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New route to target RAS Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-10
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The impact of, and expectations for, lipid nanoparticle technology: From cellular targeting to organelle targeting J. Control. Release (IF 10.8) Pub Date : 2024-05-09 Yusuke Sato, Takashi Nakamura, Yuma Yamada, Hideyoshi Harashima
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An ultrasound-activated nanoplatform remodels tumor microenvironment through diverse cell death induction for improved immunotherapy J. Control. Release (IF 10.8) Pub Date : 2024-05-09 Jingbo Ma, Haitao Yuan, Jingjing Zhang, Xin Sun, Letai Yi, Weihua Li, Zhifen Li, Chunjin Fu, Liuhai Zheng, Xiaolong Xu, Xiaoxian Wang, Fujing Wang, Da Yin, Jimin Yuan, Chengchao Xu, Zhijie Li, Xin Peng, Jigang Wang
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WRN inhibitors squeeze cancer cell vulnerability Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-08
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Development of Chinese innovative drugs in the USA Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-08
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First, do no harm: a global perspective on diversity and inclusion in clinical trials Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-08 Katharine Wright, Willyanne DeCormier Plosky, Hayat R. Ahmed, Sarah A. White, Barbara E. Bierer
New requirements for clinical trial sponsors to submit diversity action plans to the US Food and Drug Administration (FDA) are an important step to embed planning for diverse representation in clinical trial research. These must not, however, be implemented in ways that are detrimental to other countries’ health and research interests.
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Half-life extension via ABD-fusion leads to higher tumor uptake of an affibody-drug conjugate compared to PAS- and XTENylation. J. Control. Release (IF 10.8) Pub Date : 2024-05-08 Jie Zhang, Vitalina Bodenko, Maria Larkina, Ekaterina Bezverkhniaia, Tianqi Xu, Yunqi Liao, Ayman Abouzayed, Evgenii Plotnikov, Maria Tretyakova, Feruza Yuldasheva, Mikhail V. Belousov, Anna Orlova, Vladimir Tolmachev, Torbjörn Gräslund, Anzhelika Vorobyeva
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Multidimensional opioid abuse deterrence using a nanoparticle-polymer hybrid formulation J. Control. Release (IF 10.8) Pub Date : 2024-05-08 Sheryhan F. Gad, Anastasiia Vasiukhina, Joseph S. Keller, Luis Solorio, Yoon Yeo
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Knocking down of Xkr8 enhances chemotherapy efficacy through modulating tumor immune microenvironment J. Control. Release (IF 10.8) Pub Date : 2024-05-08 Yuang Chen, Chien-Yu Chen, Haozhe Huang, Zhangyi Luo, Yiqing Mu, Shichen Li, Yixian Huang, Song Li
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A CARM1 Inhibitor Potently Suppresses Breast Cancer Both In Vitro and In Vivo J. Med. Chem. (IF 7.3) Pub Date : 2024-05-07 Bing-ling Peng, Ting Ran, Xue Chen, Jian-cheng Ding, Zi-rui Wang, Wen-juan Li, Wen Liu
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Development of Inhibitors, Probes, and PROTAC Provides a Complete Toolbox to Study PARK7 in the Living Cell J. Med. Chem. (IF 7.3) Pub Date : 2024-05-07 Yuqing Jia, Merve Oyken, Robbert Q. Kim, Rayman T.N. Tjokrodirijo, Arnoud H. de Ru, Antonius P. A. Janssen, Stephan M. Hacker, Peter A. van Veelen, Paul P. Geurink, Aysegul Sapmaz
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Brain-Penetrant Macrocycles: Design Considerations, Future Prospects, and Call for Papers J. Med. Chem. (IF 7.3) Pub Date : 2024-05-07 Cori A. Malinky, Aaron M. Bender
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Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update J. Med. Chem. (IF 7.3) Pub Date : 2024-05-06 Laura Hillebrand, Xiaojun Julia Liang, Ricardo A. M. Serafim, Matthias Gehringer
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Antitumor Activity and Mechanistic Insights of a Mitochondria-Targeting Cu(I) Complex J. Med. Chem. (IF 7.3) Pub Date : 2024-05-06 Siyu Xu, Yashuai Hao, Xinyi Xu, Lu Huang, Yuqiong Liang, Jia Liao, Jie-Ru Yang, Yang Zhou, Mingdong Huang, Ke-Zhao Du, Cen Zhang, Peng Xu
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Discovery of 2,6-Naphthyridine Analogues as Selective FGFR4 Inhibitors for Hepatocellular Carcinoma J. Med. Chem. (IF 7.3) Pub Date : 2024-05-05 Heesook Oh, Jisook Kim, Seung Hyun Jung, Tae Hee Ha, Young Gil Ahn, Gibeom Nam, Kyeongwon Moon, Pargat Singh, In Su Kim
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Discovery of BIO-8169─A Highly Potent, Selective, and Brain-Penetrant IRAK4 Inhibitor for the Treatment of Neuroinflammation J. Med. Chem. (IF 7.3) Pub Date : 2024-05-02 Magnus Pfaffenbach, Philippe N. Bolduc, Zhili Xin, Fang Gao, Ryan Evans, Terry Fang, Jayanth V. Chodaparambil, Kate L. Henry, Pei Li, Steven Mathieu, Claire Metrick, Jorge A. Vera Rebollar, Rong-Fang Gu, Christie-Ann Mccarl, John Silbereis, Emily A. Peterson
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Designing novel macrocyclic drugs Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-07
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Targeting ephrin signalling in sepsis Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-07
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ASO to treat Timothy syndrome Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-07
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Cell selective BCL-2 inhibition enabled by lipid nanoparticles alleviates lung fibrosis J. Control. Release (IF 10.8) Pub Date : 2024-05-06 Rimpy Diwan, Himanshu N. Bhatt, Rui Dong, Igor L. Estevao, Armando Varela-Ramirez, Md Nurunnabi
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Biodegradable pyroptosis inducer with multienzyme-mimic activity kicks up reactive oxygen species storm for sensitizing immunotherapy J. Control. Release (IF 10.8) Pub Date : 2024-05-06 Junrong Wang, Luying Qiao, Guoqing Zhu, Qianqian Sun, Yulin Xie, Man Wang, Yaqi Xu, Chunxia Li
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Long-term combined blockade of CXCR4 and PD-L1 with in vivo reassembly for intensive tumor interference J. Control. Release (IF 10.8) Pub Date : 2024-05-06 Zhen-Wei Deng, Jian-Ke Yang, Kai-Jin Qiu, Ting-Jie Zhang, Zheng He, Na Wang, Xi-Guang Chen, Ya Liu
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Small extracellular vesicles of organoid-derived human retinal stem cells remodel Müller cell fate via miRNA: A novel remedy for retinal degeneration J. Control. Release (IF 10.8) Pub Date : 2024-05-05 Shudong Huang, Yuxiao Zeng, Qiang Guo, Ting Zou, Zheng Qin Yin
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UiO-66(Zr) as drug delivery system for non-steroidal anti-inflammatory drugs J. Control. Release (IF 10.8) Pub Date : 2024-05-05 Javier Salazar, Yoan Hidalgo-Rosa, Pia C. Burboa, Yi-nan Wu, Néstor Escalona, Angel Leiva, Ximena Zarate, Eduardo Schott
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Design, Synthesis, Bioactive Evaluation, and Molecular Dynamics Simulation of Novel 4H-Pyrano[3,2-c]pyridine Analogues as Potential Sterol 14α-Demethylase (CYP51) Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-05-04 Ailing Bao, Wenjing Jiang, Xiansong Xie, Deyuan Wang, Ziquan Deng, Jingwen Wang, Weiyi Li, Xiaorong Tang, Yingkun Yan
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Triazoles in Medicinal Chemistry: Physicochemical Properties, Bioisosterism, and Application J. Med. Chem. (IF 7.3) Pub Date : 2024-05-03 Qianwen Guan, Shuaishuai Xing, Lei Wang, Jiawei Zhu, Can Guo, Chunlei Xu, Qun Zhao, Yulan Wu, Yao Chen, Haopeng Sun
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Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2 J. Med. Chem. (IF 7.3) Pub Date : 2024-05-02 Yunhang Guo, Hai Xue, Nan Hu, Ye Liu, Hanzi Sun, Desheng Yu, Ling Qin, Gongyin Shi, Fan Wang, Lei Xin, Weihua Sun, Fan Zhang, Xiaomin Song, Shuran Li, Qiang Wei, Ying Guo, Yong Li, Xiaoxin Liu, Shuaishuai Chen, Taichang Zhang, Yue Wu, Dan Su, Yutong Zhu, Aiying Xu, Haipeng Xu, Shasha Yang, Zhijun Zheng, Junhua Liu, Xuefei Yang, Xi Yuan, Yuan Hong, Xuebing Sun, Yin Guo, Changyou Zhou, Xuesong Liu, Lai
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Histidine-Covalent Stapled Alpha-Helical Peptides Targeting hMcl-1 J. Med. Chem. (IF 7.3) Pub Date : 2024-05-02 Giulia Alboreggia, Parima Udompholkul, Carlo Baggio, Kendall Muzzarelli, Zahra Assar, Maurizio Pellecchia
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Differential Bioactivation Profiles of Different GS-441524 Prodrugs in Cell and Mouse Models: ProTide Prodrugs with High Cell Permeability and Susceptibility to Cathepsin A Are More Efficient in Delivering Antiviral Active Metabolites to the Lung J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Jiapeng Li, Daniel Macedo de Melo Jorge, Weiwen Wang, Shuxin Sun, Tristan Frum, Yu-An Hang, Yueting Liu, Xingwu Zhou, Jingcheng Xiao, Xinwen Wang, Jason R. Spence, Christiane E. Wobus, Hao-Jie Zhu
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Discovery of a Novel and Potent Cyclin-Dependent Kinase 8/19 (CDK8/19) Inhibitor for the Treatment of Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Jianyu Xu, Hongyun Qi, Zhen Wang, Ling Wang, Barbara Steurer, Xin Cai, Jinxin Liu, Alex Aliper, Man Zhang, Feng Ren, Alex Zhavoronkov, Xiao Ding
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Discovery of Selective Proteolysis-Targeting Chimera Degraders Targeting PTP1B as Long-Term Hypoglycemic Agents J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Zunhua Yang, Yuqi Ying, Shaobing Cheng, Jiamin Wu, Ziwei Zhang, Pei Hu, Jian Xiong, Huilan Li, Qing Zeng, Zhifang Cai, Yulin Feng, Yuanying Fang
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Alpha-galactosylceramide improves the potency of mRNA LNP vaccines against cancer and intracellular bacteria J. Control. Release (IF 10.8) Pub Date : 2024-05-04 Sofie Meulewaeter, Ilke Aernout, Joke Deprez, Yanou Engelen, Margo De Velder, Lorenzo Franceschini, Karine Breckpot, Serge Van Calenbergh, Caroline Asselman, Katie Boucher, Francis Impens, Stefaan C. De Smedt, Rein Verbeke, Ine Lentacker
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Mapping cysteine ligandability Nat. Rev. Drug. Disc. (IF 120.1) Pub Date : 2024-05-03
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Molecular Pathways Governing the Termination of Liver Regeneration Pharmacol. Rev. (IF 21.1) Pub Date : 2024-05-01 Lianne R. de Haan, Rowan F. van Golen, Michal Heger, Martin Michel
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Steatotic Liver Disease: Pathophysiology and Emerging Pharmacotherapies Pharmacol. Rev. (IF 21.1) Pub Date : 2024-05-01 Michail Kokkorakis, Emir Muzurović, Špela Volčanšek, Marlene Chakhtoura, Michael A. Hill, Dimitri P. Mikhailidis, Christos S. Mantzoros, Ali Eid
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MDM2 Inhibitors for Cancer Therapy: The Past, Present, and Future Pharmacol. Rev. (IF 21.1) Pub Date : 2024-05-01 Wei Wang, Najah Albadari, Yi Du, Josef F. Fowler, Hannah T. Sang, Wa Xian, Frank McKeon, Wei Li, Jia Zhou, Ruiwen Zhang, Michael Gottesman
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Prostaglandin E2 in the Tumor Microenvironment, a Convoluted Affair Mediated by EP Receptors 2 and 4 Pharmacol. Rev. (IF 21.1) Pub Date : 2024-05-01 Ana Santiso, Akos Heinemann, Julia Kargl, Michael Gottesman
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Adrenoceptor Desensitization: Current Understanding of Mechanisms Pharmacol. Rev. (IF 21.1) Pub Date : 2024-05-01 Dina Maaliki, Aneese A. Jaffa, Suzanne Nasser, Amirhossein Sahebkar, Ali H. Eid, Paul Insel, Martin Michel
G-protein coupled receptors (GPCRs) transduce a wide range of extracellular signals. They are key players in the majority of biologic functions including vision, olfaction, chemotaxis, and immunity. However, as essential as most of them are to body function and homeostasis, overactivation of GPCRs has been implicated in many pathologic diseases such as cancer, asthma, and heart failure (HF). Therefore
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New Advances in the Pharmacology and Toxicology of Lithium: A Neurobiologically Oriented Overview Pharmacol. Rev. (IF 21.1) Pub Date : 2024-05-01 Analia Bortolozzi, Giovanna Fico, Michael Berk, Marco Solmi, Michele Fornaro, Joao Quevedo, Carlos A. Zarate, Lars V. Kessing, Eduard Vieta, Andre F. Carvalho, Robert Dantzer
Over the last six decades, lithium has been considered the gold standard treatment for the long-term management of bipolar disorder due to its efficacy in preventing both manic and depressive episodes as well as suicidal behaviors. Nevertheless, despite numerous observed effects on various cellular pathways and biologic systems, the precise mechanism through which lithium stabilizes mood remains elusive
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From cells to subcellular organelles: Next-generation cancer therapy based on peptide self-assembly Adv. Drug Deliver. Rev. (IF 16.1) Pub Date : 2024-05-03 Huayang Liu, Huaimin Wang
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Metabolic dysfunction-associated steatohepatitis treated by poly(ethylene glycol)-block-poly(cysteine) block copolymer-based self-assembling antioxidant nanoparticles J. Control. Release (IF 10.8) Pub Date : 2024-05-03 Yuta Koda, Yukio Nagasaki
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Injectable hydrogel harnessing foreskin mesenchymal stem cell-derived extracellular vesicles for treatment of chronic diabetic skin wounds J. Control. Release (IF 10.8) Pub Date : 2024-05-03 Chang Xu, Jin-Feng Cao, Yue Pei, Yujin Kim, Huiyeon Moon, Chui-Qin Fan, Mao-Chuan Liao, Xing-Yu Wang, Fei Yao, Yu-Jun Zhang, Shao-Hui Zhang, Jian Zhang, Jian-Zhang Li, Jong Seung Kim, Lian Ma, Zhong-Jian Xie
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Metal coordination nanotheranostics mediated by nucleoside metabolic inhibitors potentiate STING pathway activation for cancer metalloimmunotherapy J. Control. Release (IF 10.8) Pub Date : 2024-05-03 Lianyi Yang, Yazhen Wang, Yujun Song, Zeya Li, Lei Lei, Hanmei Li, Bin He, Jun Cao, Huile Gao
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Biomaterials-mediated radiation-induced diseases treatment and radiation protection J. Control. Release (IF 10.8) Pub Date : 2024-05-02 Jianping Man, Yanhua Shen, Yujie Song, Kai Yang, Pei Pei, Lin Hu
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Novel Inhibitory Site Revealed by XAP044 Mode of Action on the Metabotropic Glutamate 7 Receptor Venus Flytrap Domain J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Nunzia Cristiano, Alexandre Cabayé, Isabelle Brabet, Ralf Glatthar, Amelie Tora, Cyril Goudet, Hugues-Olivier Bertrand, Anne Goupil-Lamy, Peter J. Flor, Jean-Philippe Pin, Isabelle McCort-Tranchepain, Francine C. Acher
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[52Mn]Mn-BPPA-Trastuzumab: A Promising HER2-Specific PET Radiotracer J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Ngô Minh Toàn, Adrienn Vágner, Gábor Nagy, Gábor Ország, Tamás Nagy, Csaba Csikos, Balázs Váradi, Gergő Zoltán Sajtos, István Kapus, Zoltán Szoboszlai, Dezső Szikra, György Trencsényi, Gyula Tircsó, Ildikó Garai
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Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Lianchao Liu, Abhijit Parolia, Yihan Liu, Caiyun Hou, Tongchen He, Yuanyuan Qiao, Sanjana Eyunni, Jie Luo, Chungen Li, Yongxing Wang, Fengtao Zhou, Weixue Huang, Xiaomei Ren, Zhen Wang, Arul M. Chinnaiyan, Ke Ding
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A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19 J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Charlotte M. N. Allerton, Joel T. Arcari, Lisa M. Aschenbrenner, Melissa Avery, Bruce M. Bechle, Mohammad Amin Behzadi, Britton Boras, Leanne M. Buzon, Rhonda D. Cardin, Natasha R. Catlin, Anthony A. Carlo, Karen J. Coffman, Alyssa Dantonio, Li Di, Heather Eng, Kathleen A. Farley, Rose Ann Ferre, Steven S. Gernhardt, Scott A. Gibson, Samantha E. Greasley, Siennah R. Greenfield, Brett L. Hurst, Amit
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Discovery of a New Anti-Inflammatory Agent from Anemoside B4 Derivatives and Its Therapeutic Effect on Colitis by Targeting Pyruvate Carboxylase J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Lijuan Lv, Qiurong Li, Kexin Wang, Jianping Zhao, Kejun Deng, Ran Zhang, Zhong Chen, Ikhlas A. Khan, Chunshan Gui, Suxiang Feng, Shilin Yang, Yanli Liu, Qiongming Xu
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A Nonbactericidal Anionic Antimicrobial Peptide Provides Prophylactic and Therapeutic Efficacies against Bacterial Infections in Mice by Immunomodulatory–Antithrombotic Duality J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Yanmei He, Shimei Ruan, Guozhu Liang, Jing Hao, Xiaoyan Zhou, Zhuorui Li, Lixian Mu, Jing Wu, Hailong Yang
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New Improved cGMP Analogues to Target Rod Photoreceptor Degeneration J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Oswaldo Pérez, Agnese Stanzani, Li Huang, Nicolaas Schipper, Thorsteinn Loftsson, Martin Bollmark, Valeria Marigo
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Oral targeted drug delivery to post-gastrointestinal sites J. Control. Release (IF 10.8) Pub Date : 2024-05-01 Rongze Han, Haisheng He, Yi Lu, Huiping Lu, Shun Shen, Wei Wu
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Enhancing calvarial defects repair with PDGF-BB mimetic peptide hydrogels J. Control. Release (IF 10.8) Pub Date : 2024-05-01 Xia Wu, Mingming Yan, Jun Shen, Yatong Xiang, Ke Jian, Xiaoyun Pan, Dan Yuan, Junfeng Shi
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Biomaterial-based scaffolds for direct in situ programming of tumor-infiltrating T lymphocytes J. Control. Release (IF 10.8) Pub Date : 2024-05-01 V.V. Inamdar, S. Hao, S.B. Stephan, M.T. Stephan
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Emerging advances in delivery systems for mRNA cancer vaccines J. Control. Release (IF 10.8) Pub Date : 2024-05-01 Zhimei Jiang, Yanhua Xu, Guangsheng Du, Xun Sun
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Site-selective antibody-lipid conjugates for surface functionalization of red blood cells and targeted drug delivery J. Control. Release (IF 10.8) Pub Date : 2024-05-01 Biquan Li, Dingdong Yuan, Hongfei Chen, Xun Wang, Yujie Liang, Clarence T.T. Wong, Jiang Xia
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Illuminating Dark Chemical Matter Using the Cell Painting Assay J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Axel Pahl, Jie Liu, Sohan Patil, Soheila Rezaei Adariani, Beate Schölermann, Jens Warmers, Jana Bonowski, Sandra Koska, Yasemin Akbulut, Carina Seitz, Sonja Sievers, Slava Ziegler, Herbert Waldmann
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Novel Isoalantolactone-Based Derivatives as Potent NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Min Zhao, Neng Ye, Ling Liu, Rui-Jia Zhang, Na Li, Jing Peng, Xiao-Ying Cai, Xue-Qin Jiang, Kai-Yue Su, Xin-Lu Zhang, Qian-Ru Rao, Kong-Jun Liu, De-Xin Deng, Ai-Hua Peng, Ming-Hai Tang, Li-Juan Chen, Wen-Shuang Wu, Hao-Yu Ye
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Discovery of Potent Multikinase Type-II Inhibitors Targeting CDK5 in the DFG-out Inactive State with Promising Potential against Glioblastoma J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Zahra R. Khan, Philip J. Welsby, Izabela Stasik, Joseph M. Hayes
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Multitarget μ-Opioid Receptor Agonists─Neuropeptide FF Receptor Antagonists Induce Potent Antinociception with Reduced Adverse Side Effects J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Jolien De Neve, Khadija Elhabazi, Simon Gonzalez, Claire Herby, Séverine Schneider, Valérie Utard, Rosine Fellmann-Clauss, Nathalie Petit-Demouliere, Sandra Lecat, Mélanie Kremer, Aurelia Ces, François Daubeuf, Charlotte Martin, Steven Ballet, Frédéric Bihel, Frédéric Simonin