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Agonist antibody lowers blood pressure Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-09-23
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The AMR Accelerator: from individual organizations to efficient antibiotic development partnerships Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-09-23 Josepine Fernow, Marie Olliver, William Couet, Sophie Lagrange, Meindert H. Lamers, Ole F. Olesen, Kristina Orrling, Michel Pieren, Derek J. Sloan, Juan José Vaquero, Timothy J. Miles, Anders Karlén
The AMR Accelerator is an Innovative Medicines Initiative programme integrating nine projects with the shared goal of progressing the development of new antibiotics and building antimicrobial resistance research capability. Five years in, we reflect on the programme’s value, results and key challenge: ensuring the sustainability of assets, infrastructures and expertise.
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Post-hospitalisation COVID-19 cognitive deficits at one year are global and associated with elevated brain injury markers and grey matter volume reduction Nat. Med. (IF 58.7) Pub Date : 2024-09-23 Greta K. Wood, Brendan F. Sargent, Zain-Ul-Abideen Ahmad, Kukatharmini Tharmaratnam, Cordelia Dunai, Franklyn N. Egbe, Naomi H. Martin, Bethany Facer, Sophie L. Pendered, Henry C. Rogers, Christopher Hübel, Daniel J. van Wamelen, Richard A. I. Bethlehem, Valentina Giunchiglia, Peter J. Hellyer, William Trender, Gursharan Kalsi, Edward Needham, Ava Easton, Thomas A. Jackson, Colm Cunningham, Rachel
The spectrum, pathophysiology, and recovery trajectory of persistent post-COVID-19 cognitive deficits are unknown, limiting our ability to develop prevention and treatment strategies. We report the one-year cognitive, serum biomarker, and neuroimaging findings from a prospective, national study of cognition in 351 COVID-19 patients who had required hospitalisation, compared to 2,927 normative matched
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Patient attitudes toward the AI doctor Nat. Med. (IF 58.7) Pub Date : 2024-09-23 Aaron Fanous, Kirsten Steffner, Roxana Daneshjou
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Molecular profiling of BRAF-V600E-mutant metastatic colorectal cancer in the phase 3 BEACON CRC trial Nat. Med. (IF 58.7) Pub Date : 2024-09-23 Scott Kopetz, Danielle A. Murphy, Jie Pu, Fortunato Ciardiello, Jayesh Desai, Eric Van Cutsem, Harpreet Singh Wasan, Takayuki Yoshino, Hedieh Saffari, Xiaosong Zhang, Phineas Hamilton, Tao Xie, Rona Yaeger, Josep Tabernero
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A toolbox for surfacing health equity harms and biases in large language models Nat. Med. (IF 58.7) Pub Date : 2024-09-23 Stephen R. Pfohl, Heather Cole-Lewis, Rory Sayres, Darlene Neal, Mercy Asiedu, Awa Dieng, Nenad Tomasev, Qazi Mamunur Rashid, Shekoofeh Azizi, Negar Rostamzadeh, Liam G. McCoy, Leo Anthony Celi, Yun Liu, Mike Schaekermann, Alanna Walton, Alicia Parrish, Chirag Nagpal, Preeti Singh, Akeiylah Dewitt, Philip Mansfield, Sushant Prakash, Katherine Heller, Alan Karthikesalingam, Christopher Semturs, Joelle
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A Novel HER2 Protein Identification Methodology in Breast Cancer Cells Using Raman Spectroscopy and Raman Imaging: An Analytical Validation Study J. Med. Chem. (IF 6.8) Pub Date : 2024-09-21 Halina Abramczyk, Jakub Maciej Surmacki, Monika Kopeć
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High-Throughput Screening of Antioxidant Drug Candidates from Natural Antioxidants with a “Zero” Intrinsic Fluorescence Peroxynitrite Sensing Precursor J. Med. Chem. (IF 6.8) Pub Date : 2024-09-21 Hong Zhang, Guan-Nan Zhu, Fei-Fan Xiang, Yu-Jin Chen, Shan-Yong Chen, Min Wu, Kun Li
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Targeting Plasmodium falciparum IspD in the Methyl-d-erythritol Phosphate Pathway: Urea-Based Compounds with Nanomolar Potency on Target and Low-Micromolar Whole-Cell Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Daan Willocx, Lorenzo Bizzarri, Alaa Alhayek, Deepika Kannan, Patricia Bravo, Boris Illarionov, Katharina Rox, Jonas Lohse, Markus Fischer, Andreas M. Kany, Hannes Hahne, Matthias Rottmann, Matthias Witschel, Audrey Odom John, Mostafa M. Hamed, Eleonora Diamanti, Anna K. H. Hirsch
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Development of Fragment-Based Inhibitors of the Bacterial Deacetylase LpxC with Low Nanomolar Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Sebastian Mielniczuk, Katharina Hoff, Fady Baselious, Yunqi Li, Jörg Haupenthal, Andreas M. Kany, Maria Riedner, Holger Rohde, Katharina Rox, Anna K. H. Hirsch, Isabelle Krimm, Wolfgang Sippl, Ralph Holl
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Small-Molecule Radiotracers for Visualization of V-Domain Immunoglobulin Suppressor of T Cell Activation. J. Med. Chem. (IF 6.8) Pub Date : 2024-09-21 Jia Liu,Yuanyuan Liang,Hongzhang Yang,Xueqi Wang,Xinying Zeng,Rongqiang Zhuang,Jin Du,Xianzhong Zhang,Zhide Guo
V-domain immunoglobulin suppressor of T cell activation (VISTA) plays a critical role in regulating innate and adaptive immune responses within the tumor immune microenvironment. Quantifying VISTA expression is necessary to determine whether patients respond to a related combination immunotherapy. This study developed two 68Ga-labeled small-molecule probes ([68Ga]Ga-DCA and [68Ga]Ga-DNCA) for visualizing
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Optimization of the Central α-Amino Acid in Cystobactamids to the Broad-Spectrum, Resistance-Breaking Antibiotic CN-CC-861 J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Daniel Kohnhäuser, Tim Seedorf, Katarina Cirnski, Dominik Heimann, Janetta Coetzee, Sylvie Sordello, Jana Richter, Moritz Stappert, Jean-Francois Sabuco, David Corbett, Eric Bacqué, Katharina Rox, Jennifer Herrmann, Aurelie Vassort, Rolf Müller, Andreas Kirschning, Mark Brönstrup
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Viral Protein Dimerization Quality Control: A Design Strategy for a Potential Viral Inhibitor J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Shaoqing Du, Xinyong Liu, Xueping Hu, Peng Zhan
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Fully Synthetic TF-Based Self-Adjuvanting Vaccine Simultaneously Triggers iNKT Cells and Mincle and Protects Mice against Tumor Development J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Deying Yang, Xiaohui Li, Jinmei Li, Zichun Liu, Tongtong Li, Pan Liao, Xiang Luo, Zhongqiu Liu, Wenbo Ming, Guochao Liao
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Structure Optimization of c-Jun N-terminal Kinase 1 Inhibitors for Treating Idiopathic Pulmonary Fibrosis J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Yi Huang, Fengling Liu, Shuhua Ren, Yuanqing Ding, Man Chi, Weiwei Huang, Wenjing Gu, Hewen Qian, Yaxia Yuan, Shurong Hou, Xiabin Chen, Lei Ma
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Deep-Learning-Driven Discovery of SN3–1, a Potent NLRP3 Inhibitor with Therapeutic Potential for Inflammatory Diseases J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Cheng Shi, Tongfei Gao, Weiping Lyu, Bo Qiang, Yanming Chen, Qixuan Chen, Liangren Zhang, Zhenming Liu
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Synthesis and Antiosteoporotic Characterization of Diselenyl Maleimides: Discovery of a Potent Agent for the Treatment of Osteoporosis by Targeting RANKL J. Med. Chem. (IF 6.8) Pub Date : 2024-09-19 Bin Li, Yao Wu, Linkun Ying, Weiwei Zhu, Jingyi Yang, Lingling Zhou, Lele Yi, Tianle Jiang, Haofu Jiang, Xiangrui Song, Weiwei Xue, Guang Liang, Shengbin Huang, Zengqiang Song
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Polypharmacological Drug Design Guided by Integrating Phenotypic and Restricted Fragment Docking Strategies J. Med. Chem. (IF 6.8) Pub Date : 2024-09-19 Shang Li, Xinxin Li, Liangliang Ma, Zhongwen Luo, Fucheng Yin, Yonglei Zhang, Yifan Chen, Siyuan Wan, Han Zhou, Xiaobing Wang, Lingyi Kong
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Design, Synthesis, and Biological Evaluation of Lysine-Stapled Peptide Inhibitors of p53-MDM2/MDMX Interactions with Potent Antitumor Activity In Vivo J. Med. Chem. (IF 6.8) Pub Date : 2024-09-19 Lei Xu, Xin Fan, Yi He, Xuefeng Xia, Jinqiang Zhang
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High-throughput identification of repurposable neuroactive drugs with potent anti-glioblastoma activity Nat. Med. (IF 58.7) Pub Date : 2024-09-20 Sohyon Lee, Tobias Weiss, Marcel Bühler, Julien Mena, Zuzanna Lottenbach, Rebekka Wegmann, Miaomiao Sun, Michel Bihl, Bartłomiej Augustynek, Sven P. Baumann, Sandra Goetze, Audrey van Drogen, Patrick G. A. Pedrioli, David Penton, Yasmin Festl, Alicia Buck, Daniel Kirschenbaum, Anna M. Zeitlberger, Marian C. Neidert, Flavio Vasella, Elisabeth J. Rushing, Bernd Wollscheid, Matthias A. Hediger, Michael
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Lipid profiling identifies modifiable signatures of cardiometabolic risk in children and adolescents with obesity Nat. Med. (IF 58.7) Pub Date : 2024-09-20 Yun Huang, Karolina Sulek, Sara E. Stinson, Louise Aas Holm, Min Kim, Kajetan Trost, Kourosh Hooshmand, Morten Asp Vonsild Lund, Cilius E. Fonvig, Helene Bæk Juel, Trine Nielsen, Lars Ängquist, Peter Rossing, Maja Thiele, Aleksander Krag, Jens-Christian Holm, Cristina Legido-Quigley, Torben Hansen
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Publisher Correction: Strategies to therapeutically modulate cytokine action. Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-09-20 Warren J Leonard,Jian-Xin Lin
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Emerging Pharmacotherapies for Obesity: A Systematic Review. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-09-20 Michail Kokkorakis,Marlene Chakhtoura,Caline Rhayem,Jana Al Rifai,Malak Ghezzawi,Laura Valenzuela-Vallejo,Christos S Mantzoros
The history of anti-obesity pharmacotherapies is marked by disappointments, often entangled with societal pressure promoting weight loss and the conviction that excess body weight signifies a lack of willpower. However, categories of emerging pharmacotherapies generate hope to reduce obesity rates. This systematic review of phase 2 and phase 3 trials in adults with overweight/obesity investigates the
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Neuroactive Kynurenines as Pharmacological Targets: New Experimental Tools and Exciting Therapeutic Opportunities. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-09-20 Ana Pocivavsek,Robert Schwarcz,Sophie Erhardt
Both pre-clinical and clinical studies implicate functional impairments of several neuroactive metabolites of the kynurenine pathway (KP), the major degradative cascade of the essential amino acid tryptophan in mammals, in the pathophysiology of neurological and psychiatric diseases. A number of KP enzymes, such as tryptophan 2,3-dioxygenase (TDO2), indoleamine 2,3-dioxygenases (IDO1 and IDO2), kynurenine
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From Hit to Lead: Discovery of First-In-Class Furanone Glycoside D228 Derived from Chimonanthus salicifolius for the Treatment of Inflammatory Bowel Disease J. Med. Chem. (IF 6.8) Pub Date : 2024-09-19 Mei-Lin Tang, Xiao-Yu Xiong, Heyanhao Zhang, Yun-Zhi Wang, Rong-Qian Cheng, Jianping Zuo, Lin Jin, Ze-Min Lin, Jun Chang
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Developing a Rhodium(III) Complex to Reprogram the Tumor Immune and Metabolic Microenvironments: Overcoming Multidrug Resistance and Metastasis in Non-Small Cell Lung Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-09-19 Wenjuan Li, Shanhe Li, Minghui Zhu, Gang Xu, Xueyu Man, Zhenlei Zhang, Hong Liang, Feng Yang
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Structure-Based Optimization of a Series of Covalent, Cell Active Bfl-1 Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-09-18 Simon C. C. Lucas, J. Henry Blackwell, Ulf Börjesson, David Hargreaves, Alexander G. Milbradt, Mark J. Bostock, Samiyah Ahmed, Kevin Beaumont, Tony Cheung, Sylvain Demanze, Andrea Gohlke, Carine Guerot, Afreen Haider, Vasudev Kantae, Gregory W. Kauffman, Olaf Kinzel, Lea Kupcova, Michael D. Lainchbury, Michelle L. Lamb, Leonardo Leon, Adeline Palisse, Claudia Sacchetto, R. Ian Storer, Nancy Su, Clare
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siRNA therapy lowers triglycerides in patients with rare condition Nat. Med. (IF 58.7) Pub Date : 2024-09-19
Plozasiran reduced triglyceride levels by 80% and lowered the risk of pancreatitis in patients with persistent chylomicronemia, with or without a genetic diagnosis.
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Echocardiographic screening for heart failure and optimization of the care pathway for individuals with pacemakers: a randomized controlled trial Nat. Med. (IF 58.7) Pub Date : 2024-09-19 Maria F. Paton, John Gierula, Haqeel A. Jamil, Sam Straw, Judith E. Lowry, Rowena Byrom, Thomas A. Slater, Alasdair M. Fellows, Richard G. Gillott, Hemant Chumun, Paul Smith, Richard M. Cubbon, Deborah D. Stocken, Mark T. Kearney, Klaus K. Witte
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Peptidomimetic Analogues Act as Effective Inhibitors against SARS-CoV-2 by Blocking the Function of Cathepsin L J. Med. Chem. (IF 6.8) Pub Date : 2024-09-18 Weilong Deng, Xiao Hu, Xiaoman Tian, Yuanyuan Zhang, Weijuan Shang, Leike Zhang, Luqing Shang
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SAR Analysis of Novel Coxsackie virus A9 Capsid Binders J. Med. Chem. (IF 6.8) Pub Date : 2024-09-18 Chiara Tammaro, Zlatka Plavec, Laura Myllymäki, Cristopher Mitchell, Sara Consalvi, Mariangela Biava, Alessia Ciogli, Aušra Domanska, Valtteri Leppilampi, Cienna Buckner, Simone Manetto, Pietro Sciò, Antonio Coluccia, Mira Laajala, Giulio M. Dondio, Chiara Bigogno, Varpu Marjomäki, Sarah J. Butcher, Giovanna Poce
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Ursodeoxycholic Acid Platinum(IV) Conjugates as Antiproliferative and Antimetastatic Agents: Remodel the Tumor Microenvironment through Suppressing JAK2/STAT3 Signaling J. Med. Chem. (IF 6.8) Pub Date : 2024-09-18 Yan Chen, Ming Zhang, Zhifang Liu, Ning Zhang, Qingpeng Wang
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RNA-Binding Small Molecules in Drug Discovery and Delivery: An Overview from Fundamentals J. Med. Chem. (IF 6.8) Pub Date : 2024-09-17 Siyi Chen, Qi Mao, Hong Cheng, Wanyi Tai
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WazaGaY: An Innovative Aza-BODIPY-Derived Near-Infrared Fluorescent Probe for Enhanced Tumor Imaging J. Med. Chem. (IF 6.8) Pub Date : 2024-09-17 Mohamed Bendellaa, Charlotte Cave, Amélie Godard, Fabien Dalonneau, Annika Sickinger, Christine Goze, Olivier Maury, Pierre Le Gendre, Ewen Bodio, Benoit Busser, Lucie Sancey
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GPCRSPACE: A New GPCR Real Expanded Library Based on Large Language Models Architecture and Positive Sample Machine Learning Strategies J. Med. Chem. (IF 6.8) Pub Date : 2024-09-17 Shiming Chen, Feisheng Zhong
The quest for novel therapeutics targeting G protein-coupled receptors (GPCRs), essential in numerous physiological processes, is crucial in drug discovery. Despite the abundance of GPCR-targeting drugs, many receptors lack selective modulators, indicating a significant untapped therapeutic potential. To bridge this gap, we introduce GPCRSPACE, a novel GPCR-focused purchasable real chemical library
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Improving primary healthcare with generative AI Nat. Med. (IF 58.7) Pub Date : 2024-09-18 Winnie Yip
Studies in China show how large language models can improve primary healthcare systems, but equitably scaling this technology will require attention to rural, low-resource settings and the companion policies that support its implementation.
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Navigating treatment combinations in small-cell lung cancer Nat. Med. (IF 58.7) Pub Date : 2024-09-18 Ning Li, Si-Yu Wang
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Human outbreaks of a novel reassortant Oropouche virus in the Brazilian Amazon region Nat. Med. (IF 58.7) Pub Date : 2024-09-18 Felipe Gomes Naveca, Tatiana Amaral Pires de Almeida, Victor Souza, Valdinete Nascimento, Dejanane Silva, Fernanda Nascimento, Matilde Mejía, Yasmin Silva de Oliveira, Luisa Rocha, Natana Xavier, Janis Lopes, Rodrigo Maito, Cátia Meneses, Tatyana Amorim, Luciana Fé, Fernanda Sindeaux Camelo, Samyly Coutinho de Aguiar Silva, Alexsandro Xavier de Melo, Leíse Gomes Fernandes, Marco Aurélio Almeida de
The Brazilian western Amazon is experiencing its largest laboratory-confirmed Oropouche virus (OROV) outbreak, with more than 6,300 reported cases between 2022 and 2024. Here, we sequenced and analyzed 382 OROV genomes from human samples collected in Amazonas, Acre, Rondônia, and Roraima states, between August 2022 and February 2024, to uncover the origin and genetic evolution of OROV in the current
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Countering the impact of the climate crisis on health will require data Nat. Med. (IF 58.7) Pub Date : 2024-09-17
As drastically rising global temperatures threaten the health and wellbeing of populations, solutions that drive policy action must be based on scientific evidence of which strategies work in different scenarios.
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Exposure to extreme heat increases perinatal mortality in sub-Saharan Africa Nat. Med. (IF 58.7) Pub Date : 2024-09-17
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Data-driven risk stratification and precision management of pulmonary nodules detected on chest computed tomography Nat. Med. (IF 58.7) Pub Date : 2024-09-17 Chengdi Wang, Jun Shao, Yichu He, Jiaojiao Wu, Xingting Liu, Liuqing Yang, Ying Wei, Xiang Sean Zhou, Yiqiang Zhan, Feng Shi, Dinggang Shen, Weimin Li
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Design, synthesis and biological evaluation of plant-derived miliusol derivatives achieve TNBC profound regression in vivo Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-09-18 Xi Zhao, Xiaoling Cheng, Zhiying Liu, Weiji Chen, Wenli Hao, Shuangshuang Ma, Jin Zhang, Wei Huang, Dahong Yao
Triple-negative breast cancer has become a major problem in clinical treatment due to its high heterogeneity, and Plant-derived drug discovery has been the focus of attention for novel anti-tumor therapeutics. In this study, Miliusol, a natural product isolated from the rarely reported plant Miliusa tenuistipitata, was identified as the lead compound, and 25 miliusol derivatives were designed and synthesized
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Hybrids of 3-Hydroxypyridin-4(1H)-ones and Long-Chain 4-Aminoquinolines as Potent Biofilm Inhibitors of Pseudomonas aeruginosa Potentiate Tobramycin and Polymyxin B Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-09-17 Zhi-Ying Miao, Xiao-Yi Zhang, Hao-Zhong Long, Jing Lin, Wei-Min Chen
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Discovery of Novel [1,2,4]Triazolo[1,5-a]pyrimidine Derivatives as Novel Potent S-Phase Kinase-Associated Protein 2 (SKP2) Inhibitors for the Treatment of Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-09-16 Kaizhao Hu, Yongqiang Luo, Peipei Miao, Lidan Zhao, Bing Zhao, Xiao-Jing Shi, Hong-Min Liu
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In vivo CAR T cells move into clinical trials Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-09-16
Drug developers want to reprogramme immune cells directly in the body, opening up new gene therapy frontiers in cancer and autoimmunity.
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Discovery of A-910, a Highly Potent and Orally Bioavailable Dual MerTK/Axl-Selective Tyrosine Kinase Inhibitor J. Med. Chem. (IF 6.8) Pub Date : 2024-09-16 Yiyun Yu, Miyeon Jang, Julie Miyashiro, Richard F. Clark, Gui-Dong Zhu, Jane Gong, Yujia Dai, Robin R. Frey, Thomas D. Penning, Hadong Kim, Hyung Ki Lee, Jin Kwan Kim, Ki Moon Ryu, Seong Jin Park, Taeyoung Yoon, Tao Li, Matthew D. Kurnick, Nicolas J. Kapecki, Leiming Li, Jacob V. Gorman, Debra A. Montgomery, Vlasios Manaves, Kenneth D. Bromberg, Stella Z. Doktor, Ashish Thakur, Jin Wang, Heath A. Smith
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Enhanced Recognition Memory through Dual Modulation of Brain Carbonic Anhydrases and Cholinesterases J. Med. Chem. (IF 6.8) Pub Date : 2024-09-16 Alessio Nocentini, Alessia Costa, Alessandro Bonardi, Andrea Ammara, Simone Giovannuzzi, Andrea Petreni, Gianluca Bartolucci, Barbara Rani, Manuela Leri, Monica Bucciantini, José G. Fernández-Bolaños, Óscar López, Maria Beatrice Passani, Gustavo Provensi, Paola Gratteri, Claudiu T. Supuran
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ctDNA-based molecular residual disease and survival in resectable colorectal cancer Nat. Med. (IF 58.7) Pub Date : 2024-09-16 Yoshiaki Nakamura, Jun Watanabe, Naoya Akazawa, Keiji Hirata, Kozo Kataoka, Mitsuru Yokota, Kentaro Kato, Masahito Kotaka, Yoshinori Kagawa, Kun-Huei Yeh, Saori Mishima, Hiroki Yukami, Koji Ando, Masaaki Miyo, Toshihiro Misumi, Kentaro Yamazaki, Hiromichi Ebi, Kenji Okita, Atsushi Hamabe, Hiroki Sokuoka, Satoshi Kobayashi, George Laliotis, Vasily N. Aushev, Shruti Sharma, Adham Jurdi, Minetta C. Liu
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Neoadjuvant nivolumab or nivolumab plus ipilimumab in early-stage triple-negative breast cancer: a phase 2 adaptive trial Nat. Med. (IF 58.7) Pub Date : 2024-09-16 Iris Nederlof, Olga I. Isaeva, Manon de Graaf, Robbert C. A. M. Gielen, Noor A. M. Bakker, Adrianne L. Rolfes, Hannah Garner, Bram Boeckx, Joleen J. H. Traets, Ingrid A. M. Mandjes, Michiel de Maaker, Thomas van Brussel, Maksim Chelushkin, Elisa Champanhet, Marta Lopez-Yurda, Koen van de Vijver, José G. van den Berg, Ingrid Hofland, Natasja Klioueva, Ritse M. Mann, Claudette E. Loo, Frederieke H. van
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Targeted therapy guided by circulating tumor DNA analysis in advanced gastrointestinal tumors Nat. Med. (IF 58.7) Pub Date : 2024-09-16 Yoshiaki Nakamura, Hiroshi Ozaki, Makoto Ueno, Yoshito Komatsu, Satoshi Yuki, Taito Esaki, Hiroya Taniguchi, Yu Sunakawa, Kensei Yamaguchi, Ken Kato, Tadamichi Denda, Tomohiro Nishina, Naoki Takahashi, Taroh Satoh, Hisateru Yasui, Hironaga Satake, Eiji Oki, Takeshi Kato, Takashi Ohta, Nobuhisa Matsuhashi, Masahiro Goto, Naohiro Okano, Koushiro Ohtsubo, Kentaro Yamazaki, Riu Yamashita, Naoko Iida, Mihoko
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Discovery of 1(2H)-phthalazinone and 1(2H)-isoquinolinone derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-09-16 Jingjing Peng, Xiaoyu Ding, Pei-Yu Shih, Qingyuan Meng, Xiao Ding, Man Zhang, Alex Aliper, Feng Ren, Hongfu Lu, Alex Zhavoronkov
Although immune checkpoint inhibitors (ICIs) have been a revelation for treating several cancers, an unmet need remains to broaden ICI therapeutic scope and increase their response rates in clinical trials. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of T cell activation and has previously been identified as a promising target for immunotherapy. Herein, we report the discovery
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Discovery and In Vivo Exploration of 1,3,4-Oxadiazole and α-Fluoroacrylate Containing IL-17 Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-09-14 Juraj Velcicky, Matthias R. Bauer, Achim Schlapbach, Guillaume Lapointe, Arndt Meyer, Markus Vögtle, Ernst Blum, Estelle Ngo, Catherine Rolando, Pierre Nimsgern, Sylvie Teixeira-Fouchard, Hansjoerg Lehmann, Pascal Furet, Frédéric Berst, Jens Schümann, Rowan Stringer, Patrice Larger, Cindy Schmid, Catriona T. Prendergast, Simone Riek, Patrick Schmutz, Sylvie Lehmann, Jörg Berghausen, Clemens Scheufler
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Neoadjuvant nivolumab and relatlimab in locally advanced MMR-deficient colon cancer: a phase 2 trial Nat. Med. (IF 58.7) Pub Date : 2024-09-15 Peter G. M. de Gooyer, Yara L. Verschoor, Lauren D. W. van den Dungen, Sara Balduzzi, Hendrik A. Marsman, Marnix H. Geukes Foppen, Cecile Grootscholten, Simone Dokter, Anne G. den Hartog, Wieke H. M. Verbeek, Karlijn Woensdregt, Joris J. van den Broek, Steven J. Oosterling, Ton N. Schumacher, Koert F. D. Kuhlmann, Regina G. H. Beets-Tan, John B. A. G. Haanen, Monique E. van Leerdam, Jose G. van den
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Datopotamab–deruxtecan in early-stage breast cancer: the sequential multiple assignment randomized I-SPY2.2 phase 2 trial Nat. Med. (IF 58.7) Pub Date : 2024-09-14 Katia Khoury, Jane L. Meisel, Christina Yau, Hope S. Rugo, Rita Nanda, Marie Davidian, Butch Tsiatis, A. Jo Chien, Anne M. Wallace, Mili Arora, Mariya Rozenblit, Dawn L. Hershman, Alexandra Zimmer, Amy S. Clark, Heather Beckwith, Anthony D. Elias, Erica Stringer-Reasor, Judy C. Boughey, Chaitali Nangia, Christos Vaklavas, Coral Omene, Kathy S. Albain, Kevin M. Kalinsky, Claudine Isaacs, Jennifer Tseng
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Datopotamab–deruxtecan plus durvalumab in early-stage breast cancer: the sequential multiple assignment randomized I-SPY2.2 phase 2 trial Nat. Med. (IF 58.7) Pub Date : 2024-09-14 Rebecca A. Shatsky, Meghna S. Trivedi, Christina Yau, Rita Nanda, Hope S. Rugo, Marie Davidian, Butch Tsiatis, Anne M. Wallace, A. Jo Chien, Erica Stringer-Reasor, Judy C. Boughey, Coral Omene, Mariya Rozenblit, Kevin Kalinsky, Anthony D. Elias, Christos Vaklavas, Heather Beckwith, Nicole Williams, Mili Arora, Chaitali Nangia, Evanthia T. Roussos Torres, Brittani Thomas, Kathy S. Albain, Amy S. Clark
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Development of Novel Indole-Based Covalent Inhibitors of TEAD as Potential Antiliver Cancer Agents J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Chen Zhou, Chunbao Sun, Wei Zhou, Tian Tian, Daniel C. Schultz, Tong Wu, Mu Yu, Lizi Wu, Liya Pi, Chenglong Li
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Between Theory and Practice: Computational/Experimental Integrated Approaches to Understand the Solubility and Lipophilicity of PROTACs J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Andrea Venturi, Stefano Di Bona, Jenny Desantis, Michela Eleuteri, Matteo Bartalucci, Massimo Baroni, Paolo Benedetti, Laura Goracci, Gabriele Cruciani
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Discovery and Development of Highly Potent and Orally Bioavailable Nonpeptidic αvβ6 Integrin Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Panayiotis A. Procopiou, John Barrett, Matthew H. J. Crawford, Richard J. D. Hatley, Ashley P. Hancock, John M. Pritchard, James E. Rowedder, Royston C. B. Copley, Robert J. Slack, Steven L. Sollis, Lee R. Thorp, Rhys A. Lippa, Simon J. F. Macdonald, Tim N. Barrett
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Design, Synthesis, and Bioevaluation of Novel NLRP3 Inhibitor with IBD Immunotherapy from the Virtual Screen J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Ziwen Zhang, Hongyu Wu, Kai Yin, Xinru Zheng, Zhonglian Cao, Wei Guo, Chunchang Zhao, Xianfeng Gu
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Targeting Thyroid-Stimulating Hormone Receptor: A Perspective on Small-Molecule Modulators and Their Therapeutic Potential J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Yu Zhang, Ye Tan, Zian Zhang, Xi Cheng, Jia Duan, Yi Li