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X-ray Structure-Guided Discovery of a Potent Benzimidazole Glutaminyl Cyclase Inhibitor That Shows Activity in a Parkinson’s Disease Mouse Model J. Med. Chem. (IF 7.3) Pub Date : 2024-05-31 Jun Mou, Xiang-Li Ning, Xin-Yue Wang, Shu-Yan Hou, Fan-Bo Meng, Cong Zhou, Jing-Wei Wu, Chunyan Li, Tao Jia, Xiaoai Wu, Yong Wu, Yongping Chen, Guo-Bo Li
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Discovery of Potent and Selective Covalent Inhibitors of HER2WT and HER2YVMA J. Med. Chem. (IF 7.3) Pub Date : 2024-05-31 Erik J. Hicken, Karin Brown, Natalie C. Dwulet, John J. Gaudino, Erik P. Hansen, Dylan P. Hartley, John P. Kowalski, Ellen R. Laird, Nicholas C. Lazzara, Bin Li, Tung-Chung Mou, Marie F. Mutryn, Lauren Oko, Spencer Pajk, Robert W. Pipal, Rachel Z. Rosen, Russell Shelp, Anurag Singh, Jing Wang, Courtney E. Wise, Christina Wong, Jim Y. Wong
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Newly Designed Quasi-intrinsic Photosensitizers for Fluorescence Image-Guided Two-Photon Photodynamic Therapy with Type I/II Photoreactions J. Med. Chem. (IF 7.3) Pub Date : 2024-05-30 Xixi Cui, Hongxiu Yuan, Xiaolin Chen, Qingtian Meng, Changzhe Zhang
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Trastuzumab deruxtecan versus trastuzumab emtansine in HER2-positive metastatic breast cancer: long-term survival analysis of the DESTINY-Breast03 trial Nat. Med. (IF 82.9) Pub Date : 2024-06-02 Javier Cortés, Sara A. Hurvitz, Seock-Ah Im, Hiroji Iwata, Giuseppe Curigliano, Sung-Bae Kim, Joanne W. Y. Chiu, Jose L. Pedrini, Wei Li, Kan Yonemori, Giampaolo Bianchini, Sherene Loi, Giuliano S. Borges, Xian Wang, Thomas Bachelot, Shunsuke Nakatani, Shahid Ashfaque, Zhengkang Liang, Anton Egorov, Erika Hamilton
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Inhibition of lysine acetyltransferase KAT6 in ER+HER2− metastatic breast cancer: a phase 1 trial Nat. Med. (IF 82.9) Pub Date : 2024-06-01 Toru Mukohara, Yeon Hee Park, David Sommerhalder, Kan Yonemori, Erika Hamilton, Sung-Bae Kim, Jee Hyun Kim, Hiroji Iwata, Toshinari Yamashita, Rachel M. Layman, Monica Mita, Timothy Clay, Yee Soo Chae, Catherine Oakman, Fengting Yan, Gun Min Kim, Seock-Ah Im, Geoffrey J. Lindeman, Hope S. Rugo, Marlon Liyanage, Michelle Saul, Christophe Le Corre, Athanasia Skoura, Li Liu, Meng Li, Patricia M. LoRusso
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Fruquintinib plus paclitaxel versus placebo plus paclitaxel for gastric or gastroesophageal junction adenocarcinoma: the randomized phase 3 FRUTIGA trial Nat. Med. (IF 82.9) Pub Date : 2024-06-01 Feng Wang, Lin Shen, Weijian Guo, Tianshu Liu, Jin Li, Shukui Qin, Yuxian Bai, Zhendong Chen, Jufeng Wang, Yueyin Pan, Yongqian Shu, Fuyou Zhao, Ying Cheng, Feng Ye, Kangsheng Gu, Tao Zhang, Hongming Pan, Haijun Zhong, Fuxiang Zhou, Yanru Qin, Lei Yang, Weidong Mao, Qiu Li, Wenxiang Dai, Wei Li, Shubin Wang, Yong Tang, Dong Ma, Xianli Yin, Yanhong Deng, Ying Yuan, Man Li, Wenwei Hu, Donghui Chen, Guoxin
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Pembrolizumab for advanced urothelial carcinoma: exploratory ctDNA biomarker analyses of the KEYNOTE-361 phase 3 trial Nat. Med. (IF 82.9) Pub Date : 2024-06-01 Thomas Powles, Yen-Hwa Chang, Yoshiaki Yamamoto, Jose Munoz, Felipe Reyes-Cosmelli, Avivit Peer, Graham Cohen, Evan Y. Yu, Anja Lorch, Abhishek Bavle, Blanca Homet Moreno, Julia Markensohn, Mackenzie Edmondson, Cai Chen, Razvan Cristescu, Carol Pena, Jared Lunceford, Seyda Gunduz
Circulating tumor DNA (ctDNA) is emerging as a potential biomarker in early-stage urothelial cancer but its utility in metastatic disease remains unknown. In the phase 3 KEYNOTE-361 study, pembrolizumab with and without chemotherapy was compared with chemotherapy alone in patients with metastatic urothelial cancer. The study did not meet prespecified efficacy thresholds for statistical significance
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Surgery versus no surgery in platinum-sensitive relapsed ovarian cancer: final overall survival analysis of the SOC-1 randomized phase 3 trial Nat. Med. (IF 82.9) Pub Date : 2024-06-01 Rong Jiang, Yanling Feng, Yulian Chen, Xi Cheng, Tingyan Shi, Wen Gao, Huixun Jia, Shiyang Jiang, Yi Guo, Xiao Huang, Dongsheng Tu, Yuqin Zhang, Huijuan Yang, Ping Zhang, Jihong Liu, Jianqing Zhu, Rongyu Zang
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Mutations in the U4 snRNA gene RNU4-2 cause one of the most prevalent monogenic neurodevelopmental disorders Nat. Med. (IF 82.9) Pub Date : 2024-05-31 Daniel Greene, Chantal Thys, Ian R. Berry, Joanna Jarvis, Els Ortibus, Andrew D. Mumford, Kathleen Freson, Ernest Turro
Most people with intellectual disability (ID) do not receive a molecular diagnosis following genetic testing. To identify new etiologies of ID, we performed a genetic association analysis comparing the burden of rare variants in 41,132 non-coding genes between 5,529 unrelated cases and 46,401 unrelated controls. RNU4-2, which encodes U4 snRNA, a critical component of the spliceosome, was the most strongly
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Building trust and transparency in biomedical sciences through data walks Nat. Med. (IF 82.9) Pub Date : 2024-05-31 Layla Fattah, Jay Johnson, Uraina Clark, Leona Hess, Ann-Gel Palermo, Dania M. Figueroa Acosta, Talia H. Swartz
In biomedical education, inequities are driven mainly by systemic, structural and cultural issues1. These include disparities in access to educational resources, biases in admissions and unequal opportunities in research and clinical experiences2, with a curriculum that may not always cater to all students’ diverse needs and backgrounds. Additional challenges come from the varied nature of laboratory
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Structure-Based Design and Optimization of Methionine Adenosyltransferase 2A (MAT2A) Inhibitors with High Selectivity, Brain Penetration, and In Vivo Efficacy J. Med. Chem. (IF 7.3) Pub Date : 2024-05-31 Faridoon, Jiyue Zheng, Tao Zhang, Shuilong Tong, Tao Liu, Jiuen Cui, Haojie Xu, Di Hu, Ying Shen, Yajing Yin, Danhua Zhao, Chensheng Tan, Xue Dong, Jiali Chen, Feihong Ji, Chenhua Tong, Jie Jack Li, Jiapeng Li, Guiping Zhang
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Multiaction Pt(IV) Prodrugs Releasing Cisplatin and Dasatinib Are Potent Anticancer and Anti-Invasive Agents Displaying Synergism between the Two Drugs J. Med. Chem. (IF 7.3) Pub Date : 2024-05-31 Lenka Markova, Moumita Maji, Hana Kostrhunova, Vojtech Novohradsky, Jana Kasparkova, Dan Gibson, Viktor Brabec
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Systematic Structure–Activity Relationship Study of Nalfurafine Analogues toward Development of Potentially Nonaddictive Pain Management Treatments J. Med. Chem. (IF 7.3) Pub Date : 2024-05-30 Celsey M. St. Onge, Piyusha P. Pagare, Yi Zheng, Michelle Arriaga, David L. Stevens, Rolando E. Mendez, Justin L. Poklis, Matthew S. Halquist, Dana E. Selley, William L. Dewey, Matthew L. Banks, Yan Zhang
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Reducing seizures with senolytic drugs Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-31
Discover the world’s best science and medicine | Nature.com
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Assessing accuracy of AlphaFold2 Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-31
Discover the world’s best science and medicine | Nature.com
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Predicting ligand–protein interactions Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-31
Discover the world’s best science and medicine | Nature.com
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Designing reversible anticoagulants Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-31
Discover the world’s best science and medicine | Nature.com
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The changing landscape of cancer cell therapies: clinical trials and real-world data Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-31
Discover the world’s best science and medicine | Nature.com
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A Unique Hybridization Route to Access Hydrazylnaphthalimidols as Novel Structural Scaffolds of Multitargeting Broad-Spectrum Antifungal Candidates J. Med. Chem. (IF 7.3) Pub Date : 2024-05-30 Jin-Xin Wang, Peng-Li Zhang, Lavanya Gopala, Jing-Song Lv, Jian-Mei Lin, Cheng-He Zhou
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Design, Synthesis, and Structure–Activity Relationships of Novel Peptide Derivatives of the Severe Acute Respiratory Syndrome-Coronavirus-2 Spike-Protein that Potently Inhibit Nicotinic Acetylcholine Receptors J. Med. Chem. (IF 7.3) Pub Date : 2024-05-30 Arik J. Hone, Ulises Santiago, Peta J. Harvey, Bassel Tekarli, Joanna Gajewiak, David J. Craik, Carlos J. Camacho, J. Michael McIntosh
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Potency-Enhanced Peptidomimetic VHL Ligands with Improved Oral Bioavailability J. Med. Chem. (IF 7.3) Pub Date : 2024-05-29 Hao Wu, Jeremy Murray, Noriko Ishisoko, Alexandra Frommlet, Gauri Deshmukh, Antonio DiPasquale, Melinda M. Mulvihill, Donglu Zhang, John G. Quinn, Robert A. Blake, Wayne J. Fairbrother, Jakob Fuhrmann
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Discovery of Novel ERα and Aromatase Dual-Targeting PROTAC Degraders to Overcome Endocrine-Resistant Breast Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-05-29 Lilan Xin, Chao Wang, Yan Cheng, Hongli Wang, Xinyi Guo, Xiaofei Deng, Xiangping Deng, Baohua Xie, Hankun Hu, Chang Min, Chune Dong, Hai-Bing Zhou
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Searching for Synthetic Opioid Rescue Agents: Identification of a Potent Opioid Agonist with Reduced Respiratory Depression J. Med. Chem. (IF 7.3) Pub Date : 2024-05-29 Loan Y. Vu, Dan Luo, Kai Johnson, Emily D. Denehy, Judy C. Songrady, Jocelyn Martin, Riya Trivedi, Alexia R. Alsum, Jakob D. Shaykin, Chhabi L. Chaudhary, Eric J. Woloshin, Lindsay Kornberger, Nazmul Bhuiyan, Sean Parkin, Qianru Jiang, Tao Che, Warren Alilain, Jill R. Turner, Michael T. Bardo, Thomas E. Prisinzano
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2-Aryl-1H-imidazo[4,5-f][1,10]phenanthroline-Based Binuclear Ru(II)/Ir(III)/Re(I) Complexes as Mitochondria Targeting Cancer Stem Cell Therapeutic Agents# J. Med. Chem. (IF 7.3) Pub Date : 2024-05-29 Binoy Kar, Shanooja Shanavas, Arun Karmakar, Apoorva H. Nagendra, Seshu Vardhan, Suban K Sahoo, Bipasha Bose, Subrata Kundu, Priyankar Paira
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Discovery of Novel Non-Nucleoside Inhibitors Interacting with Dizinc Ions of CD73 J. Med. Chem. (IF 7.3) Pub Date : 2024-05-29 Cunjian Shi, Longfeng Chang, Jie Wang, Jingqi Dai, Wenyue Xu, Jiangyang Tang, Wenyi Mei, Chen Zhang, Zedong Wang, Yichen Liao, Xingsen Zhang, Wenzhe Jiang, Guozhen Zhang, Zhenjiang Zhao, Yufang Xu, Lili Zhu, Honglin Li
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Discovery of BMS-986308: A Renal Outer Medullary Potassium Channel Inhibitor for the Treatment of Heart Failure J. Med. Chem. (IF 7.3) Pub Date : 2024-05-29 Jeremy M. Richter, Prashantha Gunaga, Navnath Yadav, Rajesh Onkardas Bora, Rajeev Bhide, Nagendra Rajugowda, Kavitha Govindrajulu, Sreenivasulu Godesi, Nagarjuna Akuthota, Prasanna Rao, Aneesh Sivaraman, Manoranjan Panda, Mahammed Kaspady, Anuradha Gupta, Arvind Mathur, Paul C. Levesque, Jyoti Gulia, Manoj Dokania, Manjunath Ramarao, Prashant Kole, Silvi Chacko, Kimberley A. Lentz, Sankara Sivaprasad
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Point-of-care testing for sepsis in remote Australia and for First Nations peoples Nat. Med. (IF 82.9) Pub Date : 2024-05-30 Brooke Spaeth, Sean Taylor, Mark Shephard, Richard L. Reed, Rodney Omond, Jonathan Karnon, Billie Bonevski, Chris Rissel, Shahid Ullah, Tina Noutsos, Jacqueline H. Stephens, James A. Smith, Annabelle Wilson, Brett Abbenbroek, Emma de Courcy-Ireland, Simon Finfer
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Multimodal assessment improves neuroprognosis performance in clinically unresponsive critical-care patients with brain injury Nat. Med. (IF 82.9) Pub Date : 2024-05-30 B. Rohaut, C. Calligaris, B. Hermann, P. Perez, F. Faugeras, F. Raimondo, J-.R. King, D. Engemann, C. Marois, L. Le Guennec, L. Di Meglio, A. Sangaré, E. Munoz Musat, M. Valente, A. Ben Salah, A. Demertzi, L. Belloli, D. Manasova, L. Jodaitis, M. O. Habert, V. Lambrecq, N. Pyatigorskaya, D. Galanaud, L. Puybasset, N. Weiss, S. Demeret, F. X. Lejeune, J. D. Sitt, L. Naccache
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Three-year outcomes of post-acute sequelae of COVID-19 Nat. Med. (IF 82.9) Pub Date : 2024-05-30 Miao Cai, Yan Xie, Eric J. Topol, Ziyad Al-Aly
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Tumor infiltrating lymphocyte approval heralds new era for precision cancer immunotherapy Nat. Med. (IF 82.9) Pub Date : 2024-05-30
FDA approval of Iovance’s lifileucel for melanoma shows the promise of tumor-infiltrating lymphocytes for the treatment of solid tumors, with trials ongoing for lung cancer, cervical cancer and more.
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Dual-acting GLP-1 conjugate enhances weight loss Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-29
Discover the world’s best science and medicine | Nature.com
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Drug discovery for ageing: SIMPs, NEDs and screening challenges Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-29 Richard G. A. Faragher, Richard C. Hartley
Drugs that modulate fundamental mechanisms of ageing offer the promise of substantially improving the health of ageing populations, but innovative approaches to identify and evaluate such ‘gerotherapeutics’ are needed.
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A surprising abundance of pancreatic pre-cancers Nat. Med. (IF 82.9) Pub Date : 2024-05-29
AI-based three-dimensional genomic mapping reveals a large abundance of cancer precursors in normal pancreatic tissue — prompting new insights and research directions.
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Affordable and simplified whole-body MRI Nat. Med. (IF 82.9) Pub Date : 2024-05-29
A whole-body scanner developed using a permanent 0.05-tesla magnet and deep learning has demonstrated its versatility in imaging various anatomical structures, showcasing its potential to address unmet clinical needs.
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Discovery and Optimization of N-Arylated Tetracyclic Dicarboximides That Target Primary Glioma Stem-like Cells J. Med. Chem. (IF 7.3) Pub Date : 2024-05-28 Hua-Yu Wang, Thu P. Nguyen, Alex C. Sternisha, Christopher L. Carroll, Bethany Cross, Lorraine Morlock, Noelle S. Williams, Samuel McBrayer, Deepak Nijhawan, Jef K. De Brabander
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Discovery of ITI-333, a Novel Orally Bioavailable Molecule Targeting Multiple Receptors for the Treatment of Pain and Other Disorders J. Med. Chem. (IF 7.3) Pub Date : 2024-05-28 Peng Li, Qiang Zhang, Hailin Zheng, Yupu Qiao, Gretchen L. Snyder, Terry Martin, Wei Yao, Lei Zhang, Robert E. Davis
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Discovery of the Selective and Orally Available Galectin-1 Inhibitor GB1908 as a Potential Treatment for Lung Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-05-28 Fredrik R. Zetterberg, Kristoffer Peterson, Ulf J. Nilsson, Kajsa Andréasson Dahlgren, Carl Diehl, Ian Holyer, Maria Håkansson, Areej Khabut, Barbro Kahl-Knutson, Hakon Leffler, Alison C. MacKinnon, James A. Roper, Robert J. Slack, Reihaneh Zarrizi, Anders Pedersen
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Discovery of GLPG3667, a Selective ATP Competitive Tyrosine Kinase 2 Inhibitor for the Treatment of Autoimmune Diseases J. Med. Chem. (IF 7.3) Pub Date : 2024-05-28 Oscar Mammoliti, Sébastien Martina, Pieter Claes, Ghjuvanni Coti, Roland Blanque, Catherine Jagerschmidt, Kenji Shoji, Monica Borgonovi, Steve De Vos, Florence Marsais, Line Oste, Evelyne Quinton, Miriam López-Ramos, David Amantini, Reginald Brys, Juan-Miguel Jimenez, René Galien, Steven van der Plas
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Chb-M′, an Inhibitor of the RUNX Family Binding to DNA, Induces Apoptosis in p53-Mutated Non-Small Cell Lung Cancer and Inhibits Tumor Growth and Repopulation In Vivo J. Med. Chem. (IF 7.3) Pub Date : 2024-05-27 Yuki Hirose, Shinsuke Sato, Kaori Hashiya, Mitsuharu Ooga, Toshikazu Bando, Hiroshi Sugiyama
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Discovery of 3-((4-Benzylpyridin-2-yl)amino)benzamides as Potent GPR52 G Protein-Biased Agonists J. Med. Chem. (IF 7.3) Pub Date : 2024-05-24 Ryan E. Murphy, Pingyuan Wang, Saghir Ali, Hudson R. Smith, Daniel E. Felsing, Haiying Chen, Jia Zhou, John A. Allen
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Generating clinical evidence for treatment and prevention options for long COVID Nat. Med. (IF 82.9) Pub Date : 2024-05-28 Stephanie Buchholz, Eugenia Di Meco, Ewa Z. Bałkowiec-Iskra, Bruno Sepodes, Marco Cavaleri
Long COVID is a chronic and debilitating disease affecting more than 36 million people in the European Union (EU)1. Most patients are of working age, creating a high burden on healthcare and social systems2. At present, there are no EU-approved medicines for the treatment or prevention of long COVID. The long COVID therapeutic field is at a crossroads, with many study designs being proposed and used
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Noninvasive assessment of organ-specific and shared pathways in multi-organ fibrosis using T1 mapping Nat. Med. (IF 82.9) Pub Date : 2024-05-28 Victor Nauffal, Marcus D. R. Klarqvist, Matthew C. Hill, Danielle F. Pace, Paolo Di Achille, Seung Hoan Choi, Joel T. Rämö, James P. Pirruccello, Pulkit Singh, Shinwan Kany, Cody Hou, Kenney Ng, Anthony A. Philippakis, Puneet Batra, Steven A. Lubitz, Patrick T. Ellinor
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How medical schools can prepare students for new technologies Nat. Med. (IF 82.9) Pub Date : 2024-05-27 Chantal Mathieu
Patient educators and nurses can demonstrate the real-life use of health technologies.
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Novel quinoxaline analogs as telomeric G-quadruplex ligands exert antitumor effects related to enhanced immunomodulation Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-05-27 Jia-Xin Wang, Xiao-Dong Wang, Ming-Hao Hu
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Correction to “Unleashing the Potential of Camptothecin: Exploring Innovative Strategies for Structural Modification and Therapeutic Advancements” J. Med. Chem. (IF 7.3) Pub Date : 2024-05-22 Zheng Chen, Maoyu Liu, Ningyu Wang, Wenjing Xiao, Jianyou Shi
Page 3260. The structure of VIP236 (44) was incorrect in Figure 6. The corrected structure is shown here: Pages 3265 and 3266. In section 4.3.3, the payload released by VIP236 (44) was identified incorrectly; it is 21 and neither 19 nor 45 as written in the text on these pages. Three paragraphs in that section should be revised as follows: And VIP236 (44, Figure 6) is a SMDC that utilized an αvβ3 integrin-targeting
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What the SELECT trial of semaglutide means for clinicians Nat. Med. (IF 82.9) Pub Date : 2024-05-25 Naveed Sattar, Matthew M. Y. Lee, Darren K. McGuire
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IL-6 inhibition with clazakizumab in patients receiving maintenance dialysis: a randomized phase 2b trial Nat. Med. (IF 82.9) Pub Date : 2024-05-25 Glenn M. Chertow, Anna Marie Chang, G. Michael Felker, Mark Heise, Elena Velkoska, Bengt Fellström, David M. Charytan, Regina Clementi, C. Michael Gibson, Shaun G. Goodman, Meg Jardine, Adeera Levin, Yuliya Lokhnygina, Jenny Mears, Roxana Mehran, Peter Stenvinkel, Angela Wang, David C. Wheeler, Carmine Zoccali, Paul M. Ridker, Kenneth W. Mahaffey, Pierluigi Tricoci, Myles Wolf
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Long-term kidney outcomes of semaglutide in obesity and cardiovascular disease in the SELECT trial Nat. Med. (IF 82.9) Pub Date : 2024-05-25 Helen M. Colhoun, Ildiko Lingvay, Paul M. Brown, John Deanfield, Kirstine Brown-Frandsen, Steven E. Kahn, Jorge Plutzky, Koichi Node, Alexander Parkhomenko, Lars Rydén, John P. H. Wilding, Johannes F. E. Mann, Katherine R. Tuttle, Thomas Idorn, Naveen Rathor, A. Michael Lincoff
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Immune signatures of disease stages and outcomes in myocardial infarction Nat. Med. (IF 82.9) Pub Date : 2024-05-24
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Cyanomethylquinolones as a New Class of Potential Multitargeting Broad-Spectrum Antibacterial Agents J. Med. Chem. (IF 7.3) Pub Date : 2024-05-24 Yi-Min Tan, Jing Zhang, Yu-Jia Wei, Yue-Gao Hu, Shu-Rui Li, Shao-Lin Zhang, Cheng-He Zhou
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Design, Synthesis, and Biological Evaluation of New 2,6,7-Substituted Purine Derivatives as Toll-like Receptor 7 Agonists for Intranasal Vaccine Adjuvants J. Med. Chem. (IF 7.3) Pub Date : 2024-05-24 Morgan Kim, Kyungseob Noh, Pyeongkeun Kim, Jae Ho Kim, Byeong Wook Choi, Ravi Singh, Junho Choi, Soo Bong Han, Seong Soon Kim, Eun-Young Lee, Myung Ae Bae, Daeho Shin, Meehyein Kim, Jin Hee Ahn
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Emerging Targets and Therapeutics in Immuno-Oncology: Insights from Landscape Analysis J. Med. Chem. (IF 7.3) Pub Date : 2024-05-24 Kavita A. Iyer, Julian Ivanov, Rumiana Tenchov, Krittika Ralhan, Yacidzohara Rodriguez, Janet M. Sasso, Sabina Scott, Qiongqiong Angela Zhou
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Structure-Based Design of a Potent and Selective YTHDC1 Ligand J. Med. Chem. (IF 7.3) Pub Date : 2024-05-24 František Zálešák, Francesco Nai, Marcin Herok, Elena Bochenkova, Rajiv K. Bedi, Yaozong Li, Francesco Errani, Amedeo Caflisch
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Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε J. Med. Chem. (IF 7.3) Pub Date : 2024-05-23 Fernando H. de Souza Gama, Luiz A. Dutra, Michael Hawgood, Caio Vinícius dos Reis, Ricardo A. M. Serafim, Marcos A. Ferreira, Jr., Bruno V. M. Teodoro, Jéssica Emi Takarada, André S. Santiago, Dimitrios-Ilias Balourdas, Ann-Sofie Nilsson, Bruno Urien, Vitor M. Almeida, Carina Gileadi, Priscila Z. Ramos, Anita Salmazo, Stanley N. S. Vasconcelos, Micael R. Cunha, Susanne Mueller, Stefan Knapp, Katlin
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Construction of 5-Fluorouracil and Gallium Corrole Conjugates for Enhanced Photodynamic Therapy J. Med. Chem. (IF 7.3) Pub Date : 2024-05-23 Jing-He Cen, Qi-Hu Xie, Geng-Hong Guo, Shi-Yin Xu, Ze-Yu Liu, Yu-Hui Liao, Xiao-Ping Zhong, Hai-Yang Liu
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In Silico Assisted Identification, Synthesis, and In Vitro Pharmacological Characterization of Potent and Selective Blockers of the Epilepsy-Associated KCNT1 Channel J. Med. Chem. (IF 7.3) Pub Date : 2024-05-23 Nunzio Iraci, Lidia Carotenuto, Tania Ciaglia, Giorgio Belperio, Francesca Di Matteo, Ilaria Mosca, Giusy Carleo, Manuela Giovanna Basilicata, Paolo Ambrosino, Rita Turcio, Deborah Puzo, Giacomo Pepe, Isabel Gomez-Monterrey, Maria Virginia Soldovieri, Veronica Di Sarno, Pietro Campiglia, Francesco Miceli, Alessia Bertamino, Carmine Ostacolo, Maurizio Taglialatela
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Anti-TNF Thioester Glucocorticoid Antibody–Drug Conjugate Fully Inhibits Inflammation with Minimal Effect on Systemic Corticosterone Levels in a Mouse Arthritis Model J. Med. Chem. (IF 7.3) Pub Date : 2024-05-23 Christopher C. Marvin, Adrian D. Hobson, Michael J. McPherson, Martin E. Hayes, Meena V. Patel, Diana L. Schmidt, Tongmei Li, John T. Randolph, Agnieszka K. Bischoff, Julia Fitzgibbons, Lu Wang, Lu Wang, Axel Hernandez, Jr, Ying Jia, Christian A. Goess, Shaughn H. Bryant, Suzanne L. Mathieu, Jianwen Xu
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Site-Specific Antimicrobial Activity of a Dual-Responsive Ciprofloxacin Prodrug J. Med. Chem. (IF 7.3) Pub Date : 2024-05-23 Catherine L. Ross, Aggie Lawer, Kathleen J. Sircombe, Daniel Pletzer, Allan B. Gamble, Sarah Hook
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Study of the Conformational Dynamics of Prolyl Oligopeptidase by Mass Spectrometry: Lessons Learned J. Med. Chem. (IF 7.3) Pub Date : 2024-05-23 Roos Van Elzen, Anne-Marie Lambeir