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Epigenetic editor silences prion protein Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-07-25
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Oral miniproteins treat IBD Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-07-25
Discover the world’s best science and medicine | Nature.com
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Proteogenomics identifies anticancer targets Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-07-25
Discover the world’s best science and medicine | Nature.com
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Opioid antidote gets a boost Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-07-25
Discover the world’s best science and medicine | Nature.com
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Discovery of Preclinical Candidate AD1058 as a Highly Potent, Selective, and Brain-Penetrant ATR Inhibitor for the Treatment of Advanced Malignancies J. Med. Chem. (IF 6.8) Pub Date : 2024-07-25 Zhi Liu, Kailong Jiang, Yan Liu, Junfei Li, Siqi Huang, Ping Li, Lei Xu, Xiaomin Xu, Xiaobei Hu, Xia Zeng, Zehui Huang, Yubo Zhou, Jia Li, Kai Long, Mingliang Wang
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Structure of Designer Antibody-like Peptides Binding to the Human C5a with Potential to Modulate the C5a Receptor Signaling J. Med. Chem. (IF 6.8) Pub Date : 2024-07-25 Manaswini Ghosh, Pulkit Kr. Gupta, Lalita Mohan Behera, Soumendra Rana
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Peptidic Boronic Acid Plasmodium falciparum SUB1 Inhibitors with Improved Selectivity over Human Proteasome J. Med. Chem. (IF 6.8) Pub Date : 2024-07-25 Chrislaine Withers-Martinez, Elina Lidumniece, Fiona Hackett, Christine R. Collins, Zahie Taha, Michael J. Blackman, Aigars Jirgensons
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Mining Medicinally Relevant Bioreduction Substrates Inspired by Ligand-Based Drug Design J. Med. Chem. (IF 6.8) Pub Date : 2024-07-25 Alexander J. Rago, Ioanna Zoi, Jackson A. Gartman, Kelly A. McDaniel, Navendu Jana, Dachun Liu, Wen-Ju Bai
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Identification of 6-Fluorine-Substituted Coumarin Analogues as POLRMT Inhibitors with High Potency and Safety for Treatment of Pancreatic Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-07-24 Shengnan Zhou, Xiaotong Ze, Dazhi Feng, Lihua Liu, Yuning Shi, Minghui Yu, Lijuan Huang, Yunyue Wang, Hanlu Men, Jianbing Wu, Zhenwei Yuan, Mengze Zhou, Jinyi Xu, Xinnan Li, Hong Yao
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Design, Synthesis, and Characterization of New δ Opioid Receptor-Selective Fluorescent Probes and Applications in Single-Molecule Microscopy of Wild-Type Receptors J. Med. Chem. (IF 6.8) Pub Date : 2024-07-23 Antonios Drakopoulos, Zsombor Koszegi, Kerstin Seier, Harald Hübner, Damien Maurel, Rémy Sounier, Sébastien Granier, Peter Gmeiner, Davide Calebiro, Michael Decker
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A Comprehensive In Vitro Characterization of a New Class of Indole-Based Compounds Developed as Selective Haspin Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-07-22 Vincenzo Vestuto, Tania Ciaglia, Simona Musella, Veronica Di Sarno, Gerardina Smaldone, Francesca Di Matteo, Maria Carmina Scala, Valeria Napolitano, Maria Rosaria Miranda, Giuseppina Amodio, Sara Novi, Giacomo Pepe, Manuela Giovanna Basilicata, Erica Gazzillo, Simona Pace, Isabel M. Gomez-Monterrey, Marina Sala, Giuseppe Bifulco, Mario Felice Tecce, Pietro Campiglia, Carmine Ostacolo, Gianluigi Lauro
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Discovery of a NCOA4 Degrader for Labile Iron-Dependent Ferroptosis Inhibition J. Med. Chem. (IF 6.8) Pub Date : 2024-07-24 Jian’ai Ji, Yuhui Jin, Sinan Ma, Yuxuan Zhu, Xinyu Bi, Qidong You, Zhengyu Jiang
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Design and Discovery of New Collagen V-Derived FGF2-Blocking Natural Peptides Inhibiting Lung Squamous Cell Carcinoma In Vitro and In Vivo J. Med. Chem. (IF 6.8) Pub Date : 2024-07-24 Keli Kuang, Xiang Chen, Maolin Wang, Weijing Han, Xue Qiu, Taoli Jin, Rong Xu, Bing Yuan, Meiqi Qian, Chunyan Li, Run Xiang, Fei Li, Shuwen Zhang, Zi Yang, Junrong Du, Dapeng Li, Chun Zhang, Qiantao Wang, Tao Jia
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New Class of Hsp90 C-Terminal Domain Inhibitors with Anti-tumor Properties against Triple-Negative Breast Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-07-23 Živa Zajec, Jaka Dernovšek, Jernej Cingl, Iza Ogris, Marius Gedgaudas, Asta Zubrienė, Ana Mitrović, Simona Golič Grdadolnik, Martina Gobec, Tihomir Tomašič
Triple-negative breast cancer (TNBC) remains a treatment challenge and requires innovative therapies. Hsp90, crucial for the stability of numerous oncogenic proteins, has emerged as a promising therapeutic target. In this study, we present the optimization of the Hsp90 C-terminal domain (CTD) inhibitor TVS21. Biochemical methods, NMR binding studies, and molecular modeling were employed to investigate
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Discovery of NO Donor-Aurovertin Hybrids as Dual Ferroptosis and Apoptosis Inducers for Treating Triple Negative Breast Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-07-23 Lie-Feng Ma, Li−Li Xu, Ling-Jie Yuan, Xi Yang, Rui Wu, Shu-Min Bao, Yi-Li Chen, Hong-Liang Duan, Luo Fang, Hua-Jun Zhao, Zha-Jun Zhan
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Discovery of ZJCK-6-46: A Potent, Selective, and Orally Available Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A Inhibitor for the Treatment of Alzheimer’s Disease J. Med. Chem. (IF 6.8) Pub Date : 2024-07-23 Huanhua Chen, Xudong Gao, Xinzhu Li, Chong Yu, Wenwu Liu, Jingsong Qiu, Wenjie Liu, Hefeng Geng, Fangyuan Zheng, Hao Gong, Zihua Xu, Jingming Jia, Qingchun Zhao
Targeting dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) has been verified to regulate the progression of tau pathology as a promising treatment for Alzheimer’s disease (AD), while the research progress on DYRK1A inhibitors seemed to be in a bottleneck period. In this work, we identified 32 (ZJCK-6-46) as the most potential DYRK1A inhibitor (IC50 = 0.68 nM) through rational
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Advancing Tumor-Targeted Chemo-Immunotherapy: Development of the CAR-M-derived Exosome-Drug Conjugate J. Med. Chem. (IF 6.8) Pub Date : 2024-07-23 Yunhan Jiang, Xiaoqiu Xu, Dongmei Fan, Pingxian Liu, Meng Zhou, Mengdi Cheng, Jiasheng Huang, Youfu Luo, Yingqiang Guo, Tao Yang
Traditional antibody–drug conjugates (ADCs) mainly suppress tumor growth through either chemotherapy with cytotoxic payloads or immunotherapy with immuno-modulators. However, a single therapeutic modality may limit their exploration. Herein, we developed a new type of drug conjugate termed CAR-EDC (CAR-M-derived exosome-drug conjugate) by using CAR-exosomes from CAR-M cells as the targeting drug carrier
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Discovery of Potent and Selective G9a Degraders for the Treatment of Pancreatic Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-07-23 Yunkai Shi, Qianqian Shen, Ruikai Long, Yiwen Mao, Shuaihang Tong, Yaxi Yang, Jing Gao, Hu Zhou, Yi Chen, Bing Zhou
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Natural Product-Inspired Dopamine Receptor Ligands J. Med. Chem. (IF 6.8) Pub Date : 2024-07-22 Michael Dorogan, Hari K. Namballa, Wayne W. Harding
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Discovery of Novel Pyrimidine-Based Derivatives as Nav1.2 Inhibitors with Efficacy in Mouse Models of Epilepsy J. Med. Chem. (IF 6.8) Pub Date : 2024-07-22 Guoxue He, Yueming Zheng, Shunzhen Chang, Long Wang, Xiaohao Yang, Haishuang Hao, Jiyuan Li, Xian Zhang, Fuyun Tian, Xuewu Liang, Haiyan Xu, Pei Wang, Xueqin Chen, Zeyu Cao, Sui Fang, Zhaobing Gao, Hong Liu
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Development of Preladenant-Based Radiotracers for Imaging A2AR in Tumors J. Med. Chem. (IF 6.8) Pub Date : 2024-07-22 Xueyuan Zeng, Hongwu Liu, Guolong Huang, Yanjie Wang, Wuhao Zhou, Yike Wang, Xuedong Chen, Xingxing Cheng, Rongqiang Zhuang, Jindian Li, Jianyang Fang, Lumei Huang, Xianzhong Zhang, Zhide Guo
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Design, Synthesis, and Evaluation of the Selective and Orally Active LSD1 Inhibitor with the Potential of Treating Heart Failure J. Med. Chem. (IF 6.8) Pub Date : 2024-07-22 Ming-Jie Huang, Jiale Xu, Hui Qiao, Wen Zhao, Lihua Huang
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Design and Synthesis of sEH/HDAC6 Dual-Targeting Inhibitors for the Treatment of Inflammatory Pain J. Med. Chem. (IF 6.8) Pub Date : 2024-07-21 Huashen Xu, Yuanguang Chen, Hua Tong, Lu Chen, Christophe Morisseau, Zijian Zhou, Junning Zhuang, Chuqiao Song, Pengcheng Cai, Zhongbo Liu, Bruce D. Hammock, Guoliang Chen
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Rationally Designed Highly Potent NKT Cell Agonists with Different Cytokine Selectivity through Hydrogen-Bond Interaction J. Med. Chem. (IF 6.8) Pub Date : 2024-07-20 Yu Wen, Dong Ding, Meng-Qiang Luo, Xiao-Qian Peng, En-Yang Wang, Ye-Hui Wu, Shi-Hao Zhou, Jun Guo
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Discovery of Novel HDAC3 Inhibitors with PD-L1 Downregulating/Degrading and Antitumor Immune Effects J. Med. Chem. (IF 6.8) Pub Date : 2024-07-20 Zhiqiang Sun, Chenglong Xu, Jinmei Cheng, Zichao Yang, Ting Liu, Bulian Deng, Xuewen Zhang, Xiaopeng Peng, Jianjun Chen
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Synthesis of Lipidated Ligands and Formulation of Glia-Specific LNPs for RNAi-Mediated BBB Protection J. Med. Chem. (IF 6.8) Pub Date : 2024-07-20 Hai Xiao, Xuemei Bao, Nuomin Bai, Wunile Zhu, Saqirila Saqirila, Xin Hu, Qingming Bao, Huricha Baigude
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Back-Pocket Optimization of 2-Aminopyrimidine-Based Macrocycles Leads to Potent EPHA2/GAK Kinase Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-07-19 Joshua Gerninghaus, Rezart Zhubi, Andreas Krämer, Marwah Karim, Do Hoang Nhu Tran, Andreas C. Joerger, Christian Schreiber, Lena M. Berger, Benedict-Tilman Berger, Theresa A.L. Ehret, Lewis Elson, Christopher Lenz, Krishna Saxena, Susanne Müller, Shirit Einav, Stefan Knapp, Thomas Hanke
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Rational In Silico Design of Selective TMPRSS6 Peptidomimetic Inhibitors via Exploitation of the S2 Subpocket J. Med. Chem. (IF 6.8) Pub Date : 2024-07-19 Michael Desgagné, Antoine Désilets, Sára Ferková, Matthieu Lepage, Olivier Perreault, Alexandre Joushomme, Gabriel Lemieux, Walid Guerrab, Ulrike Froehlich, Christian Comeau, Philippe Sarret, Richard Leduc, Pierre-Luc Boudreault
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Discovery of a Highly Potent, Selective and Efficacious USP7 Degrader for the Treatment of Acute Lymphoblastic Leukemia J. Med. Chem. (IF 6.8) Pub Date : 2024-07-19 Miaomiao Xu, Jingfeng Fu, Yuan Pei, Mengna Li, Weijuan Kan, Ruyu Yan, Chaoyue Xia, Jingkun Ma, Peipei Wang, Yan Zhang, Yue Gao, Yaxi Yang, Yubo Zhou, Jia Li, Bing Zhou
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Structural Biology in Drug Discovery and Development: Call for Papers J. Med. Chem. (IF 6.8) Pub Date : 2024-07-19 David E. Heppner, Simone V. Bigi-Botterill, Andrew P. Riley, Kelly Chibale, Craig W. Lindsley
Visualizing the three-dimensional binding modes of potential drug molecules within their target sites has significantly impacted the drug discovery paradigm. (1) As such, “structurally enabled” drug development campaigns are naturally accelerated. Structural information provides a roadmap for designing molecules that enhance target profile parameters while avoiding alterations that may compromise binding
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Deuterium Editing of Small Molecules: A Case Study on Antitumor Activity of 1,4-Benzodiazepine-2,5-dione Derivatives J. Med. Chem. (IF 6.8) Pub Date : 2024-07-18 Wenjun Yu, Shiping Fang, Xilei Xie, Wenwu Liu, Xinhua Liu, Yanan Du, Purong Zheng, Gang Liu
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Correction to “Discovery of Novel Acridane-Based Tubulin Polymerization Inhibitors with Anticancer and Potential Immunomodulatory Effects” J. Med. Chem. (IF 6.8) Pub Date : 2024-07-18 Xiaopeng Peng, Yichang Ren, Wanyi Pan, Jin Liu, Jianjun Chen
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Antibody sniffs out tau Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-07-23
Discover the world’s best science and medicine | Nature.com
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AI reverse-engineers antibodies Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-07-23
Discover the world’s best science and medicine | Nature.com
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Molecular glue degrader for sickle cell disease Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-07-23
Discover the world’s best science and medicine | Nature.com
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New epilepsy therapies in development Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-07-22 Pavel Klein, Rafal M. Kaminski, Matthias Koepp, Wolfgang Löscher
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Discovery of Two Highly Selective Structurally Orthogonal Chemical Probes for Activin Receptor-like Kinases 1 and 2 J. Med. Chem. (IF 6.8) Pub Date : 2024-07-18 Václav Němec, Marek Remeš, Petr Beňovský, Michael C. Böck, Eliška Šranková, Jong Fu Wong, Julien Cros, Eleanor Williams, Lap Hang Tse, David Smil, Deeba Ensan, Methvin B. Isaac, Rima Al-Awar, Regina Gomolková, Vlad-Constantin Ursachi, Bohumil Fafílek, Zuzana Kahounová, Ráchel Víchová, Ondřej Vacek, Benedict-Tilman Berger, Carrow I. Wells, Cesear R. Corona, James D. Vasta, Matthew B. Robers, Pavel Krejci
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Discovery of 2-Methyl-5-(1H-pyrazol-4-yl)pyridines and Related Heterocycles as Promising M4 mAChR Positive Allosteric Modulators for the Treatment of Neurocognitive Disorders J. Med. Chem. (IF 6.8) Pub Date : 2024-07-18 Boqun Liu, Geoff Thompson, Manuela Jörg, Nicholas Barnes, David M. Thal, Arthur Christopoulos, Ben Capuano, Celine Valant, Peter J. Scammells
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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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Predicting the Intravenous Pharmacokinetics of Covalent Drugs in Animals and Humans J. Med. Chem. (IF 6.8) Pub Date : 2024-07-17 Rowan Stringer, Tobias Kaster
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Discovery, Synthesis, and Activity Evaluation of Novel Five-Membered Sulfur-Containing Heterocyclic Nucleosides as Potential Anticancer Agents In Vitro and In Vivo J. Med. Chem. (IF 6.8) Pub Date : 2024-07-17 Er-Jun Hao, Yan Zhao, Min Yu, Xian-Jia Li, Ke-Xin Wang, Fu-Ying Su, Yu-Ru Liang, Yang Wang, Hai-Ming Guo
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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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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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Chromatin remodellers as therapeutic targets Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-07-16 Hayden A. Malone, Charles W. M. Roberts
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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
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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 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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Data science in pharmaceutical R&D: the DISRUPT-DS industry roundtable Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-07-15 Najat S. Khan, Thomas Senderovitz, James Weatherall, Janice Branson, Benedikt Egersdoerfer, Eric Genevois-Marlin, Sai Jasti, Mustaqhusain Kazi, Ranjit Kumble, Patrick Loerch, Justine Rochon, Venkat Sethuraman, Matt Studney, Xiaoying Wu, Ryan Copping, Priya Chandran, Dhruv Jayanth, Christoph Meier
The DISRUPT-DS roundtable, which brings together data science leaders from large pharmaceutical companies, aims to be a forum for sharing experiences and networking, for shaping industry-level topics and for amplifying the role of data science across pharmaceutical R&D.
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FDA new drug approvals in Q2 2024 Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-07-15
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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
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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
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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