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Engineered parasite delivers proteins to the brain Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-08-23
Discover the world’s best science and medicine | Nature.com
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Degrading cell-free DNA to prevent recurrent stroke Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-08-22
Discover the world’s best science and medicine | Nature.com
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Design, Synthesis, and Evaluation of the Antitubercular Activity of 5-Phenyl Substituted-5, 6-dihydropyrido[2, 3-d]pyrimidine-4, 7(3H, 8H)-dione Compounds J. Med. Chem. (IF 6.8) Pub Date : 2024-08-21 Lianqi Sun, Shibo Kou, Bin Wang, Yongjian Wang, Jianzhou Meng, Tianfu Liu, Yuanyuan Ma, Jianyuan Zhao, Hong Yi, Shan Cen, Yu Lu, Zhuorong Li
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Design, Synthesis, and Biological Evaluation of 5-Amino-4-fluoro-1H-benzo[d]imidazole-6-carboxamide Derivatives as Novel and Potential MEK/RAF Complex Inhibitors Based on the “Clamp” Strategy J. Med. Chem. (IF 6.8) Pub Date : 2024-08-21 Peng Wang, Yongting Yuan, Tao Yang, Yurong Zou, Minghai Tang, Ziyan Ma, Weichen Bo, Songhui Qin, Yong Chen, Tao Guo, Zhongning Guo, Jianhong Yang, Mingli Xiang, Lijuan Chen
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Discovery of Novel Antiosteoporosis Leads with Bone Resorption Inhibition and Anabolic Promotion through a Chemotype-Assembly Approach J. Med. Chem. (IF 6.8) Pub Date : 2024-08-21 Dane Huang, Chao Zhao, Ruyue Li, Nan Yao, Jun Xu, Qiong Gu
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Synthesis and Photodynamic Activities of Pyridine- or Pyridinium-Substituted Aza-BODIPY Photosensitizers J. Med. Chem. (IF 6.8) Pub Date : 2024-08-21 Chang Liu, Chuan Liu, Xin Ji, Weili Zhao, Xiaochun Dong
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Discovery of Pyrazolo[1,5-a]pyridine Derivatives as Potent and Selective PI3Kγ/δ Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-08-20 Chun Wang, Fengming Zou, Ziping Qi, Qingwang Liu, Lijuan Shen, Xinyu Yuan, Maoqing Deng, Aoli Wang, Beilei Wang, Li Wang, Xiaofei Liang, Qingsong Liu, Jing Liu
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Examining Hemin and its Derivatives: Induction of Heme-Oxygenase-1 Activity and Oxidative Stress in Breast Cancer Cells through Collaborative Experimental Analysis and Molecular Dynamics Simulations J. Med. Chem. (IF 6.8) Pub Date : 2024-08-19 Amir M. Alsharabasy, Panagiotis I. Lagarias, Konstantinos D. Papavasileiou, Antreas Afantitis, Pau Farràs, Sharon Glynn, Abhay Pandit
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Discovery of a Covalent Inhibitor of Pro-Caspase-1 Zymogen Blocking NLRP3 Inflammasome Activation and Pyroptosis J. Med. Chem. (IF 6.8) Pub Date : 2024-08-19 Dongyi Cao, Ruiying Xi, Hongye Li, Zhonghui Zhang, Xiaoke Shi, Shanshan Li, Yujie Jin, Wanli Liu, Guolin Zhang, Xiaohua Liu, Shunxi Dong, Xiaoming Feng, Fei Wang
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Identification of CDK4/6 Inhibitors as Small Molecule NLRP3 Inflammasome Activators that Facilitate IL-1β Secretion and T Cell Adjuvanticity J. Med. Chem. (IF 6.8) Pub Date : 2024-08-20 Adam M. Weiss, Marcos A. Lopez II, Matthew G. Rosenberger, Jeremiah Y. Kim, Jingjing Shen, Qing Chen, Trevor Ung, Udoka M. Ibeh, Hannah Riley Knight, Nakisha S. Rutledge, Bradley Studnitzer, Stuart J. Rowan, Aaron P. Esser-Kahn
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Development of Nitric Oxide-Donating Netarsudil Derivatives as a Synergistic Therapy for Glaucoma with Reduced Ocular Irritation J. Med. Chem. (IF 6.8) Pub Date : 2024-08-20 Cunrui Li, Mingchao Zhu, Songqi Liu, Jiaming Zhang, Hui Ye, Chen Zhang, Duorui Ji, Haoyang Tang, Yihua Zhang, Jianbing Wu, Zhangjian Huang
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Structure-Based Drug Design of 2-Amino-[1,1′-biphenyl]-3-carboxamide Derivatives as Selective PKMYT1 Inhibitors for the Treatment of CCNE1-Amplified Breast Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-08-20 Chaofan Wang, Yan Fang, Ziqin Zhou, Zhuoheng Liu, Fang Feng, Xuan Wan, Yan Li, Shuang Liu, Jian Ding, Zhi-Min Zhang, Hua Xie, Xiaoyun Lu
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Investigating Active Site Binding of Ligands to High and Low Activity Carbonic Anhydrase Enzymes Using Native Mass Spectrometry J. Med. Chem. (IF 6.8) Pub Date : 2024-08-20 Yezhou Yu, Louise M. Sternicki, David H. Hilko, Russell J. Jarrott, Giovanna Di Trapani, Kathryn F. Tonissen, Sally-Ann Poulsen
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Rational Design of a Novel 6H-Benzo[c]chromen Series as Selective PI3Kα Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-08-19 Xue Shi, Heng Feng, Haigang Tian, Haibiao Ma, Xiaomeng Pang, Chenhan Mao, Peng Xiang, Zhengze Xu, Weidong Han, Yuxiang Yan, Wei Chen, Yuqing Nan, Guanjun Nan, Zhenyue Hu, Lingyun Hui, Chenglong Li, Yiping Li
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Discovery of 1,2,4-Triazole-3-thione Derivatives as Potent and Selective DCN1 Inhibitors for Pathological Cardiac Fibrosis and Remodeling J. Med. Chem. (IF 6.8) Pub Date : 2024-08-19 Zhang-Xu He, Ge Gao, Hui Qiao, Guan-jun Dong, Zengyangzong Dan, Ya-lan Li, Yu-ruo Qi, Qian Zhang, Shuo Yuan, Hong-Min Liu, Jianzeng Dong, Wen Zhao, Li-Ying Ma
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Evo312: An Evodiamine Analog and Novel PKCβI Inhibitor with Potent Antitumor Activity in Gemcitabine-Resistant Pancreatic Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-08-16 Eun Seo Bae, Junhwa Hong, Yijae Lim, Woong Sub Byun, Simin Chun, Suckchang Hong, Sang Kook Lee
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Arcopilins: A New Family of Staphylococcus aureus Biofilm Disruptors from the Soil Fungus Arcopilus navicularis J. Med. Chem. (IF 6.8) Pub Date : 2024-08-14 Esteban Charria-Girón, Haoxuan Zeng, Tatiana E. Gorelik, Alexandra Pahl, Khai-Nghi Truong, Hedda Schrey, Frank Surup, Yasmina Marin-Felix
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FDA approves IDH1 and IDH2 inhibitor for brain cancer Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-08-16
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FDA approves first TCR-engineered T cell therapy, for rare soft-tissue cancer Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-08-16
Discover the world’s best science and medicine | Nature.com
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Design, Synthesis, and Biological Activity of Novel Quinone Derivatives as Potent STAT3 Inhibitors for Psoriasis Treatment J. Med. Chem. (IF 6.8) Pub Date : 2024-08-16 Ling Chen, Liuliu Wang, Jinlei Gao, Yuanzhu Xie, Xu Deng, Guang Tian, Mingjian Li, Zhongtai Sui, Cailin Luo, Li Liu, Xinyu Huang, Xinyu Zhu, Shuaiwen Zhu, Zhiyong Luo, Dayou Ma, Suyou Liu
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Small Molecular Inhibitors That Target ATM for Drug Discovery: Current Research and Potential Prospective J. Med. Chem. (IF 6.8) Pub Date : 2024-08-16 Chunlin Qian, Xiaoxue Li, Jifa Zhang, Yuxi Wang
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Methyl-Transferase-Like Protein 16 (METTL16): The Intriguing Journey of a Key Epitranscriptomic Player Becoming an Emerging Biological Target J. Med. Chem. (IF 6.8) Pub Date : 2024-08-16 Simona Barone, Carmen Cerchia, Vincenzo Summa, Margherita Brindisi
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Discovery of KT-474─a Potent, Selective, and Orally Bioavailable IRAK4 Degrader for the Treatment of Autoimmune Diseases J. Med. Chem. (IF 6.8) Pub Date : 2024-08-16 Xiaozhang Zheng, Nan Ji, Veronica Campbell, Anthony Slavin, Xiao Zhu, Dapeng Chen, Haojing Rong, Brad Enerson, Michele Mayo, Kirti Sharma, Chris M. Browne, Christine R. Klaus, Haoran Li, Ginny Massa, Alice A. McDonald, Yatao Shi, Mike Sintchak, Stephanie Skouras, Dirk M. Walther, Karen Yuan, Yi Zhang, Joe Kelleher, Guang Liu, Xinbo Luo, Nello Mainolfi, Matthew M. Weiss
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Chemoenzymatic Synthesis of DNP-Functionalized FGFR1-Binding Peptides as Novel Peptidomimetic Immunotherapeutics for Treating Lung Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-08-15 Xiaohui Li, Haiyan Liu, Shengjie Ding, Ziyu Tian, Jia Song, Huayu Zhong, Luwei Fu, Xiaojun Cai, Fengyu Huang, Kun Wang, Lilong Dong, Weixin Zhao, Yuepiao Cai, Shijie Dai
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Peptide-Mediated Small Molecule Lysosome-Targeting Chimeras for Targeted Degradation of Membrane and Intracellular Proteins J. Med. Chem. (IF 6.8) Pub Date : 2024-08-15 Shuqiang Chen, Wei Wang, Zhipeng Chen, Ruyan Li, Zhe Wu, Guoqiang Dong, Chunquan Sheng
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Rational Design of a Hetero-multinuclear Gadolinium(III)–Copper(II) Complex: Integrating Magnetic Resonance Imaging, Photoacoustic Imaging, Mild Photothermal Therapy, Chemotherapy and Immunotherapy of Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-08-14 Xueyu Man, Wenjuan Li, Minghui Zhu, Shanhe Li, Gang Xu, Zhenlei Zhang, Hong Liang, Feng Yang
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Predicting tissue distribution and tumor delivery of nanoparticles in mice using machine learning models J. Control. Release (IF 10.5) Pub Date : 2024-08-16 Kun Mi, Wei-Chun Chou, Qiran Chen, Long Yuan, Venkata N. Kamineni, Yashas Kuchimanchi, Chunla He, Nancy A. Monteiro-Riviere, Jim E. Riviere, Zhoumeng Lin
Nanoparticles (NPs) can be designed for targeted delivery in cancer nanomedicine, but the challenge is a low delivery efficiency (DE) to the tumor site. Understanding the impact of NPs' physicochemical properties on target tissue distribution and tumor DE can help improve the design of nanomedicines. Multiple machine learning and artificial intelligence models, including linear regression, support
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Acoustically responsive scaffolds: Unraveling release kinetics and mechanisms for sustained, steady drug delivery J. Control. Release (IF 10.5) Pub Date : 2024-08-16 Haijun Xiao, Mitra Aliabouzar, Mario L. Fabiilli
Hydrogels can serve as local drug delivery depots that protect the biological activity of labile therapeutics. However, drug release from conventional hydrogels is typically rapid, which is not ideal for many therapeutic agents. We developed a composite hydrogel that enables sustained drug release in response to ultrasound. The composite, termed an acoustically responsive scaffold (ARS), consists of
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Targeting Solvent-Front Mutations for Kinase Drug Discovery: From Structural Basis to Design Strategies J. Med. Chem. (IF 6.8) Pub Date : 2024-08-15 Yang Zhou, Jibo Kang, Xiaoyun Lu
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Nonpeptidic Irreversible Inhibitors of SARS-CoV-2 Main Protease with Potent Antiviral Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-08-15 Angelo Oneto, Ghazl Al Hamwi, Laura Schäkel, Nadine Krüger, Katharina Sylvester, Marvin Petry, Rasha Abu Shamleh, Thanigaimalai Pillaiyar, Tobias Claff, Anke C. Schiedel, Norbert Sträter, Michael Gütschow, Christa E. Müller
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Allosteric Activation of Protein Phosphatase 5 with Small Molecules J. Med. Chem. (IF 6.8) Pub Date : 2024-08-15 Qiuyue Zhang, Ling Yan, Lixiao Zhang, Jia Yu, Zeyu han, Hua Liu, Jinying Gu, Keran Wang, Jiayi Wang, Fangsu Chen, Rongde Zhao, Yang Yan, Cheng Jiang, Qidong You, Lei Wang
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Discovery of a Novel Benzimidazole Derivative Targeting Histone Deacetylase to Induce Ferroptosis and Trigger Immunogenic Cell Death J. Med. Chem. (IF 6.8) Pub Date : 2024-08-15 Meng Liu, Shan Gao, Yong Wang, Xinying Yang, Hao Fang, Xuben Hou
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Ocotillol Derivatives Mitigate Retinal Ischemia-Reperfusion Injury by Regulating the Keap1/Nrf2/ARE Signaling Pathway J. Med. Chem. (IF 6.8) Pub Date : 2024-08-15 Xin Zhang, Wen Zhang, Laien Zhao, Gongshan Ma, Yanmei Huang, Zhiyuan Geng, Qian Jiang, Xiaomei Wen, Yuqi Lin, Qingguo Meng, Zhuhong Zhang, Yi Bi
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Design and Evaluation of 3-Phenyloxetane Derivative Agonists of the Glucagon-Like Peptide-1 Receptor J. Med. Chem. (IF 6.8) Pub Date : 2024-08-14 Zhimin Zhang, Hao Pan, Liubin Guo, Cancan Cai, Tingni Chen, Zhiping Zhang, Xu Yang, Haowen Zheng, Chunhua Jiang, Zhiyong Wang, Yacheng Yang, Zhe Wang, Xiaohua Zhang, Yuchen Zhang, Dongzhou Liu
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Optimization of Ethoxzolamide Analogs with Improved Pharmacokinetic Properties for In Vivo Efficacy against Neisseria gonorrhoeae J. Med. Chem. (IF 6.8) Pub Date : 2024-08-14 Molly S. Youse, Nader S. Abutaleb, Alessio Nocentini, Abdallah S Abdelsattar, Farman Ali, Claudiu T. Supuran, Mohamed N. Seleem, Daniel P. Flaherty
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A golden age of muscarinic acetylcholine receptor modulation in neurological diseases Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-08-14 Andrew B. Tobin
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Intestinal Barrier, Immunity and Microbiome: Partners in the Depression Crime Pharmacol. Rev. (IF 19.3) Pub Date : 2024-09-01 Eva M. Medina-Rodríguez, José Martínez-Raga, Yolanda Sanz, Habibeh Khoshbouei
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The Development of Cannabinoids as Therapeutic Agents in the United States Pharmacol. Rev. (IF 19.3) Pub Date : 2024-09-01 Conor H. Murray, Brenda M. Gannon, Peter J. Winsauer, Ziva D. Cooper, Marcus S. Delatte, Matthew Banks
Cannabis is one of the oldest and widely used substances in the world. Cannabinoids within the cannabis plant, known as phytocannabinoids, mediate cannabis’ effects through interactions with the body’s endogenous cannabinoid system. This endogenous system, the endocannabinoid system, has important roles in physical and mental health. These roles point to the potential to develop cannabinoids as therapeutic
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The Art of Finding the Right Drug Target: Emerging Methods and Strategies Pharmacol. Rev. (IF 19.3) Pub Date : 2024-09-01 Zi-Chang Jia, Xue Yang, Yi-Kun Wu, Min Li, Debatosh Das, Mo-Xian Chen, Jian Wu, Martin Michel
Drug targets are specific molecules in biological tissues and body fluids that interact with drugs. Drug target discovery is a key component of drug discovery and is essential for the development of new drugs in areas such as cancer therapy and precision medicine. Traditional in vitro or in vivo target discovery methods are time-consuming and labor-intensive, limiting the pace of drug discovery. With
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Pharmacology of Hydrogen Sulfide and Its Donors in Cardiometabolic Diseases Pharmacol. Rev. (IF 19.3) Pub Date : 2024-09-01 Hai-Jian Sun, Qing-Bo Lu, Xue-Xue Zhu, Zhang-Rong Ni, Jia-Bao Su, Xiao Fu, Guo Chen, Guan-Li Zheng, Xiao-Wei Nie, Jin-Song Bian, Richard Ye
Cardiometabolic diseases (CMDs) are major contributors to global mortality, emphasizing the critical need for novel therapeutic interventions. Hydrogen sulfide (H2S) has garnered enormous attention as a significant gasotransmitter with various physiological, pathophysiological, and pharmacological impacts within mammalian cardiometabolic systems. In addition to its roles in attenuating oxidative stress
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Conotoxins Targeting Voltage-Gated Sodium Ion Channels Pharmacol. Rev. (IF 19.3) Pub Date : 2024-09-01 Shengrong Pei, Nan Wang, Zaoli Mei, Dongting Zhangsun, David J. Craik, J. Michael McIntosh, Xiaopeng Zhu, Sulan Luo, Thomas Gudermann
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Cardiovascular Pharmacogenetics: From Discovery of Genetic Association to Clinical Adoption of Derived Test Pharmacol. Rev. (IF 19.3) Pub Date : 2024-09-01 Benoît Delabays, Katerina Trajanoska, Joshua Walonoski, Vincent Mooser, Rhian Touyz
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Topically Applied Therapies for the Treatment of Skin Disease: Past, Present, and Future Pharmacol. Rev. (IF 19.3) Pub Date : 2024-09-01 Marc Brown, Adrian Williams, Robert P. Chilcott, Brendan Brady, Jon Lenn, Charles Evans, Lynn Allen, William J. McAuley, Mubinah Beebeejaun, Jasmin Haslinger, Claire Beuttel, Raquel Vieira, Florencia Guidali, Margarida Miranda, Clive Page
The purpose of this review is to summarize essential biological, pharmaceutical, and clinical aspects in the field of topically applied medicines that may help scientists when trying to develop new topical medicines. After a brief history of topical drug delivery, a review of the structure and function of the skin and routes of drug absorption and their limitations is provided. The most prevalent diseases
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International Union of Basic and Clinical Pharmacology CXIV: Orexin Receptor Function, Nomenclature and Pharmacology Pharmacol. Rev. (IF 19.3) Pub Date : 2024-09-01 Jyrki. P. Kukkonen, Laura H. Jacobson, Daniel Hoyer, Maiju K. Rinne, Stephanie L. Borgland, Eliot Ohlstein
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NIR-triggered and Thermoresponsive Core-shell nanoparticles for synergistic anticancer therapy J. Control. Release (IF 10.5) Pub Date : 2024-08-15 Hong Zhang, Xiao Wang, Xiaorong Yang, Zehua Wu, Qin Chen, Qiaolin Wei, Yong Guo, Quan Hu, Jia-Wei Shen
Recent advancements in cancer treatment have underscored the inadequacy of conventional monotherapies in addressing complex malignant tumors. Consequently, there is a growing interest in synergistic therapies capable of overcoming the limitations of monotherapies, leading to more personalized and effective approaches. Among these, the combination of photothermal therapy (PTT) and chemotherapy has emerged
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Systemically targeting monocytic myloid-derrived suppressor cells using dendrimers and their cell-level biodistribution kinetics J. Control. Release (IF 10.5) Pub Date : 2024-08-15 Chad A. Littrell, Gregory P. Takacs, Chenikkayala Siva Sankara, Alexandra Sherman, Kai A. Rubach, Julia S. Garcia, Coral A. Bell, Tejashwini Lnu, Jeffrey K. Harrison, Fan Zhang
The focus of nanoparticles trafficking has been mostly on their tissue-level biodistribution and clearance. Recent progress in the nanomedicine field suggests that the targeting of nanoparticles to immune cells can be used to modulate the immune response and enhance therapeutic delivery to the diseased tissue. In the presence of tumor lesions, monocytic-myeloid-derived suppressor cells (M-MDSCs) expand
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The breast cancer drug market Nat. Rev. Drug. Disc. (IF 122.7) Pub Date : 2024-08-13
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ZIF-8-modified hydrogel sequentially delivers angiogenic and osteogenic growth factors to accelerate vascularized bone regeneration J. Control. Release (IF 10.5) Pub Date : 2024-08-14 Xiaolian Niu, Shengzhao Xiao, Ruoyu Huang, Di Huang, Katerina E. Aifantis, Han Yu, Chao Xue, Lan Yin, Nicholas Dunne, Xiaoming Li
To realize high-quality vascularized bone regeneration, we developed a multifunctional hydrogel (SHPP-ZB) by incorporating BMP-2@ZIF-8/PEG-NH nanoparticles (NPs) into a sodium alginate/hydroxyapatite/polyvinyl alcohol hydrogel loaded with PDGF-BB, allowing for the sequential release of angiogenic and osteogenic growth factors (GFs) during bone repair. ZIF-8 served as a protective host for BMP-2 from
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EV20/Omomyc: A novel dual MYC/HER3 targeting immunoconjugate J. Control. Release (IF 10.5) Pub Date : 2024-08-14 Sandra Bibbò, Emily Capone, Giulio Lovato, Sara Ponziani, Alessia Lamolinara, Manuela Iezzi, Rossano Lattanzio, Katia Mazzocco, Martina Morini, Francesco Giansanti, Vincenzo De Laurenzi, Jonathan Whitfield, Stefano Iacobelli, Rodolfo Ippoliti, Marie-Eve Beaulieu, Laura Soucek, Arturo Sala, Gianluca Sala
MYC is one of the most important therapeutic targets in human cancer. Many attempts have been made to develop small molecules that could be used to curb its activity in patients, but most failed to identify a suitable direct inhibitor. After years of preclinical characterization, a tissue-penetrating peptide MYC inhibitor, called Omomyc, has been recently successfully used in a Phase I dose escalation
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Modified montmorillonite armed probiotics with enhanced on-site mucus-depleted intestinal colonization and H2S scavenging for colitis treatment J. Control. Release (IF 10.5) Pub Date : 2024-08-14 Jiali Yang, Shengchan Ge, Shaochong Tan, Hua Liu, Mingzhu Yang, Wei Liu, Kaixiang Zhang, Zhenzhong Zhang, Junjie Liu, Jinjin Shi, Zhi-Hao Wang, Jitian Li
Inflammatory bowel diseases (IBD) are often associated with dysregulated gut microbiota and excessive inflammatory microenvironment. Probiotic therapy combined with inflammation management is a promising approach to alleviate IBD, but the efficacy is hindered by the inferior colonization of probiotics in mucus-depleted inflammatory bowel segments. Here, we present modified montmorillonite armed probiotic
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Design and Synthesis of 7-Oxabicyclo[2.2.1]heptane-2,3-dicarboxylic Acid Derivatives as PP5 Inhibitors To Reverse Temozolomide Resistance in Glioblastoma Multiforme J. Med. Chem. (IF 6.8) Pub Date : 2024-08-13 Zekun Li, Mochen Guo, Mingxiao Gu, Zhongtian Cai, Qiuyu Wu, Jia Yu, Meilun Tang, Chenxi He, Yuxuan Wang, Piaoyang Sun, Qidong You, Lei Wang
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Engineered bacterial membrane vesicle as safe and efficient nano-heaters to reprogram tumor microenvironment for enhanced immunotherapy J. Control. Release (IF 10.5) Pub Date : 2024-08-13 Kunguo Liu, Shiyu Du, Jiawei Yang, Juanjuan Li, Shijie Wang, Zhibin Zhang, Wen Luo, Chao Chen, Jingjing Yang, Xin Han
The immunosuppressive tumor microenvironment (TME) in solid tumors often impedes the efficacy of immunotherapy. Bacterial outer membrane vesicles (OMVs), as a promising cancer vaccine that can potently stimulate immune responses, have garnered interest as a potential platform for cancer therapy. However, the low yield of OMVs limits their utilization. To address this limitation, we developed a novel
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Synthesis and Characterization of Folic Acid-Conjugated Terbium Complexes as Luminescent Probes for Targeting Folate Receptor-Expressing Cells J. Med. Chem. (IF 6.8) Pub Date : 2024-08-13 Grace T. McMullon, Aiarpi Ezdoglian, Anna C. Booth, Pilar Jimenez-Royo, Philip S. Murphy, Gerrit Jansen, Conny J. van der Laken, Stephen Faulkner
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Discovery of Potent STT3A/B Inhibitors and Assessment of Their Multipathogen Antiviral Potential and Safety J. Med. Chem. (IF 6.8) Pub Date : 2024-08-13 Joseph E. Pero, Elizabeth A. Mueller, Ashley M. Adams, Ramona S. Adolph, Parikshit Bagchi, Dale Balce, Marcus Bantscheff, Ona Barauskas, Istvan Bartha, Dana Bohan, Haiying Cai, Esteban Carabajal, James Cassidy, Matthew Cato, Khuram W. Chaudhary, Dingjun Chen, Yi-Pei Chen, Christophe Colas, Isra Darwech, H. Christian Eberl, Beth Fernandez, Earl Gordon, Johannes Grosse, Justin Hansen, Belinda Hetzler
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Correction to “Design and Synthesis of Novel Cereblon Binders for Use in Targeted Protein Degradation” J. Med. Chem. (IF 6.8) Pub Date : 2024-08-13 Stephen Norris, Xiaochu Ba, Jayce Rhodes, Dehua Huang, Gody Khambatta, Jennifer Buenviaje, Surendra Nayak, Joseph Meiring, Samantha Reiss, Shuichan Xu, Lihong Shi, Brandon Whitefield, Matt Alexander, Evan J. Horn, Matthew Correa, Lida Tehrani, Joshua D. Hansen, Patrick Papa, Deborah S. Mortensen, Jean-François Brazeau
Addition: The author list has been updated to include Jean-François Brazeau, Bristol Myers Squibb, San Diego, California 92121, United States. Addition: Specific references to patent litearture disclosures have been added (refs (2−11) here), where we had previously referenced only a review article of the patent literature. We have also added one reference from the scientific literature found during
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Synthesis and Biological Evaluation of Pyrazole–Pyrimidones as a New Class of Correctors of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) J. Med. Chem. (IF 6.8) Pub Date : 2024-08-13 Christian Vaccarin, Guido Veit, Tamas Hegedus, Odalys Torres, Adriana Chilin, Gergely L. Lukacs, Giovanni Marzaro
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Pharmacophore Identification and Structure–Activity Relationship Analysis of a Series of Substituted Azaindoles as Inhibitors of Trypanosoma brucei J. Med. Chem. (IF 6.8) Pub Date : 2024-08-13 Lori Ferrins, Rosario Diaz, Carlos Cordon-Obras, Domingo Rojas-Barros, Antonio Quotadamo, Daniel P. Oehme, Gloria Ceballos-Pérez, Uma Swaminathan, Guiomar Pérez-Moreno, Cristina Bosch-Navarrete, Raquel García-Hernández, Claudia Gomez-Liñan, Andreu Saura, Luis Miguel Ruiz-Perez, Francisco Gamarro, Maria Santos Martinez-Martinez, Pilar Manzano, Dolores González-Pacanowska, Miguel Navarro, Michael P.
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Restoration of the Lost Human Beta Defensin-1 Protein in Cancer as a Strategy to Improve the Efficacy of Chemotherapy J. Med. Chem. (IF 6.8) Pub Date : 2024-08-13 Raghu Pandurangi, Thillai Sekar, Ramasamy Paulmurugan
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Synthesis and Biological Evaluation of Novel Psidium Meroterpenoid Derivatives against Cisplatin-Induced Acute Kidney Injury J. Med. Chem. (IF 6.8) Pub Date : 2024-08-13 Ying-Da Zang, Hai-Jie Wu, Xin-Yi Chen, Zhi-Ling Ma, Chuang-Jun Li, Jie Ma, Xiao-Guang Chen, Li Sheng, Sen Zhang, Dong-Ming Zhang