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New route to target RAS Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-10
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Studying paired patient tissue and blood enables insights into immunotherapy toxicity Nat. Med. (IF 82.9) Pub Date : 2024-05-09
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Gene therapy trials deliver double win Nat. Med. (IF 82.9) Pub Date : 2024-05-09
Final results of two studies — whose preliminary data led to regulatory approval of the gene therapy exagamglogene autotemcel — describe highly effective treatment of sickle-cell disease and transfusion-dependent β-thalassemia.
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Single-cell transcriptomic analyses reveal distinct immune cell contributions to epithelial barrier dysfunction in checkpoint inhibitor colitis Nat. Med. (IF 82.9) Pub Date : 2024-05-09 Molly Fisher Thomas, Kamil Slowikowski, Kasidet Manakongtreecheep, Pritha Sen, Nandini Samanta, Jessica Tantivit, Mazen Nasrallah, Leyre Zubiri, Neal P. Smith, Alice Tirard, Swetha Ramesh, Benjamin Y. Arnold, Linda T. Nieman, Jonathan H. Chen, Thomas Eisenhaure, Karin Pelka, Yuhui Song, Katherine H. Xu, Vjola Jorgji, Christopher J. Pinto, Tatyana Sharova, Rachel Glasser, PuiYee Chan, Ryan J. Sullivan
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WRN inhibitors squeeze cancer cell vulnerability Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-08
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Development of Chinese innovative drugs in the USA Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-08
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First, do no harm: a global perspective on diversity and inclusion in clinical trials Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-08 Katharine Wright, Willyanne DeCormier Plosky, Hayat R. Ahmed, Sarah A. White, Barbara E. Bierer
New requirements for clinical trial sponsors to submit diversity action plans to the US Food and Drug Administration (FDA) are an important step to embed planning for diverse representation in clinical trial research. These must not, however, be implemented in ways that are detrimental to other countries’ health and research interests.
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Using AI to improve medication safety Nat. Med. (IF 82.9) Pub Date : 2024-05-08 Johanna I. Westbrook, Nasir Wabe, Magdalena Z. Raban
Large language models can translate the archaic language of pharmacy prescriptions into plain English, but reducing medication errors for patients will require interventions that go further.
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BiTE therapy for rheumatoid arthritis Nat. Med. (IF 82.9) Pub Date : 2024-05-08 Frances Humby, Bruce Kirkham, Leonie Taams
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Adequate information about clinical trial results must be given to participants Nat. Med. (IF 82.9) Pub Date : 2024-05-08 Rafael Dal-Ré, Arthur L. Caplan, Søren Holm, Reecha Sofat, Richard Stephens
The lay summary of trial results to be provided to participants should be written in plain language, use infographics and be concise — something that currently is almost never achieved.
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An updated framework for SARS-CoV-2 variants reflects the unpredictability of viral evolution Nat. Med. (IF 82.9) Pub Date : 2024-05-08 Lorenzo Subissi, James Richard Otieno, Nathalie Worp, Homa Attar Cohen, Bas B. Oude Munnink, Laith J. Abu-Raddad, Erik Alm, Amal Barakat, Wendy S. Barclay, Jinal N. Bhiman, Leon Caly, Meera Chand, Mark Chen, Ann Cullinane, Tulio de Oliveira, Christian Drosten, Julian Druce, Paul Effler, Ihab El Masry, Adama Faye, Elodie Ghedin, Rebecca Grant, Bart L. Haagmans, Christian Happi, Belinda L. Herring, Emma
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Effects of a personalized nutrition program on cardiometabolic health: a randomized controlled trial Nat. Med. (IF 82.9) Pub Date : 2024-05-08 Kate M. Bermingham, Inbar Linenberg, Lorenzo Polidori, Francesco Asnicar, Alberto Arrè, Jonathan Wolf, Fatema Badri, Hannah Bernard, Joan Capdevila, William J. Bulsiewicz, Christopher D. Gardner, Jose M. Ordovas, Richard Davies, George Hadjigeorgiou, Wendy L. Hall, Linda M. Delahanty, Ana M. Valdes, Nicola Segata, Tim D. Spector, Sarah E. Berry
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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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Designing novel macrocyclic drugs Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-07
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Targeting ephrin signalling in sepsis Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-07
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ASO to treat Timothy syndrome Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-07
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Exome sequencing in a Chinese cohort of children with cerebral palsy identifies likely pathogenic variants Nat. Med. (IF 82.9) Pub Date : 2024-05-07
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The future of brain–computer interfaces in medicine Nat. Med. (IF 82.9) Pub Date : 2024-05-07
Growing interest in non-invasive brain–computer interfaces, rather than implants, might improve accessibility for patients, but resolution needs to be improved.
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APOE4 homozygosity is a new genetic form of Alzheimer’s disease Nat. Med. (IF 82.9) Pub Date : 2024-05-06 Qin Xu, Zherui Liang, Yadong Huang
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APOE4 homozygozity represents a distinct genetic form of Alzheimer’s disease Nat. Med. (IF 82.9) Pub Date : 2024-05-06 Juan Fortea, Jordi Pegueroles, Daniel Alcolea, Olivia Belbin, Oriol Dols-Icardo, Lídia Vaqué-Alcázar, Laura Videla, Juan Domingo Gispert, Marc Suárez-Calvet, Sterling C. Johnson, Reisa Sperling, Alexandre Bejanin, Alberto Lleó, Víctor Montal
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Pemigatinib in previously treated solid tumors with activating FGFR1–FGFR3 alterations: phase 2 FIGHT-207 basket trial Nat. Med. (IF 82.9) Pub Date : 2024-05-06 Jordi Rodón, Silvia Damian, Muhammad Furqan, Jesús García-Donas, Hiroo Imai, Antoine Italiano, Iben Spanggaard, Makoto Ueno, Tomoya Yokota, Maria Luisa Veronese, Natalia Oliveira, Xin Li, Aidan Gilmartin, Michael Schaffer, Lipika Goyal
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A hierarchical kidney outcome using win statistics in patients with heart failure from the DAPA-HF and DELIVER trials Nat. Med. (IF 82.9) Pub Date : 2024-05-06 Toru Kondo, Pardeep S. Jhund, Samvel B. Gasparyan, Mingming Yang, Brian L. Claggett, Finnian R. McCausland, Paolo Tolomeo, Muthiah Vadagunathan, Hiddo J. L. Heerspink, Scott D. Solomon, John J. V. McMurray
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Discovery of potent small molecule ubiquitin-specific protease 10 inhibitors with anti-hepatocellular carcinoma activity through regulating YAP expression Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-05-05 Yang Lu, Jian Gao, Peipei Wang, Haifeng Chen, Xinjun He, Mengxin Luo, Yu Guo, Linjie Li, Weihao Zhuang, Bo Zhang, Nengming Lin, Jia Li, Yubo Zhou, Xiaowu Dong, Jinxin Che
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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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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 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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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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Anticancer activity of 8-hydroxyquinoline-triphenylphosphine rhodium(III) complexes targeting mitophagy pathways Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-05-04 Xiao-Qiong Huang, Run-Chun Wu, Jian-Min Liang, Zhen Zhou, Qi-Pin Qin, Hong Liang
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Discovery of LHQ490 as a highly selective fibroblast growth factor receptor 2 (FGFR2) inhibitor Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-05-04 Huiqiong Li, Ran Ke, Yang Zhou, Shaohua Chang, Jie Wang, Chen Su, Pinglian Wu, Bowen Yang, Zhen Wang, Ke Ding, Dawei Ma
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Design, synthesis, and evaluation of N1,N3-dialkyldioxonaphthoimidazoliums as antibacterial agents against methicillin-resistant Staphylococcus aureus Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-05-04 Taewoo Kim, Shin-Yae Choi, Hee-Won Bae, Hyun Su Kim, Hoon Jeon, Haejun Oh, Sung-Hoon Ahn, Jongkook Lee, Young-Ger Suh, You-Hee Cho, Seok-Ho Kim
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Mapping cysteine ligandability Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-03
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Equitable implementation of a precision digital health program for glucose management in individuals with newly diagnosed type 1 diabetes Nat. Med. (IF 82.9) Pub Date : 2024-05-03 Priya Prahalad, David Scheinker, Manisha Desai, Victoria Y. Ding, Franziska K. Bishop, Ming Yeh Lee, Johannes Ferstad, Dessi P. Zaharieva, Ananta Addala, Ramesh Johari, Korey Hood, David M. Maahs
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Molecular Pathways Governing the Termination of Liver Regeneration Pharmacol. Rev. (IF 21.1) Pub Date : 2024-05-01 Lianne R. de Haan, Rowan F. van Golen, Michal Heger, Martin Michel
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Steatotic Liver Disease: Pathophysiology and Emerging Pharmacotherapies Pharmacol. Rev. (IF 21.1) Pub Date : 2024-05-01 Michail Kokkorakis, Emir Muzurović, Špela Volčanšek, Marlene Chakhtoura, Michael A. Hill, Dimitri P. Mikhailidis, Christos S. Mantzoros, Ali Eid
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MDM2 Inhibitors for Cancer Therapy: The Past, Present, and Future Pharmacol. Rev. (IF 21.1) Pub Date : 2024-05-01 Wei Wang, Najah Albadari, Yi Du, Josef F. Fowler, Hannah T. Sang, Wa Xian, Frank McKeon, Wei Li, Jia Zhou, Ruiwen Zhang, Michael Gottesman
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Prostaglandin E2 in the Tumor Microenvironment, a Convoluted Affair Mediated by EP Receptors 2 and 4 Pharmacol. Rev. (IF 21.1) Pub Date : 2024-05-01 Ana Santiso, Akos Heinemann, Julia Kargl, Michael Gottesman
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Adrenoceptor Desensitization: Current Understanding of Mechanisms Pharmacol. Rev. (IF 21.1) Pub Date : 2024-05-01 Dina Maaliki, Aneese A. Jaffa, Suzanne Nasser, Amirhossein Sahebkar, Ali H. Eid, Paul Insel, Martin Michel
G-protein coupled receptors (GPCRs) transduce a wide range of extracellular signals. They are key players in the majority of biologic functions including vision, olfaction, chemotaxis, and immunity. However, as essential as most of them are to body function and homeostasis, overactivation of GPCRs has been implicated in many pathologic diseases such as cancer, asthma, and heart failure (HF). Therefore
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New Advances in the Pharmacology and Toxicology of Lithium: A Neurobiologically Oriented Overview Pharmacol. Rev. (IF 21.1) Pub Date : 2024-05-01 Analia Bortolozzi, Giovanna Fico, Michael Berk, Marco Solmi, Michele Fornaro, Joao Quevedo, Carlos A. Zarate, Lars V. Kessing, Eduard Vieta, Andre F. Carvalho, Robert Dantzer
Over the last six decades, lithium has been considered the gold standard treatment for the long-term management of bipolar disorder due to its efficacy in preventing both manic and depressive episodes as well as suicidal behaviors. Nevertheless, despite numerous observed effects on various cellular pathways and biologic systems, the precise mechanism through which lithium stabilizes mood remains elusive
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Recent discovery and development of AXL inhibitors as antitumor agents Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-05-03 Zihang Liu, Li Chen, Jifa Zhang, Jun Yang, Xue Xiao, Lianhai Shan, Wuyu Mao
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Synthesis and Evaluation of diaryl ether modulators of the leukotriene A4 hydrolase aminopeptidase activity Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-05-03 Greg Petruncio, Kyung Hyeon Lee, Michael Girgis, Zachary Shellnutt, Zach Beaulac, Jiangdong Xiang, Soo Hyeon Lee, Xuejun Peng, Marie Burdick, Schroeder M. Noble, Yun M. Shim, Mikell Paige
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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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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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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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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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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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Adapting vision–language AI models to cardiology tasks Nat. Med. (IF 82.9) Pub Date : 2024-05-01 Rima Arnaout
Vision–language models can be trained to read cardiac ultrasound images with implications for improving clinical workflows, but additional development and validation will be required before such models can replace humans.
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Exome sequencing reveals genetic heterogeneity and clinically actionable findings in children with cerebral palsy Nat. Med. (IF 82.9) Pub Date : 2024-05-01 Yangong Wang, Yiran Xu, Chongchen Zhou, Ye Cheng, Niu Qiao, Qing Shang, Lei Xia, Juan Song, Chao Gao, Yimeng Qiao, Xiaoli Zhang, Ming Li, Caiyun Ma, Yangyi Fan, Xirui Peng, Silin Wu, Nan Lv, Bingbing Li, Yanyan Sun, Bohao Zhang, Tongchuan Li, Hongwei Li, Jin Zhang, Yu Su, Qiaoli Li, Junying Yuan, Lei Liu, Andres Moreno-De-Luca, Alastair H. MacLennan, Jozef Gecz, Dengna Zhu, Xiaoyang Wang, Changlian
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Novel pyxinol amide derivatives bearing an aliphatic heterocycle as P-glycoprotein modulators for overcoming multidrug resistance Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-05-01 Liping Yu, Ruiyin Ren, Shuang Li, Chen Zhang, Cheng Chen, Hanqi Lv, Zongji Zou, Xinjie Pei, Zhihua Song, Peng Zhang, Hongbo Wang, Gangqiang Yang
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Synthesis and clinical application of representative small-molecule dipeptidyl Peptidase-4 (DPP-4) inhibitors for the treatment of type 2 diabetes mellitus (T2DM) Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-05-01 Dong-Wei Shao, Li-Jie Zhao, Jin-Feng Sun