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Identification and Biological Evaluation of a Potent and Selective JAK1 Inhibitor for the Treatment of Pulmonary Fibrosis J. Med. Chem. (IF 7.3) Pub Date : 2023-11-30 Eunsun Park, Seolhee Park, Sun Joo Lee, Dayeon Jeong, Hee Jin, Heegyum Moon, Boksik Cha, Dayea Kim, Seonghee Ma, Wonhyo Seo, Seung-Hee Han, Yun-Sil Lee, Soosung Kang
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Arthur A. Patchett Memorial Issue J. Med. Chem. (IF 7.3) Pub Date : 2023-11-30 Matthew Wyvratt, William Greenlee
Arthur A. Patchett was born in Middletown, New York, on May 28, 1929. After graduating from Middletown High School as the class valedictorian, Art continued his education at Princeton University, first as an English major (as he would frequently point out to his co-authors) before he changed his major to chemistry. Art graduated summa cum laude from Princeton University in 1951 and was a Fulbright
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Trehalose-Bearing Carriers to Target Impaired Autophagy and Protein Aggregation Diseases J. Med. Chem. (IF 7.3) Pub Date : 2023-11-29 Ali Maruf, Małgorzata Milewska, Máté Varga, Ilona Wandzik
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Structure–Interaction Relationship of Polymyxins with Lung Surfactant J. Med. Chem. (IF 7.3) Pub Date : 2023-11-29 Xukai Jiang, Nitin A. Patil, Yuwen Xu, Hasini Wickremasinghe, Qi Tony Zhou, Fanfan Zhou, Philip E. Thompson, Lushan Wang, Min Xiao, Kade D. Roberts, Tony Velkov, Jian Li
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Discovery of Novel 2,3-Dihydro-1H-indene-5-sulfonamide NLRP3 Inflammasome Inhibitors Targeting Colon as a Potential Therapy for Colitis J. Med. Chem. (IF 7.3) Pub Date : 2023-11-29 Simin Sun, Zhuoyue Li, Chao Huang, Jinyu Liu, Qixin Yu, Xiaolin Jiang, Kairui Yue, Jianchun Zhao, Tongqiang Xu, Yankai Liu, Xiaoyang Li, Chong Qin, Yuqi Jiang
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Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer J. Med. Chem. (IF 7.3) Pub Date : 2023-11-29 Xufen Yu, Dongxu Li, Jithesh Kottur, Huen Suk Kim, Laura E. Herring, Yao Yu, Ling Xie, Xiaoping Hu, Xian Chen, Ling Cai, Jing Liu, Aneel K. Aggarwal, Gang Greg Wang, Jian Jin
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Free Energy Perturbation Approach for Accurate Crystalline Aqueous Solubility Predictions J. Med. Chem. (IF 7.3) Pub Date : 2023-11-28 Richard S. Hong, Ana V. Rojas, Rajni Miglani Bhardwaj, Lingle Wang, Alessandra Mattei, Nathan S. Abraham, Kevin P. Cusack, M. Olivia Pierce, Sayan Mondal, Nada Mehio, Shailendra Bordawekar, Philip R. Kym, Robert Abel, Ahmad Y. Sheikh
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Peptide TK-HR from the Skin of Chinese Folk Medicine Frog Hoplobatrachus Rugulosus Accelerates Wound Healing via the Activation of the Neurokinin-1 Receptor J. Med. Chem. (IF 7.3) Pub Date : 2023-11-28 Jiena Wu, Weichen Xiong, Jinqiao Li, Hang Liao, Jinwei Chai, Xiaowen Huang, Shian Lai, Sergey Kozlov, Xinwei Chu, Xueqing Xu
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A Novel Bifunctional μOR Agonist and σ1R Antagonist with Potent Analgesic Responses and Reduced Adverse Effects J. Med. Chem. (IF 7.3) Pub Date : 2023-11-28 Zhuang Miao, Yuhan Zhong, Yu Gan, Kequan Fu, Wencheng Liu, Zhihua Cao, Tiantian Zhao, Ziyuan Li, Ao Hai, Yanlai Peng, Zeping Zuo, Tian Zhang, Shilong Hu, Chunxia Chen, Ting Kang, Tianguang Huang, Dong Guo, Bowen Ke
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Discovery of Amino Alcohols as Highly Potent, Selective, and Orally Efficacious Inhibitors of Leukotriene A4 Hydrolase J. Med. Chem. (IF 7.3) Pub Date : 2023-11-28 Gebhard Thoma, Christian Markert, Rainer Lueoend, Wolfgang Miltz, Carsten Spanka, Birgit Bollbuck, Romain M. Wolf, Honnappa Srinivas, Carlos A. Penno, Michael Kiffe, Monika Gajewska, Dallas Bednarczyk, Grazyna Wieczorek, Amanda Evans, Christian Beerli, Till A. Röhn
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Identification of Small Molecule Inhibitors and Ligand Directed Degraders of Calcium/Calmodulin Dependent Protein Kinase Kinase 1 and 2 (CaMKK1/2) J. Med. Chem. (IF 7.3) Pub Date : 2023-11-27 Young Chen, Brandon Whitefield, Erin Nevius, Mark Hill, Joselyn DelRosario, Nadia Sinitsyna, Veerabahu Shanmugasundaram, Debarati Mukherjee, Lihong Shi, Christopher Glenn Mayne, Anne-Marie Rousseau, Steffen M. Bernard, Jennifer Buenviaje, Gody Khambatta, Miriam El Samin, Michael Wallace, Zhe Nie, Pallavur Sivakumar, Lawrence G. Hamann, Donald P. McDonnell, Laura Akullian D’Agostino
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Design, Synthesis, Electrochemical, and Biological Evaluation of Fluorescent Chlorido[N,N′-bis(methoxy/hydroxy)salicylidene-1,2-bis(4-methoxyphenyl)ethylenediamine]iron(III) Complexes as Anticancer Agents J. Med. Chem. (IF 7.3) Pub Date : 2023-11-27 Astrid Dagmar Bernkop-Schnürch, Donja Chavooshi, Hubert Aaron Descher, Daniel Leitner, Heribert Talasz, Martin Hermann, Klaus Wurst, Stephan Hohloch, Ronald Gust, Brigitte Kircher
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Discovery of New Broad-Spectrum Anti-Infectives for Eukaryotic Pathogens Using Bioorganometallic Chemistry J. Med. Chem. (IF 7.3) Pub Date : 2023-11-27 Yan Lin, Hyeim Jung, Christina A. Bulman, James Ng, Robin Vinck, Cillian O’Beirne, Shuai Zhong, Matthew S. Moser, Nancy Tricoche, Ricardo Peguero, Robert W. Li, Joseph F. Urban, Jr., Patrice Le Pape, Fabrice Pagniez, Marco Moretto, Tobias Weil, Sara Lustigman, Kevin Cariou, Makedonka Mitreva, Judy A. Sakanari, Gilles Gasser
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Exploiting the “Hot-Spots” of Hsp70–Bim Protein–Protein Interaction to Optimize the 1-Oxo-1H-phenalene-2,3-dicarbonitrile Analogues as Specific Hsp70–Bim Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2023-11-27 Ziqian Wang, Hong Zhang, Xin Li, Yang Song, Yuying Wang, Zhiyuan Hu, Qishuang Gao, Maojun Jiang, Fangkui Yin, Linjie Yuan, Jingjing Liu, Ting Song, Shaohua Lu, Guanghong Xu, Zhichao Zhang
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Discovery of a Dual Tubulin and Neuropilin-1 (NRP1) Inhibitor with Potent In Vivo Anti-Tumor Activity via Pharmacophore-based Docking Screening, Structure Optimization, and Biological Evaluation J. Med. Chem. (IF 7.3) Pub Date : 2023-11-24 Lufeng Zheng, Yunting Zou, Tianyuan Xie, Xiuyuan Wu, Yuchen Tan, Shuang Mei, Yifei Geng, Shutong Chen, Shengtao Xu, Miao-Miao Niu
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Discovery of a First-in-Class Small-Molecule Ligand for WDR91 Using DNA-Encoded Chemical Library Selection Followed by Machine Learning J. Med. Chem. (IF 7.3) Pub Date : 2023-11-23 Shabbir Ahmad, Jin Xu, Jianwen A. Feng, Ashley Hutchinson, Hong Zeng, Pegah Ghiabi, Aiping Dong, Paolo A. Centrella, Matthew A. Clark, Marie-Aude Guié, John P. Guilinger, Anthony D. Keefe, Ying Zhang, Thomas Cerruti, John W. Cuozzo, Moritz von Rechenberg, Albina Bolotokova, Yanjun Li, Peter Loppnau, Alma Seitova, Yen-Yen Li, Vijayaratnam Santhakumar, Peter J. Brown, Suzanne Ackloo, Levon Halabelian
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Identification of LY3522348: A Highly Selective and Orally Efficacious Ketohexokinase Inhibitor J. Med. Chem. (IF 7.3) Pub Date : 2023-11-22 Timothy B. Durham, Junliang Hao, Patrick Spinazze, Douglas R. Stack, James L. Toth, Steven Massey, Curren T. Mbofana, Richard D. Johnston, Jayana P. Lineswala, Aaron Wrobleski, Jose Miguel Mínguez, Carlos Perez, Daryl L. Smith, Jason Lamar, Rebecca Leon, Christopher Corkins, Jim Durbin, Frances Tung, Sherry Guo, Ryan J. Linder, Nathan Yumibe, Wei Wang, James MacKrell, Meghan Antonellis, Bethany Mascaro
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1,4-Benzothiazepines with Cyclopropanol Groups and Their Structural Analogues Exhibit Both RyR2-Stabilizing and SERCA2a-Stimulating Activities J. Med. Chem. (IF 7.3) Pub Date : 2023-11-22 Gyuzel Y. Mitronova, Christine Quentin, Vladimir N. Belov, Jörg W. Wegener, Kamila A. Kiszka, Stephan E. Lehnart
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Design, Synthesis, and Biological Evaluation of Trisubstituted Piperazine Derivatives as Noncovalent Severe Acute Respiratory Syndrome Coronavirus 2 Main Protease Inhibitors with Improved Antiviral Activity and Favorable Druggability J. Med. Chem. (IF 7.3) Pub Date : 2023-11-22 Shenghua Gao, Letian Song, Katharina Sylvester, Beatrice Mercorelli, Arianna Loregian, Karoly Toth, Renato H. Weiße, Abibe Useini, Norbert Sträter, Mianling Yang, Bing Ye, Ann E. Tollefson, Christa E. Müller, Xinyong Liu, Peng Zhan
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Design, Synthesis, and Pharmacological Evaluation of Isoindoline Analogues as New HPK1 Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2023-11-22 Chenghu Xie, Bo Liu, Zilan Song, Ye Yang, Mengdi Dai, Yinglei Gao, Yujia Yao, Chunyong Ding, Jing Ai, Ao Zhang
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Spiropiperidine-Based Oligomycin-Analog Ligands To Counteract the Ischemia–Reperfusion Injury in a Renal Cell Model J. Med. Chem. (IF 7.3) Pub Date : 2023-11-22 Giulia Turrin, Ettore Lo Cascio, Noah Giacon, Anna Fantinati, Virginia Cristofori, Davide Illuminati, Delia Preti, Giampaolo Morciano, Paolo Pinton, Esther Densu Agyapong, Claudio Trapella, Alessandro Arcovito
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Design and Synthesis of Novel Cereblon Binders for Use in Targeted Protein Degradation J. Med. Chem. (IF 7.3) Pub Date : 2023-11-22 Stephen Norris, Xiaochu Ba, Jayce Rhodes, Dehua Huang, Gody Khambatta, Jennifer Buenviaje, Surendra Nayak, Joseph Meiring, Samantha Reiss, Shuichan Xu, Lihong Shi, Brandon Whitefield, Matt Alexander, Evan J. Horn, Matthew Correa, Lida Tehrani, Joshua D. Hansen, Patrick Papa, Deborah S. Mortensen
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Novel Psilocin Prodrugs with Altered Pharmacological Properties as Candidate Therapies for Treatment-Resistant Anxiety Disorders J. Med. Chem. (IF 7.3) Pub Date : 2023-11-20 Sheetal A. Raithatha, Jillian M. Hagel, Kaveh Matinkhoo, Lisa Yu, David Press, Sarah G. Cook, Govinda Sharma, D. Dhananjaya, Glynnis Jensen, Jessica B. Lee, Charlie Cai, Jonathan Gallant, Jaideep Bains, Joseph E. Tucker, Peter J. Facchini
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Cyclic Peptides as Aggregation Inhibitors for Sickle Cell Disease J. Med. Chem. (IF 7.3) Pub Date : 2023-11-21 Vasco Neto, Bruno Lourenço Victor, Nuno Galamba
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Imidazolone as an Amide Bioisostere in the Development of β-1,3-N-Acetylglucosaminyltransferase 2 (B3GNT2) Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2023-11-21 Jeffrey J. Jackson, Aaron C. Siegmund, Wen-Ju Bai, Anthony B. Reed, Adam B. Birkholz, Iain D. G. Campuzano, Amandine Créquer-Grandhomme, Ruozhen Hu, Rucha V. Modak, Athena Sudom, Noelle Javier, Christiana Sanders, Mei-Chu Lo, Fang Xie, Victor J. Cee, Paolo Manzanillo, John G. Allen
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Optimization of Novel α7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulators and the Discovery of a Preclinical Development Candidate Molecule (RGH-560) J. Med. Chem. (IF 7.3) Pub Date : 2023-11-21 István Ledneczki, Zsolt Némethy, Katalin Dudásné Molnár, Pál Tapolcsányi, Viktor Ilkei, István Vágó, Sándor Kolok, Márta Thán, Judit Laszy, Ottilia Balázs, Balázs Krámos, Áron Szigetvári, Imre Bata, Attila Makó, András Visegrády, László Fodor, Mónika Vastag, György Lévay, Balázs Lendvai, István Greiner, János Éles
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New Genetically Engineered Derivatives of Antibacterial Darobactins Underpin Their Potential for Antibiotic Development J. Med. Chem. (IF 7.3) Pub Date : 2023-11-21 Carsten E. Seyfert, Alison V. Müller, Danica J. Walsh, Joy Birkelbach, Andreas M. Kany, Christoph Porten, Biao Yuan, Daniel Krug, Jennifer Herrmann, Thomas C. Marlovits, Anna K. H. Hirsch, Rolf Müller
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Adapting to the Changing Landscape of Biotech-Driven Drug Discovery J. Med. Chem. (IF 7.3) Pub Date : 2023-11-21 Dean G. Brown
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Discovery of New Fusobacterium nucleatum Inhibitors to Attenuate Migratory Capability of Colon Cancer Cells by the Drug Repositioning Strategy J. Med. Chem. (IF 7.3) Pub Date : 2023-11-20 Zhizhi Pan, Chenchen Zhou, Xuexin Bai, Fangfang Wang, Jie Hong, Jing-Yuan Fang, Yahui Huang, Chunquan Sheng
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Discovery and Evaluation of C6-Substituted Pyrazolopyrimidine-Based Bisphosphonate Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase and Evaluation of Their Antitumor Efficacy in Multiple Myeloma, Pancreatic Ductal Adenocarcinoma, and Colorectal Cancer J. Med. Chem. (IF 7.3) Pub Date : 2023-11-20 Rebecca Boutin, Hiu-Fung Lee, Tian Lai Guan, Tan Trieu Nguyen, Xian Fang Huang, Daniel D. Waller, Jordan Lu, Iok In Christine Chio, René P. Michel, Michael Sebag, Youla S. Tsantrizos
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Discovery of 5-(Pyrimidin-2-ylamino)-1H-indole-2-carboxamide Derivatives as Nur77 Modulators with Selective and Potent Activity Against Triple-Negative Breast Cancer J. Med. Chem. (IF 7.3) Pub Date : 2023-11-20 Jingbo Qin, Boning Niu, Xiaohui Chen, Cheng Hu, Sheng Lu, Hongsheng Li, Weihao Liu, Jiayi Li, Zihao Teng, Yinghuang Yang, Hongyu Hu, Yang Xu, Shuaidong Huo, Zhen Wu, Yingkun Qiu, Hu Zhou, Meijuan Fang
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Discovery of Pyrazolo[1,5-a]pyrimidine Derivative as a Novel and Selective ALKBH5 Inhibitor for the Treatment of AML J. Med. Chem. (IF 7.3) Pub Date : 2023-11-20 Ying-Zhe Wang, Hong-Yu Li, Yan Zhang, Rui-Xin Jiang, Jun Xu, Jing Gu, Zheng Jiang, Zheng-Yu Jiang, Qi-Dong You, Xiao-Ke Guo
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Discovery of Biaryl Amide Derivatives as Potent, Selective, and Orally Bioavailable RORγt Agonists for Cancer Immunotherapy J. Med. Chem. (IF 7.3) Pub Date : 2023-11-20 Lixue Lu, Yafei Huang, Meiqi Song, Nannan Sun, Li Xia, Mingcheng Yu, Meiling Zhao, Ruomeng Qiu, Ji-an Chen, Yunpeng Zhao, Haojie Wang, Huimin Guo, Yan Li, Di Zhu, Yonghui Wang, Qiong Xie
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Synthesis and Biological Evaluation of Enantiomerically Pure (R)- and (S)-[18F]OF-NB1 for Imaging the GluN2B Subunit-Containing NMDA Receptors J. Med. Chem. (IF 7.3) Pub Date : 2023-11-18 Marvin Korff, Ahmad Chaudhary, Yinlong Li, Xin Zhou, Chunyu Zhao, Jian Rong, Jiahui Chen, Zhiwei Xiao, Nehal H. Elghazawy, Wolfgang Sippl, April T. Davenport, James B. Daunais, Lu Wang, Carmen Abate, Hazem Ahmed, Ron Crowe, Thomas J. Schmidt, Steven H. Liang, Simon M. Ametamey, Bernhard Wünsch, Ahmed Haider
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3-Hydroxypyridin-4(1H)-one Derivatives as pqs Quorum Sensing Inhibitors Attenuate Virulence and Reduce Antibiotic Resistance in Pseudomonas aeruginosa J. Med. Chem. (IF 7.3) Pub Date : 2023-11-18 Zhi-Ying Miao, Xiao-Yi Zhang, Ming-Han Yang, Yong-Jun Huang, Jing Lin, Wei-Min Chen
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Beware the Receptor Variants J. Med. Chem. (IF 7.3) Pub Date : 2023-11-17 Julien Hanson
The MAS-related genes (also known as MRGPRs) are a complex family of G protein-coupled receptors initially discovered in sensory neurons. Most of them are orphans, which means that they have no known validated endogenous ligands. Although MRGPRs bear great potential as drug targets, notably in itch and nociception, their study has been hampered by the scarcity or absence of potent and selective ligands
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Discovery of Novel 8-Hydroxyquinoline Derivatives with Potent In Vitro and In Vivo Antifungal Activity J. Med. Chem. (IF 7.3) Pub Date : 2023-11-17 Liping Li, Hao Wu, Jiayin Wang, Zhe Ji, Ting Fang, Hui Lu, Lan Yan, Fuming Shen, Dazhi Zhang, Yuanying Jiang, Tingjunhong Ni
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A Celebration of the Publication of the 100th Volume of Organic Syntheses J. Med. Chem. (IF 7.3) Pub Date : 2023-11-17 Margaret M. Faul, Kay M. Brummond
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Development and Pharmacochemical Characterization Discover a Novel Brain-Permeable HDAC11-Selective Inhibitor with Therapeutic Potential by Regulating Neuroinflammation in Mice J. Med. Chem. (IF 7.3) Pub Date : 2023-11-16 Ping Bai, Yan Liu, Liuyue Yang, Weihua Ding, Prasenjit Mondal, Na Sang, Gang Liu, Xiaoxia Lu, Thanh Tu Ho, Yanting Zhou, Rui Wu, Vishal C. Birar, Moses Q. Wilks, Rudolph E. Tanzi, Hening Lin, Can Zhang, Weimin Li, Shiqian Shen, Changning Wang
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Discovery of Efficient Hypoxia-Targeted NO Donor Compounds to Alleviate Hypoxia Cardiac Disease J. Med. Chem. (IF 7.3) Pub Date : 2023-11-16 Wanxiang Yang, Wen Zhou, Shaohua Gou
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An NIR-II Probe with High PSMA Affinity Demonstrates an Unexpected Excellent Bone Imaging Ability J. Med. Chem. (IF 7.3) Pub Date : 2023-11-16 Longfei Zhang, Xiaojing Shi, Yuying Li, Xiaojiang Duan, Xing Yang, Zhenhua Hu, Mengchao Cui
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Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe J. Med. Chem. (IF 7.3) Pub Date : 2023-11-15 Erin Bradley, Lucia Fusani, Chun-wa Chung, Peter D. Craggs, Emmanuel H. Demont, Philip G. Humphreys, Darren J. Mitchell, Alex Phillipou, Inmaculada Rioja, Rishi R. Shah, Christopher R. Wellaway, Rab K. Prinjha, David S. Palmer, William J. Kerr, Marc Reid, Ian D. Wall, Rosa Cookson
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Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers J. Med. Chem. (IF 7.3) Pub Date : 2023-11-15 David B. Freeman, Tamara D. Hopkins, Peter J. Mikochik, Joseph P. Vacca, Hua Gao, Adel Naylor-Olsen, Sonali Rudra, Huixu Li, Marius S. Pop, Rosa A. Villagomez, Christina Lee, Heng Li, Minyun Zhou, Douglas C. Saffran, Nathalie Rioux, Tressa R. Hood, Melinda A. L. Day, Michael R. McKeown, Charles Y. Lin, Norbert Bischofberger, B. Wesley Trotter
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Discovery of Potent Agonists for the Predominant Variant of the Orphan MAS-Related G Protein-Coupled Receptor X4 (MRGPRX4) J. Med. Chem. (IF 7.3) Pub Date : 2023-11-15 Daniel Marx, Mohamed Wessam Alnouri, Sophie Clemens, Robin Gedschold, Yvonne Riedel, Ghazl Al Hamwi, Thanigaimalai Pillaiyar, Jörg Hockemeyer, Vigneshwaran Namasivayam, Christa E. Müller
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Discovery of PVD-06 as a Subtype-Selective and Efficient PTPN2 Degrader J. Med. Chem. (IF 7.3) Pub Date : 2023-11-15 Linghao Hu, Huiyun Li, Junlin Qin, Dan Yang, Jieming Liu, Xiaomin Luo, Jingkun Ma, Cheng Luo, Fei Ye, Yubo Zhou, Jia Li, Mingliang Wang
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Discovery of Orally Bioavailable Phthalazinone Analogues as an ENPP1 Inhibitor for STING-Mediated Cancer Immunotherapy J. Med. Chem. (IF 7.3) Pub Date : 2023-11-14 Yeonguk Cho, Miso Kang, Su Hyun Ji, Hee Jin Jeong, Jae Eun Jung, Do Hee Oh, Sunyoung Park, Yong-Yea Park, Junghwan Choi, Sungjoon Kim, Nam-Jung Kim, Duck-Hyung Lee, Chan Sun Park, Seo-Jung Han, Sanghee Lee, Junwon Choi
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DNA-Functionalized Porphyrinic Metal–Organic Framework-Based Drug Delivery System for Targeted Bimodal Cancer Therapy J. Med. Chem. (IF 7.3) Pub Date : 2023-11-14 Qiu-Ge Zhao, Yun-Jie Zhou, Dong-Xiao Cao, An-Na Tang, De-Ming Kong
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Developing a Hetero-Trinuclear Erbium(III)–Copper(II) Complex Based on Apoferritin: Targeted Photoacoustic Imaging and Multimodality Therapy of Tumor J. Med. Chem. (IF 7.3) Pub Date : 2023-11-13 Minghui Zhu, Xueyu Man, Yang Tongfu, Wenjuan Li, Shanhe Li, Gang Xu, Zhenlei Zhang, Hong Liang, Feng Yang
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Tuning the Organelle-Specific Imaging and Photodynamic Therapeutic Efficacy of Theranostic Mono- and Trinuclear Organometallic Iridium(III) Complexes J. Med. Chem. (IF 7.3) Pub Date : 2023-11-11 Bishnu Das, Subhadeep Gupta, Anushka Mondal, Kalyan Jyoti Kalita, Amirul Islam Mallick, Parna Gupta
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Identification and Optimization of Novel Inhibitors of the Polyketide Synthase 13 Thioesterase Domain with Antitubercular Activity J. Med. Chem. (IF 7.3) Pub Date : 2023-11-10 Simon R. Green, Caroline Wilson, Thomas C. Eadsforth, Avinash S. Punekar, Fabio K. Tamaki, Gavin Wood, Nicola Caldwell, Barbara Forte, Neil R. Norcross, Michael Kiczun, John M. Post, Eva Maria Lopez-Román, Curtis A. Engelhart, Iva Lukac, Fabio Zuccotto, Ola Epemolu, Helena I. M. Boshoff, Dirk Schnappinger, Chris Walpole, Ian H. Gilbert, Kevin D. Read, Paul G. Wyatt, Beatriz Baragaña
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Discovery of tert-Butyl Ester Based 6-Diazo-5-oxo-l-norleucine Prodrugs for Enhanced Metabolic Stability and Tumor Delivery J. Med. Chem. (IF 7.3) Pub Date : 2023-11-10 Kateřina Novotná, Lukáš Tenora, Eva Prchalová, James Paule, Jesse Alt, Vijay Veeravalli, Jenny Lam, Ying Wu, Ivan Šnajdr, Sadakatali Gori, Vijaya Saradhi Mettu, Takashi Tsukamoto, Pavel Majer, Barbara S. Slusher, Rana Rais
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Design, Synthesis, and Biological Evaluation of an Orally Bioavailable, Potent, and Selective ROCK2 Inhibitor for Psoriasis Treatment J. Med. Chem. (IF 7.3) Pub Date : 2023-11-09 Yun Huang, Chu-Ru Mao, Yijie Lou, Shuai Zhan, Zhe Chen, Wanjing Ding, Zhongjun Ma
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Hydrolytic Activity of Mitochondrial F1FO-ATP Synthase as a Target for Myocardial Ischemia–Reperfusion Injury: Discovery and In Vitro and In Vivo Evaluation of Novel Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2023-11-09 Panagiota-Efstathia Nikolaou, George Lambrinidis, Maria Georgiou, Dimitrios Karagiannis, Panagiotis Efentakis, Pavlos Bessis-Lazarou, Konstantina Founta, Stavros Kampoukos, Vasilis Konstantin, Carlos M. Palmeira, Sean M. Davidson, Nikolaos Lougiakis, Panagiotis Marakos, Nicole Pouli, Emmanuel Mikros, Ioanna Andreadou
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Molecular Graph-Based Deep Learning Algorithm Facilitates an Imaging-Based Strategy for Rapid Discovery of Small Molecules Modulating Biomolecular Condensates J. Med. Chem. (IF 7.3) Pub Date : 2023-11-08 Peng Gao, Qi Zhang, Devin Keely, Don W. Cleveland, Yihong Ye, Wei Zheng, Min Shen, Haiyang Yu
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Development of N-Terminally Modified Variants of the CXCR4-Antagonistic Peptide EPI-X4 for Enhanced Plasma Stability J. Med. Chem. (IF 7.3) Pub Date : 2023-11-08 Mirja Harms, Rikke Fabech Hansson, Andrea Gilg, Yasser Almeida-Hernández, Jessica Löffler, Armando Rodríguez-Alfonso, Monica M. W. Habib, Dan Albers, Nermin S. Ahmed, Ashraf H. Abadi, Gordon Winter, Volker Rasche, Ambros J. Beer, Gilbert Weidinger, Nico Preising, Ludger Ständker, Sebastian Wiese, Elsa Sanchez-Garcia, Alexander N. Zelikin, Jan Münch
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Amino Acids as Chelating Ligands for Platinum: Enhanced Stability in an Aqueous Environment Promoted by Biocompatible Molecules J. Med. Chem. (IF 7.3) Pub Date : 2023-11-08 Andrea Cucchiaro, Amelie Scherfler, Davide Corinti, Giel Berden, Jos Oomens, Klaus Wurst, Ronald Gust, Maria Elisa Crestoni, Brigitte Kircher, Monika Cziferszky
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Diester Prodrugs of a Phosphonate Butyrophilin Ligand Display Improved Cell Potency, Plasma Stability, and Payload Internalization J. Med. Chem. (IF 7.3) Pub Date : 2023-11-07 Umed Singh, Girija Pawge, Sarita Rani, Chia-Hung Christine Hsiao, Andrew J. Wiemer, David F. Wiemer
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Integrated Direct-to-Biology Platform for the Nanoscale Synthesis and Biological Evaluation of PROTACs J. Med. Chem. (IF 7.3) Pub Date : 2023-11-07 Rebecca Stevens, Enrique Bendito-Moll, David J. Battersby, Afjal H. Miah, Natalie Wellaway, Robert P. Law, Peter Stacey, Diana Klimaszewska, Justyna M. Macina, Glenn A. Burley, John D. Harling
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Discovery of a Hydroxylamine-Based Brain-Penetrant EGFR Inhibitor for Metastatic Non-Small-Cell Lung Cancer J. Med. Chem. (IF 7.3) Pub Date : 2023-11-07 Jarvis Hill, Robert M. Jones, David Crich
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Herbert Waldmann─Celebrating More than Three Decades in Academia J. Med. Chem. (IF 7.3) Pub Date : 2023-11-07 Voices in Chemical Biology
How has Herbert Waldmann shaped the field of chemical biology over the last three decades? This article has not yet been cited by other publications.
更新日期：2023-11-29
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