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A Novel HER2 Protein Identification Methodology in Breast Cancer Cells Using Raman Spectroscopy and Raman Imaging: An Analytical Validation Study J. Med. Chem. (IF 6.8) Pub Date : 2024-09-21 Halina Abramczyk, Jakub Maciej Surmacki, Monika Kopeć
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High-Throughput Screening of Antioxidant Drug Candidates from Natural Antioxidants with a “Zero” Intrinsic Fluorescence Peroxynitrite Sensing Precursor J. Med. Chem. (IF 6.8) Pub Date : 2024-09-21 Hong Zhang, Guan-Nan Zhu, Fei-Fan Xiang, Yu-Jin Chen, Shan-Yong Chen, Min Wu, Kun Li
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Targeting Plasmodium falciparum IspD in the Methyl-d-erythritol Phosphate Pathway: Urea-Based Compounds with Nanomolar Potency on Target and Low-Micromolar Whole-Cell Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Daan Willocx, Lorenzo Bizzarri, Alaa Alhayek, Deepika Kannan, Patricia Bravo, Boris Illarionov, Katharina Rox, Jonas Lohse, Markus Fischer, Andreas M. Kany, Hannes Hahne, Matthias Rottmann, Matthias Witschel, Audrey Odom John, Mostafa M. Hamed, Eleonora Diamanti, Anna K. H. Hirsch
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Development of Fragment-Based Inhibitors of the Bacterial Deacetylase LpxC with Low Nanomolar Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Sebastian Mielniczuk, Katharina Hoff, Fady Baselious, Yunqi Li, Jörg Haupenthal, Andreas M. Kany, Maria Riedner, Holger Rohde, Katharina Rox, Anna K. H. Hirsch, Isabelle Krimm, Wolfgang Sippl, Ralph Holl
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Optimization of the Central α-Amino Acid in Cystobactamids to the Broad-Spectrum, Resistance-Breaking Antibiotic CN-CC-861 J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Daniel Kohnhäuser, Tim Seedorf, Katarina Cirnski, Dominik Heimann, Janetta Coetzee, Sylvie Sordello, Jana Richter, Moritz Stappert, Jean-Francois Sabuco, David Corbett, Eric Bacqué, Katharina Rox, Jennifer Herrmann, Aurelie Vassort, Rolf Müller, Andreas Kirschning, Mark Brönstrup
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Viral Protein Dimerization Quality Control: A Design Strategy for a Potential Viral Inhibitor J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Shaoqing Du, Xinyong Liu, Xueping Hu, Peng Zhan
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Fully Synthetic TF-Based Self-Adjuvanting Vaccine Simultaneously Triggers iNKT Cells and Mincle and Protects Mice against Tumor Development J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Deying Yang, Xiaohui Li, Jinmei Li, Zichun Liu, Tongtong Li, Pan Liao, Xiang Luo, Zhongqiu Liu, Wenbo Ming, Guochao Liao
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Structure Optimization of c-Jun N-terminal Kinase 1 Inhibitors for Treating Idiopathic Pulmonary Fibrosis J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Yi Huang, Fengling Liu, Shuhua Ren, Yuanqing Ding, Man Chi, Weiwei Huang, Wenjing Gu, Hewen Qian, Yaxia Yuan, Shurong Hou, Xiabin Chen, Lei Ma
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Deep-Learning-Driven Discovery of SN3–1, a Potent NLRP3 Inhibitor with Therapeutic Potential for Inflammatory Diseases J. Med. Chem. (IF 6.8) Pub Date : 2024-09-20 Cheng Shi, Tongfei Gao, Weiping Lyu, Bo Qiang, Yanming Chen, Qixuan Chen, Liangren Zhang, Zhenming Liu
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Synthesis and Antiosteoporotic Characterization of Diselenyl Maleimides: Discovery of a Potent Agent for the Treatment of Osteoporosis by Targeting RANKL J. Med. Chem. (IF 6.8) Pub Date : 2024-09-19 Bin Li, Yao Wu, Linkun Ying, Weiwei Zhu, Jingyi Yang, Lingling Zhou, Lele Yi, Tianle Jiang, Haofu Jiang, Xiangrui Song, Weiwei Xue, Guang Liang, Shengbin Huang, Zengqiang Song
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Polypharmacological Drug Design Guided by Integrating Phenotypic and Restricted Fragment Docking Strategies J. Med. Chem. (IF 6.8) Pub Date : 2024-09-19 Shang Li, Xinxin Li, Liangliang Ma, Zhongwen Luo, Fucheng Yin, Yonglei Zhang, Yifan Chen, Siyuan Wan, Han Zhou, Xiaobing Wang, Lingyi Kong
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Design, Synthesis, and Biological Evaluation of Lysine-Stapled Peptide Inhibitors of p53-MDM2/MDMX Interactions with Potent Antitumor Activity In Vivo J. Med. Chem. (IF 6.8) Pub Date : 2024-09-19 Lei Xu, Xin Fan, Yi He, Xuefeng Xia, Jinqiang Zhang
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From Hit to Lead: Discovery of First-In-Class Furanone Glycoside D228 Derived from Chimonanthus salicifolius for the Treatment of Inflammatory Bowel Disease J. Med. Chem. (IF 6.8) Pub Date : 2024-09-19 Mei-Lin Tang, Xiao-Yu Xiong, Heyanhao Zhang, Yun-Zhi Wang, Rong-Qian Cheng, Jianping Zuo, Lin Jin, Ze-Min Lin, Jun Chang
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Developing a Rhodium(III) Complex to Reprogram the Tumor Immune and Metabolic Microenvironments: Overcoming Multidrug Resistance and Metastasis in Non-Small Cell Lung Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-09-19 Wenjuan Li, Shanhe Li, Minghui Zhu, Gang Xu, Xueyu Man, Zhenlei Zhang, Hong Liang, Feng Yang
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Structure-Based Optimization of a Series of Covalent, Cell Active Bfl-1 Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-09-18 Simon C. C. Lucas, J. Henry Blackwell, Ulf Börjesson, David Hargreaves, Alexander G. Milbradt, Mark J. Bostock, Samiyah Ahmed, Kevin Beaumont, Tony Cheung, Sylvain Demanze, Andrea Gohlke, Carine Guerot, Afreen Haider, Vasudev Kantae, Gregory W. Kauffman, Olaf Kinzel, Lea Kupcova, Michael D. Lainchbury, Michelle L. Lamb, Leonardo Leon, Adeline Palisse, Claudia Sacchetto, R. Ian Storer, Nancy Su, Clare
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Peptidomimetic Analogues Act as Effective Inhibitors against SARS-CoV-2 by Blocking the Function of Cathepsin L J. Med. Chem. (IF 6.8) Pub Date : 2024-09-18 Weilong Deng, Xiao Hu, Xiaoman Tian, Yuanyuan Zhang, Weijuan Shang, Leike Zhang, Luqing Shang
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SAR Analysis of Novel Coxsackie virus A9 Capsid Binders J. Med. Chem. (IF 6.8) Pub Date : 2024-09-18 Chiara Tammaro, Zlatka Plavec, Laura Myllymäki, Cristopher Mitchell, Sara Consalvi, Mariangela Biava, Alessia Ciogli, Aušra Domanska, Valtteri Leppilampi, Cienna Buckner, Simone Manetto, Pietro Sciò, Antonio Coluccia, Mira Laajala, Giulio M. Dondio, Chiara Bigogno, Varpu Marjomäki, Sarah J. Butcher, Giovanna Poce
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Ursodeoxycholic Acid Platinum(IV) Conjugates as Antiproliferative and Antimetastatic Agents: Remodel the Tumor Microenvironment through Suppressing JAK2/STAT3 Signaling J. Med. Chem. (IF 6.8) Pub Date : 2024-09-18 Yan Chen, Ming Zhang, Zhifang Liu, Ning Zhang, Qingpeng Wang
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RNA-Binding Small Molecules in Drug Discovery and Delivery: An Overview from Fundamentals J. Med. Chem. (IF 6.8) Pub Date : 2024-09-17 Siyi Chen, Qi Mao, Hong Cheng, Wanyi Tai
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WazaGaY: An Innovative Aza-BODIPY-Derived Near-Infrared Fluorescent Probe for Enhanced Tumor Imaging J. Med. Chem. (IF 6.8) Pub Date : 2024-09-17 Mohamed Bendellaa, Charlotte Cave, Amélie Godard, Fabien Dalonneau, Annika Sickinger, Christine Goze, Olivier Maury, Pierre Le Gendre, Ewen Bodio, Benoit Busser, Lucie Sancey
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GPCRSPACE: A New GPCR Real Expanded Library Based on Large Language Models Architecture and Positive Sample Machine Learning Strategies J. Med. Chem. (IF 6.8) Pub Date : 2024-09-17 Shiming Chen, Feisheng Zhong
The quest for novel therapeutics targeting G protein-coupled receptors (GPCRs), essential in numerous physiological processes, is crucial in drug discovery. Despite the abundance of GPCR-targeting drugs, many receptors lack selective modulators, indicating a significant untapped therapeutic potential. To bridge this gap, we introduce GPCRSPACE, a novel GPCR-focused purchasable real chemical library
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Endoplasmic reticulum-targeted biomimetic nanoparticles induce apoptosis and ferroptosis by regulating endoplasmic reticulum function in colon cancer. J. Control. Release (IF 10.5) Pub Date : 2024-09-18 Hongxin Tan,Ziqi Shen,Xiaohua Wang,Sicheng Shu,Jie Deng,Li Lu,Ziyan Fan,Danni Hu,Pu Cheng,Xi Cao,Qi Huang
Colorectal cancer (CRC) is a major threat to human health, as it is one of the most common malignancies with a high incidence and mortality rate. The cancer cell membrane (CCM) has significant potential in targeted tumor drug delivery due to its membrane antigen-mediated homologous targeting ability. The endoplasmic reticulum (ER) in cancer cells plays a crucial role in apoptosis and ferroptosis. In
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Hybrids of 3-Hydroxypyridin-4(1H)-ones and Long-Chain 4-Aminoquinolines as Potent Biofilm Inhibitors of Pseudomonas aeruginosa Potentiate Tobramycin and Polymyxin B Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-09-17 Zhi-Ying Miao, Xiao-Yi Zhang, Hao-Zhong Long, Jing Lin, Wei-Min Chen
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Discovery of Novel [1,2,4]Triazolo[1,5-a]pyrimidine Derivatives as Novel Potent S-Phase Kinase-Associated Protein 2 (SKP2) Inhibitors for the Treatment of Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-09-16 Kaizhao Hu, Yongqiang Luo, Peipei Miao, Lidan Zhao, Bing Zhao, Xiao-Jing Shi, Hong-Min Liu
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In vivo CAR T cells move into clinical trials Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-09-16
Drug developers want to reprogramme immune cells directly in the body, opening up new gene therapy frontiers in cancer and autoimmunity.
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Synergistic Integration of mRNA-LNP with CAR-Engineered Immune Cells: Pioneering Progress in Immunotherapy. Mol. Ther. (IF 12.1) Pub Date : 2024-09-17 Zhaozhao Chen,Jinhui Shu,Yu Hu,Heng Mei
Chimeric antigen receptor T-cell (CAR-T) therapy has emerged as a revolutionary approach in the treatment of malignancies. Despite its remarkable successes, this field continues to grapple with challenges such as scalability, safety concerns, limited therapeutic effect, in vivo persistence, and the need for precise control over CAR expression. In the post-pandemic era of COVID-19 vaccine immunization
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Therapeutic CRISPR Epigenome Editing of Inflammatory Receptors in the Intervertebral Disc. Mol. Ther. (IF 12.1) Pub Date : 2024-09-17 Joshua D Stover,Matthew A R Trone,Jacob Weston,Christian Lewis,Hunter Levis,Niloofar Farhang,Matthew Philippi,Michelle Zeidan,Brandon Lawrence,Robby D Bowles
Low back pain (LBP) ranks among the leading causes of disability worldwide and generates a tremendous socioeconomic cost. Disc degeneration, a leading contributor to LBP, can be characterized by the breakdown of the extracellular matrix of the intervertebral disc (IVD), disc height loss, and inflammation. The inflammatory cytokine TNF-α has multiple signaling pathways, including proinflammatory signaling
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Hypermethylation and downregulation of microRNA219a-2 activates the ALDH1L2/GSH/PAI-1 pathway for fibronectin degradation in renal fibrosis. Mol. Ther. (IF 12.1) Pub Date : 2024-09-17 Qingqing Wei,Xiao Xiao,Emily Huo,Chunyuan Guo,Xiangjun Zhou,Xiaoru Hu,Charles Dong,Huidong Shi,Zheng Dong
Epigenetic regulations, such as DNA methylation and microRNAs, play an important role in renal fibrosis. Here, we report the regulation of microRNA-219a-2 by DNA methylation in fibrotic kidneys, unveiling the crosstalk between these epigenetic mechanisms. Through genome-wide DNA methylation analysis and pyro-sequencing, we detected the hypermethylation of microRNA219a-2 in renal fibrosis induced by
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Intranasal vaccination with engineered BCG expressing CCL2 induces a stronger immune barrier against Mycobacterium tuberculosis than BCG. Mol. Ther. (IF 12.1) Pub Date : 2024-09-17 Shaohua Guo,Jiangshan Ouyang,Zhiming Hu,Ting Cao,Chunxu Huang,Jun Mou,Xinxia Gu,Jie Liu
Intradermal Mycobacterium bovis Bacillus Calmette-Guérin (BCG) vaccination is currently the only licensed strategy for preventing tuberculosis (TB). It provides limited protection against pulmonary TB. To enhance the efficacy of BCG, we developed a recombinant BCG expressing exogenous monocyte chemoattractant CC chemokine ligand 2 (CCL2), termed rBCG-CCL2. Co-culturing macrophages with rBCG-CCL2 enhances
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Toward life without sickle cell disease. Mol. Ther. (IF 12.1) Pub Date : 2024-09-17 Utpal P Davé,Jörg Bungert
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Immune responses to cells and proteins after hematopoietic stem cell gene therapy for inherited diseases: A cause for concern. Mol. Ther. (IF 12.1) Pub Date : 2024-09-17 Nathan Jeffreys,Robert Wynn
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VSTM2A reverses immunosuppression in colorectal cancer through antagonizing PD-L1/PD-1 interaction. Mol. Ther. (IF 12.1) Pub Date : 2024-09-17 Yujuan Dong,Jiaxun Jade Liu,Yunfei Zhou,Wei Kang,Shanglin Li,Alvin Hk Cheung,Hu Yi,Rui Liao,Nathalie Wong,Chi Chun Wong,Simon Ng,Jun Yu
Immunoglobulin VSTM2A is a top-ranked secretory protein that frequently silenced during colorectal carcinogenesis, however, its role in immune modulation remains largely unknown. Bioinformatic and immunohistochemistry analysis of human colorectal specimens and Vstm2a+/- knockout mice indicated that VSTM2A positively correlated with CD8a and immune infiltration in both physiological and pathological
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Cyanocobalamin-loaded dissolving microneedles diminish skin inflammation in vivo. J. Control. Release (IF 10.5) Pub Date : 2024-09-17 Antonio José Guillot,Miquel Martínez-Navarrete,Rosa Maria Giner,Maria Carmen Recio,Helder A Santos,Ana Sara Cordeiro,Ana Melero
Inflammatory diseases of the skin have a considerable high prevalence worldwide and negatively impact the patients' quality of life. First line, standard therapies for these conditions inherently entail important side effects when used long term, particularly complicating the management of chronic cases. Therefore, there is a need to develop novel therapeutic strategies to offer reliable alternative
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Near-infrared and ultrasound triggered Pt/Pd-engineered cluster bombs for the treatment of solid tumors. J. Control. Release (IF 10.5) Pub Date : 2024-09-17 Min Liao,Qi Zhang,Jianbo Huang,Xiaotong Huang,Chong Cheng,Juan Tu,Dong Zhang,Qiang Lu,Lang Ma
Owing to the dense extracellular matrix and high interstitial fluid pressure in the tumor microenvironment, methods which enhance the permeation and retention of nano drugs into liver tumors remain unsatisfactory for successful tumor treatment. We designed a near-infrared (NIR)- and ultrasound (US)-triggered Pt/Pd-engineered "cluster bomb" (Pt/Pd-CB) which actively penetrates liver cancer cell membranes
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Discovery of A-910, a Highly Potent and Orally Bioavailable Dual MerTK/Axl-Selective Tyrosine Kinase Inhibitor J. Med. Chem. (IF 6.8) Pub Date : 2024-09-16 Yiyun Yu, Miyeon Jang, Julie Miyashiro, Richard F. Clark, Gui-Dong Zhu, Jane Gong, Yujia Dai, Robin R. Frey, Thomas D. Penning, Hadong Kim, Hyung Ki Lee, Jin Kwan Kim, Ki Moon Ryu, Seong Jin Park, Taeyoung Yoon, Tao Li, Matthew D. Kurnick, Nicolas J. Kapecki, Leiming Li, Jacob V. Gorman, Debra A. Montgomery, Vlasios Manaves, Kenneth D. Bromberg, Stella Z. Doktor, Ashish Thakur, Jin Wang, Heath A. Smith
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Enhanced Recognition Memory through Dual Modulation of Brain Carbonic Anhydrases and Cholinesterases J. Med. Chem. (IF 6.8) Pub Date : 2024-09-16 Alessio Nocentini, Alessia Costa, Alessandro Bonardi, Andrea Ammara, Simone Giovannuzzi, Andrea Petreni, Gianluca Bartolucci, Barbara Rani, Manuela Leri, Monica Bucciantini, José G. Fernández-Bolaños, Óscar López, Maria Beatrice Passani, Gustavo Provensi, Paola Gratteri, Claudiu T. Supuran
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Optimizing high-intensity focused ultrasound-induced immunogenic cell-death using passive cavitation mapping as a monitoring tool. J. Control. Release (IF 10.5) Pub Date : 2024-09-18 Yanou Engelen,Dmitri V Krysko,Iuliia Effimova,Karine Breckpot,Michel Versluis,Stefaan De Smedt,Guillaume Lajoinie,Ine Lentacker
Over the past decade, ultrasound (US) has gathered significant attention and research focus in the realm of medical treatments, particularly within the domain of anti-cancer therapies. This growing interest can be attributed to its non-invasive nature, precision in delivery, availability, and safety. While the conventional objective of US-based treatments to treat breast, prostate, and liver cancer
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Switchable PAMAM megamers for deep tumor penetration and enhanced cell uptake. J. Control. Release (IF 10.5) Pub Date : 2024-09-16 Effat Nekoueifard,Fatemeh Radmanesh,Ibrahim Zarkesh,Marzieh Ebrahimi,Mohamad Raoufi,Hamid Sadeghi Abandansari,Hossein Baharvand,Rassoul Dinarvand
Nanoparticles fabricated to deliver anticancer drugs are usually designed to present optimized tumor penetration and cell internalization. However, there are some barriers and difficulties with most current technologies. Herein, size and charge switchable polyamidoamine (PAMAM) megamers (SChPMs) were prepared for the delivery of doxorubicin (DOX). SChPMs were fabricated by connecting PAMAM dendrimers
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A new therapeutic strategy for infectious diseases against intracellular multidrug-resistant bacteria. J. Control. Release (IF 10.5) Pub Date : 2024-09-16 Zhao-Jie Wang,Yan-Yan Zhu,Li-Yu Bai,Dong-Mei Tang,Zhong-Shun Zhou,Mei-Zhen Wei,Jin-Biao He,Yu-Duan,Xiao-Dong Luo
Bacterial infections result in 7,700,000 deaths per year globally, with intracellular bacteria causing repeated and resistant infection. No drug is currently licenced for the treatment of intracellular bacteria. A new screening platform mimicking the host milieu has been established to explore phytochemical antibiotic adjuvants. Previously neglected isoprenylated flavonoids were found to be effective
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Thin-film freeze-drying of an influenza virus hemagglutinin mRNA vaccine in unilamellar lipid nanoparticles with blebs. J. Control. Release (IF 10.5) Pub Date : 2024-09-16 Qin Li,Ruiqi Shi,Haiyue Xu,Khaled AboulFotouh,Molly M H Sung,Thomas H Oguin,Madeline Hayes,Chaeho Moon,Huy M Dao,Houping Ni,Sawittree Sahakijpijarn,Chris Cano,Gregory J Davenport,Robert O Williams,Jon Le Huray,Zhengrong Cui,Drew Weissman
Messenger RNA (mRNA) vaccines have revolutionized the fight against infectious diseases and are poised to transform other therapeutic areas. Lipid nanoparticles (LNP) represent the most successful delivery system for mRNA. While the mRNA-LNP products currently in clinics are stored as frozen suspensions, there is evidence that freeze-drying mRNA-LNP into dry powders can potentially enable their storage
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Laser-responsive erastin-loaded chondroitin sulfate nanomedicine targeting CD44 and system xc- in liver cancer: A non-ferroptotic approach. J. Control. Release (IF 10.5) Pub Date : 2024-09-16 So-Yeol Yoo,Hyun Young Kim,Dong Hyun Kim,Wan Seob Shim,Sang Min Lee,Dong Hwan Lee,Jang Mo Koo,Ji Hoon Yoo,Seokjin Koh,Jong Chan Park,Jieun Yu,Jang Su Jeon,Min-Jun Baek,Dae-Duk Kim,Ji-Yoon Lee,Soo Jin Oh,Sang Kyum Kim,Jae-Young Lee,Keon Wook Kang
Erastin, a ferroptosis-inducing system xc- inhibitor, faces clinical challenges due to suboptimal physicochemical and pharmacokinetic properties, as well as relatively low potency and off-target toxicity. Addressing these, we developed ECINs, a novel laser-responsive erastin-loaded nanomedicine utilizing indocyanine green (ICG)-grafted chondroitin sulfate A (CSA) derivatives. Our aim was to improve
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Discovery and In Vivo Exploration of 1,3,4-Oxadiazole and α-Fluoroacrylate Containing IL-17 Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-09-14 Juraj Velcicky, Matthias R. Bauer, Achim Schlapbach, Guillaume Lapointe, Arndt Meyer, Markus Vögtle, Ernst Blum, Estelle Ngo, Catherine Rolando, Pierre Nimsgern, Sylvie Teixeira-Fouchard, Hansjoerg Lehmann, Pascal Furet, Frédéric Berst, Jens Schümann, Rowan Stringer, Patrice Larger, Cindy Schmid, Catriona T. Prendergast, Simone Riek, Patrick Schmutz, Sylvie Lehmann, Jörg Berghausen, Clemens Scheufler
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Elastase-targeting biomimic nanoplatform for neurovascular remodeling by inhibiting NETosis mediated AlM2 inflammasome activation in ischemic stroke. J. Control. Release (IF 10.5) Pub Date : 2024-09-18 Chunming Tang,Feng Jia,Min Wu,Yanling Wang,Xiaowei Lu,Jinyu Li,Yan Ding,Weilin Chen,Xufeng Chen,Feng Han,Huae Xu
Neutrophil elastase (NE) is a protease released by activated neutrophils in the brain parenchyma after cerebral ischemia, which plays a pivotal role in the regulation of neutrophil extracellular traps (NETs) formation. The excess NETs could lead to blood-brain barrier (BBB) breakdown, overwhelming neuroinflammation, and neuronal injury. While the potential of targeting neutrophils and inhibiting NE
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Wearable nitric oxide-releasing antibacterial insert for preventing device-associated infections. J. Control. Release (IF 10.5) Pub Date : 2024-09-15 Manjyot Kaur Chug,Aasma Sapkota,Mark Stephen Garren,Elizabeth J Brisbois
Medical device-associated infections are a pervasive global healthcare concern, often leading to severe complications. Bacterial biofilms that form on indwelling medical devices, such as catheters, are significant contributors to infections like bloodstream and urinary tract infections. This study addresses the challenge of biofilms on medical devices by introducing a portable antimicrobial catheter
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Development of Novel Indole-Based Covalent Inhibitors of TEAD as Potential Antiliver Cancer Agents J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Chen Zhou, Chunbao Sun, Wei Zhou, Tian Tian, Daniel C. Schultz, Tong Wu, Mu Yu, Lizi Wu, Liya Pi, Chenglong Li
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Between Theory and Practice: Computational/Experimental Integrated Approaches to Understand the Solubility and Lipophilicity of PROTACs J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Andrea Venturi, Stefano Di Bona, Jenny Desantis, Michela Eleuteri, Matteo Bartalucci, Massimo Baroni, Paolo Benedetti, Laura Goracci, Gabriele Cruciani
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Discovery and Development of Highly Potent and Orally Bioavailable Nonpeptidic αvβ6 Integrin Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Panayiotis A. Procopiou, John Barrett, Matthew H. J. Crawford, Richard J. D. Hatley, Ashley P. Hancock, John M. Pritchard, James E. Rowedder, Royston C. B. Copley, Robert J. Slack, Steven L. Sollis, Lee R. Thorp, Rhys A. Lippa, Simon J. F. Macdonald, Tim N. Barrett
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Design, Synthesis, and Bioevaluation of Novel NLRP3 Inhibitor with IBD Immunotherapy from the Virtual Screen J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Ziwen Zhang, Hongyu Wu, Kai Yin, Xinru Zheng, Zhonglian Cao, Wei Guo, Chunchang Zhao, Xianfeng Gu
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Targeting Thyroid-Stimulating Hormone Receptor: A Perspective on Small-Molecule Modulators and Their Therapeutic Potential J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Yu Zhang, Ye Tan, Zian Zhang, Xi Cheng, Jia Duan, Yi Li
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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
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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
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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.
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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
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Biofilm-camouflaged Prussian blue synergistic mitochondrial mass enhancement for Alzheimer's disease based on Cu2+ chelation and photothermal therapy J. Control. Release (IF 10.5) Pub Date : 2024-09-13 Lianxin Li, Yu Xiong, Yuewen Zhang, Yujiao Yan, Ruixin Zhao, Fengmei Yang, Meng Xie
Alzheimer's disease (AD) is one of the most common neurodegenerative diseases characterized by cognitive and memory impairment. Metal ion imbalance and Mitochondrial dysfunction, leading to abnormal aggregation of β-amyloid protein (Aβ), are key factors in the pathogenesis of AD. Therefore, we designed a composite nanometer system of red blood cell (RBC) membranes-encapsulated Prussian blue nanoparticles
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Melittin-incorporated nanomedicines for enhanced cancer immunotherapy J. Control. Release (IF 10.5) Pub Date : 2024-09-13 Xuefeng Duan, Haoyang Zou, Jiazhen Yang, Shixian Liu, Tianmin Xu, Jianxun Ding
Immunotherapy is a rapidly developing and effective strategy for cancer therapy. Among various immunotherapy approaches, peptides have garnered significant attention due to their potent immunomodulatory effects. In particular, melittin emerged as a promising candidate to enhance cancer immunotherapy by inducing immunogenic cell death, promoting the maturation of antigen-presenting cells, activating
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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
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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
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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