-
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.
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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.
-
Navigating treatment combinations in small-cell lung cancer Nat. Med. (IF 58.7) Pub Date : 2024-09-18 Ning Li, Si-Yu Wang
-
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
-
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.
-
Exposure to extreme heat increases perinatal mortality in sub-Saharan Africa Nat. Med. (IF 58.7) Pub Date : 2024-09-17
-
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
-
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 Thomson,John Vales,Yunhua Chen
Bfl-1, a member of the Bcl-2 family of proteins, plays a crucial role in apoptosis regulation and has been implicated in cancer cell survival and resistance to venetoclax therapy. Due to the unique cysteine residue in the BH3 binding site, the development of covalent inhibitors targeting Bfl-1 represents a promising strategy for cancer treatment. Herein, the optimization of a covalent cellular tool
-
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
-
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
-
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.
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
Discovery of SIRT1-Activating Hydrogen Sulfide Donating Derivatives for Efficient Resistant of Myocardial Ischemic Injury J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Shenglin Wang, Dongyan Feng, Weirenbo Wang, Chao Zheng, Chaowei Liang, Siqing Li, Haonan Li, Fanxing Xu, Hao Cao, Huiming Hua, Maosheng Cheng, Dahong Li
-
Antibacterial and Anti-Inflammatory Activity of Branched Peptides Derived from Natural Host Defense Sequences J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Giada Meogrossi, Eva Tollapi, Alessandro Rencinai, Jlenia Brunetti, Silvia Scali, Eugenio Paccagnini, Mariangela Gentile, Pietro Lupetti, Simona Pollini, Gian Maria Rossolini, Andrea Bernini, Alessandro Pini, Luisa Bracci, Chiara Falciani
-
Creating an AI-first drug discovery engine Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-09-13
Najat Khan — Chief R&D Officer and Chief Commercial Officer at Recursion — discusses the proposed merger of Recursion and Exscientia.
-
Advancing ASO therapies from development to implementation Nat. Med. (IF 58.7) Pub Date : 2024-09-13 Rebecca Schuele, Matthis Synofzik, Holm Graessner, Annemieke Aartsma-Rus
-
Post-approval evidence generation: a shared responsibility for healthcare Nat. Med. (IF 58.7) Pub Date : 2024-09-13 Ali Abbasi, Donna Rivera, Lesley H. Curtis, Robert M. Califf
-
Trastuzumab deruxtecan in HER2-positive advanced breast cancer with or without brain metastases: a phase 3b/4 trial Nat. Med. (IF 58.7) Pub Date : 2024-09-13 Nadia Harbeck, Eva Ciruelos, Guy Jerusalem, Volkmar Müller, Naoki Niikura, Giuseppe Viale, Rupert Bartsch, Christian Kurzeder, Michaela J. Higgins, Roisin M. Connolly, Sally Baron-Hay, María Gión, Valentina Guarneri, Giampaolo Bianchini, Hans Wildiers, Santiago Escrivá-de-Romaní, Manoj Prahladan, Helen Bridge, Nataliya Kuptsova-Clarkson, Nana Scotto, Sunil Verma, Nancy U. Lin
-
Initiating second-trimester medical abortions at home Nat. Med. (IF 58.7) Pub Date : 2024-09-12
In people undergoing medical abortion after 12 weeks of pregnancy, those who took the first dose of misoprostol at home were less likely to require overnight hospitalization.
-
Author Correction: Antimalarial drug discovery: progress and approaches. Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-09-13 Jair L Siqueira-Neto,Kathryn J Wicht,Kelly Chibale,Jeremy N Burrows,David A Fidock,Elizabeth A Winzeler
-
Novel mechanistic insights – A brand new Era for anti-HBV drugs Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-09-13 Weiping Lyu, Haoming Qin, Qi Li, Dehua Lu, Cheng Shi, Kangchen Zhao, Shengran Zhang, Ruohan Yu, Huiying Zhang, Xiaonan Zhou, Sitian Xia, Liangren Zhang, Xiaoqian Wang, Xiaowei Chi, Zhenming Liu
Hepatitis B Virus (HBV) remains a critical global health issue, with substantial morbidity and mortality. Current therapies, including interferons and nucleoside analogs, often fail to achieve complete cure or functional eradication. This review explores recent advances in anti-HBV agents, focusing on their innovative mechanisms of action. HBV entry inhibitors target the sodium taurocholate cotransporting
-
CETZOLE Analogs as Potent Ferroptosis Inducers and Their Target Identification Using Covalent/Affinity Probes J. Med. Chem. (IF 6.8) Pub Date : 2024-09-12 Samkeliso Dlamini, Shahrzad Mohajeri, Nishanth Kuganesan, Shaimaa H. Sindi, Endri Karaj, Dewmi S. Rathnayake, Jade McDaniel, William R. Taylor, L. M. Viranga Tillekeratne
-
Discovery of 2-Aryl-4-aminoquinazolin-Based LSD1 Inhibitors to Activate Immune Response in Gastric Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-09-12 Bo Wang, Shu-Wu Wang, Ying Zhou, Shao-Peng Wang, Ya Gao, Hui-Min Liu, Shi-Kun Ji, Sai-Qi Wang, Yi-Chao Zheng, Cheng Zhang, Adil Mardinoglu, Hong-Min Liu, Xiao-Bing Chen, Xing-Jie Dai
-
Evaluation of Efficiency of Liposome-Entrapped Iridium(III) Complexes Inhibiting Tumor Growth In Vitro and In Vivo J. Med. Chem. (IF 6.8) Pub Date : 2024-09-12 Huiyan Hu, Jing Chen, Fan Zhang, Zhujun Sheng, Yan Yang, Yufeng Xie, Lin Zhou, Yunjun Liu
-
Development of a First-in-Class DNMT1/HDAC Inhibitor with Improved Therapeutic Potential and Potentiated Antitumor Immunity J. Med. Chem. (IF 6.8) Pub Date : 2024-09-12 Yingjie Chang, Huahui Guo, Xue Li, Liangyi Zong, Jiale Wei, Zhihai Li, Cheng Luo, Xinying Yang, Hao Fang, Xiangqian Kong, Xuben Hou
-
Tuning RXR Modulators for PGC1α Recruitment J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Felix Nawa, Minh Sai, Jan Vietor, Roman Schwarzenbach, Anesa Bitić, Sina Wolff, Niklas Ildefeld, Jörg Pabel, Thomas Wein, Julian A. Marschner, Jan Heering, Daniel Merk
-
Inhibition of the EphA2-Sam/Ship2-Sam Association through Peptide Ligands: Studying the Combined Effect of Charge and Aromatic Character J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Marian Vincenzi, Flavia A. Mercurio, Rosanna Palumbo, Sara La Manna, Luciano Pirone, Daniela Marasco, Emilia M. Pedone, Marilisa Leone
-
Dually Labeled Neurotensin NTS1R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Fabian J. Ertl, Sergei Kopanchuk, Nicola C. Dijon, Santa Veikšina, Maris-Johanna Tahk, Tõnis Laasfeld, Franziska Schettler, Albert O. Gattor, Harald Hübner, Nataliya Archipowa, Johannes Köckenberger, Markus R. Heinrich, Peter Gmeiner, Roger J. Kutta, Nicholas D. Holliday, Ago Rinken, Max Keller
-
Targeting HSP90 for Cancer Therapy: Current Progress and Emerging Prospects J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Xinqi Liang, Ruixian Chen, Chengdi Wang, Yuxi Wang, Jifa Zhang
-
The European Health Data Space can be a boost for research beyond borders Nat. Med. (IF 58.7) Pub Date : 2024-09-12 Andrea Ganna, Angel Carracedo, Christian F. Christiansen, Emanuele Di Angelantonio, Pearl A. Dykstra, Angel M. Dzhambov, Roland Eils, Sara Green, Katharina L. Schneider, Tibor V. Varga, Anna-Leena Vuorinen, Luisa Zuccolo, Naja Hulvej Rod, Klaus Hoeyer
The European Health Data Space provides an opportunity to benefit patients and the public.
-
An open-source framework for end-to-end analysis of electronic health record data Nat. Med. (IF 58.7) Pub Date : 2024-09-12 Lukas Heumos, Philipp Ehmele, Tim Treis, Julius Upmeier zu Belzen, Eljas Roellin, Lilly May, Altana Namsaraeva, Nastassya Horlava, Vladimir A. Shitov, Xinyue Zhang, Luke Zappia, Rainer Knoll, Niklas J. Lang, Leon Hetzel, Isaac Virshup, Lisa Sikkema, Fabiola Curion, Roland Eils, Herbert B. Schiller, Anne Hilgendorff, Fabian J. Theis
-
Safety and antiviral effect of a triple combination of HIV-1 broadly neutralizing antibodies: a phase 1/2a trial Nat. Med. (IF 58.7) Pub Date : 2024-09-12 Boris Julg, Victoria E. K. Walker-Sperling, Kshitij Wagh, Malika Aid, Kathryn E. Stephenson, Rebecca Zash, Jinyan Liu, Joseph P. Nkolola, Amelia Hoyt, Mike Castro, Leonid Serebryannyy, Katherine Yanosick, Tessa Speidel, Erica N. Borducchi, Tetyana Murzda, Lori Maxfield, Roberto Arduino, Adrian B. McDermott, Lucio Gama, Elena E. Giorgi, Richard A. Koup, Michael S. Seaman, Charlotte-Paige Rolle, Edwin
-
Overview of the PRMT6 modulators in cancer treatment: Current progress and emerged opportunity Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-09-12 Jinjin Peng, Bin Ni, Deping Li, Binbin Cheng, Renze Yang
Protein Arginine Methyltransferase 6 (PRMT6) is a Type I PRMT enzyme that plays a role in the epigenetic regulation of gene expression by methylating histone and non-histone proteins. It is also involved in various cellular processes, including alternative splicing, DNA repair, and cell signaling. Furthermore, PRMT6 exerts multiple effects on cellular processes such as growth, migration, invasion,
-
Discovery of the therapeutic potential of PPARδ agonist bearing 1,3,4- thiadiazole in inflammatory disorders Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-09-12 Jina Kim, Tara Man Kadayat, Jae-Eon Lee, Sugyeong Kwon, Kyungjin Jung, Ji Sun Hwang, Oh-bin Kwon, Ye Jin Kim, Yeon-Kyung Choi, Keun-Gyu Park, Hayoung Hwang, Sung Jin Cho, Taeho Lee, Yong Hyun Jeon, Jungwook Chin
As a defense mechanism against deleterious stimuli, inflammation plays a vital role in the development of many disorders, including atherosclerosis, inflammatory bowel disease, experimental autoimmune encephalomyelitis, septic and non-septic shock, and non-alcoholic fatty liver disease (NAFLD). Despite the serious adverse effects of extended usage, traditional anti-inflammatory medications, such as
-
Discovery, synthesis and biological evaluation of novel isoquinoline derivatives as potent indoleamine 2, 3-dioxygenase 1 and tryptophan 2, 3-dioxygenase dual inhibitors Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-09-12 Zhiqian Lin, Xiangli Ning, Ruizhi Lai, Li Hai, Ruifang Nie, Li Guo, Guobo Li, Zhongzhen Yang, Yong Wu
Indoleamine 2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO) play a pivotal role in regulating kynurenine catabolism pathway and immunosuppressive environment, which are promising drug targets for cancer immunotherapy. In this work, a variety of isoquinoline derivatives were designed, synthesized and evaluated for the inhibitory activity against IDO1 and TDO. The enzymatic assay and structure-activity
-
Discovery of SILA-123 as a Highly Potent FLT3 Inhibitor for the Treatment of Acute Myeloid Leukemia with Various FLT3 Mutations J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Tian-Hua Wei, Zi-Xuan Wang, Meng-Yi Lu, Yu-Jing Xu, Jin Yang, Xing-Feng Ni, Yang Cheng, Meng-Yuan Zhang, Jia-Chuan Liu, Qing-Qing Li, Jiao Cai, Zi-Jun Chen, Ji-Bo Kang, Nan Li, Wei-Chen Dai, Ning Ding, Yan-Cheng Yu, Xue-Jiao Leng, Xin Xue, Xiao-Long Wang, Shan-Liang Sun, Ye Yang, Nian-Guang Li, Zhi-Hao Shi
-
Preclinical Evaluation of Dihydropyrazole-Cored Positron Emission Tomography (PET) Ligands for Imaging of Receptor-Interacting Serine/Threonine Protein Kinase 1 (RIPK1) in the Brain J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Wanqing Li, Xiaojun Zhang, Jie Ma, Jingyin Zhou, Xuan Di, Donglan Huang, Kaixiang Zhou, Jinming Zhang, Lu Wang, Hualong Fu, Mengchao Cui
-
Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Robert L. Hudkins, Eric Allen, Alexandra Balcer, Isaac D. Hoffman, Samhita Iyer, Melissa Neal, Kirk J. Nelson, Marc Rideout, Qing Ye, Jacqueline H. Starrett, Piyush Patel, Todd Harris, Ronald V. Swanson, Daniel C. Bensen
-
Discovery of N-Aryl-N′-[4-(aryloxy)cyclohexyl]squaramide-Based Inhibitors of LXR/SREBP-1c Signaling Pathway Ameliorating Steatotic Liver Disease: Navigating the Role of SIRT6 Activation J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Long Huu Nguyen, Ye Eun Cho, Soyeong Kim, Yeonsoo Kim, Jinsook Kwak, Jung-Soo Suh, Jinyoung Lee, Kyuwon Son, Minseong Kim, Eun Seo Jang, Naghyun Song, BuChul Choi, Jiah Kim, Yealin Tak, Taeyeon Hwang, Jeyun Jo, Eun-Woo Lee, Sang-Bum Kim, Sanghyun Kim, Oh-Bin Kwon, Sangok Kim, Seoung Rak Lee, Haeseung Lee, Tae-Jin Kim, Seonghwan Hwang, Hwayoung Yun
-
Membrane-Targeting Amphiphilic Honokiol Derivatives Containing an Oxazole Moiety as Potential Antibacterials against Methicillin-Resistant Staphylococcus aureus J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Ruige Yang, Liping Cui, Shengnan Xu, Yan Zhong, Ting Xu, Jifeng Liu, Zhenwei Lan, Shangshang Qin, Yong Guo