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The benefits of translating biomedical research at drug discovery institutes Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-09-26 David J. Huggins, Jonathan Baell, Paul E. Brennan, Alex Burgin, Duncan E. Scott
Drug discovery institutes comprised of experienced drug discovery scientists collaborating with fundamental biomedical researchers provide solutions to many of the challenges in translating biomedical research.
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Syntheses of LSD1/HDAC Inhibitors with Demonstrated Efficacy against Colorectal Cancer: In Vitro and In Vivo Studies Including Patient-Derived Organoids J. Med. Chem. (IF 6.8) Pub Date : 2024-09-25 Po-Yu Chou, Mei-Jung Lai, Kelvin K. Tsai, Li-Hsin Cheng, Yi-Wen Wu, Mei-Chuan Chen, Shiow-Lin Pan, Hsiu-O Ho, Kunal Nepali, Jing-Ping Liou
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Design, Synthesis, and Biological Evaluation of Covalently Mucoadhesive Derivatives as Nonsystemic Intestine-Targeted TGR5 Agonists J. Med. Chem. (IF 6.8) Pub Date : 2024-09-25 Shizhen Zhao, Le Wang, Xiaotong Huang, Yali Xiao, Mengqi Li, Xueyuan Huang, Xueyu Chen, Shengjie Li, Jing Xie, Peng Liu, Yan-Dong Wang, Wei-Dong Chen
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First Demonstration of In Vivo PDE11A4 Target Engagement for Potential Treatment of Age-Related Memory Disorders J. Med. Chem. (IF 6.8) Pub Date : 2024-09-25 Shams ul Mahmood, Jeremy Eberhard, Charles S. Hoffman, Dennis Colussi, John Gordon, Wayne Childers, Elvis Amurrio, Janvi Patel, Michy P. Kelly, David P. Rotella
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68Ga/177Lu-Labeled Theranostic Pair for Targeting Fibroblast Activation Protein with Improved Tumor Uptake and Retention J. Med. Chem. (IF 6.8) Pub Date : 2024-09-25 Jiawen Huang, Xiaojun Zhang, Qingxing Liu, Fengping Gong, Yanchao Huang, Shun Huang, Lilan Fu, Ganghua Tang
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A Highly Atom-Efficient Prodrug Approach to Generate Synergy between H2S and Nonsteroidal Anti-inflammatory Drugs and Improve Safety J. Med. Chem. (IF 6.8) Pub Date : 2024-09-24 Wen Peng, Lixiao Qin, Tianci Wang, Yangqian Sun, Zhen Li, David J. Lefer, Cheng Luo, Fei Ye, Binghe Wang, Weiwei Guo, Yueqin Zheng
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New Applications of Sulfonyl Fluorides: A Microcosm of the Deep Integration of Chemistry and Biology in Drug Design J. Med. Chem. (IF 6.8) Pub Date : 2024-09-24 Shaoqing Du, Xueping Hu, Craig W. Lindsley, Peng Zhan
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Career Transitions That Require a Lot of Energy and Take You to Excited States Will Eventually Result in Brighter Professional Achievements J. Med. Chem. (IF 6.8) Pub Date : 2024-09-24 Cristiano R. W. Guimarães
People who know me well must have figured out by this point that I have a weak spot for bad jokes, puns, and analogies. So, it was not that difficult to come up with a dorky title for an Editorial in J. Med. Chem. about career transitions, based on my personal experience, that has resonance (pun intended) with chemists beyond the topic at hand. In the early 1990s, living in Rio de Janeiro, still in
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Boosting Med Chem Education: Integrating Biology for Drug Discovery Talents J. Med. Chem. (IF 6.8) Pub Date : 2024-09-24 Qiu Sun, Liang Ouyang
In the rapidly evolving field of drug discovery and development, the close collaboration between medicinal chemistry and biological science has reached unprecedented strategic heights. With the continuous deepening of understanding of disease mechanisms and the expansion of drug target diversity, breakthroughs in a single discipline are no longer sufficient to meet the needs of complex disease treatment
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Targeting neurofibrosis reverses metabolic dysfunction Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-09-25
Discover the world’s best science and medicine | Nature.com
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A tale of two ecosystems: the biopharma landscape in China and India Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-09-25
Discover the world’s best science and medicine | Nature.com
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Agonist antibody lowers blood pressure Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-09-23
Discover the world’s best science and medicine | Nature.com
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The AMR Accelerator: from individual organizations to efficient antibiotic development partnerships Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-09-23 Josepine Fernow, Marie Olliver, William Couet, Sophie Lagrange, Meindert H. Lamers, Ole F. Olesen, Kristina Orrling, Michel Pieren, Derek J. Sloan, Juan José Vaquero, Timothy J. Miles, Anders Karlén
The AMR Accelerator is an Innovative Medicines Initiative programme integrating nine projects with the shared goal of progressing the development of new antibiotics and building antimicrobial resistance research capability. Five years in, we reflect on the programme’s value, results and key challenge: ensuring the sustainability of assets, infrastructures and expertise.
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Publisher Correction: Strategies to therapeutically modulate cytokine action Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-09-20 Warren J. Leonard, Jian-Xin Lin
Correction to: Nature Reviews Drug Discovery https://doi.org/10.1038/s41573-023-00746-x, published online 4 August 2023.
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Use of the Novel Site-Directed Enzyme Enhancement Therapy (SEE-Tx) Drug Discovery Platform to Identify Pharmacological Chaperones for Glutaric Acidemia Type 1 J. Med. Chem. (IF 6.8) Pub Date : 2024-09-23 Madalena Barroso, Alexandra Puchwein-Schwepcke, Lars Buettner, Ingrid Goebel, Katrin Küchler, Ania C. Muntau, Aida Delgado, Ana M. Garcia-Collazo, Marc Martinell, Xavier Barril, Elena Cubero, Søren W. Gersting
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Discovery of AK-1690: A Potent and Highly Selective STAT6 PROTAC Degrader J. Med. Chem. (IF 6.8) Pub Date : 2024-09-23 Atsunori Kaneshige, Yiqing Yang, Longchuan Bai, Mi Wang, Renqi Xu, Leena Mallik, Krishnapriya Chinnaswamy, Hoda Metwally, Yu Wang, Donna McEachern, Jelena Tošović, Chao-Yie Yang, Paul D. Kirchhoff, Jennifer L. Meagher, Jeanne A. Stuckey, Shaomeng Wang
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Novel 18F-Labeled Benzimidazolone-Based Radioligands as Highly Selective Sigma-2 Receptor Probes for Tumor Imaging J. Med. Chem. (IF 6.8) Pub Date : 2024-09-23 Jingqi Wang, Tao Wang, Tiantian Mou, Tao Yang, Xu Gao, Xiaodan An, Biao Hu, Jinming Zhang, Xiaoli Zhang, Winnie Deuther-Conrad, Yiyun Huang, Hongmei Jia
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Discovery of a Potent, Orally Active, and Long-Lasting P2X7 Receptor Antagonist as a Preclinical Candidate for Delaying the Progression of Chronic Kidney Disease J. Med. Chem. (IF 6.8) Pub Date : 2024-09-23 Ruijia Zhang, Kaiyue Su, Letian Yang, Huaichuan Duan, Lei Tang, Minghai Tang, Min Zhao, Neng Ye, Xiaoying Cai, Xueqin Jiang, Na Li, Jing Peng, Xinlu Zhang, Lingkai Tang, Qiang Qiu, Lijuan Chen, Wenshuang Wu, Jianping Hu, Liang Ma, Haoyu Ye
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Ruthenium(ii)–Arene Complex Triggers Immunogenic Ferroptosis for Reversing Drug Resistance J. Med. Chem. (IF 6.8) Pub Date : 2024-09-23 Mengdi Lv, Yue Zheng, Xiangyu Dai, Jingyue Zhao, Guojing Hu, Meng Ren, Zhengqi Shen, Zhi Su, Chao Wu, Hong-Ke Liu, Xuling Xue, Zong-Wan Mao
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Computationally Driven Discovery of a BCR-ABL1 Kinase Inhibitor with Activity in Multidrug-Resistant Chronic Myeloid Leukemia J. Med. Chem. (IF 6.8) Pub Date : 2024-09-23 Jarvis Hill, R. Houston Givhan, Bin Yi, Robert M. Jones, Eugene F. Douglass, Yaguang Xi, Henry F. Schaefer III, David Crich
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Journal of Medicinal Chemistry Collection: Drug Discovery in Japan J. Med. Chem. (IF 6.8) Pub Date : 2024-09-23 Takayoshi Suzuki, Haruto Kurata, Tomohiko Ohwada, Hideyuki Onodera
The Journal of Medicinal Chemistry is pleased to introduce a Collection on Drug Discovery in Japan, featuring articles published in the journal between January 2020 and June 2024. The history of drug discovery in Japan began in 1887, when Dr. Nagayoshi Nagai extracted ephedrine from the ephedra herb, which later became a remedy for asthma. Subsequently, many natural products and natural product-based
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Small-Molecule Radiotracers for Visualization of V-Domain Immunoglobulin Suppressor of T Cell Activation J. Med. Chem. (IF 6.8) Pub Date : 2024-09-21 Jia Liu, Yuanyuan Liang, Hongzhang Yang, Xueqi Wang, Xinying Zeng, Rongqiang Zhuang, Jin Du, Xianzhong Zhang, Zhide Guo
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Single-cell RNA-sequencing reveals anti-tumor potency of CD56+ NK cells and CD8+ T cells in humanized mice via PD-1 and TIGIT co-targeting. Mol. Ther. (IF 12.1) Pub Date : 2024-09-23 Wai Nam Liu,Sarah L Harden,Shawn Lu Wen Tan,Rachel Jun Rou Tan,Shin Yie Fong,Sue Yee Tan,Min Liu,Isha Karnik,Timothy Wai Ho Shuen,Han Chong Toh,Yong Fan,Seng Gee Lim,Jerry Kok Yen Chan,Qingfeng Chen
In solid tumors, the exhaustion of natural killer (NK) cells and cytotoxic T cells in the immunosuppressive tumor microenvironment poses challenges for effective tumor control. Conventional humanized mouse models of hepatocellular carcinoma-patient-derived xenografts (HCC-PDX) encounter limitations in NK-cell infiltration, hindering studies on NK-cell immunobiology. Here, we introduce an improved humanized
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CITED4 gene therapy: Can it be cited for preventing maladaptive post-ischemic cardiac remodeling? Mol. Ther. (IF 12.1) Pub Date : 2024-09-23 Henry Nording,Oliver J Müller
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Microfluidic formulation, cryoprotection and long-term stability of paclitaxel-loaded π electron-stabilized polymeric micelles. J. Control. Release (IF 10.5) Pub Date : 2024-09-23 Rahaf Mihyar,Armin Azadkhah Shalmani,Viktor Wildt,Maryam Sheybanifard,Alec Wang,Jan-Niklas May,Saba Shahzad,Eva Miriam Buhl,Stephan Rütten,Diana Behrens,Wolfgang Walther,Mattia Tiboni,Luca Casettari,Johannes F Buyel,Cristianne J F Rijcken,Wim E Hennink,Saskia von Stillfried,Fabian Kiessling,Yang Shi,Josbert M Metselaar,Twan Lammers,Quim Peña
Controlled manufacturing and long-term stability are key challenges in the development and translation of nanomedicines. This is exemplified by the mRNA-nanoparticle vaccines against COVID-19, which require (ultra-)cold temperatures for storage and shipment. Various cryogenic protocols have been explored to prolong nanomedicine shelf-life. However, freezing typically induces high mechanical stress
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Dual osmotic controlled release platform for antibiotics to overcome antimicrobial-resistant infections and promote wound healing. J. Control. Release (IF 10.5) Pub Date : 2024-09-23 Wanni Cai,Yan Song,Qing Xie,Shiyu Wang,Donghong Yin,Shuyun Wang,Song Wang,Rui Zhang,Min Lee,Jinju Duan,Xiao Zhang
Methicillin-Resistant Staphylococcus aureus forming into biofilms can trigger chronic inflammation and disrupt skin wound healing processes. Prolonged and excessive use of antibiotics can expedite the development of resistance, primarily because of their limited ability to penetrate microbial membranes and biofilms, especially antibiotics with intracellular drug targets. Herein, we devise a strategy
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Enhanced browning of adipose tissue by mirabegron-microspheres. J. Control. Release (IF 10.5) Pub Date : 2024-09-23 Zheming Niu,Staffan Hildebrand,Sebastian Kappes,Mohamed Ehab Ali,Matthias Vogel,Mickel Mikhael,Danli Ran,Jan Kozak,Maria Wiedner,Dirk F Richter,Alf Lamprecht,Alexander Pfeifer
Thermogenic brown adipose tissue (BAT) has emerged as an attractive target for combating obesity. However, pharmacological activation of energy expenditure by BAT and/or induction of browning of white adipose tissue (WAT) has been hampered by cardiovascular side effects. To address these concerns, we developed polylactide-co-glycolide acid (PLGA) microspheres loaded with mirabegron (MIR), a selective
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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 : 2024-09-22 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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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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An inhalable nanoparticle enabling virulence factor elimination and antibiotics delivery for pneumococcal pneumonia therapy. J. Control. Release (IF 10.5) Pub Date : 2024-09-21 Huiyue Dong,Yuxin Zhao,Shihong Li,Qiongwei Wang,Mengli Li,Kaikai Zhao,Zhenzhong Zhang,Jinjin Shi,Xiu Zhao,Junjie Liu
Streptococcus pneumoniae (S. pneumoniae) is a major cause of community-acquired pneumonia. Current standard clinical therapies mainly focus on combating S. pneumoniae through antibiotics. However, the limited delivery of antibiotics and the undetoxified hydrogen peroxide (H2O2) virulence factor secreted by S. pneumoniae impede the therapeutic outcomes. Here we report an inhalable catalase (CAT)-tannic
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Albumin-based co-loaded sonosensitizer and STING agonist nanodelivery system for enhanced sonodynamic and immune combination antitumor therapy J. Control. Release (IF 10.5) Pub Date : 2024-09-21 Huaping Huang, Lihua Du, Rishun Su, Zhuoyuan Li, Yu Shao, Yeling Yuan, Chen Wang, Changzheng Lu, Yulong He, Haozhe He, Changhua Zhang
STING agonists can activate natural and adaptive immune responses, and are expected to become a new type of immunotherapy drug for tumor therapy. However, how to target deliver STING agonists to tumor tissues is a key factor affecting the efficacy of tumor treatment. Sonodynamic therapy (SDT) has become a research hotspot in the field of cancer treatment due to its non-invasive, spatiotemporally controllable
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Charge balanced aggregation: A universal approach to aqueous organic nanocrystals J. Control. Release (IF 10.5) Pub Date : 2024-09-21 Wenwen Zhao, Qiu Li, Peng He, Changqing Li, Muna Aryal, Mario L. Fabiilli, Haijun Xiao
Organic nanocrystals, particularly those composed of conjugated molecules, hold immense potential for various applications. However, their practical utility is often hindered by the challenge of achieving stable aqueous dispersions, which are essential for biological compatibility and effective delivery. This study introduces a novel and versatile strategy for preparing stable aqueous organic nanocrystals
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Cyanocobalamin-loaded dissolving microneedles diminish skin inflammation in vivo J. Control. Release (IF 10.5) Pub Date : 2024-09-21 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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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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Emerging Pharmacotherapies for Obesity: A Systematic Review. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-09-20 Michail Kokkorakis,Marlene Chakhtoura,Caline Rhayem,Jana Al Rifai,Malak Ghezzawi,Laura Valenzuela-Vallejo,Christos S Mantzoros
The history of anti-obesity pharmacotherapies is marked by disappointments, often entangled with societal pressure promoting weight loss and the conviction that excess body weight signifies a lack of willpower. However, categories of emerging pharmacotherapies generate hope to reduce obesity rates. This systematic review of phase 2 and phase 3 trials in adults with overweight/obesity investigates the
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Neuroactive Kynurenines as Pharmacological Targets: New Experimental Tools and Exciting Therapeutic Opportunities. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-09-20 Ana Pocivavsek,Robert Schwarcz,Sophie Erhardt
Both pre-clinical and clinical studies implicate functional impairments of several neuroactive metabolites of the kynurenine pathway (KP), the major degradative cascade of the essential amino acid tryptophan in mammals, in the pathophysiology of neurological and psychiatric diseases. A number of KP enzymes, such as tryptophan 2,3-dioxygenase (TDO2), indoleamine 2,3-dioxygenases (IDO1 and IDO2), kynurenine
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Approval of the first TCR-based cell therapy. Mol. Ther. (IF 12.1) Pub Date : 2024-09-20 Nathan Singh
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Gastrointestinal-inert prebiotic micro-composites improve the growth and community diversity of mucosal-associated bacteria. J. Control. Release (IF 10.5) Pub Date : 2024-09-20 Linh P. Ta, Sarah Corrigan, Chris Tselepis, Tariq H Iqbal, Christian Ludwig, Richard D. Horniblow
The process of microencapsulation and the development of microparticle-based drug formulations have gained increased pharmaceutical interest, particularly for drug delivery and bacterial-encapsulation purposes for probiotic delivery. Existing studies have examined microcomposite (MC) responses to gastrointestinal (GI) conditions with the aim of controlling disintegration, and thus release, across the
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LNP-mRNA vaccine prevents type 1 diabetes in non-obese diabetes mice J. Control. Release (IF 10.5) Pub Date : 2024-09-20 Jiayin Chen, Yiqi Hu, Yan Chen, Ziqi Zhou, Yiming Shen, Yan Wang, Zichuan Liu, Xianglong Li, Zhigui Su, Jie Wu
Islet-antigen-specific tolerization is a key goal of experimental immunotherapies for type 1 diabetes. mRNA-based vaccines have demonstrated the feasibility of RNA delivery in inducing antigen tolerance in autoimmune diseases. In this study, mRNA vaccine, encoded tandem glutamic acid decarboxylase 65 (GAD65) epitopes and cholera toxin B subunit (CTB-GADIII), prepared by an in vitro transcription (IVT)
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Switchable PAMAM megamers for deep tumor penetration and enhanced cell uptake J. Control. Release (IF 10.5) Pub Date : 2024-09-20 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 : 2024-09-20 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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In situ formed reactive oxygen species-responsive dipyridamole prodrug hydrogel: Spatiotemporal drug delivery for chemoimmunotherapy J. Control. Release (IF 10.5) Pub Date : 2024-09-20 Bing Xiao, Xueying Shi, Xiaodan Xu, Jiwei Liu, Yixuan Pan, Hongxia Xu, Wenjing Sun, Nigel K.H. Slater, Hirak K. Patra, Jianqing Gao, Youqing Shen, Jianbin Tang
In the realm of combined cancer immunotherapy, the strategic combination of therapeutics targeting both cancer cells and macrophages holds immense potential. However, the major challenges remain on how to achieve facile spatiotemporal delivery of these therapies, allowing ease of manipulation and ensuring differential drug release for enhanced synergistic therapeutic effects. In the present study,
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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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Confined copper depletion via a hydrogel platform for reversing dabrafenib/cetuximab resistance in BRAFV600E-mutant colorectal cancer. J. Control. Release (IF 10.5) Pub Date : 2024-09-23 Jue Wang,Xiangshi Sun,Zhiwen Zhao,Guanru Wang,Dangge Wang,Yaping Li
BRAFV600E-mutant colorectal cancer (CRC) is resistant to most first-line therapeutics, including the BRAF inhibitor dabrafenib and epidermal growth factor receptor (EGFR) inhibitor cetuximab. Although copper depletion shows promise in reversing dabrafenib/cetuximab resistance in BRAFV600E-mutant CRC, its application is limited by the potential for excessive copper depletion in non-tumor objects. In
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Sirens and sphingolipids: What lures hematopoietic stem cells to the nervous system? Mol. Ther. (IF 12.1) Pub Date : 2024-09-19 Yedda Li,Florian S Eichler
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Tumor-intrinsic kinase: A promising target for overcoming resistance to immune checkpoint blockade therapies. Mol. Ther. (IF 12.1) Pub Date : 2024-09-19 Jianhui Wang,Gaowei Xia,Bin Meng,Xingang Guan
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Hydrogelation of peptides and carnosic acid as regulators of adaptive immunity against postoperative recurrence of cutaneous melanoma. J. Control. Release (IF 10.5) Pub Date : 2024-09-19 Mengdi Ren,Yang Wang,Xiaoqiang Zheng,Wenguang Yang,Mutian Liu,Siyun Xie,Yu Yao,Jin Yan,Wangxiao He
The in-situ activation of adaptive immunity at the surgical site has demonstrated remarkable efficacy in inhibiting various forms of tumour recurrence and even holds the promise of a potential cure. However, extensive research and bioinformatic analysis conducted in this study have unveiled the formidable challenge posed by melanoma-intrinsic β-catenin signaling, which hinders the infiltration of cytotoxic
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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 : 2024-09-19 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