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Rigid Fe(III) Chelate with Phosphonate Pendants: A Stable and Effective Extracellular MRI Contrast Agent J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Ling He, Haiyu Wang, Zuhua Zeng, Lei Zhong, Qingxuan Tang, Junlai Yu, Jia Tian, Tianwei Liu, Jiang Zhu
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Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Marie-Gabrielle Braun, Avi Ashkenazi, Ramsay E. Beveridge, Georgette Castanedo, Heidi Ackerly Wallweber, Maureen H. Beresini, Kevin R. Clark, Tom De Bruyn, Liqiang Fu, Paul Gibbons, Fan Jiang, Susan Kaufman, David Kan, James R. Kiefer, Jean-Philippe Leclerc, Alexandre Lemire, Cuong Ly, Ehud Segal, Jessica Sims, Weiru Wang, Wentao Wei, Liang Zhao, Jacob B. Schwarz, Joachim Rudolph
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Explorations of Agonist Selectivity for the α9* nAChR with Novel Substituted Carbamoyl/Amido/Heteroaryl Dialkylpiperazinium Salts and Their Therapeutic Implications in Pain and Inflammation J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Hina Andleeb, Roger L. Papke, Clare Stokes, Katrin Richter, Sara M. Herz, Ka Chiang, Siva R. Raju Kanumuri, Abhisheak Sharma, M. Imad Damaj, Veronika Grau, Nicole A. Horenstein, Ganesh A. Thakur
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Identification of Novel Potent NSD2-PWWP1 Ligands Using Structure-Based Design and Computational Approaches J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Luca Carlino, Peter C. Astles, Bryony Ackroyd, Afshan Ahmed, Christina Chan, Gavin W. Collie, Ian L. Dale, Daniel H. O’Donovan, Caroline Fawcett, Paolo di Fruscia, Andrea Gohlke, Xiaoxiao Guo, Jessie Hao-Ru Hsu, Bethany Kaplan, Alexander G. Milbradt, Sarah Northall, Dušan Petrović, Emma L. Rivers, Elizabeth Underwood, Alice Webb
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Two-Photon Photodegradation of E3 Ubiquitin Ligase Cereblon by a Ru(II) Complex: Inducing Ferroptosis in Cisplatin-Resistant Tumor Cells J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Xinlin Lin, Mengsi Zheng, Kai Xiong, Fa Wang, Yu Chen, Liangnian Ji, Hui Chao
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Discovery of Small and Bifunctional Molecules Targeting PD-L1/CD73 for Cancer Dual Immunotherapy J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Shuanghu Wang, Zhihua Kong, Yaru Shi, Chuxiao Shao, Wei Wang, Zhenhong Su, Jin Liu, Yingxing Zhou, Xiaoting Fei, Binbin Cheng, Jianjun Chen, Yiyu Lu, Jian Xiao
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Nonclassical Zwitterions as a Design Principle to Reduce Lipophilicity without Impacting Permeability J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Henrik Möbitz, Birger Dittrich, Stephane Rodde, Ross Strang
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Enhancing Molecular Property Prediction through Task-Oriented Transfer Learning: Integrating Universal Structural Insights and Domain-Specific Knowledge J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Yanjing Duan, Xixi Yang, Xiangxiang Zeng, Wenxuan Wang, Youchao Deng, Dongsheng Cao
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Structure–Activity Relationships toward the Identification of a High-Potency Selective Human Toll-like Receptor-7 Agonist J. Med. Chem. (IF 7.3) Pub Date : 2024-05-13 Deepender Kaushik, Arshpreet Kaur, Madhuri T. Patil, Binita Sihag, Sakshi Piplani, Isaac Sakala, Yoshikazu Honda-Okubo, Saravanan Ramakrishnan, Nikolai Petrovsky, Deepak B. Salunke
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Discovery of Oral AMP-Activated Protein Kinase Activators for Treating Hyperlipidemia J. Med. Chem. (IF 7.3) Pub Date : 2024-05-13 Mingchao Wang, Zunsheng Han, Baoyan Fan, Kai Qu, Wenxuan Zhang, Wei Li, Jingya Li, Li Li, Jin Li, Hui Li, Song Wu, Dongmei Wang, Haibo Zhu
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Discovery of Novel Small-Molecule-Based Potential PD-L1/EGFR Dual Inhibitors with High Druggability for Glioblastoma Immunotherapy J. Med. Chem. (IF 7.3) Pub Date : 2024-05-13 Zichao Yang, Ziqing Liu, Shanhe Wan, Jianwei Xu, Yaqi Huang, Haiqi He, Ting Liu, Ling Li, Yichang Ren, Jiajie Zhang, Jianjun Chen
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Tumor-Targeted Oxaliplatin(IV) Prodrug Delivery Based on ROS-Regulated Cancer-Selective Glycan Labeling J. Med. Chem. (IF 7.3) Pub Date : 2024-05-13 Jiajia Wang, Wei Cao, Wei Zhang, Biao Dou, Xin Ding, Menghe Wang, Jing Ma, Xia Li
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Modular Biomimetic Strategy Enables Discovery and SAR Exploration of Oxime Macrocycles as Influenza A Virus (H1N1) Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-05-12 Dandan Xu, Ying Gong, Lianju Zhang, Fu Xiao, Xinran Wang, Ji Qin, Lin Tan, Teng Yang, Zeng Lin, Zhongliang Xu, Xiujuan Liu, Fuling Xiao, Feili Zhang, Feng Tang, Jianping Zuo, Xiaomin Luo, Wei Huang, Li Yang, Weibo Yang
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Impact of Combinatorial Histone Modifications on Acetyllysine Recognition by the ATAD2 and ATAD2B Bromodomains J. Med. Chem. (IF 7.3) Pub Date : 2024-05-11 Margaret Phillips, Kiera L. Malone, Brian W. Boyle, Cameron Montgomery, Isabelle A. Kressy, Faith M. Joseph, Kathleen M. Bright, Samuel P. Boyson, Sunsik Chang, Jay C. Nix, Nicolas L. Young, Victoria Jeffers, Seth Frietze, Karen C. Glass
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Discovery of Nelutroctiv (CK-136), a Selective Cardiac Troponin Activator for the Treatment of Cardiovascular Diseases Associated with Reduced Cardiac Contractility J. Med. Chem. (IF 7.3) Pub Date : 2024-05-10 Antonio Romero, Luke Ashcraft, Aroop Chandra, Vincent DiMassa, Peadar Cremin, Scott E. Collibee, Chihyuan Chuang, James Hartman, Darren T. Hwee, David St. Jean, Justin Malinowski, Mikkel DeBenedetto, David Moebius, Joshua Payette, Richard Vargas, John Yeoman, Alykhan Motani, Jeffrey Reagan, Fady I. Malik, Bradley P. Morgan
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A β-Carboline Derivate PAD4 Inhibitor Reshapes Neutrophil Phenotype and Improves the Tumor Immune Microenvironment against Triple-Negative Breast Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-05-10 Di Zhu, Yu Lu, Zhanchao Yan, Qian Deng, Bo Hu, Yinsong Wang, Wenjing Wang, Yanming Wang, Yuji Wang
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Glycyrrhetinic Acid as a Hepatocyte Targeting Ligand-Functionalized Platinum(IV) Complexes for Hepatocellular Carcinoma Therapy and Overcoming Multidrug Resistance J. Med. Chem. (IF 7.3) Pub Date : 2024-05-10 Xiaochao Huang, Guimei Li, Huifang Li, Wentian Zhong, Guiyang Jiang, Jinyuan Cai, Qingping Xiong, Chuang Wu, Kangning Su, Rizhen Huang, Shiliu Xu, Zhikun Liu, Meng Wang, Hengshan Wang
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Discovery of LLC355 as an Autophagy-Tethering Compound for the Degradation of Discoidin Domain Receptor 1 J. Med. Chem. (IF 7.3) Pub Date : 2024-05-10 Lianchao Liu, Lijie Zhao, Lujun Yang, Minxue Chai, Zhengyong Liu, Nan Ma, Yongxing Wang, Qinxue Wu, Jing Guo, Fengtao Zhou, Weixue Huang, Xiaomei Ren, Jian Wang, Ming Ding, Zhen Wang, Ke Ding
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Discovery of the Clinical Candidate IDOR-1117-2520: A Potent and Selective Antagonist of CCR6 for Autoimmune Diseases J. Med. Chem. (IF 7.3) Pub Date : 2024-05-10 Emmanuel A. Meyer, Andrew L. Croxford, Carmela Gnerre, Paulina Kulig, Mark J. Murphy, Elise M. Jacob, Gabriel Schäfer, Sylvia Richard-Bildstein, Hamed Aissaoui, Patrick Bouis, Eric A. Ertel, Ruben de Kanter, Marcel P. Keller, Urs Lüthi, Eva Caroff
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Ligandability Assessment of IL-1β by Integrated Hit Identification Approaches J. Med. Chem. (IF 7.3) Pub Date : 2024-05-10 Anna Vulpetti, Jean-Michel Rondeau, Marie-Hélène Bellance, Jutta Blank, Ralf Boesch, Andreas Boettcher, Frédéric Bornancin, Sylvia Buhr, Lauren E. Connor, Christoph E. Dumelin, Oliver Esser, Michael Hediger, Samuel Hintermann, Ulrich Hommel, Elke Koch, Guillaume Lapointe, Lukas Leder, Sylvie Lehmann, Philipp Lehr, Peter Meier, Lionel Muller, Daniela Ostermeier, Paul Ramage, Sihame Schiebel-Haddad,
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Rational Design and Pharmacomodulation of 18F-Labeled Biotin/FAPI-Conjugated Heterodimers J. Med. Chem. (IF 7.3) Pub Date : 2024-05-10 Xuedong Chen, Dongsheng Xia, Xueyuan Zeng, Lingxin Meng, Yanjie Wang, Huifeng Li, Jingru Zhang, Zuoquan Zhao, Rongqiang Zhuang, Jianyang Fang, Xianzhong Zhang, Zhide Guo
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Discovery of LC-MI-3: A Potent and Orally Bioavailable Degrader of Interleukin-1 Receptor-Associated Kinase 4 for the Treatment of Inflammatory Diseases J. Med. Chem. (IF 7.3) Pub Date : 2024-05-09 Lingfeng Chen, Ruixiang Luo, Lin Ma, Ying Xu, Jiaqi Cao, Zheng Jiang, Shiyan Chen, Xiaohao Huang, Mingwan Zhang, Lei Zheng, Yawen Zhang, Lina Yin, Jie Yu, Xiaochun Zheng, Lulu Zheng, Ping Huang, Guang Liang
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Design of FK866-Based Degraders for Blocking the Nonenzymatic Functions of Nicotinamide Phosphoribosyltransferase J. Med. Chem. (IF 7.3) Pub Date : 2024-05-09 Tiangong Lu, Fangfang Chen, Jian Yao, Zixuan Bu, Armita Kyani, Benji Liang, Shaoting Chen, Yuxiang Zheng, Hong Liang, Nouri Neamati, Yanghan Liu
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Discovery and Optimization of Tambjamines as a Novel Class of Antileishmanial Agents J. Med. Chem. (IF 7.3) Pub Date : 2024-05-09 Papireddy Kancharla, Diana Ortiz, Corinne M. Fargo, Xiaowei Zhang, Yuexin Li, Marco Sanchez, Amrendra Kumar, Monish Yeluguri, Rozalia A. Dodean, Diana Caridha, Michael S. Madejczyk, Monica Martin, Xiannu Jin, Cameron Blount, Ravi Chetree, Kristina Pannone, Hieu T. Dinh, Jesse DeLuca, Martin Evans, Robert Nadeau, Chau Vuong, Susan Leed, William E. Dennis, Norma Roncal, Brandon S. Pybus, Patricia J.
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Identification of 1,3,4-Thiadiazolyl-Containing Thiazolidine-2,4-dione Derivatives as Novel PTP1B Inhibitors with Antidiabetic Activity J. Med. Chem. (IF 7.3) Pub Date : 2024-05-09 Mengyue Li, Huiyun Li, Xiaofeng Min, Jinping Sun, Bingwen Liang, Lei Xu, Jia Li, Shao-Hua Wang, Xuetao Xu
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Selenization of Small Molecule Drugs: A New Player on the Board J. Med. Chem. (IF 7.3) Pub Date : 2024-05-08 Cristina Morán-Serradilla, Daniel Plano, Carmen Sanmartín, Arun K. Sharma
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Exploring the Structural Attributes of Yoda1 for the Development of New-Generation Piezo1 Agonist Yaddle1 as a Vaccine Adjuvant Targeting Optimal T Cell Activation J. Med. Chem. (IF 7.3) Pub Date : 2024-05-08 Sunny Goon, Chinky Shiu Chen Liu, Uddipta Ghosh Dastidar, Barnali Paul, Suravi Mukherjee, Himadri Sekhar Sarkar, Milie Desai, Rituparna Jana, Sourav Pal, Namala Venkata Sreedevi, Dipyaman Ganguly, Arindam Talukdar
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Discovery of Glutamate Carboxypeptidase III Ligands to Compete the Uptake of [177Lu]Lu-PSMA-617 in Healthy Organs J. Med. Chem. (IF 7.3) Pub Date : 2024-05-08 Marco Müller, Laura Lucaroni, Nicholas Favalli, Gabriele Bassi, Dario Neri, Samuele Cazzamalli, Sebastian Oehler
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Synthesis of Heterocyclic Ring-Fused Bisnoralcohol Derivatives as Novel Small-Molecule Antiosteoporosis Agents J. Med. Chem. (IF 7.3) Pub Date : 2024-05-08 De-Jie Zhang, Rong Chen, Yu-Xin Zhang, Chen-Chen Li, Ruo-Nan Ning, Min Jiang, Wen-Wei Qiu
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Construction and Activity Evaluation of Novel Bifunctional Inhibitors and a COF Carrier Based on a Fungal Infection Microenvironment J. Med. Chem. (IF 7.3) Pub Date : 2024-05-08 Shuai Yu, Yan-Qin He, Yating Liu, Shilei Ji, Yajing Wang, Bin Sun
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Rational Design and Comparison of Novel 99mTc-Labeled FAPI Dimers for Visualization of Multiple Tumor Types J. Med. Chem. (IF 7.3) Pub Date : 2024-05-08 Lingxin Meng, Jianyang Fang, Jingru Zhang, Huifeng Li, Dongsheng Xia, Rongqiang Zhuang, Haojun Chen, Jinxiong Huang, Yesen Li, Xianzhong Zhang, Zhide Guo
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A CARM1 Inhibitor Potently Suppresses Breast Cancer Both In Vitro and In Vivo J. Med. Chem. (IF 7.3) Pub Date : 2024-05-07 Bing-ling Peng, Ting Ran, Xue Chen, Jian-cheng Ding, Zi-rui Wang, Wen-juan Li, Wen Liu
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Development of Inhibitors, Probes, and PROTAC Provides a Complete Toolbox to Study PARK7 in the Living Cell J. Med. Chem. (IF 7.3) Pub Date : 2024-05-07 Yuqing Jia, Merve Oyken, Robbert Q. Kim, Rayman T.N. Tjokrodirijo, Arnoud H. de Ru, Antonius P. A. Janssen, Stephan M. Hacker, Peter A. van Veelen, Paul P. Geurink, Aysegul Sapmaz
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Brain-Penetrant Macrocycles: Design Considerations, Future Prospects, and Call for Papers J. Med. Chem. (IF 7.3) Pub Date : 2024-05-07 Cori A. Malinky, Aaron M. Bender
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Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update J. Med. Chem. (IF 7.3) Pub Date : 2024-05-06 Laura Hillebrand, Xiaojun Julia Liang, Ricardo A. M. Serafim, Matthias Gehringer
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Antitumor Activity and Mechanistic Insights of a Mitochondria-Targeting Cu(I) Complex J. Med. Chem. (IF 7.3) Pub Date : 2024-05-06 Siyu Xu, Yashuai Hao, Xinyi Xu, Lu Huang, Yuqiong Liang, Jia Liao, Jie-Ru Yang, Yang Zhou, Mingdong Huang, Ke-Zhao Du, Cen Zhang, Peng Xu
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Discovery of 2,6-Naphthyridine Analogues as Selective FGFR4 Inhibitors for Hepatocellular Carcinoma J. Med. Chem. (IF 7.3) Pub Date : 2024-05-05 Heesook Oh, Jisook Kim, Seung Hyun Jung, Tae Hee Ha, Young Gil Ahn, Gibeom Nam, Kyeongwon Moon, Pargat Singh, In Su Kim
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Discovery of BIO-8169─A Highly Potent, Selective, and Brain-Penetrant IRAK4 Inhibitor for the Treatment of Neuroinflammation J. Med. Chem. (IF 7.3) Pub Date : 2024-05-02 Magnus Pfaffenbach, Philippe N. Bolduc, Zhili Xin, Fang Gao, Ryan Evans, Terry Fang, Jayanth V. Chodaparambil, Kate L. Henry, Pei Li, Steven Mathieu, Claire Metrick, Jorge A. Vera Rebollar, Rong-Fang Gu, Christie-Ann Mccarl, John Silbereis, Emily A. Peterson
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Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis J. Med. Chem. (IF 7.3) Pub Date : 2024-05-07 Martin K. Himmelbauer, Bekim Bajrami, Rebecca Basile, Andrew Capacci, TeYu Chen, Colin K. Choi, Rab Gilfillan, Felix Gonzalez-Lopez de Turiso, Chungang Gu, Marc Hoemberger, Douglas S. Johnson, J. Howard Jones, Ekta Kadakia, Melissa Kirkland, Edward Y. Lin, Ying Liu, Bin Ma, Tom Magee, Srinivasa Mantena, Isaac E. Marx, Claire M. Metrick, Michael Mingueneau, Paramasivam Murugan, Cathy A. Muste, Prasad
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Design, Synthesis, Bioactive Evaluation, and Molecular Dynamics Simulation of Novel 4H-Pyrano[3,2-c]pyridine Analogues as Potential Sterol 14α-Demethylase (CYP51) Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-05-04 Ailing Bao, Wenjing Jiang, Xiansong Xie, Deyuan Wang, Ziquan Deng, Jingwen Wang, Weiyi Li, Xiaorong Tang, Yingkun Yan
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Triazoles in Medicinal Chemistry: Physicochemical Properties, Bioisosterism, and Application J. Med. Chem. (IF 7.3) Pub Date : 2024-05-03 Qianwen Guan, Shuaishuai Xing, Lei Wang, Jiawei Zhu, Can Guo, Chunlei Xu, Qun Zhao, Yulan Wu, Yao Chen, Haopeng Sun
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Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2 J. Med. Chem. (IF 7.3) Pub Date : 2024-05-02 Yunhang Guo, Hai Xue, Nan Hu, Ye Liu, Hanzi Sun, Desheng Yu, Ling Qin, Gongyin Shi, Fan Wang, Lei Xin, Weihua Sun, Fan Zhang, Xiaomin Song, Shuran Li, Qiang Wei, Ying Guo, Yong Li, Xiaoxin Liu, Shuaishuai Chen, Taichang Zhang, Yue Wu, Dan Su, Yutong Zhu, Aiying Xu, Haipeng Xu, Shasha Yang, Zhijun Zheng, Junhua Liu, Xuefei Yang, Xi Yuan, Yuan Hong, Xuebing Sun, Yin Guo, Changyou Zhou, Xuesong Liu, Lai
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Histidine-Covalent Stapled Alpha-Helical Peptides Targeting hMcl-1 J. Med. Chem. (IF 7.3) Pub Date : 2024-05-02 Giulia Alboreggia, Parima Udompholkul, Carlo Baggio, Kendall Muzzarelli, Zahra Assar, Maurizio Pellecchia
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Discovery of a Novel and Potent Cyclin-Dependent Kinase 8/19 (CDK8/19) Inhibitor for the Treatment of Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Jianyu Xu, Hongyun Qi, Zhen Wang, Ling Wang, Barbara Steurer, Xin Cai, Jinxin Liu, Alex Aliper, Man Zhang, Feng Ren, Alex Zhavoronkov, Xiao Ding
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Novel Inhibitory Site Revealed by XAP044 Mode of Action on the Metabotropic Glutamate 7 Receptor Venus Flytrap Domain J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Nunzia Cristiano, Alexandre Cabayé, Isabelle Brabet, Ralf Glatthar, Amelie Tora, Cyril Goudet, Hugues-Olivier Bertrand, Anne Goupil-Lamy, Peter J. Flor, Jean-Philippe Pin, Isabelle McCort-Tranchepain, Francine C. Acher
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[52Mn]Mn-BPPA-Trastuzumab: A Promising HER2-Specific PET Radiotracer J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Ngô Minh Toàn, Adrienn Vágner, Gábor Nagy, Gábor Ország, Tamás Nagy, Csaba Csikos, Balázs Váradi, Gergő Zoltán Sajtos, István Kapus, Zoltán Szoboszlai, Dezső Szikra, György Trencsényi, Gyula Tircsó, Ildikó Garai
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A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19 J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Charlotte M. N. Allerton, Joel T. Arcari, Lisa M. Aschenbrenner, Melissa Avery, Bruce M. Bechle, Mohammad Amin Behzadi, Britton Boras, Leanne M. Buzon, Rhonda D. Cardin, Natasha R. Catlin, Anthony A. Carlo, Karen J. Coffman, Alyssa Dantonio, Li Di, Heather Eng, Kathleen A. Farley, Rose Ann Ferre, Steven S. Gernhardt, Scott A. Gibson, Samantha E. Greasley, Siennah R. Greenfield, Brett L. Hurst, Amit
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New Improved cGMP Analogues to Target Rod Photoreceptor Degeneration J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Oswaldo Pérez, Agnese Stanzani, Li Huang, Nicolaas Schipper, Thorsteinn Loftsson, Martin Bollmark, Valeria Marigo
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Differential Bioactivation Profiles of Different GS-441524 Prodrugs in Cell and Mouse Models: ProTide Prodrugs with High Cell Permeability and Susceptibility to Cathepsin A Are More Efficient in Delivering Antiviral Active Metabolites to the Lung J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Jiapeng Li, Daniel Macedo de Melo Jorge, Weiwen Wang, Shuxin Sun, Tristan Frum, Yu-An Hang, Yueting Liu, Xingwu Zhou, Jingcheng Xiao, Xinwen Wang, Jason R. Spence, Christiane E. Wobus, Hao-Jie Zhu
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Discovery of Selective Proteolysis-Targeting Chimera Degraders Targeting PTP1B as Long-Term Hypoglycemic Agents J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Zunhua Yang, Yuqi Ying, Shaobing Cheng, Jiamin Wu, Ziwei Zhang, Pei Hu, Jian Xiong, Huilan Li, Qing Zeng, Zhifang Cai, Yulin Feng, Yuanying Fang
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Illuminating Dark Chemical Matter Using the Cell Painting Assay J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Axel Pahl, Jie Liu, Sohan Patil, Soheila Rezaei Adariani, Beate Schölermann, Jens Warmers, Jana Bonowski, Sandra Koska, Yasemin Akbulut, Carina Seitz, Sonja Sievers, Slava Ziegler, Herbert Waldmann
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Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Lianchao Liu, Abhijit Parolia, Yihan Liu, Caiyun Hou, Tongchen He, Yuanyuan Qiao, Sanjana Eyunni, Jie Luo, Chungen Li, Yongxing Wang, Fengtao Zhou, Weixue Huang, Xiaomei Ren, Zhen Wang, Arul M. Chinnaiyan, Ke Ding
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Discovery of a New Anti-Inflammatory Agent from Anemoside B4 Derivatives and Its Therapeutic Effect on Colitis by Targeting Pyruvate Carboxylase J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Lijuan Lv, Qiurong Li, Kexin Wang, Jianping Zhao, Kejun Deng, Ran Zhang, Zhong Chen, Ikhlas A. Khan, Chunshan Gui, Suxiang Feng, Shilin Yang, Yanli Liu, Qiongming Xu
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A Nonbactericidal Anionic Antimicrobial Peptide Provides Prophylactic and Therapeutic Efficacies against Bacterial Infections in Mice by Immunomodulatory–Antithrombotic Duality J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Yanmei He, Shimei Ruan, Guozhu Liang, Jing Hao, Xiaoyan Zhou, Zhuorui Li, Lixian Mu, Jing Wu, Hailong Yang
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Novel Isoalantolactone-Based Derivatives as Potent NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Min Zhao, Neng Ye, Ling Liu, Rui-Jia Zhang, Na Li, Jing Peng, Xiao-Ying Cai, Xue-Qin Jiang, Kai-Yue Su, Xin-Lu Zhang, Qian-Ru Rao, Kong-Jun Liu, De-Xin Deng, Ai-Hua Peng, Ming-Hai Tang, Li-Juan Chen, Wen-Shuang Wu, Hao-Yu Ye
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Discovery of Potent Multikinase Type-II Inhibitors Targeting CDK5 in the DFG-out Inactive State with Promising Potential against Glioblastoma J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Zahra R. Khan, Philip J. Welsby, Izabela Stasik, Joseph M. Hayes
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Multitarget μ-Opioid Receptor Agonists─Neuropeptide FF Receptor Antagonists Induce Potent Antinociception with Reduced Adverse Side Effects J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Jolien De Neve, Khadija Elhabazi, Simon Gonzalez, Claire Herby, Séverine Schneider, Valérie Utard, Rosine Fellmann-Clauss, Nathalie Petit-Demouliere, Sandra Lecat, Mélanie Kremer, Aurelia Ces, François Daubeuf, Charlotte Martin, Steven Ballet, Frédéric Bihel, Frédéric Simonin
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Concurrent Optimizations of Efficacy and Blood–Brain Barrier Permeability in New Macrocyclic LRRK2 Inhibitors for Potential Parkinson’s Disease Therapeutics J. Med. Chem. (IF 7.3) Pub Date : 2024-04-29 Kewon Kim, Ahyoung Jang, Hochul Shin, Inhae Ye, Ji Eun Lee, Taeho Kim, Hwangseo Park, Sungwoo Hong
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Exploring Subsite Selectivity within Plasmodium vivax N-Myristoyltransferase Using Pyrazole-Derived Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-04-29 Diego Rodríguez-Hernández, Michael K. Fenwick, Rachael Zigweid, Banumathi Sankaran, Peter J. Myler, Per Sunnerhagen, Alexis Kaushansky, Bart L. Staker, Morten Grøtli
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Identification of Potent and Selective Inhibitors of Acanthamoeba: Structural Insights into Sterol 14α-Demethylase as a Key Drug Target J. Med. Chem. (IF 7.3) Pub Date : 2024-04-29 Tatiana Y. Hargrove, David C. Lamb, Zdzislaw Wawrzak, Marcus Hull, Steven L. Kelly, F. Peter Guengerich, Galina I. Lepesheva