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Discovery of GS-7682, a Novel 4′-Cyano-Modified C-Nucleoside Prodrug with Broad Activity against Pneumo- and Picornaviruses and Efficacy in RSV-Infected African Green Monkeys J. Med. Chem. (IF 6.8) Pub Date : 2024-07-17 Dustin S. Siegel, Hon C. Hui, Jared Pitts, Meghan S. Vermillion, Kazuya Ishida, Davin Rautiola, Michael Keeney, Hammad Irshad, Lijun Zhang, Kwon Chun, Gregory Chin, Bindu Goyal, Edward Doerffler, Hai Yang, Michael O. Clarke, Chris Palmiotti, Arya Vijjapurapu, Nicholas C. Riola, Kirsten Stray, Eisuke Murakami, Bin Ma, Ting Wang, Xiaofeng Zhao, Yili Xu, Gary Lee, Bruno Marchand, Minji Seung, Arabinda
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Detection of a Mitochondrial Fragmentation and Integrated Stress Response Using the Cell Painting Assay J. Med. Chem. (IF 6.8) Pub Date : 2024-07-17 Soheila Rezaei Adariani, Daya Agne, Sandra Koska, Annina Burhop, Carina Seitz, Jens Warmers, Petra Janning, Malte Metz, Axel Pahl, Sonja Sievers, Herbert Waldmann, Slava Ziegler
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Addressing the Opioids Lipophilicity Challenge via a Straightforward and Simultaneous 1H NMR-Based logP/D Determination, Both Separately and in Mixtures J. Med. Chem. (IF 6.8) Pub Date : 2024-07-16 Dina Yeffet, Ishay Columbus, Galit Parvari, Yoav Eichen, Sigal Saphier, Lee Ghindes-Azaria, Orit Redy-Keisar, Dafna Amir, Eyal Drug, Eytan Gershonov, Iris Binyamin, Yoram Cohen, Naama Karton-Lifshin, Yossi Zafrani
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Development of Zalfermin, a Long-Acting Proteolytically Stabilized FGF21 Analog J. Med. Chem. (IF 6.8) Pub Date : 2024-07-16 Kristian Sass-Ørum, Tina Møller Tagmose, Jørgen Olsen, Annika Sjölander, Per-Olof Wahlund, Dan Han, Andreas Vegge, Steffen Reedtz-Runge, Zhe Wang, Xiang Gao, Birgit Wieczorek, Kasper Lamberth, Kirsten Lykkegaard, Peter Kresten Nielsen, Henning Thøgersen, Mingrui Yu, Jianhua Wang, Jørn Drustrup, Xujia Zhang, Patrick Garibay, Kristian Hansen, Ann Maria Kruse Hansen, Birgitte Andersen
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FAP Radioligand Linker Optimization Improves Tumor Dose and Tumor-to-Healthy Organ Ratios in 4T1 Syngeneic Model J. Med. Chem. (IF 6.8) Pub Date : 2024-07-16 Spencer D. Lindeman, Owen C. Booth, Pooja Tudi, Taylor C. Schleinkofer, Jackson N. Moss, Nicholas B. Kearney, Ramesh Mukkamala, Lauren K. Thompson, Mollie A. Modany, Madduri Srinivasarao, Philip S. Low
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Design, Synthesis, and Biological Evaluation of 1,4-Dihydropyridine–Indole as a Potential Antidiabetic Agent via GLUT4 Translocation Stimulation J. Med. Chem. (IF 6.8) Pub Date : 2024-07-16 Sarita Katiyar, Shadab Ahmad, Abhishek Kumar, Alisha Ansari, Amol Chhatrapati Bisen, Ishbal Ahmad, Farah Gulzar, Rabi Sankar Bhatta, Akhilesh K. Tamrakar, Koneni V. Sashidhara
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Discovery of Biphenyl Derivatives to Target Hsp70-Bim Protein–Protein Interaction in Chronic Myeloid Leukemia by Scaffold Hopping Strategy J. Med. Chem. (IF 6.8) Pub Date : 2024-07-16 Maojun Jiang, Hong Zhang, Yang Song, Fangkui Yin, Zhiyuan Hu, Xin Li, Yuying Wang, Zheming Wang, Yitong Li, Zihan Wang, Yanxin Zhang, Siyao Wang, Shaohua Lu, Guanghong Xu, Ting Song, Ziqian Wang, Zhichao Zhang
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ERAP Inhibitors in Autoimmunity and Immuno-Oncology: Medicinal Chemistry Insights J. Med. Chem. (IF 6.8) Pub Date : 2024-07-16 Vasileios Fougiaxis, Ben He, Tuhina Khan, Rodolphe Vatinel, Nikoletta M. Koutroumpa, Antreas Afantitis, Laetitia Lesire, Pierre Sierocki, Benoit Deprez, Rebecca Deprez-Poulain
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Molecular Transformers: Adaptive Multitarget Ligands for Esterase-Induced Transition from Analgesics to Anesthetics J. Med. Chem. (IF 6.8) Pub Date : 2024-07-16 Tianguang Huang, Chi Song, Yuhao Chen, Yu Gan, Shilong Hu, Ao Hai, Wencheng Liu, Ting Kang, Yi Zhao, Zhuang Miao, Xing Wang, Yihang Fu, Bowen Ke
Multitarget strategies are essential in addressing complex diseases, yet developing multitarget-directed ligands (MTDLs) is particularly challenging when aiming to engage multiple therapeutic targets across different tissues. Here, we present a molecular transformer strategy, enhancing traditional MTDLs. By utilizing esterase-driven hydrolysis, this approach mimics the adaptive nature of transformers
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Correction to “Discovery of Novel and Highly Potent Resorcinol Dibenzyl Ether-Based PD-1/PD-L1 Inhibitors with Improved Drug-like and Pharmacokinetic Properties for Cancer Treatment” J. Med. Chem. (IF 6.8) Pub Date : 2024-07-16 Binbin Cheng, Wei Wang, Xiaoge Niu, Yichang Ren, Ting Liu, Hao Cao, Shuanghu Wang, Yingfeng Tu, Jingxuan Chen, Shuwen Liu, Xuchao Yang, Jianjun Chen
The authors extend their apologies for an unintentional oversight in the presentation of the subfigures within Figure 7A and Figure 7C of the article that has been published. This error occurred due to a technical issue during the image preparation process. We have reviewed the original data and have now corrected the original Figure 7 as detailed below and all authors have agreed to the changes. Figure
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Chasing Red Herrings: Palladium Metal Salt Impurities Feigning KRAS Activity in Biochemical Assays J. Med. Chem. (IF 6.8) Pub Date : 2024-07-15 Thomas Gerstberger, Helmut Berger, Frank H. Büttner, Michael Gmachl, Dirk Kessler, Manfred Koegl, Simon Lucas, Laetitia J. Martin, Moriz Mayer, Darryl B. McConnell, Sophie Mitzner, Guido Scholz, Matthias Treu, Bernhard Wolkerstorfer, Stephan Zahn, Krzysztof M. Zak, Philipp A. Jaeger, Peter Ettmayer
Identifying promising chemical starting points for small molecule inhibitors of active, GTP-loaded KRAS “on” remains of great importance to clinical oncology and represents a significant challenge in medicinal chemistry. Here, we describe broadly applicable learnings from a KRAS hit finding campaign: While we initially identified KRAS inhibitors in a biochemical high-throughput screen, we later discovered
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Structure-Based Design and Discovery of a Potent and Cell-Active LC3A/B Covalent Inhibitor J. Med. Chem. (IF 6.8) Pub Date : 2024-07-15 Zhenfei Zhou, Siqi Huang, Shijie Fan, Xueyuan Li, Chengyu Wang, Wanlin Yu, Daohai Du, Yuanyuan Zhang, Kaixian Chen, Wei Fu, Cheng Luo
Autophagy is a highly conserved cellular homeostasis maintenance mechanism in eukaryotes. Microtubule-associated protein light chain 3 (LC3) plays a crucial role in autophagy. It has multiple pairs of protein–protein interactions (PPIs) with other proteins, and these PPIs have an effect on the regulation of autophagosome formation and the recruitment of autophagic substrates. In our previous work,
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Multifunctional Molecular Hybrids Photoreleasing Nitric Oxide: Advantages, Pitfalls, and Opportunities J. Med. Chem. (IF 6.8) Pub Date : 2024-07-15 Cristina Parisi, Francesca Laneri, Aurore Fraix, Salvatore Sortino
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Discovery of a Highly Potent Lysine Methyltransferases G9a/NSD2 Dual Inhibitor to Treat Solid Tumors J. Med. Chem. (IF 6.8) Pub Date : 2024-07-15 Chunju Yang, Bang Li, Zongbo Feng, Huaxuan Li, Hong Yang, Zhenjiao Yang, Li Liu, Qiongyu Shi, Hong Wang, Zhong-Zhu Chen, Xun Huang, Junjian Wang, Yuanxiang Wang
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Electrophile Determines Cellular Phenotypes among XPO1-Targeting Small Molecules J. Med. Chem. (IF 6.8) Pub Date : 2024-07-15 Yi Fan Chen, Yanqiu Shen, David F. Yan, Maryam Ghazala, Marc A. Scemama de Gialluly, Ramya Srinivasan, Amanda N. Farrar, Ryan M. Friedrich, Drew J. Adams
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Identification of 6-Anilino Imidazo[4,5-c]pyridin-2-ones as Selective DNA-Dependent Protein Kinase Inhibitors and Their Application as Radiosensitizers J. Med. Chem. (IF 6.8) Pub Date : 2024-07-15 Cho R. Hong, Lydia P. Liew, Way W. Wong, Benjamin D. Dickson, Gary Cheng, Avik Shome, Rebecca Airey, Jagdish Jaiswal, Barbara Lipert, Stephen M. F. Jamieson, William R. Wilson, Michael P. Hay
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Identification of a Novel Protein Phosphatase 2A Activator, PPA24, as a Potential Therapeutic for FOLFOX-Resistant Colorectal Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-07-14 Hannah Johnson, Amandeep Singh, Asif Raza, Congzhou M. Sha, Jian Wang, Krishne Gowda, Zhihang Shen, Haritha Nair, Chenglong Li, Nikolay V. Dokholyan, Satya Narayan, Arun K. Sharma
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Discovery of New Phenyltetrazolium Derivatives as Ferroptosis Inhibitors for Treating Ischemic Stroke: An Example Development from Free Radical Scavengers J. Med. Chem. (IF 6.8) Pub Date : 2024-07-12 Yang Lu, Zexu Shen, Yaping Xu, Haoran Lin, Liteng Shen, Yizhen Jin, Yu Guo, Jialiang Lu, Linjie Li, Yuxin Zhuang, Yuheng Jin, Weihao Zhuang, Wenhai Huang, Xiaowu Dong, Haibin Dai, Jinxin Che
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The Development of a Highly Potent and Selective Human Toll-like Receptor 2 Agonist: Synthesis and Biological Evaluation of CaLGL-1 and Its Derivatives J. Med. Chem. (IF 6.8) Pub Date : 2024-07-12 Hongbin Jia, Zhikuan Luo, Ruijun Jing, Bowen Yao, Tinghong Lv, Haixue Zheng, Xiaolei Wang
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Near-Infrared II Fluorescence Imaging and Image-Guided siRNA Therapy of Atherosclerosis J. Med. Chem. (IF 6.8) Pub Date : 2024-07-12 Jialu Gao, Kai Yu, Qiusi Luo, Mingbo Deng, Xiaowen Hou, Wumei Wang, Xiaodong Zeng, Xiaoxing Xiong, Yong He, Xuechuan Hong, Yuling Xiao
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Development of Novel N-Acylhydrazone Derivatives with High Anti-obesity Activity and Improved Safety by Exploring the Pharmaceutical Properties of Aldehyde Group J. Med. Chem. (IF 6.8) Pub Date : 2024-07-12 Zhi Jiang, Yu-Tao Hu, Shi-Yao Guo, Yi-Xian Li, Dan-Dan Zhao, Li-Yuan Wei, Yu-Wei Lin, Shu-Min Xu, Shi-Liang Huang, Qingjiang Li, Jia-Heng Tan, Yong Rao, Shuo-Bin Chen, Zhi-Shu Huang
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Reaching Out and Moving Forward J. Med. Chem. (IF 6.8) Pub Date : 2024-07-11 Carolyn J. Straub
Pursuing addiction recovery is harrowing under the best of circumstances. As a college student, it felt damn near impossible. As I disclosed in my 2022 J. Med. Chem. editorial, I developed a substance addiction during my freshman year in response to the symptoms of my then-undiagnosed bipolar disorder. I used my drug of choice for long enough to lose most of what I valued in life─all before my 21st
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Amphiphilic Heparinoids as Potent Antiviral Agents against SARS-CoV-2 J. Med. Chem. (IF 6.8) Pub Date : 2024-07-12 Mohit Chhabra, Chethan D. Shanthamurthy, Nanjudaswamy Vijendra Kumar, Sandhya Mardhekar, Sharath S. Vishweshwara, Norbert Wimmer, Naphak Modhiran, Daniel Watterson, Alberto A. Amarilla, Jonathan S. Cha, James R. Beckett, James J. De Voss, Yasmin Kayal, Israel Vlodavsky, Lauren R. Dorsett, Raymond A. A. Smith, Neha S. Gandhi, Raghavendra Kikkeri, Vito Ferro
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Ligand-Directed Labeling of the Adenosine A1 Receptor in Living Cells J. Med. Chem. (IF 6.8) Pub Date : 2024-07-12 Eleonora Comeo, Joëlle Goulding, Chia-Yang Lin, Marleen Groenen, Jeanette Woolard, Nicholas D. Kindon, Clare R. Harwood, Simon Platt, Stephen J. Briddon, Laura E. Kilpatrick, Peter J. Scammells, Stephen J. Hill, Barrie Kellam
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Discovery of Novel Diaryl-Substituted Fused Heterocycles Targeting Katanin and Tubulin with Potent Antitumor and Antimultidrug Resistance Efficacy J. Med. Chem. (IF 6.8) Pub Date : 2024-07-12 Fuhao Jiang, Min Yu, Yuru Liang, Kuiling Ding, Yang Wang
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An Update on the Nitrogen Heterocycle Compositions and Properties of U.S. FDA-Approved Pharmaceuticals (2013–2023) J. Med. Chem. (IF 6.8) Pub Date : 2024-07-12 Christopher M. Marshall, John G. Federice, Chloe N. Bell, Philip B. Cox, Jon T. Njardarson
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Repurposing GnRH-A as a Near-Infrared Fluorescent Probe for Diagnosis and Surgical Navigation of Breast Cancer Tumors and Metastases J. Med. Chem. (IF 6.8) Pub Date : 2024-07-12 Haoran Xu, Zhuoyi Ye, Xin Gao, Yue Dai, Yang Luo, Zhihao Han, Yueqing Gu
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Discovery of a Series of Orally Bioavailable Androgen Receptor Degraders for the Treatment of Prostate Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-07-11 Sharan K. Bagal, Peter C. Astles, Coura Diène, Argyrides Argyrou, Claire Crafter, Doyle J. Cassar, Charlene Fallan, Andreas Hock, Thomas Jones, Kevin Moreau, Gillian M. Lamont, Scott Lamont, Chrysiis Michaloglou, Martin J. Packer, Andy Pike, Antonio Ramos-Montoya, James S. Scott, Joseph Shaw, Ziyanda Shologu
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Directly Suppressing MYC Function with Novel Alkynyl-Substituted Phenylpyrazole Derivatives that Induce Protein Degradation and Perturb MYC/MAX Interaction J. Med. Chem. (IF 6.8) Pub Date : 2024-07-11 Can Zhao, Fang Zhao, Liuqing Yang, Yang Wang, Henian Wang, Fang Fang, Haojie Zuo, Zhi Li, Ge He, Wenhu Zhan, Xiaodong Ma
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Exploring the Potential of Cyclic Peptidyl Antitumor Agents Derived from Natural Macrocyclic Peptide Phakellistatin 13 J. Med. Chem. (IF 6.8) Pub Date : 2024-07-11 Tong Li, Shitian Jiang, Tingting Li, Hongyu Xu, Xiong Zhang, Rui Yan, Xiaodan Wu, Yingxue Jin, Zhiqiang Wang
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Highly Selective Drug-Derived Fluorescent Probes for the Cannabinoid Receptor Type 1 (CB1R) J. Med. Chem. (IF 6.8) Pub Date : 2024-07-11 Leonard Mach, Anahid Omran, Jara Bouma, Silke Radetzki, David A. Sykes, Wolfgang Guba, Xiaoting Li, Calvin Höffelmeyer, Axel Hentsch, Thais Gazzi, Yelena Mostinski, Malgorzata Wasinska-Kalwa, Fabio de Molnier, Cas van der Horst, Jens Peter von Kries, Marc Vendrell, Tian Hua, Dmitry B. Veprintsev, Laura H. Heitman, Uwe Grether, Marc Nazare
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Targeting Myeloperoxidase Ameliorates Gouty Arthritis: A Virtual Screening Success Story J. Med. Chem. (IF 6.8) Pub Date : 2024-07-11 Isaac de A. Matos, Jorge L. Dallazen, Lorenna R. Reis, Luiz Felipe Souza, Regina C. Bevevino, Rafael D. de Moura, Graziella E. Ronsein, Nicolas Carlos Hoch, Nivan Bezerra da Costa Júnior, Soraia Kátia P. Costa, Flavia C. Meotti
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Discovery of Novel Peptide Antagonists Targeting GPR55 for Liver Inflammation and Fibrosis J. Med. Chem. (IF 6.8) Pub Date : 2024-07-11 Zihan Shi, Xianyan Liu, Shuohan Wu, Nazi Song, Qinglin Tang, Haonan Li, Suijia Luo, Albert S. C. Chan, Xiaoqing Cai, Han Liu, Xianxing Jiang
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Structure–Activity Relationship Studies of Aryl Sulfoxides as Reversible Monoacylglycerol Lipase Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-07-11 Ming Jiang, Mirjam C. W. Huizenga, Florian Mohr, Avand Amedi, Renze Bakker, Richard J. B. H. N. van den Berg, Hui Deng, Tom van der Wel, Constant A.A. van Boeckel, Mario van der Stelt
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Targeting hTERT Promoter G-Quadruplex DNA Structures with Small-Molecule Ligand to Downregulate hTERT Expression for Triple-Negative Breast Cancer Therapy J. Med. Chem. (IF 6.8) Pub Date : 2024-07-10 Wei Long, Yao-Xun Zeng, Bo-Xin Zheng, Yu-Bo Li, Ya-Kun Wang, Ka-Hin Chan, Meng-Ting She, Yu-Jing Lu, Chunyang Cao, Wing-Leung Wong
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Correction to “Structure–Activity Relationship of a Pyrrole Based Series of PfPKG Inhibitors as Anti-Malarials” J. Med. Chem. (IF 6.8) Pub Date : 2024-07-10 John A. Gilleran, Kutub Ashraf, Melvin Delvillar, Tyler Eck, Raheel Fondekar, Edward B. Miller, Ashley Hutchinson, Aiping Dong, Alma Seitova, Mariana Laureano De Souza, David Augeri, Levon Halabelian, John Siekierka, David P. Rotella, John Gordon, Wayne E. Childers, Mark C. Grier, Bart L. Staker, Jacques Y. Roberge, Purnima Bhanot
Page 3474. In the subsection of the Results with the heading R3–In VitroSAR Trend, the sentence “However, our analysis of the 3-methylpiperidine analogs 40–41 (cis and trans racemates), noted a marked improvement in potency, particularly in the EC50 measurements in cellular assays.” should read “However, our analysis of the 3-methylpiperidine analogs 38–39 (cis and trans racemates) noted a marked improvement
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High-Throughput SFC-MS/MS Method to Measure EPSA and Predict Human Permeability J. Med. Chem. (IF 6.8) Pub Date : 2024-07-08 Yue-Ting Wang, Edward Price, Mei Feng, Jason Hulen, Stella Doktor, David M. Stresser, Estelle M. Maes, Qin C. Ji, Gary J. Jenkins
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Recent Progress toward the Discovery of Small Molecules as Novel Anti-Respiratory Syncytial Virus Agents J. Med. Chem. (IF 6.8) Pub Date : 2024-07-06 Tommaso Felicetti, Chiara Sarnari, Roberta Gaito, Oriana Tabarrini, Giuseppe Manfroni
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Discovery of MT-1207: A Novel, Potent Multitarget Inhibitor as a Promising Clinical Candidate for the Treatment of Hypertension J. Med. Chem. (IF 6.8) Pub Date : 2024-07-05 Peng Wang, Huajian Zhu, Jia-Sheng Tian, Wenjian Zhu, Shengtao Xu, Hong Yao, Jie Liu, Zheying Zhu, Chao-Yu Miao, Jinyi Xu
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Fixing the Achilles Heel of Pfizer’s Paxlovid for COVID-19 Treatment J. Med. Chem. (IF 6.8) Pub Date : 2024-07-05 Lennart Brewitz, Christopher J. Schofield
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Recent Advances in Targeted Cancer Therapy: Are PDCs the Next Generation of ADCs? J. Med. Chem. (IF 6.8) Pub Date : 2024-07-09 Baochen Zhang, Mo Wang, Li Sun, Jiawei Liu, Libinghan Yin, Mingjing Xia, Ling Zhang, Xifu Liu, Yu Cheng
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Development of Peptide-Based Probes for Molecular Imaging of the Postsynaptic Density in the Brain J. Med. Chem. (IF 6.8) Pub Date : 2024-07-09 Eduardo F. A. Fernandes, Mikael Palner, Nakul Ravi Raval, Troels E. Jeppesen, Daniela Danková, Simone L. Bærentzen, Christian Werner, Janna Eilts, Hans M. Maric, Sören Doose, Sanjay Sagar Aripaka, Sanne Simone Kaalund, Susana Aznar, Andreas Kjaer, Andreas Schlosser, Linda M. Haugaard-Kedström, Gitte M. Knudsen, Matthias M. Herth, Kristian Stro̷mgaard
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Targeted Protein Degradation: Current and Emerging Approaches for E3 Ligase Deconvolution J. Med. Chem. (IF 6.8) Pub Date : 2024-07-09 Yufeng Xiao, Yaxia Yuan, Yi Liu, Zongtao Lin, Guangrong Zheng, Daohong Zhou, Dongwen Lv
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Identification of Psychoplastogenic Tropanes Lacking Muscarinic Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-07-09 Hunter T. Warren, Winston L. Chow, Milan Chytil, Kurt Rasmussen, David E. Olson
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Machine-Learning-Guided Peptide Drug Discovery: Development of GLP-1 Receptor Agonists with Improved Drug Properties J. Med. Chem. (IF 6.8) Pub Date : 2024-07-08 Jens Christian Nielsen, Claudia Hjo̷rringgaard, Mads Mo̷rup Nygaard, Anita Wester, Lisbeth Elster, Trine Porsgaard, Randi Bonke Mikkelsen, Silas Rasmussen, Andreas Nygaard Madsen, Morten Schlein, Niels Vrang, Kristoffer Rigbolt, Louise S. Dalbo̷ge
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Development of an Orally Bioavailable LCK PROTAC Degrader as a Potential Therapeutic Approach to T-Cell Acute Lymphoblastic Leukemia J. Med. Chem. (IF 6.8) Pub Date : 2024-07-08 Jamie A. Jarusiewicz, Satoshi Yoshimura, Marisa Actis, Yong Li, Xiang Fu, Lei Yang, Shilpa Narina, Shondra M. Pruett-Miller, Suiping Zhou, Xusheng Wang, Anthony A. High, Gisele Nishiguchi, Jun J. Yang, Zoran Rankovic
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New Strategies for Responding to SARS-CoV-2: The Present and Future of Dual-Target Drugs J. Med. Chem. (IF 6.8) Pub Date : 2024-07-05 Wenyi Zhang, Lecheng Xiao, Dianyang Li, Yuxuan Hu, Wenying Yu
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Isosteric Replacement of Sulfur to Selenium in a Thiosemicarbazone: Promotion of Zn(II) Complex Dissociation and Transmetalation to Augment Anticancer Efficacy J. Med. Chem. (IF 6.8) Pub Date : 2024-07-05 Busra Kaya, Mahan Gholam Azad, Mediha Suleymanoglu, Jeffrey R. Harmer, Tharushi P. Wijesinghe, Vera Richardson, Xiao Zhao, Paul V. Bernhardt, Mahendiran Dharmasivam, Des R. Richardson
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Targeting Relevant HDACs to Support the Survival of Cone Photoreceptors in Inherited Retinal Diseases: Identification of a Potent Pharmacological Tool with In Vitro and In Vivo Efficacy J. Med. Chem. (IF 6.8) Pub Date : 2024-07-04 Gabriele Carullo, Noemi Orsini, Ilaria Piano, Luca Pozzetti, Alessandro Papa, Anna Fontana, Debora Napoli, Francesca Corsi, Beatrice Di Marco, Alessia Galante, Ludovica Marotta, Giovanna Panzeca, Justine O’Brien, Alicia Gomez Sanchez, Harry Doherty, Niamh Mahon, Leni Clarke, Chiara Contri, Silvia Pasquini, Beatrice Gorelli, Simona Saponara, Massimo Valoti, Fabrizio Vincenzi, Katia Varani, Anna Ramunno
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Discovery of Potent and Selective c-Met Degraders for Hepatocellular Carcinoma Treatment J. Med. Chem. (IF 6.8) Pub Date : 2024-07-04 Wenjian Min, Huanaoyu Yang, Dawei Wang, Chunling Chen, Yanyin Wang, Yi Hou, Yasheng Zhu, Chengliang Sun, Xiao Wang, Kai Yuan, Peng Yang
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NN1213 – A Potent, Long-Acting, and Selective Analog of Human Amylin J. Med. Chem. (IF 6.8) Pub Date : 2024-07-03 Kirsten Dahl, Kirsten Raun, Jakob Lerche Hansen, Christian Poulsen, Charlotta D. de la Cour, Trine Ryberg Clausen, Ann Maria Kruse Hansen, Linu M. John, Annette Plesner, Gao Sun, Morten Schlein, Rikke Bjerring Skyggebjerg, Thomas Kruse
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Lipid Trolling to Optimize A3 Adenosine Receptor-Positive Allosteric Modulators (PAMs) J. Med. Chem. (IF 6.8) Pub Date : 2024-07-03 Balaram Pradhan, Matteo Pavan, Courtney L. Fisher, Veronica Salmaso, Tina C. Wan, Robert F. Keyes, Noah Rollison, R. Rama Suresh, T. Santhosh Kumar, Zhan-Guo Gao, Brian C. Smith, John A. Auchampach, Kenneth A. Jacobson
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More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication J. Med. Chem. (IF 6.8) Pub Date : 2024-07-03 Han Wee Ong, Xuan Yang, Jeffery L. Smith, Rebekah J. Dickmander, Jason W. Brown, Tammy M. Havener, Sharon Taft-Benz, Stefanie Howell, Marcia K. Sanders, Jacob L. Capener, Rafael M. Couñago, Edcon Chang, Andreas Krämer, Nathaniel J. Moorman, Mark Heise, Alison D. Axtman, David H. Drewry, Timothy M. Willson
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New Horizons of Synthetic Lethality in Cancer: Current Development and Future Perspectives J. Med. Chem. (IF 6.8) Pub Date : 2024-07-02 Viola Previtali, Greta Bagnolini, Andrea Ciamarone, Giovanni Ferrandi, Francesco Rinaldi, Samuel Harry Myers, Marinella Roberti, Andrea Cavalli
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Small Molecule Targeting PPM1A Activates Autophagy for Mycobacterium tuberculosis Host-Directed Therapy J. Med. Chem. (IF 6.8) Pub Date : 2024-07-03 Zhipeng Yu, Yi Chu Liang, Stefania Berton, Liping Liu, Jiaqi Zou, Lu Chen, Zhongliang Xu, Cheng Luo, Jim Sun, Weibo Yang
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Discovery of a Series of 4-Amide-thiophene-2-carboxyl Derivatives as Highly Potent P2Y14 Receptor Antagonists for Inflammatory Bowel Disease Treatment J. Med. Chem. (IF 6.8) Pub Date : 2024-07-03 Yu-hang Wang, Chun-xiao Liu, Yi-han Zhang, Ya-lian Yang, Yan Zhao, Lu Han, Qian-qian Wang, Wen Xiao, Qing-hua Hu, Zhen-hua Ding, Meng-ze Zhou, Cheng Jiang
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Novel Jatrophane Diterpenoids from Euphorbia esula Promotes Lipid Clearance by Transcriptional Regulation of PCSK9 J. Med. Chem. (IF 6.8) Pub Date : 2024-07-03 Tong Chen, Aijun Hou, Pengju Guo, Shou Peng, Guoqing Qin, Aoxue Ding, Xianggang Hu, Yelin Duan, Jing Chen, Likun Gong, Lijiang Xuan
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Backbone-Determined Antiarrhythmic Structure–Activity Relationships for a Mirror Image, Oligomeric Depsipeptide Natural Product J. Med. Chem. (IF 6.8) Pub Date : 2024-07-03 Madelaine P. Thorpe, Daniel J. Blackwell, Bjorn C. Knollmann, Jeffrey N. Johnston
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The First Discovery of Marine Polyoxygenated Cembranolides as Potential Agents for the Treatment of Ulcerative Colitis J. Med. Chem. (IF 6.8) Pub Date : 2024-07-03 Yuan-Yuan Cui, Yang Jin, Ruo-Nan Sun, Xue Wang, Cheng-Long Gao, Xiao-Yun Cui, Kai-Xian Chen, Yi-Li Sun, Yue-Wei Guo, Jia Li, Xu-Wen Li
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Structure-Guided Design of Potent Coronavirus Inhibitors with a 2-Pyrrolidone Scaffold: Biochemical, Crystallographic, and Virological Studies J. Med. Chem. (IF 6.8) Pub Date : 2024-07-02 Chamandi S. Dampalla, Yunjeong Kim, Alexandria Zabiegala, Dennis J. Howard, Harry Nhat Nguyen, Trent K. Madden, Hayden A. Thurman, Anne Cooper, Lijun Liu, Kevin P. Battaile, Scott Lovell, Kyeong-Ok Chang, William C. Groutas