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Prioritization of Eleven-Nineteen-Leukemia Inhibitors as Orally Available Drug Candidates for Acute Myeloid Leukemia J. Med. Chem. (IF 6.8) Pub Date : 2024-11-12 Xuejiao Shirley Guo, Sandeep Atla, Satyanarayana Nyalata, Yugendar R. Alugubelli, Peng-Hsun Chase Chen, Shiqing Xu, Wenshe Ray Liu
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Proline Analogues in Drug Design: Current Trends and Future Prospects J. Med. Chem. (IF 6.8) Pub Date : 2024-11-12 Vladimir Kubyshkin, Pavel K. Mykhailiuk
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DNA damage response inhibitors in cancer therapy: lessons from the past, current status and future implications Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-11-12 Yvette Drew, Frank T Zenke, Nicola J Curtin
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Unnatural Amino Acids: Strategies, Designs, and Applications in Medicinal Chemistry and Drug Discovery J. Med. Chem. (IF 6.8) Pub Date : 2024-11-11 Krishna K. Sharma, Komal Sharma, Kamya Rao, Anku Sharma, Gajanan K. Rathod, Shams Aaghaz, Naina Sehra, Rajesh Parmar, Brett VanVeller, Rahul Jain
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Synthesis and Pharmacological Characterization of Fluorescent Ligands Targeting the Angiotensin II Receptors Derived from Agonists, β-Arrestin-Biased Agonists, and Antagonists J. Med. Chem. (IF 6.8) Pub Date : 2024-11-11 Céline Delaitre, Michel Boisbrun, Samir Acherar, André Dias, Alexandra Kleinclauss, Mathilde Achard, Mélissa Colin, Trung Minh Nguyen, Nicolas Humbert, Khawla Chmeis, Karen L. Martinez, Nicolas Gilles, Philippe Robin, Sandra Lecat, François Dupuis
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Modulatory Role of Pantropic Cell Signaling Pathways in the Antimigratory and Antiproliferative Action of Triazole Chelated Iridium(III) Complexes in Cervical Cancer Cells J. Med. Chem. (IF 6.8) Pub Date : 2024-11-11 Anushka Mondal, Bishnu Das, Souvik Karmakar, Soumili Pani, Shrabani Khan, Parna Gupta, Jayasri Das Sarma
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Discovery of the First-in-Class Dual-Target ROCK/HDAC Inhibitor with Potent Antitumor Efficacy in Vivo That Trigger Antitumor Immunity J. Med. Chem. (IF 6.8) Pub Date : 2024-11-10 Churu Mao, Jiebin Fang, Shijie Zou, Yun Huang, Xiaoming Chen, Xia Ding, Zhangyun Fang, Ningjing Zhang, Yijie Lou, Zhe Chen, Wanjing Ding, Zhongjun Ma
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Structure-Guided Design of Affinity/Covalent-Bond Dual-Driven Inhibitors Targeting the AMP Site of FBPase J. Med. Chem. (IF 6.8) Pub Date : 2024-11-09 Hongxuan Cao, Zeyue Huang, Zheng Liu, Xiao Zhang, Yanliang Ren, Muhammad Salman Hameed, Li Rao, Nokwanda P. Makunga, Georgi M. Dobrikov, Jian Wan
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Enhanced CRISPR-Cas9 RNA system delivery using cell penetrating peptides-based nanoparticles for efficient in vitro and in vivo applications J. Control. Release (IF 10.5) Pub Date : 2024-11-11 Veronica Guzman Gonzalez, Audrey Grunenberger, Olivier Nicoud, Elodie Czuba, Julien Vollaire, Véronique Josserand, Xavier Le Guével, Nail Desai, Jean-Luc Coll, Gilles Divita, Virginie Faure
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Ultrasound-activated microbubbles mediate F-actin disruptions and endothelial gap formation during sonoporation J. Control. Release (IF 10.5) Pub Date : 2024-11-12 Bram Meijlink, H. Rhodé van der Kooij, Yuchen Wang, Hongchen Li, Stephan Huveneers, Klazina Kooiman
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Understanding vaginal biofilms: The first step in harnessing antimicrobial nanomedicine J. Control. Release (IF 10.5) Pub Date : 2024-11-12 Sybil Obuobi, Nataša Škalko-Basnet
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Discovery of a Novel Macrocyclic Noncovalent CDK7 Inhibitor for Cancer Therapy J. Med. Chem. (IF 6.8) Pub Date : 2024-11-09 Hongfu Lu, Yihong Zhang, Jinxin Liu, Tao Jiang, Xiang Yu, Haoyu Zhang, Tao Liang, Jingjing Peng, Xin Cai, Xiaoling Lan, Jinmin Ren, Mei Ge, Jingyang Zhang, Jingjin Shang, Jiaojiao Yu, Hongcan Ren, Qiang Liu, Jinting Gao, Lili Tang, Xiao Ding, Man Zhang, Alex Aliper, Qiang Lu, Fusheng Zhou, Jiong Lan, Feng Ren, Alex Zhavoronkov
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Injectable nanocomposite hydrogel with cascade drug release for treatment of uveal melanoma J. Control. Release (IF 10.5) Pub Date : 2024-11-09 Zhihao Guo, Linyun Xiu, Yumei Li, Jiangcheng Tan, Cailing Wei, Junhui Sui, Shijin Zhang, Ruohua Zhu, Ji-Liang Li
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Engineering of phosphatidylserine-targeting ROS-responsive polymeric prodrug for the repair of ischemia-reperfusion-induced acute kidney injury J. Control. Release (IF 10.5) Pub Date : 2024-11-09 Jin-Hui Wang, Hai-Bo Mao, Jing-Bo Hu, Shunhua Cheng, Hao Su
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Engineered manganese-BODIPY coordinated nanoadjuvants for enhanced NIR-II photo-metalloimmunotherapy J. Control. Release (IF 10.5) Pub Date : 2024-11-09 Yushi Zhang, Xuya Yu, Lingpeng Luo, Yigang Xu, Hanjie Zhang, Zhuo Mao, Yuqin Zhang, Cuihong Yang, Lu Wang, Pengcheng Zhang, Sitong Li, Meitong Ou, Ran Luo, Dunwan Zhu, Wen Li, Lin Mei
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Lipidation-dimerization platform unlocks treatment potential of fibroblast growth factor 21 for non-alcoholic steatohepatitis J. Control. Release (IF 10.5) Pub Date : 2024-11-09 Yapeng Wang, Lei Shen, Chengcheng Wang, Yuanzhen Dong, Haoju Hua, Jun Xu, Ying Zhang, Hao Huang, Zongqing Huang, Fei Zhao, Zhiru Xu, Yunliang Qiu, Jianguang Lu, Dianwen Ju, Jun Feng
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Fluorinated dendrimer-mediated miR-30a delivery regulates the inflammation of macrophages and mitigates the symptoms of rheumatoid arthritis J. Control. Release (IF 10.5) Pub Date : 2024-11-09 Jiakai Xing, Jiaxin Jia, Hugang Zhang, Haobo Han, Quanshun Li
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Discovery of SD-436: A Potent, Highly Selective and Efficacious STAT3 PROTAC Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Renqi Xu, Haibin Zhou, Longchuan Bai, Donna McEachern, Dimin Wu, Ranjan Kumar Acharyya, Mi Wang, Jelena Tošović, Chao-Yie Yang, Krishnapriya Chinnaswamy, Jennifer L. Meagher, Jeanne A. Stuckey, Cai Liu, Meilin Wang, Bo Wen, Duxin Sun, Shaomeng Wang
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Recent Progress and Future Perspectives on Anti-Hyperuricemic Agents J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Zhiqiang Sun, Xuewen Zhang, Zean Zhao, Xiaoxun Li, Jianxin Pang, Jianjun Chen
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Closing the Design–Make–Test–Analyze Loop: Interplay between Experiments and Predictions Drives PROTACs Bioavailability J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Zulma Santisteban Valencia, Jennifer Kingston, Filip Miljković, Hannah Rowbottom, Nadia Mann, Sophie Davies, Martin Ekblad, Silvio Di Castro, Karolina Kwapień, Erik Malmerberg, Stig D. Friis, Thomas Lundbäck, Tomas Leek, Johan Wernevik
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Discovery of Thiazole Carboxamides as Novel Vanin-1 Inhibitors for Inflammatory Bowel Disease Treatment J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Tao Xie, Gao-Yao Cao, Shize Zhang, Meng-Ke Li, Xin Jin, Liu Liu, Guangji Wang, Le Zhen
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Structure–Activity Relationships and Discovery of (S)-5-(tert-Butyl)-11-(difluoromethoxy)-9-methoxy-2-oxo-1,2,5,6-tetrahydropyrido[2′,1′:2,3]imidazo[4,5-h]quinoline-3-carboxylic Acid (AB-161), a Novel Orally Available and Liver-Centric HBV RNA Destabilizer J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Dimitar Gotchev, Shuai Chen, Benjamin Dugan, Bruce D. Dorsey, Xu Wang, Muhammad Sheraz, Rose Kowalski, Fei Liu, Sunny Tang, Tim Chiu, Troy Harasym, Ingrid E. Graves, Emily P. Thi, Jeremy D. Mason, Nathan Overholt, Ravi Dugyala, Angela M. Lam, Andrew G. Cole, Michael J. Sofia
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A Fast Method to Monitor Tyrosine Kinase Inhibitor Mechanisms J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Alejandro Fernández, Margarida Gairí, María Teresa González, Miquel Pons
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Discovery of CHD1 Antagonists for PTEN-Deficient Prostate Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Rebecca L. Johnson, Amanda L. Graboski, Fengling Li, Jacqueline L. Norris-Drouin, William G. Walton, Cheryl H. Arrowsmith, Matthew R. Redinbo, Stephen V. Frye, Lindsey I. James
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Discovery of SZJK-0421: A Novel Potent, Low Toxicity, Selective Second Generation of CRM1 Inhibitor for the Treatment of Both Hematological and Solid Tumors J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Hang Miao, Yanru Qin, DingLu Shao, Qinghua Chen, Yupeng Pan, Meng Lei, Ruokun Wu, Xinran Ye, Xueyuan Wang, Yongqiang Zhu
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Cerebral biomimetic nano-drug delivery systems: A frontier strategy for immunotherapy J. Control. Release (IF 10.5) Pub Date : 2024-11-08 Hao Tian, Jiaxin Yao, Qi Ba, Yuanyuan Meng, Yanan Cui, Liangzhu Quan, Wei Gong, Yuli Wang, Yang Yang, Meiyan Yang, Chunsheng Gao
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Controlled release of mesenchymal stem cell-derived nanovesicles through glucose- and reactive oxygen species-responsive hydrogels accelerates diabetic wound healing J. Control. Release (IF 10.5) Pub Date : 2024-11-07 Fangzhou Du, Shumang Zhang, Shikai Li, Shaocong Zhou, Dongao Zeng, Jingzhong Zhang, Shuang Yu
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Reactive oxygen species-responsive polydopamine-PtCuTe nanoparticle-loaded microneedle system for promoting the healing of infected skin wounds J. Control. Release (IF 10.5) Pub Date : 2024-11-07 Hongfan Che, Junzhi Xu, Dong Wu, Siliang Chen, Chengkang Liu, Chongbao Zhao, Kun Peng
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Leveraging machine learning to streamline the development of liposomal drug delivery systems J. Control. Release (IF 10.5) Pub Date : 2024-11-08 Remo Eugster, Markus Orsi, Giorgio Buttitta, Nicola Serafini, Mattia Tiboni, Luca Casettari, Jean-Louis Reymond, Simone Aleandri, Paola Luciani
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Combination of multivalent DR5 receptor clustering agonists and histone deacetylase inhibitors for treatment of colon cancer J. Control. Release (IF 10.5) Pub Date : 2024-11-08 Jiahui Li, Jaden Arnold, Monika Sima, Hasan Al Faruque, Jacob Galang, Sophia Hu-Lieskovan, Jindřich Kopeček, Jiyuan Yang
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Advancing osteosarcoma 3D modeling in vitro for novel tumor microenvironment-targeted therapies development J. Control. Release (IF 10.5) Pub Date : 2024-11-08 Sofia Costa, João Rodrigues, Carolina Vieira, Sofia Dias, Juliana Viegas, Flávia Castro, Bruno Sarmento, Catarina Leite Pereira
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Benchmarking recruitment rates for phase III trials Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-11-08
Discover the world’s best science and medicine | Nature.com
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Development of N-(4-(1H-Imidazol-1-yl)phenyl)-4-chlorobenzenesulfonamide, a Novel Potent Inhibitor of β-Catenin with Enhanced Antitumor Activity and Metabolic Stability J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Michela Puxeddu, Lele Ling, Silvia Ripa, Michele D’Ambrosio, Marianna Nalli, Anastasia Parisi, Pietro Sciò, Antonio Coluccia, Arianna Granese, Martina Santelli, Domiziana Masci, Petra Cuřínová, Chiara Naro, Claudio Sette, Arianna Pastore, Mariano Stornaiuolo, Chiara Bigogno, Giulio Dondio, Laura Di Magno, Gianluca Canettieri, Te Liu, Romano Silvestri, Giuseppe La Regina
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Discovery of 5-Nitro-N-(3-(trifluoromethyl)phenyl) Pyridin-2-amine as a Novel Pure Androgen Receptor Antagonist against Antiandrogen Resistance J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Huating Wang, Xuwen Wang, Haiyang Zhong, Lvtao Cai, Weitao Fu, Xin Chai, Jianing Liao, Rong Sheng, Luhu Shan, Xiaohong Xu, Lei Xu, Peichen Pan, Tingjun Hou, Dan Li
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Small-Molecule Modulators Targeting Coactivator-Associated Arginine Methyltransferase 1 (CARM1) as Therapeutic Agents for Cancer Treatment: Current Medicinal Chemistry Insights and Emerging Opportunities J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Shuqing Li, Wanyi Pan, Chengpeng Tao, Zhihao Hu, Binbin Cheng, Jianjun Chen, Xiaopeng Peng
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Antiplasmodial and Insecticidal Activities of Third-Generation Ivermectin Hybrids J. Med. Chem. (IF 6.8) Pub Date : 2024-11-06 Parth, Sofia Santana, Catarina Rôla, Carla Bastos Oliveira, Miguel Prudêncio, Kamaljit Singh, Diana Fontinha
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Single Amine or Guanidine Modification on Norvancomycin and Vancomycin to Overcome Multidrug-Resistance through Augmented Lipid II Binding and Increased Membrane Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-11-06 Xiaolei Bian, Zhifu Chen, Fang Li, Yuanyuan Xie, Yi Li, Youhong Luo, Xiangman Zou, Hui Wang, Jingwen Zhang, Xiaowen Wang, Jinyong Zhang, Dongliang Guan
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Medicinal Chemistry Education: Emphasize Fundamentals and Skillfully Integrate Knowledge J. Med. Chem. (IF 6.8) Pub Date : 2024-11-06 Shaoqing Du, Xueping Hu, Craig W. Lindsley, Peng Zhan
Medicinal chemistry is an interdisciplinary field that aims to discover innovative drugs and synthesize drug molecules at the intersection of chemistry and biology. In the field of medicinal chemistry education, it is essential to establish a robust foundation by emphasizing fundamental principles of chemistry and biology. This strategy not only imparts students with a comprehensive understanding of
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Surface-engineered mesenchymal stem cell for refractory asthma therapy: Reversing airway remodeling J. Control. Release (IF 10.5) Pub Date : 2024-11-06 Xing-Yue He, Meng-Meng Han, Yu-Chen Zhao, Ling Tang, Yi Wang, Lei Xing, Ning Wei, Jing Wang, Guang-Ji Wang, Fang Zhou, Jee-Heon Jeong, Hu-Lin Jiang
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Inhibition of Human Salivary and Pancreatic α-Amylase by Resveratrol Oligomers J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Rizliya Visvanathan, Dang Truong Le, Sushil Dhital, Topul Rali, Rohan A. Davis, Gary Williamson
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Optimization of Antiproliferative Properties of Triimine Copper(II) Complexes J. Med. Chem. (IF 6.8) Pub Date : 2024-11-04 Katarzyna Choroba, Bartosz Zowiślok, Sławomir Kula, Barbara Machura, Anna M. Maroń, Karol Erfurt, Cristiana Marques, Sandra Cordeiro, Pedro V. Baptista, Alexandra R. Fernandes
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Corrigendum to “Bacteria-mimetic nanomedicine for targeted eradication of intracellular MRSA” [Journal of Controlled Release 357 (2023) 371–378] J. Control. Release (IF 10.5) Pub Date : 2024-11-06 Beibei Xie, Huichao Zhao, Ruixue Zhang, Yuanfu Ding, Cheng Gao, Yun He, Ruibing Wang
The authors regret that the tissue sections for histological examination (HE staining) related to Fig. 5a were inadvertently mixed among several different groups from two concurrent projects by the first author, resulting in the misplacements of multiple HE staining images in this figure. This oversight was recently discovered by the first author himself. To ensure that the correct tissue sections
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Conquering dual challenges: A sialic-modified liposome for targeting activated neutrophils to tackle comorbid lung inflammation and cancer metastasis J. Control. Release (IF 10.5) Pub Date : 2024-11-06 Cong Li, Zhihang Li, Lihong Wang, Kexin Zhang, Zehao Li, Yating Ji, Jing Li, Yifan Zhang, Lijiang Chen
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Phage-liposome nanoconjugates for orthopedic biofilm eradication J. Control. Release (IF 10.5) Pub Date : 2024-11-06 Lei Wang, Tamta Tkhilaishvili, Zheng Jiang, Rima Fanaei Pirlar, Yu Ning, Adrián Millán Laleona, Jiaxing Wang, Jin Tang, Qiaojie Wang, Andrej Trampuz, Mercedes Gonzalez Moreno, Xianlong Zhang
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A reactive oxygen species-triggerable theranostic prodrug system J. Control. Release (IF 10.5) Pub Date : 2024-11-06 Feiyang Liu, Lingyan Liu, Peng Wei, Tao Yi
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Microparticle and nanoparticle-based influenza vaccines J. Control. Release (IF 10.5) Pub Date : 2024-11-06 Luis Ontiveros-Padilla, Eric M. Bachelder, Kristy M. Ainslie
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Spatiotemporally cascade-driven “Lipomicelles” enhance extracellular matrix penetration and remodel intercellular crosstalk in pulmonary fibrosis J. Control. Release (IF 10.5) Pub Date : 2024-11-05 Xin Chang, Yu-Mo Han, Qiu-Ling Li, Chao Wang, Bin Guo, Hu-Lin Jiang
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Copper peroxide-decorated Prussian blue for effective bacterial elimination via photothermal-enhanced and H2O2-releasing chemodynamic therapy J. Control. Release (IF 10.5) Pub Date : 2024-11-06 Guitao Tan, Chenyang Qi, Qinqin Zhang, Haonan Hu, Bingtian Tu, Jing Tu
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Anti-CTLA-4 antibody self-presented dendritic cell nanovesicles boost the immunotherapy of hepatocellular carcinoma after microwave ablation J. Control. Release (IF 10.5) Pub Date : 2024-11-06 Tan Li, Bo Li, Liteng Lin, Gengjia Chen, Xiaobin Wang, Ye Chen, Wensou Huang, Mingyue Cai, Xintao Shuai, Kangshun Zhu
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Antimalarial drug hits cardiac fibrosis Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-11-05
Discover the world’s best science and medicine | Nature.com
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Discovery of Highly Selective Inhibitors of Microtubule-Associated Serine/Threonine Kinase-like (MASTL) J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Rebecca A. Gallego, Stephanie Scales, Chad Toledo, Marin Auth, Louise Bernier, Madeline Berry, Sonja Brun, Loanne Chung, Carl Davis, Wade Diehl, Klaus Dress, Koleen Eisele, Jeff Elleraas, Jason Ewanicki, Yvette Fobian, Samantha Greasley, Eric C. Greenwald, Ted W. Johnson, Penney Khamphavong, Jennifer Lafontaine, Jian Li, Angelica Linton, Michael Maestre, Nichol Miller, Anwar Murtaza, Ryan L. Patman
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Structure-Based Design of Covalent SARS-CoV-2 Papain-like Protease Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Bin Tan, Xueying Liang, Ahmadullah Ansari, Prakash Jadhav, Haozhou Tan, Kan Li, Francesc Xavier Ruiz, Eddy Arnold, Xufang Deng, Jun Wang
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Target Ligand Separation and Identification of Isoforsythiaside as a Histone Lysine-Specific Demethylase 1 Covalent Inhibitor Against Breast Cancer Metastasis J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Mengzhen Gu, Xiaoqing Xu, Xiaoping Wang, Yun Wang, Yu Zhao, Xiaoxian Hu, Lu Zhu, Zhenzhong Deng, Chao Han
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Expanding the Solvent/Protein Region Occupation of the Non-Nucleoside Reverse Transcriptase Inhibitor Binding Pocket for Improved Broad-Spectrum Anti-HIV-1 Efficacy: from Rigid Phenyl-Diarylpyrimidines to Flexible Hydrophilic Piperidine-Diarylpyrimidines J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Wen-Juan Huang, Christophe Pannecouque, Erik De Clercq, Angela Corona, Stefania Maloccu, Enzo Tramontano, Shuai Wang, Fen-Er Chen
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Medicinal Chemistry Education and Training J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Craig W. Lindsley
I decided to weigh in on the ongoing discussion about medicinal chemistry education and training with my thoughts on the matter, as I began my career in industry (Parke-Davis, Eli Lilly and Merck) and later moved into academia (Vanderbilt University/Warren Center for Neuroscience Drug Discovery). First and foremost, training in synthetic organic chemistry is essential. A deep understanding of mechanistic
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Synthesis and mechanism of Mg/Al layered double oxides-silica nanocomposites for sustainable multi-nutrient delivery in agricultural applications J. Control. Release (IF 10.5) Pub Date : 2024-11-05 Aihua Xiang, Yifan Li, Tuanliu Hu, Kun Liu
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Macropinocytosis-targeted peptide-docetaxel conjugate for bystander pancreatic cancer treatment J. Control. Release (IF 10.5) Pub Date : 2024-11-05 Young Seok Cho, Hanhee Cho, Ha Rin Kim, Seong Jin Park, Joo Hye Yeo, Yoon Gun Ko, Jinu Lee, Sang Yoon Kim, Kwangmeyung Kim, Youngro Byun
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Multifunctional nanoparticles potentiate in-situ tumor vaccines via reversing insufficient Photothermal therapy by disrupting tumor vasculature J. Control. Release (IF 10.5) Pub Date : 2024-11-05 Lili Zhao, Yiran Liu, Fangfei Jin, Kaiyuan Hu, Miao Lv, Yuehua Zhou, Weijun Zhao, Yiqiao Hu, Jinhui Wu, Yong Yang, Wenguang Wang
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Lundbeck pays US$2.6 billion for Longboard and its lead epilepsy drug Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-11-05
Discover the world’s best science and medicine | Nature.com
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JAK inhibition combats adverse skin reaction Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-11-05
Discover the world’s best science and medicine | Nature.com
更新日期：2024-11-12
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