Novel Chemotype for Antibiotics that Dysregulate Bacterial ClpP Proteases J. Med. Chem. (IF 6.8) Pub Date : 2024-09-02 Funing Lin, Mark F. Mabanglo, Jin Lin Zhou, Gursonika Binepal, Marim M. Barghash, Keith S. Wong, Scott D. Gray-Owen, Robert A. Batey, Walid A. Houry
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Discovery and Preclinical Profile of ALG-055009, a Potent and Selective Thyroid Hormone Receptor Beta (THR-β) Agonist for the Treatment of MASH J. Med. Chem. (IF 6.8) Pub Date : 2024-09-02 Koen Vandyck, David C. McGowan, Xuan G. Luong, Sarah K. Stevens, Andreas Jekle, Kusum Gupta, Dinah L. Misner, Sushmita Chanda, Vladimir Serebryany, Michael Welch, Haiyang Hu, Zhidan Lv, Caroline Williams, Klaus Maskos, Alfred Lammens, Antitsa D. Stoycheva, Tse-I Lin, Lawrence M. Blatt, Leonid N. Beigelman, Julian A. Symons, Pierre Raboisson, Jerome Deval
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Correction to “Optimization Efforts for Identification of Novel Highly Potent Keap1-Nrf2 Protein–Protein Interaction Inhibitors” J. Med. Chem. (IF 6.8) Pub Date : 2024-09-02 Kazuki Otake, Yoshinori Hara, Minoru Ubukata, Masafumi Inoue, Noboru Nagahashi, Dai Motoda, Naoki Ogawa, Yoshiji Hantani, Rie Hantani, Tsuyoshi Adachi, Akihiro Nomura, Keishi Yamaguchi, Mariko Maekawa, Hideaki Mamada, Takahisa Motomura, Motohide Sato, Kazuhito Harada
The correct email addresses for the two corresponding authors are as shown in this Addition/Correction. This article has not yet been cited by other publications.
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Corannulene Amino Acid-Derived Water-Soluble Amphiphilic Buckybowls as Broad-Spectrum Membrane Targeting Antibacterial Agents J. Med. Chem. (IF 6.8) Pub Date : 2024-08-30 Saroj Maji, Sariyah Akhtar, Sabyasachi Halder, Indranil Chatterjee, Devesh Pratap Verma, Neeraj Kumar Verma, Jyotshana Saroj, Deepanshi Saxena, Rahul Maitra, Juhi Sharma, Bhawana Sharma, Hidehiro Sakurai, Kalyan Mitra, Sidharth Chopra, Jimut Kanti Ghosh, Gautam Panda
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Structure–Activity Relationship Studies of Substituted 2-Phenyl-1,2,4-triazine-3,5(2H,4H)-dione Analogues: Development of Potent eEF2K Degraders against Triple-Negative Breast Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-08-29 Xiaobao Zhao, Changxin Zhong, Rongfeng Zhu, Rong Gong, Bingyan Liu, Linhao He, Sheng Tian, Jing Jin, Ting Jiang, Jing-Lei Chen, Xiaoya Wan, Wenjing Liu, Shilong Jiang, Pan Deng, Yan Cheng, Na Ye
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Harnessing Nitric Oxide-Donating Benzofuroxans for Targeted Inhibition of Carbonic Anhydrase IX in Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-08-29 Silvia Bua, Alessio Nocentini, Alessandro Bonardi, Giuseppe Palma, Giulia Ciampi, Angela Giliberti, Federica Iannelli, Francesca Bruzzese, Claudiu T. Supuran, Filomena de Nigris
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Design, Synthesis, and Biological Evaluation of Potent EZH2/LSD1 Dual Inhibitors for Prostate Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-08-28 Meiling Le, Wenhua Lu, Xiaozhuo Tan, Bingling Luo, Tiantian Yu, Yameng Sun, Zhirong Guo, Peng Huang, Daqian Zhu, Qiang Wu, A. Ganesan, Shijun Wen
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Selective Degradation of MLK3 by a Novel CEP1347-VHL-02 PROTAC Compound Limits the Oncogenic Potential of TNBC J. Med. Chem. (IF 6.8) Pub Date : 2024-08-29 Kamila Karpińska, Dawid Mehlich, Venkata R. Sabbasani, Michał Łomiak, Pedro Torres-Ayuso, Katarzyna Wróbel, Vi Nguyen-Phuong Truong, Remigiusz Serwa, Rolf E. Swenson, John Brognard, Anna A. Marusiak
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Impact of Conjugation of the Reactive Oxygen Species (ROS)-Generating Catalytic Moiety with Membrane-Active Antimicrobial Peptoids: Promoting Multitarget Mechanism and Enhancing Selectivity J. Med. Chem. (IF 6.8) Pub Date : 2024-08-29 Dasom Song, Byeongkwon Kim, Minsang Kim, Jin Kyeong Lee, Jieun Choi, Hyeju Lee, Sujin Shin, Dongmin Shin, Ho Yeon Nam, Yunho Lee, Seongsoo Lee, Yangmee Kim, Jiwon Seo
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Discovery of 6,7-Dihydropyrazolo[1,5-a]pyrazin-4(5H)-one Derivatives as mGluR2 Negative Allosteric Modulators with In Vivo Activity in a Rodent’s Model of Cognition J. Med. Chem. (IF 6.8) Pub Date : 2024-08-29 Sergio A. Alonso de Diego, María Lourdes Linares, Aránzazu García Molina, Ana Isabel de Lucas, Alcira del Cerro, Jose Manuel Alonso, Luc Ver Donck, Jose María Cid, Andrés A. Trabanco, Michiel Van Gool
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Journal of Medicinal Chemistry Collection: Drug Discovery in China J. Med. Chem. (IF 6.8) Pub Date : 2024-08-29 Bin Yu, Liang Ouyang
The Journal of Medicinal Chemistry is pleased to introduce a collection on Drug Discovery in China, featuring articles published in the journal between January 2021 and August 2024. In recent decades, China has witnessed significant progress in the field of new drug discovery and, more importantly, has seen a paradigm shift from traditional follow-on drug development to prioritizing innovative drugs
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Structure–Activity Relationship of Antibody–Oligonucleotide Conjugates: Evaluating Bioconjugation Strategies for Antibody–Phosphorodiamidate Morpholino Oligomer Conjugates for Drug Development J. Med. Chem. (IF 6.8) Pub Date : 2024-08-28 Michael Cochran, Isaac Marks, Tyler Albin, Danny Arias, Philip Kovach, Beatrice Darimont, Hanhua Huang, Usue Etxaniz, Hae Won Kwon, Yunyu Shi, Matthew Diaz, Olecya Tyaglo, Arthur Levin, Venkata Ramana Doppalapudi
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A New Class of Gold(I) NHC Complexes with Proapoptotic and Resensitizing Properties towards Multidrug Resistant Leukemia Cells Overexpressing BCL-2 J. Med. Chem. (IF 6.8) Pub Date : 2024-08-28 Franziska Bannwart, Leon F. Richter, Simon Stifel, Johanna Rueter, Holger N. Lode, João D. G. Correia, Fritz E. Kühn, Aram Prokop
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Nonlipogenic ABCA1 Inducers (NLAI) for Alzheimer’s Disease Validated in a Mouse Model Expressing Human APOE3/APOE4 J. Med. Chem. (IF 6.8) Pub Date : 2024-08-27 Ganga Reddy Velma, Megan S. Laham, Cutler Lewandowski, Ana C. Valencia-Olvera, Deebika Balu, Annabelle Moore, Martha Ackerman-Berrier, Pavel Rychetsky, Christopher Penton, Soumya Reddy Musku, Anandhan Annadurai, Maha Ibrahim Sulaiman, Nina Ma, Gregory R J Thatcher
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A Mitochondria-Targeting SIRT3 Inhibitor with Activity against Diffuse Large B Cell Lymphoma J. Med. Chem. (IF 6.8) Pub Date : 2024-08-27 Sadhan Jana, Jialin Shang, Jun Young Hong, Michael K. Fenwick, Rishi Puri, Xuan Lu, Ari M. Melnick, Meng Li, Hening Lin
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Deep Eutectic Solvents Enhancing Drug Solubility and Its Delivery J. Med. Chem. (IF 6.8) Pub Date : 2024-08-26 Anshu Sharma, Yea Rock Park, Aman Garg, Bong-Seop Lee
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Structure–Activity Relationship of Antibody–Oligonucleotide Conjugates: Evaluating Bioconjugation Strategies for Antibody–siRNA Conjugates for Drug Development J. Med. Chem. (IF 6.8) Pub Date : 2024-08-28 Michael Cochran, Danny Arias, Rob Burke, David Chu, Gulin Erdogan, Michael Hood, Philip Kovach, Hae Won Kwon, Yanling Chen, Michael Moon, Christopher D. Miller, Hanhua Huang, Arthur Levin, Venkata Ramana Doppalapudi
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Discovery of Inhibitors Targeting Protein–Protein Interaction between Bacterial RNA Polymerase and NusG as Novel Antimicrobials J. Med. Chem. (IF 6.8) Pub Date : 2024-08-28 Yingbo Zheng, Cheuk Hei Kan, Tsz Fung Tsang, Yanpeng Liu, Tiankuang Liu, Man Wai Tsang, Long Yin Lam, Xiao Yang, Cong Ma
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Exploring Degradation of Intrinsically Disordered Protein Yes-Associated Protein Induced by Proteolysis TArgeting Chimeras J. Med. Chem. (IF 6.8) Pub Date : 2024-08-27 Chen Zhou, Chunbao Sun, Miao Huang, Xin Tang, Liya Pi, Chenglong Li
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Structural and Biochemical Insights into the Mechanism of Action of the Clinical USP1 Inhibitor, KSQ-4279 J. Med. Chem. (IF 6.8) Pub Date : 2024-08-27 Martin Luke Rennie, Mehmet Gundogdu, Connor Arkinson, Steven Liness, Sheelagh Frame, Helen Walden
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Rational Design of Mono-Substituted Gd-DOTA as Highly Stable and Efficient MRI Contrast Agents for Hepatobiliary and Inflammation Imaging J. Med. Chem. (IF 6.8) Pub Date : 2024-08-27 Yinghui Ding, Xinzhong Ruan, Kun Shu, Weiyuan Xu, Yao Liu, Gengshen Mo, Jiao Xu, Yong Jian, Jilai Zhang, Lingfeng Zhang, Keren Wang, Ji-Ting Hou, Jianliang Shen, Zhihan Yan, Fangfu Ye, Jiang Zhu, Lixiong Dai
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Development of Nitric Oxide Releasing Oxoisoaporphines with Antidepressant Activities by Simultaneously Regulating MAO-A and SERT J. Med. Chem. (IF 6.8) Pub Date : 2024-08-27 Peisen Zhong, Xinyu Mao, Na Li, Li Chen, Jianbo Sun
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Selective Aurora A-TPX2 Interaction Inhibitors Have In Vivo Efficacy as Targeted Antimitotic Agents J. Med. Chem. (IF 6.8) Pub Date : 2024-08-27 Simon R. Stockwell, Duncan E. Scott, Gerhard Fischer, Estrella Guarino, Timothy P. C. Rooney, Tzu-Shean Feng, Tommaso Moschetti, Rajavel Srinivasan, Esther Alza, Alice Asteian, Claudio Dagostin, Anna Alcaide, Mathieu Rocaboy, Beata Blaszczyk, Alicia Higueruelo, Xuelu Wang, Maxim Rossmann, Trevor R. Perrior, Tom L. Blundell, David R. Spring, Grahame McKenzie, Chris Abell, John Skidmore, Ashok R. Venkitaraman
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New Potent RIPK2 Inhibitors as a Promising Therapeutic Avenue for Colitis Through the Blockade of NOD Inflammatory Pathways J. Med. Chem. (IF 6.8) Pub Date : 2024-08-27 Morgane Rivoal, Amélie Barzyck, Perrine Six, Xavier Dezitter, Min-Jeong Cornu-Choi, Mathilde Body-Malapel, Madjid Djouina, Christophe Waxin, Laurent Dubuquoy, Régis Millet, Natascha Leleu-Chavain
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Cellular, Structural Basis, and Recent Progress for Targeting Murine Double Minute X (MDMX) in Tumors J. Med. Chem. (IF 6.8) Pub Date : 2024-08-26 Qikun Yin, Yuemiao Hu, Zhiwen Dong, Jing Lu, Hongbo Wang
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Discovery of Novel Neo-Clerodane Derivatives as Potent Dual-Functional Antiosteoporosis Agents through Targeting Peroxisome Proliferator-Activated Receptor-γ J. Med. Chem. (IF 6.8) Pub Date : 2024-08-26 Xing Peng, Zhikang Zhang, Yuting Zhang, Huihao Zhou, Wenqi Li, Minxian Dai, Jinsai Shang, Jun Xu, Qiong Gu
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Discovery of Covalent MLKL PROTAC Degraders via Optimization of a Theophylline Derivative Ligand for Treating Necroptosis J. Med. Chem. (IF 6.8) Pub Date : 2024-08-24 Shang Li, Liangliang Ma, Xinxin Li, Yuhan Jiang, Zhongwen Luo, Fucheng Yin, Yonglei Zhang, Yifan Chen, Siyuan Wan, Han Zhou, Lingyi Kong, Xiaobing Wang
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Discovery of Novel 2-Aminopyridine-Based and 2-Aminopyrimidine-Based Derivatives as Potent CDK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors and Hematological Malignancies J. Med. Chem. (IF 6.8) Pub Date : 2024-08-23 Abdusaid Saidahmatov, Jianan Li, Shihao Xu, Xiaobei Hu, Xiangqian Gao, Weijuan Kan, Lixin Gao, Cong Li, Yuqiang Shi, Li Sheng, Peipei Wang, Yubo Zhou, Xuewu Liang, Jia Li, Hong Liu
更新日期：2024-09-11
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