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First-in-class IL-15 receptor agonist nabs FDA approval for bladder cancer Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-04-26
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Medicinal Chemistry Gone Wild J. Med. Chem. (IF 7.3) Pub Date : 2024-04-25 Tesko Chaganti, Chun-Yi Tsai, Yu-Pu Juang, Mohamed Abdelalim, Tim Cernak
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Design, Synthesis, Formulation, and Bioevaluation of Trisubstituted Triazines as Highly Selective mTOR Inhibitors for the Treatment of Human Breast Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-04-25 Qiwen Sun, Yuxiu Chu, Nana Zhang, Rui Chen, Lili Wang, Jiangxia Wu, Yongxi Dong, Hongliang Li, Ling Wang, Lei Tang, Changyou Zhan, Ji-Quan Zhang
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Structure-Based Rational and General Strategy for Stabilizing Single-Chain T-Cell Receptors to Enhance Affinity J. Med. Chem. (IF 7.3) Pub Date : 2024-04-25 Jia-Ling Zou, Kai-Xiang Chen, Xiao-Juan Wang, Zheng-Chang Lu, Xian-Hui Wu, Yun-Dong Wu
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Artificial Intelligence-Assisted Optimization of Antipigmentation Tyrosinase Inhibitors: De Novo Molecular Generation Based on a Low Activity Lead Compound J. Med. Chem. (IF 7.3) Pub Date : 2024-04-23 Hong Cai, Wenchao Chen, Jing Jiang, Hao Wen, Xinyu Luo, Junjie Li, Liuxin Lu, Rui Zhao, Xinhua Ni, Yinyan Sun, Jiahui Wang, Zhen Li, Bin Ju, Xiaoying Jiang, Renren Bai
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Correction to “Development of Cytotoxic GW7604-Zeise’s Salt Conjugates as Multitarget Compounds with Selectivity for Estrogen Receptor-Positive Tumor Cells” J. Med. Chem. (IF 7.3) Pub Date : 2024-04-23 Patricia Grabher, Paul Kapitza, Nikolas Hörmann, Amelie Scherfler, Martin Hermann, Michael Zwerger, Hristo P. Varbanov, Brigitte Kircher, Daniel Baecker, Ronald Gust
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Psychoplastogenic DYRK1A Inhibitors with Therapeutic Effects Relevant to Alzheimer’s Disease J. Med. Chem. (IF 7.3) Pub Date : 2024-04-22 Hunter T. Warren, Hannah N. Saeger, Robert J. Tombari, Milan Chytil, Kurt Rasmussen, David. E. Olson
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Discovery of an Ortho-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydronorthebaine Derivative as a Selective and Potent Kappa Opioid Receptor Agonist with Subsided Sedative Effect J. Med. Chem. (IF 7.3) Pub Date : 2024-04-22 Zixiang Li, Rufeng Ye, Qian He, Jiashuo Lu, Yanting Sun, Xiujian Sun, Siyuan Tang, Shuyang Hu, Jingrui Chai, Linghui Kong, Xiaoning Liu, Jing Chen, Yun Fang, Yingjie Lan, Qiong Xie, Jinggen Liu, Liming Shao, Wei Fu, Yujun Wang, Wei Li
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A facile and smart strategy to enhance bone regeneration with efficient vitamin D3 delivery through sterosome technology J. Control. Release (IF 10.8) Pub Date : 2024-04-25 Shuxi Ye, Jing Wen, Wen-Hao Ye, Zhen Li, Xiaomeng Huang, Sixu Chen, Jian-Chao Ma, Yaohong Wu, Rongchun Chen, Zhong-Kai Cui
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Integrated anti-vascular and immune-chemotherapy for colorectal carcinoma using a pH-responsive polymeric delivery system J. Control. Release (IF 10.8) Pub Date : 2024-04-25 Xiaoqian Ma, Qing Yang, Nuo Lin, Yushuo Feng, Yaqing Liu, Peifei Liu, Yiru Wang, Huaping Deng, Haizhen Ding, Hongmin Chen
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Enhanced oral and pulmonary delivery of biomacromolecules via amplified transporter targeting J. Control. Release (IF 10.8) Pub Date : 2024-04-25 Xin Xiao, Lie Zhang, Mingjie Ni, Xi Liu, Liyun Xing, Licheng Wu, Zhou Zhou, Lian Li, Jingyuan Wen, Yuan Huang
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Can in vitro/in silico tools improve colonic concentration estimations for oral extended-release formulations? A case study with upadacitinib J. Control. Release (IF 10.8) Pub Date : 2024-04-25 Alessia Favaron, Bart Hens, Maiara Camotti Montanha, Mark McAllister, Irena Tomaszewska, Shaimaa Moustafa, Marília Alvarenga de Oliveira, Abdul W. Basit, Mine Orlu
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Particulate bioaerogels for respiratory drug delivery J. Control. Release (IF 10.8) Pub Date : 2024-04-25 Hao-Ying Li, Charalampos Makatsoris, Ben Forbes
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Druglike, 18F-labeled PET Tracers Targeting Fibroblast Activation Protein J. Med. Chem. (IF 7.3) Pub Date : 2024-04-24 Muhammet Tanc, Nicolò Filippi, Yentl Van Rymenant, Sergei Grintsevich, Isabel Pintelon, Marlies Verschuuren, Joni De Loose, Emile Verhulst, Euy Sung Moon, Lorenzo Cianni, Sigrid Stroobants, Koen Augustyns, Frank Roesch, Ingrid De Meester, Filipe Elvas, Pieter Van der Veken
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Discovery of a Novel Orally Bioavailable FLT3-PROTAC Degrader for Efficient Treatment of Acute Myeloid Leukemia and Overcoming Resistance of FLT3 Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-04-24 Junwei Wang, Quanjin Rong, Lei Ye, Bingqian Fang, Yifan Zhao, Yu Sun, Haikun Zhou, Dan Wang, Jinting He, Zhenzhen Cui, Qijian Zhang, Di Kang, Lihong Hu
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Discovery of Novel Dual Inhibitors Targeting Mutant IDH1 and NAMPT for the Treatment of Glioma with IDH1Mutation J. Med. Chem. (IF 7.3) Pub Date : 2024-04-23 Fei Wen, Gang Gui, Xiaoyu Wang, Anqi Qin, Tianfang Ma, Hui Chen, Chunzheng Li, Xiaoming Zha
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Development of Prolinol Containing Inhibitors of Hypoxanthine–Guanine–Xanthine Phosphoribosyltransferase: Rational Structure-Based Drug Design J. Med. Chem. (IF 7.3) Pub Date : 2024-04-23 Dianne T. Keough, Magdalena Petrová, Gordon King, Michal Kratochvíl, Radek Pohl, Eva Doleželová, Alena Zíková, Luke W. Guddat, Dominik Rejman
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Virtual Screening Strategies for Identifying Novel Chemotypes J. Med. Chem. (IF 7.3) Pub Date : 2024-04-23 Stuart Lang, Martin J. Slater
The identification of active compounds, or a series of compounds, is the crucial first step in all drug discovery projects. Ideally these compounds should display, or have the potential to display after optimization, good physical chemistry, and drug like properties. Screening, both physical and virtual, is a process that involves interrogating a protein target of interest with large numbers of compounds
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Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity J. Med. Chem. (IF 7.3) Pub Date : 2024-04-22 Jiankang Hu, Hongrui Xu, Tianbang Wu, Cheng Zhang, Hui Shen, Ruibo Dong, Qingqing Hu, Qiuping Xiang, Shuang Chai, Guolong Luo, Xiaoshan Chen, Yumin Huang, Xiaofan Zhao, Chao Peng, Xishan Wu, Bin Lin, Yan Zhang, Yong Xu
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Discovery and Structure–Activity Relationships of 2,5-Dimethoxyphenylpiperidines as Selective Serotonin 5-HT2A Receptor Agonists J. Med. Chem. (IF 7.3) Pub Date : 2024-04-22 Emil M. Ro̷rsted, Anders A. Jensen, Gints Smits, Karla Frydenvang, Jesper L. Kristensen
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Design of Evodiamine–Glucose Conjugates with Improved In Vivo Antitumor Activity J. Med. Chem. (IF 7.3) Pub Date : 2024-04-22 Zhe Wu, Shuqiang Chen, Zhipeng Chen, Guoqiang Dong, Defeng Xu, Chunquan Sheng
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Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In Silico Investigations of Coumarin-Based Thiazoles J. Med. Chem. (IF 7.3) Pub Date : 2024-04-20 Salma M. Hefny, Tarek F. El-Moselhy, Nabaweya El-Din, Simone Giovannuzzi, Thamer Bin Traiki, Mansoor-Ali Vaali-Mohammed, Ahmed M. El-Dessouki, Koki Yamaguchi, Masaharu Sugiura, Moataz A. Shaldam, Claudiu T. Supuran, Maha-Hamadien Abdulla, Wagdy M. Eldehna, Haytham O. Tawfik
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Lead Optimization of Butyrolactone I as an Orally Bioavailable Antiallergic Agent Targeting FcγRIIB J. Med. Chem. (IF 7.3) Pub Date : 2024-04-19 Chun-Lan Xie, Hong-Xiu Xiao, Pei-Fang Song, Qing-Mei Liu, Haoxiang Wei, Liang Wu, Guang-Hao Zhu, Guang-Ming Liu, Yandong Zhang, Ping Wang, Xian-Wen Yang
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FETPY: a Diiron(I) Thio–Carbyne Complex with Prominent Anticancer Activity In Vitro and In Vivo J. Med. Chem. (IF 7.3) Pub Date : 2024-04-19 Ekatarina Mihajlović, Lorenzo Biancalana, Sanja Jelača, Lorenzo Chiaverini, Biljana Dojčinović, Duško Dunđerović, Stefano Zacchini, Sanja Mijatović, Danijela Maksimović-Ivanić, Fabio Marchetti
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RIPK3 inhibitor prevents lung damage in severe influenza infection Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-04-24
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Hybrid adipocyte-derived exosome nano platform for potent chemo-phototherapy in targeted hepatocellular carcinoma J. Control. Release (IF 10.8) Pub Date : 2024-04-24 Xinying Liu, Jiaxin Zhang, Shunzhe Zheng, Meng Li, Wenqian Xu, Jianbin Shi, Ken-ichiro Kamei, Chutong Tian
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Tailoring drug release from long-acting contraceptive levonorgestrel intrauterine systems J. Control. Release (IF 10.8) Pub Date : 2024-04-24 Suraj Fanse, Quanying Bao, Yuan Zou, Yan Wang, Diane J. Burgess
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mRNA therapy shows promise for metabolic disorder Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-04-23
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Positron emission tomography guided synergistic treatment of melanoma using multifunctional zirconium-hematoporphyrin nanosonosensitizers J. Control. Release (IF 10.8) Pub Date : 2024-04-23 Xiaodan Jiao, Xiaoyang Li, Yan Du, Yiyang Cong, Shuyang Yang, Daiqin Chen, Tao Zhang, Min Feng, Hao Hong
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Superior COL7A1 and TGM1 gene expression in difficult-to-transfect skin cell mediated by highly branched poly(β-amino esters) through stepwise fractionation J. Control. Release (IF 10.8) Pub Date : 2024-04-23 Chaolan Pan, Chenfei Wang, Yitong Zhao, Tao Bo, Liping Han, Dingjin Yao, Yumeng Wang, Xiaoxiao Wang, Linjing Shi, Anqi Zhao, Qiaoyu Cao, Fuying Chen, Wei He, Ying Ye, Si Zhang, Ming Li
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Cadherin-11 targeted cell-specific liposomes enabled skin fibrosis treatment by inducing apoptosis J. Control. Release (IF 10.8) Pub Date : 2024-04-23 Himanshu N. Bhatt, Rimpy Diwan, Igor L. Estevao, Rui Dong, Jennifer Smith, Chuan Xiao, Sandeep K. Agarwal, Md Nurunnabi
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Cell membrane-coated nanoparticles for targeting carcinogenic bacteria Adv. Drug Deliver. Rev. (IF 16.1) Pub Date : 2024-04-21 Lei Sun, Dan Wang, Kailin Feng, Jiayuan Alex Zhang, Weiwei Gao, Liangfang Zhang
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Brain-Permeable Immunoproteasome-Targeting Macrocyclic Peptide Epoxyketones for Alzheimer’s Disease J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Ji Eun Park, Chhabi L. Chaudhary, Deepak Bhattarai, Kyung Bo Kim
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Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Esra Balıkçı, Anne-Sophie M. C. Marques, Ludwig G. Bauer, Raina Seupel, James Bennett, Brigitt Raux, Karly Buchan, Klemensas Simelis, Usha Singh, Catherine Rogers, Jennifer Ward, Carol Cheng, Tamas Szommer, Kira Schützenhofer, Jonathan M. Elkins, David L. Sloman, Ivan Ahel, Oleg Fedorov, Paul E. Brennan, Kilian V. M. Huber
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Selective Elimination of Senescent Cancer Cells by Galacto-Modified PROTACs J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Mengyang Chang, Feng Gao, Giri Gnawali, Hang Xu, Yue Dong, Xiang Meng, Wenpan Li, Zhiren Wang, Byrdie Lopez, Jennifer S. Carew, Steffan T. Nawrocki, Jianqin Lu, Qing-Yu Zhang, Wei Wang
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Corneal fibrosis: From in vitro models to current and upcoming drug and gene medicines Adv. Drug Deliver. Rev. (IF 16.1) Pub Date : 2024-04-19 Laura Trujillo Cubillo, Mehmet Gurdal, Dimitrios I. Zeugolis
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Gemfibrozil-Platinum(IV) Precursors for New Enhanced-Starvation and Chemotherapy In Vitro and In Vivo J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Xue-Qing Song, Xu Guo, Yi-Xin Ding, Yi-Xuan Han, Zhi-Hao You, Yali Song, Yanan Yuan, Longfei Li
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Monophosphoryl Lipid A-Rhamnose Conjugates as a New Class of Vaccine Adjuvants J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Rajendra Rohokale, Jiatong Guo, Zhongwu Guo
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Arene–Arene Coupled Disulfamethazines (or Sulfadiazine)-Phenanthroline-Metal(II) Complexes were Synthesized by In Situ Reactions and Inhibited the Growth and Development of Triple-Negative Breast Cancer through the Synergistic Effect of Antiangiogenesis, Anti-Inflammation, Pro-Apoptosis, and Cuproptosis J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Bing-Bing Xu, Nan Jin, Ji-Cheng Liu, Ai-Qiu Liao, Hong-Yu Lin, Xiu-Ying Qin
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Discovery of a Meisoindigo-Derived PROTAC as the ATM Degrader: Revolutionizing Colorectal Cancer Therapy via Synthetic Lethality with ATR Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Ting-Ting Liu, Qing Wang, Yuxing Zhou, Baixin Ye, Tingting Liu, Linyang Yan, Jinbao Fan, Jiahao Xu, Yingjun Zhou, Zanxian Xia, Xu Deng
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RNA-editing drugs advance into clinical trials Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-04-18
ADAR-based editors that can change the mRNA code offer new opportunities in both rare genetic diseases and common complex ones.
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Discovery of a Potent Dual Son of Sevenless 1 (SOS1) and Epidermal Growth Factor Receptor (EGFR) Inhibitor for the Treatment of Prostate Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-04-17 Lufeng Zheng, Yuxin Zhang, Shuang Mei, Tianyuan Xie, Yunting Zou, Yuting Wang, Han Jing, Shengtao Xu, Pierre Dramou, Zhen Xu, Jindong Li, Yang Zhou, Miao-Miao Niu
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Neutrophil-derived nanovesicles deliver IL-37 to mitigate renal ischemia-reperfusion injury via endothelial cell targeting J. Control. Release (IF 10.8) Pub Date : 2024-04-18 Wenjie Ma, Di Wu, Chengcheng Long, Jingyu Liu, Luwei Xu, Liuhua Zhou, Quanliang Dou, Yuzheng Ge, Changcheng Zhou, Ruipeng Jia
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Structural Elucidation and Antiviral Activity of Covalent Cathepsin L Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-04-17 Sven Falke, Julia Lieske, Alexander Herrmann, Jure Loboda, Katarina Karničar, Sebastian Günther, Patrick Y. A. Reinke, Wiebke Ewert, Aleksandra Usenik, Nataša Lindič, Andreja Sekirnik, Klemen Dretnik, Hideaki Tsuge, Vito Turk, Henry N. Chapman, Winfried Hinrichs, Gregor Ebert, Dušan Turk, Alke Meents
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Design, Synthesis, and Biological Evaluation of β-Trifluoroethoxydimethyl Selenides as Potent Antiosteoporosis Agents J. Med. Chem. (IF 7.3) Pub Date : 2024-04-17 Yao Wu, Bin Li, Linkun Ying, Yao Chen, Yuxin Zhang, Chaoming Hu, Yichi Zhang, Lele Yi, Weiwei Xue, Shengbin Huang, Zengqiang Song
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Three-step cures for autoimmune diseases? Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-04-17
Robert Plenge, head of Research at Bristol Myers Squibb, discusses his vision of sequential immunotherapy for autoimmune diseases — including multiple sclerosis.
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Barcode lipids for absolute quantitation of liposomes in ocular tissues J. Control. Release (IF 10.8) Pub Date : 2024-04-17 Arto Merivaara, Jooseppi Puranen, Amir Sadeghi, Natalia Zashikhina, Lea Pirskanen, Tatu Lajunen, Tetsuya Terasaki, Seppo Auriola, Kati-Sisko Vellonen, Arto Urtti
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Nanodrugs based on co-delivery strategies to combat cisplatin resistance J. Control. Release (IF 10.8) Pub Date : 2024-04-17 Qiubo Wang, Hui Li, Taixia Wu, Bing Yu, Hailin Cong, Youqing Shen
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Recent progress on engineered micro/nanomaterials mediated modulation of gut microbiota for treating inflammatory bowel disease J. Control. Release (IF 10.8) Pub Date : 2024-04-17 Lingling Kan, Ziwen Zheng, Wanyue Fu, Yan Ma, Wanni Wang, Haisheng Qian, Lingling Xu
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Remotely controlled drug release in deep brain regions of non-human primates J. Control. Release (IF 10.8) Pub Date : 2024-04-17 Matthew G. Wilson, Taylor D. Webb, Henrik Odéen, Jan Kubanek
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The antibody–drug conjugate landscape Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-04-16
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Advancing cancer immunotherapy through siRNA-based gene silencing for immune checkpoint blockade Adv. Drug Deliver. Rev. (IF 16.1) Pub Date : 2024-04-16 Youngjin Choi, Su Hyun Seok, Hong Yeol Yoon, Ju Hee Ryu, Ick Chan Kwon
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A new era of targeting cystic fibrosis with non-viral delivery of genomic medicines Adv. Drug Deliver. Rev. (IF 16.1) Pub Date : 2024-04-16 Namratha Turuvekere Vittala Murthy, Kseniia Vlasova, Jonas Renner, Antony Jozic, Gaurav Sahay
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Synthesis and Structure–Activity Relationships for Glutamate Transporter Allosteric Modulators J. Med. Chem. (IF 7.3) Pub Date : 2024-04-16 Andréia C. K. Fontana, Adi N.R. Poli, Jitendra Gour, Yellamelli V.V. Srikanth, Nicholas Anastasi, Devipriya Ashok, Apeksha Khatiwada, Katelyn L. Reeb, Mary Hongying Cheng, Ivet Bahar, Scott M. Rawls, Joseph M. Salvino
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Mitochondria-Selective Dicationic Small-Molecule Ligand Targeting G-Quadruplex Structures for Human Colorectal Cancer Therapy J. Med. Chem. (IF 7.3) Pub Date : 2024-04-16 Bo-Xin Zheng, Wei Long, Wende Zheng, Yaoxun Zeng, Xiao-Chun Guo, Ka-Hin Chan, Meng-Ting She, Alan Siu-Lun Leung, Yu-Jing Lu, Wing-Leung Wong
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Targeting immunogenic cell stress and death for cancer therapy Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-04-15 Lorenzo Galluzzi, Emma Guilbaud, Darby Schmidt, Guido Kroemer, Francesco M. Marincola
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Hybrid biomineralized nanovesicles to enhance inflamed lung biodistribution and reduce side effect of glucocorticoid for ARDS therapy J. Control. Release (IF 10.8) Pub Date : 2024-04-15 Qi Qiao, Xiaonan Li, Xiangjun Ou, Xiong Liu, Chuansheng Fu, Yi Wang, Boning Niu, Li Kong, Conglian Yang, Zhiping Zhang
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mRNA-responsive two-in-one nanodrug for enhanced anti-tumor chemo-gene therapy J. Control. Release (IF 10.8) Pub Date : 2024-04-15 Yongfei Liu, Yuhong Lin, Han Xiao, Zhangcheng Fu, Xiaohui Zhu, Xiaoyong Chen, Chunsen Li, Chenyu Ding, Chunhua Lu
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Targeting KRAS Diversity: Covalent Modulation of G12X and Beyond in Cancer Therapy J. Med. Chem. (IF 7.3) Pub Date : 2024-04-15 Tonia Kirschner, Matthias P. Müller, Daniel Rauh
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Rational Design of a Novel Class of Human ClpP Agonists through a Ring-Opening Strategy with Enhanced Antileukemia Activity J. Med. Chem. (IF 7.3) Pub Date : 2024-04-15 Xinrong Xiang, Zhengyi Dai, Baozhu Luo, Ninglin Zhao, Song Liu, Jing Sui, Jiasheng Huang, Yuanzheng Zhou, Jinlong Gu, Jiangnan Zhang, Tao Yang, Rui Bao, Youfu Luo