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Design and Synthesis of 3-(2H-Chromen-3-yl)-5-aryl-1,2,4-oxadiazole Derivatives as Novel Toll-like Receptor 2/1 Agonists That Inhibit Lung Cancer In Vitro and In Vivo J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Yijie Wang, Xu Cheng, Xinru Liu, Jing Xu, Lin Wang, Shouguo Zhang, Shuchen Liu, Tao Peng
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Discovery of Conformationally Constrained ALK2 Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Héctor González-Álvarez, Deeba Ensan, Tao Xin, Jong Fu Wong, Carlos A. Zepeda-Velázquez, Julien Cros, Laurent Hoffer, Taira Kiyota, Brian J. Wilson, Ahmed Aman, Owen Roberts, Methvin B. Isaac, Alex N. Bullock, David Smil, Rima Al-awar
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Beyond Rule of Five and PROTACs in Modern Drug Discovery: Polarity Reducers, Chameleonicity, and the Evolving Physicochemical Landscape J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Edward Price, Manuel Weinheimer, Alexey Rivkin, Gary Jenkins, Marjoleen Nijsen, Philip B. Cox, David DeGoey
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A Selective-Tumor-Penetrating Strategy via Unidirectional Direct Transfer for Intravesical Therapy of Bladder Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Xiaowen Qin, Heng Wang, Wentao Xu, Bin Zheng, Haibao Zhang, Qi Zhang, Yang Liu, Zhenghong Liu, Li Sun, Yixuan Mou, Cenchao Yao, Wei Zheng, Yiyang Chen, Chenkai Wang, Xuanyi Zhou, Youqing Shen, Pu Zhang, Dahong Zhang
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Genome-editing medicinal products: the EMA perspective Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-03-15
Discover the world’s best science and medicine | Nature.com
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Identification of Dihydrobenzofuran Neolignans as Novel PDE4 Inhibitors and Evaluation of Antiatopic Dermatitis Efficacy in DNCB-Induced Mice Model J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Chenming Gu, Jiayuan Liu, Fei Qian, Wenchao Yu, Doudou Huang, Jingshan Shen, Chenguo Feng, Kaixian Chen, Yiming Li, Xiangrui Jiang, Yechun Xu, Liuqiang Zhang
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A timeline of biomarker changes before Alzheimer’s disease Nat. Med. (IF 82.9) Pub Date : 2024-03-15
Longitudinal data from the China Cognition and Aging Study map the sequential biomarker changes that begin almost two decades before clinical onset of Alzheimer’s disease.
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Development of Membrane-Targeting Fluorescent 2-Phenyl-1H-phenanthro[9,10-d]imidazole-Antimicrobial Peptide Mimic Conjugates against Methicillin-Resistant Staphylococcus aureus J. Med. Chem. (IF 7.3) Pub Date : 2024-03-16 Ting Xu, Xiaoting Yan, Ayue Kang, Longhua Yang, Xinhui Li, Yue Tian, Ruige Yang, Shangshang Qin, Yong Guo
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Discovery of New Tricyclic Oxime Sampangine Derivatives as Potent Antifungal Agents for the Treatment of Cryptococcosis and Candidiasis J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Wanzhen Yang, Ruxiong Liu, Zhuang Li, Jie Tu, Dongjian Xu, Na Liu, Chunquan Sheng
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Cyclic Peptide Keap1–Nrf2 Protein–Protein Interaction Inhibitors: Design, Synthesis, and In Vivo Treatment of Acute Lung Injury J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Jihua Zou, Jianyu Yan, Yifei Lu, Zhou Yu, Kai Zhang, Qianyu Han, Dan Han, Conghao Gai, Xiaoyun Chai, Qingjie Zhao, Chunlin Zhuang, Yan Zou
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Covalent Fragment Screening and Optimization Identifies the Chloroacetohydrazide Scaffold as Inhibitors for Ubiquitin C-terminal Hydrolase L1 J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Ryan D. Imhoff, Rishi Patel, Muhammad Hassan Safdar, Hannah B. L. Jones, Adan Pinto-Fernandez, Iolanda Vendrell, Hao Chen, Christine S. Muli, Aaron D. Krabill, Benedikt M. Kessler, Michael K. Wendt, Chittaranjan Das, Daniel P. Flaherty
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Identification of a Novel Selective CDK9 Inhibitor for the Treatment of CRC: Design, Synthesis, and Biological Activity Evaluation J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Ye Zhong, Jing Xu, Ruochen Zhou, Li Tang, Shaoyue Ding, Zhaohui Ren, Ning Song, Baichun Hu, Huali Yang, Yili Sun, Maosheng Cheng, Jia Li, Yang Liu
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Synthetic Approaches to the New Drugs Approved During 2022 J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Scott P. France, Erick A. Lindsey, Emma L. McInturff, Simon Berritt, Daniel W. Carney, Jacob C. DeForest, Sarah J. Fink, Andrew C. Flick, Tony S. Gibson, Kaitlyn Gray, Amber M. Johnson, Carolyn A. Leverett, Yiyang Liu, Subham Mahapatra, Rebecca B. Watson
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NASH field celebrates ‘hurrah moment’ with a first FDA drug approval for the liver disease Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-03-14
Madrigal’s resmetirom has scored a landmark FDA win, bolstering hopes for a diverse pipeline of drugs for non-alcoholic steatohepatitis.
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Telehealth enables safe medication abortion in shifting health and legal contexts Nat. Med. (IF 82.9) Pub Date : 2024-03-15 Dana M. Johnson, Abigail R. A. Aiken, Terri-Ann Thompson
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Prolonged benefits of bariatric surgery for patients with Type 2 Diabetes Nat. Med. (IF 82.9) Pub Date : 2024-03-15
People with type 2 diabetes who underwent bariatric surgery compared to medical or lifestyle interventions had better long-term outcomes, such as greater diabetes remission and less reliance on medication.
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Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET Mutations J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Zi-Xuan Wang, Qing-Qing Li, Jiao Cai, Jia-Zhen Wu, Jing-Jing Wang, Meng-Yuan Zhang, Qing-Xin Wang, Zhen-Jiang Tong, Jin Yang, Tian-Hua Wei, Yun Zhou, Wei-Chen Dai, Ning Ding, Xue-Jiao Leng, Shan-Liang Sun, Xin Xue, Yan-Cheng Yu, Ye Yang, Nian-Guang Li, Zhi-Hao Shi
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Subtle Structural Changes across the Boundary between A2AR/A2BR Dual Antagonism and A2BR Antagonism: A Novel Class of 2-Aminopyrimidine-Based Derivatives J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Haojie Wang, Xinyu Yang, Yan Li, Shuyin Ze, Bo Feng, Yuan Weng, Aoqi Gao, Gaojie Song, Mingyao Liu, Qiong Xie, Yonghui Wang, Weiqiang Lu
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Arginine-Selective Bioconjugation Reagent for Effective 18F-labeling of Native Proteins J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Pragalath Sadasivam, Shivashankar Khanapur, Siddesh V. Hartimath, Boominathan Ramasamy, Peter Cheng, Chin Zan Feng, David Green, Christopher Davis, Julian L. Goggi, Edward G. Robins, Ran Yan
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Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Lara Dötsch, Caitlin Davies, Elisabeth Hennes, Julia Schönfeld, Adarsh Kumar, Celine Da Cruz Lopes Guita, Johanna H.M. Ehrler, Kerstin Hiesinger, Sasikala Thavam, Petra Janning, Sonja Sievers, Stefan Knapp, Ewgenij Proschak, Slava Ziegler, Herbert Waldmann
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Correction to “Macrocyclic Immunoproteasome Inhibitors as a Potential Therapy for Alzheimer’s Disease” J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Min Jae Lee, Deepak Bhattarai, Hyeryung Jang, Ahreum Baek, In Jun Yeo, Seongsoo Lee, Zachary Miller, Sukyeong Lee, Jin Tae Hong, Dong-Eun Kim, Wooin Lee, Kyung Bo Kim
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DNA Interaction and Cleavage Modes of Anthraquinone-Fused Enediynes: A Study on Tiancimycins, Yangpumicins, and Their Semisynthetic Analogues J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Zhongqing Wen, Zhoukang Zhuang, Huiming Liu, Zilong Wang, Xueqiong Feng, Xiangcheng Zhu, Xiaohui Yan, Yanwen Duan, Yong Huang
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Discovery of a Novel Thienopyrimidine Compound as a Urate Transporter 1 and Glucose Transporter 9 Dual Inhibitor with Improved Efficacy and Favorable Druggability J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Xiaoyu Shi, Tong Zhao, Shuo Wang, Shujing Xu, Hui Liao, Shenghua Gao, Zhen Gao, Jian Zhang, Danhui Qi, Zhijiao Zhang, Fengxin Zheng, Youzhao Wang, Zhenqian Wang, Mingyu Yang, Qian Yang, Fan Yi, Jianxin Pang, Xinyong Liu, Peng Zhan
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Structure-Guided Design and Optimization of Covalent VHL-Targeted Sulfonyl Fluoride PROTACs J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Rishi R. Shah, Elena De Vita, Preethi S. Sathyamurthi, Daniel Conole, Xinyue Zhang, Elliot Fellows, Eleanor R. Dickinson, Carlos M. Fleites, Markus A. Queisser, John D. Harling, Edward W. Tate
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Rational Design of PARP1/c-Met Dual Inhibitors for Overcoming PARP1 Inhibitor Resistance Induced by c-Met Overexpression J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Zeren Sun, Lanjie Li, Bingxin Zhai, Mengxuan Hu, Lei Huang, Shihui Huang, Liu Ye, Xiangying Kong, Jie Xu, Jie Bai, Jingjie Yan, Qichen Zhou, Zheqi Hu, Yuchen Zhang, Yuhan Jiang, Yan Zhang, Zhou Qiao, Yi Zou, Yungen Xu, Qihua Zhu
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Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 John M. Ketcham, Stephen J. Harwood, Ruth Aranda, Athenea N. Aloiau, Briana M. Bobek, David M. Briere, Aaron C. Burns, Kersti Caddell Haatveit, Andrew Calinisan, Jeffery Clarine, Adam Elliott, Lars D. Engstrom, Robin J. Gunn, Anthony Ivetac, Benjamin Jones, Jon Kuehler, J. David Lawson, Natalie Nguyen, Cody Parker, Kelly E. Pearson, Lisa Rahbaek, Barbara Saechao, Xiaolun Wang, Anna Waters, Laura Waters
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Retro-Inverso Collagen Modulator Peptide Derived from Serpin A1 with Enhanced Stability and Activity In Vitro J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Fosca Errante, Marco Pallecchi, Gianluca Bartolucci, Elena Frediani, Francesca Margheri, Lisa Giovannelli, Anna M. Papini, Paolo Rovero
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Self-help mobile messaging intervention for depression among older adults in resource-limited settings: a randomized controlled trial Nat. Med. (IF 82.9) Pub Date : 2024-03-14 Marcia Scazufca, Carina Akemi Nakamura, Nadine Seward, Thiago Vinicius Nadaleto Didone, Felipe Azevedo Moretti, Marcelo Oliveira da Costa, Caio Hudson Queiroz de Souza, Gabriel Macias de Oliveira, Monica Souza dos Santos, Luara Aragoni Pereira, Mariana Mendes de Sá Martins, Pepijn van de Ven, William Hollingworth, Tim J. Peters, Ricardo Araya
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Acquired blood mutations cause acute kidney injury via dysregulated inflammation Nat. Med. (IF 82.9) Pub Date : 2024-03-13
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Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor Regression J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Zhixiang Chen, Mi Wang, Dimin Wu, Longchuan Bai, Tianfeng Xu, Hoda Metwally, Yu Wang, Donna McEachern, Lijie Zhao, Ruiting Li, John Takyi-Williams, Meilin Wang, Lu Wang, Qiuxia Li, Bo Wen, Duxin Sun, Shaomeng Wang
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Mechanism-Based Macrocyclic Inhibitors of Serine Proteases J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Vishnu C. Damalanka, Victoria Banas, Paolo De Bona, Maithri M. Kashipathy, Kevin Battaile, Scott Lovell, James W. Janetka
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Development of Cytotoxic GW7604-Zeise’s Salt Conjugates as Multitarget Compounds with Selectivity for Estrogen Receptor- Positive Tumor Cells J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Patricia Grabher, Paul Kapitza, Nikolas Hörmann, Amelie Scherfler, Martin Hermann, Michael Zwerger, Hristo P. Varbanov, Brigitte Kircher, Daniel Baecker, Ronald Gust
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Synthesis of Sorafenib−Ruthenium Complexes, Investigation of Biological Activities and Applications in Drug Delivery Systems as an Anticancer Agent J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Belma Zengin Kurt, Dilek Öztürk Civelek, Elmas Begüm Çakmak, Yakup Kolcuoğlu, Halil Şenol, Begüm Nurpelin Sağlık Özkan, Aydan Dag, Kadriye Benkli
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Searching for Conjugates as New Structures for Antifungal Therapies J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Izabela Muszalska-Kolos, Piotr Mariusz Dwiecki
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Discovery and Optimization of Selective Brain-Penetrant EBP Inhibitors that Enhance Oligodendrocyte Formation J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Ruth Dorel, Dawei Sun, Nicholas Carruthers, Georgette M. Castanedo, Peter M.-U. Ung, Daniel C. Factor, Tianbo Li, Hannah Baumann, Danielle Janota, Jodie Pang, Laurent Salphati, Robert Meklemburg, Allison J. Korman, Halie E. Harper, Samantha Stubblefield, Jian Payandeh, Daniel McHugh, Bradley T. Lang, Paul J. Tesar, Edward Dere, Matthieu Masureel, Drew J. Adams, Matthew Volgraf, Marie-Gabrielle Braun
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Structure-Guided Elaboration of a Fragment-Like Hit into an Orally Efficacious Leukotriene A4 Hydrolase Inhibitor J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Gebhard Thoma, Wolfgang Miltz, Honnappa Srinivas, Carlos A. Penno, Michael Kiffe, Monika Gajewska, Kai Klein, Amanda Evans, Christian Beerli, Till A. Röhn
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Correction to “MicroCycle: An Integrated and Automated Platform to Accelerate Drug Discovery” J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Cara E. Brocklehurst, Eva Altmann, Jérôme André, Corentin Bon, Thomas Caya, Holly Davis, Odile Decoret, David Dunstan, Peter Ertl, Carol Ginsburg-Moraff, Jonathan Grob, Daniel J. Gosling, Guillaume Lapointe, Dyuti Majumdar, Alexander N. Marziale, Heinrich Mues, Marco Palmieri, Sophie Racine, Richard I. Robinson, Clayton Springer, Kian Tan, William Ulmer, Laura West, René Wyler
We are adding five authors who were erroneously missing from the original author list. All five contributed significantly to the building, testing, and evaluation of the MicroCycle platform, and their inclusion as authors is well warranted. The five additional authors are Jérôme André, Thomas Caya, Odile Decoret, Dyuti Majumdar, and Laura West. The additions are reflected in the authorship of this
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Development of a Series of Pyrrolopyridone MAT2A Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-03-11 Stephen J. Atkinson, Sharan K. Bagal, Argyrides Argyrou, Sean Askin, Tony Cheung, Elisabetta Chiarparin, Muireann Coen, Iain T. Collie, Ian L. Dale, Claudia De Fusco, Keith Dillman, Laura Evans, Lyman J. Feron, Alison J. Foster, Michael Grondine, Vasudev Kantae, Gillian M. Lamont, Scott Lamont, James T. Lynch, Sten Nilsson Lill, Graeme R. Robb, Jamal Saeh, Marianne Schimpl, James S. Scott, James Smith
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The Discovery of 7-Isopropoxy-2-(1-methyl-2-oxabicyclo[2.1.1]hexan-4-yl)-N-(6-methylpyrazolo[1,5-a]pyrimidin-3-yl)imidazo[1,2-a]pyrimidine-6-carboxamide (BIO-7488), a Potent, Selective, and CNS-Penetrant IRAK4 Inhibitor for the Treatment of Ischemic Stroke J. Med. Chem. (IF 7.3) Pub Date : 2024-03-11 Ryan Evans, Philippe N. Bolduc, Magnus Pfaffenbach, Fang Gao, Tricia May-Dracka, Terry Fang, Brian T. Hopkins, Jayanth V Chodaparambil, Kate L. Henry, Pei Li, Claire Metrick, Ashley Nelson, Patrick Trapa, Ankur Thomas, Linda Burkly, Emily A. Peterson
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Design, Synthesis, and Biological Evaluation of 5-(5-Iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine (AF-353) Derivatives as Novel DHFR Inhibitors against Staphylococcus aureus J. Med. Chem. (IF 7.3) Pub Date : 2024-03-11 Zongkai Huang, Xupeng Gou, Xudong Hang, Ting Shi, Jiaxing Yang, Yan Liu, Xinlian He, Jin Li, Keao Quan, Hongkai Bi, Youfu Luo
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Upcoming market catalysts in Q2 2024 Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-03-13
Discover the world’s best science and medicine | Nature.com
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Intrathecal bivalent CAR T cells targeting EGFR and IL13Rα2 in recurrent glioblastoma: phase 1 trial interim results Nat. Med. (IF 82.9) Pub Date : 2024-03-13 Stephen J. Bagley, Meghan Logun, Joseph A. Fraietta, Xin Wang, Arati S. Desai, Linda J. Bagley, Ali Nabavizadeh, Danuta Jarocha, Rene Martins, Eileen Maloney, Lester Lledo, Carly Stein, Amy Marshall, Rachel Leskowitz, Julie K. Jadlowsky, Shannon Christensen, Bike Su Oner, Gabriela Plesa, Andrea Brennan, Vanessa Gonzalez, Fang Chen, Yusha Sun, Whitney Gladney, David Barrett, MacLean P. Nasrallah, Wei-Ting
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Engineered T cells call for back-up Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-03-12
Discover the world’s best science and medicine | Nature.com
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The European Innovation Network as a hub for medicines innovation in Europe Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-03-11 Eleonora Agricola, Caroline Auriche-Benichou, Helena Baiao, Oriane Blanquie, Teodora Bodea, Tomáš Boráň, John-Joseph Borg, Valentina Cordo’, Maria Di Marzo, Lars Dmowski Rugholm, Falk Ehmann, Rúna Hauksdóttir Hvannberg, Ralf Herold, Alar Irs, Simona Jurkovič Mlakar, Robert Klaus, Juha Kolehmainen, Christophe Lahorte, Wiebke Löbker, Anna Mäkinen Salmi, Yoana Nuevo Ordoñez, Laurence O’Dwyer, Anna Maria
The European Innovation Network is working to support the European medical innovation ecosystem by facilitating early dialogue between developers of medicines and regulators, as well as providing a platform for regulators to share information, good practices and expertise.
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Mpox continues to spread in Africa and threatens global health security Nat. Med. (IF 82.9) Pub Date : 2024-03-12 Kyeng Mercy, Bethelhem Tibebu, Mosoka Fallah, Nuno R. Faria, Nicaise Ndembi, Yenew Kebede Tebeje
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Identification of clinical disease trajectories in neurodegenerative disorders with natural language processing Nat. Med. (IF 82.9) Pub Date : 2024-03-12 Nienke J. Mekkes, Minke Groot, Eric Hoekstra, Alyse de Boer, Ekaterina Dagkesamanskaia, Sander Bouwman, Sophie M. T. Wehrens, Megan K. Herbert, Dennis D. Wever, Annemieke Rozemuller, Bart J. L. Eggen, Inge Huitinga, Inge R. Holtman
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How AI-powered handheld devices are boosting disease diagnostics - from cancer to dermatology Nat. Med. (IF 82.9) Pub Date : 2024-03-12
Nature Medicine explores the latest translational and clinical research news, with FDA approval of an AI-assisted optical reader to help in the diagnosis of skin cancer.
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MEGA CRISPR rejuvenates exhausted CAR T cells Nat. Med. (IF 82.9) Pub Date : 2024-03-11
MEGA is a new CRISPR-based RNA-editing platform with the ability to enhance the fitness of CAR T cells; it may also overcome certain limitations of conventional DNA-targeting CRISPR–Cas9 systems.
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Uncovering PROTAC Sensitivity and Efficacy by Multidimensional Proteome Profiling: A Case for STAT3 J. Med. Chem. (IF 7.3) Pub Date : 2024-03-11 Yuying Suo, Daohai Du, Chao Chen, Hongwen Zhu, Xiongjun Wang, Nixue Song, Dayun Lu, Yaxi Yang, Jiacheng Li, Jun Wang, Zhongyuan Luo, Bing Zhou, Cheng Luo, Hu Zhou
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Engineering of a Biologically Active Glycosylated Glucagon-Like Peptide-1 Analogue J. Med. Chem. (IF 7.3) Pub Date : 2024-03-11 Chaitra Chandrashekar, Feng Lin, Yuji Nishiuchi, Sam F. Mohammed, Barbara F. White, Yanni Arsenakis, Elita Yuliantie, Peishen Zhao, Sam van Dun, Anna Koijen, Yasuhiro Kajihara, Denise Wootten, Garron T. Dodd, Leendert J. van den Bos, John D. Wade, Mohammed Akhter Hossain
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Discovery of Novel PD-L1 Small-Molecular Inhibitors with Potent In Vivo Anti-tumor Immune Activity J. Med. Chem. (IF 7.3) Pub Date : 2024-03-11 Liu Liu, Honghan Zhang, Jie Hou, Yuying Zhang, Luosen Wang, Shijun Wang, Zhiying Yao, Tao Xie, Xiaoan Wen, Qinglong Xu, Liang Dai, Zhiqi Feng, Pu Zhang, Yaojun Wu, Hongbin Sun, Jun Liu, Haoliang Yuan
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Fragment-Based Discovery of Allosteric Inhibitors of SH2 Domain-Containing Protein Tyrosine Phosphatase-2 (SHP2) J. Med. Chem. (IF 7.3) Pub Date : 2024-03-10 James E. H. Day, Valerio Berdini, Joan Castro, Gianni Chessari, Thomas G. Davies, Philip J. Day, Jeffrey D. St. Denis, Hideto Fujiwara, Satoshi Fukaya, Christopher C. F. Hamlett, Keisha Hearn, Steven D. Hiscock, Rhian S. Holvey, Satoru Ito, Navrohit Kandola, Yasuo Kodama, John W. Liebeschuetz, Vanessa Martins, Kenichi Matsuo, Paul N. Mortenson, Sandra Muench, Yoko Nakatsuru, Hiroaki Ochiiwa, Nicholas
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Discovery of novel polyheterocyclic neuraminidase inhibitors with 1,3,4-oxadiazole thioetheramide as core backbone Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-12 Lin Lin Shang, Zhi Jian Zhong, Li Ping Cheng
Inspired by our earlier findings regarding neuraminidase (NA) inhibitors interacting with 150-cavity or 430-cavity of NA, sixteen novel polyheterocyclic NA inhibitors with 1,3,4-oxadiazole thioetheramide as core backbone were designed and synthesized based on the lead compound . Of the synthesized compounds, compound targeting 150-cavity exerts the best inhibitory activity against the wild-type H5N1
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Insights from structure-activity relationships and the binding mode of peptidic α-ketoamide inhibitors of the malaria drug target subtilisin-like SUB1 Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-11 Alice Legru, Fernando A. Batista, Anna K. Puszko, Anthony Bouillon, Manon Maurel, Mariano Martinez, Abdelaziz Ejjoummany, Laura Ortega Varga, Pauline Adler, Ariel Méchaly, Margot Hadjadj, Piotr Sosnowski, Gérard Hopfgartner, Pedro M. Alzari, Arnaud Blondel, Ahmed Haouz, Jean-Christophe Barale, Jean-François Hernandez
multi-resistance, including against artemisinin, seriously threatens malaria treatment and control. Hence, new drugs are urgently needed, ideally targeting different parasitic stages, which are not yet targeted by current drugs. The SUB1 protease is involved in both hepatic and blood stages due to its essential role in the egress of parasites from host cells, and, as potential new target, it would
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Novel pyrrole based CB2 agonists: New insights on CB2 receptor role in regulating neurotransmitters' tone Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-11 Simone Di Micco, Tania Ciaglia, Emanuela Salviati, Perrone Michela, Magdalena Kostrzewa, Simona Musella, Aniello Schiano Moriello, Veronica Di Sarno, Gerardina Smaldone, Francesca Di Matteo, Ilaria Capolupo, Rosmara Infantino, Giuseppe Bifulco, Giacomo Pepe, Eduardo M. Sommella, Poulami Kumar, Manuela Giovanna Basilicata, Marco Allarà, Nuria Sánchez-Fernández, Ester Aso, Isabel M. Gomez-Monterrey,
The cannabinoid system is one of the most investigated neuromodulatory systems because of its involvement in multiple pathologies such as cancer, inflammation, and psychiatric diseases. Recently, the CB2 receptor has gained increased attention considering its crucial role in modulating neuroinflammation in several pathological conditions like neurodegenerative diseases. Here we describe the rational
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Shifts in the clinical trial landscape Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-03-08
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GSK’s first-in-class antibiotic secures another phase III win, approaches regulatory run Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-03-08
Discover the world’s best science and medicine | Nature.com
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Ribosome-targeted antibiotic tackles antimicrobial resistance Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-03-06
Discover the world’s best science and medicine | Nature.com
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Photochemistry in Medicinal Chemistry and Chemical Biology J. Med. Chem. (IF 7.3) Pub Date : 2024-03-08 W. Felix Zhu, Claire Empel, Sveva Pelliccia, Rene M. Koenigs, Ewgenij Proschak, Victor Hernandez-Olmos